CLINICIAN’S HANDBOOK

PRESCRIPTION DRUGS

FM.qxd 7/6/01 9:24 AM Page i

Notice

Medicine is an ever-changing science. As new research and clin-

ical experience broaden our knowledge, changes in treatment

and drug therapy are required. The authors and the publisher of

this work have checked with sources believed to be reliable in

their efforts to provide information that is complete and gener-

ally in accord with the standards accepted at the time of

publication. However, in view of the possibility of human error

or changes in medical sciences, neither the authors nor the pub-

lisher nor any other party who has been involved in the preparation

or publication of this work warrants that the information contained

herein is in every respect accurate or complete, and they disclaim

all responsibility for any errors or omissions or for the results

obtained from use of the information contained in this work.

Readers are encouraged to confirm the information contained

herein with other sources. For example and in particular, read-

ers are advised to check the product information sheet included

in the package of each drug they plan to administer to be certain

that the information contained in this work is accurate and that

changes have not been made in the recommended dose or in the

contraindications for administration. This recommendation is of

particular importance in connection with new or infrequently

used drugs.

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CLINICIAN’S HANDBOOK

PRESCRIPTION DRUGS

Seymour Ehrenpreis, PhD

Former Chairman and Professor Emeritus of Pharmacology

Chicago Medical School

Chicago, IL

Eli D. Ehrenpreis, MD

Department of Gastroenterology

University of Chicago

Chicago, IL

McGRAW-HILL

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TABLEOF CONTENTS

Advisory Board........................................................................vi

Preface...................................................................................viii

Acknowledgements...............................................................xiii

Brand Names of Drugs..........................................................xiv

Generic Drug Entries................................................................1

Appendices............................................................................957

Food & Drug Administration Pregnancy

Categories...................................................................958

Common Aminoglycosides.............................................959

First Generation Cephalosporins.....................................961

Second Generation Cephalosporins.................................962

Third Generation Cephalosporins....................................964

Fourth Generation Cephalosporin...................................966

Macrolides: Susceptible Organisms................................967

Quinolones: General Information....................................969

Antifungal Agents............................................................972

Oral Contraceptives.........................................................975

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ADVISORY BOARD

Richard Albach, Ph.D.

Professor, Department of Microbiology and Immunology,

Chicago Medical School, North Chicago, Illinois

Jean-Lue Benoit, M.D.

Assistant Professor of Medicine, Infectious Disease Division,

University of Chicago, Chicago, Illinois.

Martin Burke, M.D.

Assistant Professor of Clinical Medicine, Cardiology Division,

University of Chicago, Chicago, Illinois

Dennis Citrin, M.D.

Associate Professor, Department of Medicine, Northwestern

University Medical School, Chicago, Illinois

Mark D. Ehrenpreis, M.D.

Associate Professor, Department of Urology, New York

Medical College, Valhalla, New York

Thomas Faust, M.D.

Assistant Professor of Clinical Medicine, Hepatology

Division, University of Chicago, Chicago, Illinois

Daniel Fintel, M.D.

Associate Professor, Department of Medicine, Director, Critical

Care, Northwestern University School of Medicine, Chicago,

Illinois

Eric Gall, M.D.

Professor and Chairman, Department of Medicine, Chicago

Medical School, North Chicago, Illinois

Phillip C. Hoffman, M.D.

Professor of Clinical Medicine, Hematology/Oncology

Division, University of Chicago, Chicago, Illinois

Nelson Kanter, M.D.

Associate Professor of Clinical Medicine, Pulmonary/Critical

Care Division, University of Chicago, Chicago, Illiniois

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Robert S. Lauren, DDS

DDS Associates Limited, Skokie, Illinois

Gerald B. Leiken, M.D.

Director, Medical Emergency Services, Rush Medical Center,

Chicago, Illinois

Michael Marshall, M.S.

Physician’s Assistant, United States Army, Seattle, Washington

Lawrence Perlmuter, Ph.D.

Professor, Department of Clinical Psychology, Chicago

Medical School, North Chicago, Illinois

Raymond Quock, Ph.D.

Professor and Chairman, Department of Pharmaceutical

Sciences, Washington State University, Pullman,

Washington

Sant Singh, M.D.

Professor, Department of Medicine, Chief, Endocrinology,

Chicago Medical School, North Chicago, Illinois

Daniel Zaitman, M.D.

Chicago Medical School, North Chicago, Illinois

ADVISORY BOARD viivii

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PREFACE

A recent article published in the New York Timesquoted the

astounding statistic that as many as 7,000–10,000 deaths in the

United States can be attributed on an annual basis to prescrip-

tion errors. Countless hospital days, loss of productivity, and

an atmosphere of distrust of modern medicine all result from

such errors. Many causes can be found for these mistakes;

drugs with completely different properties, uses, and toxicity

profiles may have similar names. Polypharmacy, a common

phenomenon in the elderly, places patients at risk for complex

drug–drug interactions. Difficulty with high-volume record

keeping and the loss of personal interaction with the “family

pharmacist” certainly result in more patients receiving the

wrong medication or dosage when a prescription is filled.

Finally, the rapid pace of modern medical practices coupled

with the ever–bewildering numbers of medications on the

market result in a situation in which the busy practitioner may

have difficulty keeping abreast of important aspects of the

drugs they are prescribing. It was with these concerns in mind

that we undertook the task of writing a manual of drug pre-

scription for the practicing clinician. No one can be expected

to commit to memory everything important about all the drugs

available on the market. It can be quite time consuming and

frustrating to search for important information on individual

entries in a large comprehensive volume such as the

Physician’s Desk Reference. Thus, our main objective in cre-

ating this book was to provide the most essential information

on all commonly prescribed drugs in a concise, accurate and

easy-to-read manner.

In producing this book, it is our hope that we can help clinicians

give the best care possible to patients taking prescription drugs.

We believe this book will benefit you in looking up drugs that

are not frequently prescribed. In addition, you will have an

opportunity to reacquaint yourself with details about familiar

drugs when using this book “at the bedside.”

viii

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PREFACE ix

The book does not have complete entries for all prescription

drugs. Some have been left out simply because of lack of suffi-

cient available information or because of very limited use. In

addition, we have not included many drug combinations because

of space considerations. Furthermore, we have restricted ourdis-

cussion in the case of drugs that are members of the same drug

class. Most if not all of the drugs in a particular pharmacologic

class have similar if not identical characteristics, for example, side

effects, drug–drug interactions, contraindications. Accordingly,

we have selected one or more drugs to serve as prototypes and

these have been given a complete entry (as described below).

For other members of the particular class, we have presented

only essential information, referring the reader in each case to

the prototype for additional details.

On the other hand, we have discussed in full a number of widely

used drugs that for one reason or another are not listed in the

Physician’s Drug Reference 2000or for which only the drug name

is stated without any details. In other instances, we provide even

more complete information than offered by the manufacturer. For

example, no drug–drug interactions are listed by the manufactur-

ers for benzodiazepines in the Physician’s Desk Reference,whereas

we list a number of these interactions that are clinically important.

The reader should note that some information provided may

differ from that contained in the manufacturer’s package insert.

The decision to include or exclude information is based on our

best judgment or on the advice of our Advisory Board after

reviewing all available data.

Ahandbook such as this, with its emphasis on conciseness, can

present only a relatively small fraction of the total knowledge

available about any particular drug. Thus, it is our considered

opinion that the clinician attempt to review available product

information sheets as approved by the Food and Drug Adminis-

tration should the need arise to expand on the information presen-

ted herein. We strongly believe that accessing the information

provided with the easy-to-follow format we have created for this

manual will make this book an important reference for clinicians

in a wide variety of settings. If, overall, we are able to assist the

health care provider to administer medications to their patients

PREFACE ix

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safely and effectively and thereby to treat their ailments as well as

prevent complications of drug therapy, we will have achieved our

desired goals.

The following format is used for all drugs:

Brand name: For drugs that have multiple brand names, we have

listed those drugs that are widely prescribed.

Mechanism of action: This is stated succinctly, using at most one

or two lines.

Indications/dosage/route: All approved indications are listed;

occasionally, widely used unapproved indications are mentioned.

For the most part, dosages recommended by the manufacturer are

listed. Dosages are mainly the usual adult dose (persons <60 or 65

years). The following specific information about dosing is

included wherever possible: initial dose, follow-up dose, mainte-

nance and maximum doses, duration of drug administration,

details for parenteral (in particular IV) administration. Wherever

available, doses for children and the elderly are included.

Adjustment of dosage: Related primarily to kidney and liver dis-

ease. Guidelines are presented for adjusting dosage in relation

to creatinine clearance or creatinine blood levels. We indicate if

there is no need to adjust dosage for kidney or liver disease or

for elderly or pediatric patients. Also stated are age limits for

prescribing the drug for children or if the drug should be pre-

scribed for this age group at all.

Onset of action,peak effect, and duration: Wherever available,

time of onset of action, peak effect, and duration are listed. This

information is considered most important for the proper spacing

of drug administration. Other aspects of pharmacokinetics—

peak serum levels, bioavailability, protein binding, half-life—as

included in many sources, are not considered of utmost impor-

tance in pharmacotherapy per se and are not included.

Food: Wherever possible, mention is made of those foods to be

avoided and whether or not the drug should be taken with food.

Pregnancy: The pregnancy category as proposed by the Food

and Drug Administration is indicated for each drug. See Table 1

on page 958 for the definition of these categories.

Lactation: Available information regarding the presence of the

drug in breast milk is given. Guidelines as set forth by the

x PREFACE

FM.qxd 7/6/01 9:24 AM Page x

American Academy of Pediatrics, if available, are presented. A

general guideline provided in a brief statement (such as “avoid

breastfeeding”) is provided.

Warnings/precautions: All warnings provided by the manufac-

turer have been set forth as succinctly as possible. Other

statements are made to alert the health provider to potential

problems with the drug and how to avoid them.

Advice to patients: This represents our opinions regarding what

the treating clinician needs to tell the patient to attempt to avoid

or minimize problems with the drug. Included are the following

“tips”: when to avoid alcohol or other CNS depressants because

of adverse interactions; how to protect oneself if the drug causes

photosensitivity reactions; when to anticipate and minimize ortho-

static hypotension; when to avoid driving; which appropriate

contraceptive measures to use; when to avoid heat, cold, extreme

exertion; how to cope with anticholinergic drug side effects;

when and how to stop taking the drug.

Adverse reactions: These are defined as common (occurring in

≥ 10% of the patients taking the drug in pre- or postmarketing

testing) and serious (potentially life threatening or with the risk

of causing organ damage). Side effects that are serious as well

as common are listed as serious but in boldface type.

Clinically important drug interactions: All too frequently, drug

compendia list too many such interactions and/or fail to indicate

which of these enhance or diminish the actions of a particular

drug. Our list of drug interactions includes only those that, by

consensus, are clinically relevant and include a statement

regarding the actual effect of the interaction.

Parameters to monitor: We consider it to be of great importance

that the treating clinician follow up on how a drug is acting on

the patient by monitoring various vital functions. If these sug-

gestions are followed, we believe many serious adverse reactions

may be avoided or minimized. The following are some of the

suggested parameters to be monitored: blood testing, hemody-

namics, blood pressure, ECG, liver and kidney function, drug

levels and efficacy of the drug in achieving its intended result.

Judgment regarding actual monitoring in individual patients

must ultimately be made by the treating clinician.

PREFACE xi

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Editorial comments: Finally, the editors and their advisors have

presented information in the form of editorial comments regard-

ing certain aspects of many of the drugs included in this manual

that are not covered by the preceding.

All drugs are listed by generic name in alphabetical order. Across

referenced list of brand name drugs is supplied in the front matter.

With respect to the actual use of this book, the authors state the

following:

1. Despite our best efforts to provide accurate information and

opinions about each drug considered, the authors, members

of the Advisory Board, and publisher do not guarantee that

all of the material presented is completely accurate. The

authors, reviewers, and publishers are not responsible for

any errors, either those of omission or commission, that may

arise in applying the enclosed information. Furthermore, not

all authorities will agree with all our facts and/or evalua-

tions. Accordingly, we can consider the material presented

only as guidelines for drug administration, not the final

word. The clinician or other health care provider must use

his or her personal, independent judgment in applying the

information in actual practice. In this regard, it is suggested

that if the clinician disagrees with something in our drug

monograph, he or she should check with the manufacturer’s

label for the particular drug before using it.

2. The authors, reviewers, and publisher disclaim any liabil-

ity for any claim for losses or alleged losses that may have

resulted from the use of the information contained herein

whether directly or indirectly applied.

3. The authors, reviewers, and publisher have no connection

with any pharmaceutical company or federal agency. They

have not received compensation from any such organiza-

tion. This book was commissioned solely by McGraw–Hill

Company and the authors have written it without endorse-

ment from any pharmaceutical company or federal agency.

Any opinions expressed herein are solely those of the

authors and members of their Advisory Board.

4. The authors, Advisory Board, and publisher will not be held

liable if the material presented is misused or not applied

appropriately by the clinician.

xii PREFACE

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5. In many instances, a particular drug may have several

brand names. We have included those that in our opinion

are commonly used. Inclusion of one or more brand names

should not be construed as an endorsement of the product

just as its exclusion does not imply that we have rejected

the product or consider it inferior to another. The publisher

does not endorse or reject any of the products described

and has no opinion regarding any of the products. The

publisher has not engaged in or provided any kind of

financial support for any of the products described herein.

ACKNOWLEDGEMENTS

We acknowledge the invaluable advice of our Advisory Board.

Their knowledge and hands-on experience in specialty patient

care has added greatly to the depth of information provided by

the book. We also acknowledge Catherine Will and Cheryl

Serdar for their excellent assistance with manuscript prepara-

tion. Special thanks go to Lynn Kaczmarz for administrative

assistance with the book and to the editors of McGraw–Hill for

their support and encouragement.

Seymour Ehrenpreis: My heartfelt thanks to my wife, Bella, for

her forbearance throughout the time devoted to the task of writ-

ing this book. Never once did she complain! It is to her that I

gratefully dedicate this book.

Eli Ehrenpreis: I would like to dedicate this book to my wife,

Ana, for her encouragement and enthusiasm during the writing

of the book and to my children, Benjamin, Jamie, and Joseph,

for being so understanding and for sacrificing time that could

have been spent with their father. Finally, I dedicate this book to

my grandfather, the late Joseph Goodman, a man of great

wisdom, energy, and humor who inspired me to achieve these

qualities in my personal and professional life.

PREFACE xiii

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Abelcet see Amphotericin B

Accolate see Zafirlukast

Accupril see Quinapril

Accurbron see Theophylline

Accutane see Isotretinoin

Achromycin see Tetracycline

Acticort see Hydrocortisone

Actic see Fentanyl

Actinin see Permethrin

Activase see Alteplase

Actonel see Riseronate

Acular see Ketorolac

Adalat see Nifedipine

Adapin see Doxepin

Adapryl see Selegiline

Adenocard see Adenosine

Adrenalin see Epinephrine

Adrucil see Fluorouracil

Aerobid see Flunisolide

Aerolate see Theophylline

Airet see Albuterol

AK-Chlor see Chloramphe-

nicol

AK-Cide see Prednisolone

AK-Dex see Dexamethasone

Albenza see Albendazole

Aldactone see Spironolactone

Aldomet see Methyldopa

Aldoril see Methyldopa Hydro-

chlorothiazide

Alesse see Estrogen-Progestin

Aleve see Naproxen

Alfenta see Alfentanil

Alkeran see Melphalan

Allegra see Fexofenadine

Aloprim see Allopurinol

Aloprin see Allopurinol

Alphatrex see Betamethasone

Altace see Ramipril

Alupent see Metaproterenol

Amaryl see Glimepiride

Ambien see Zolpidem

Ambisome see Amphotericin B

Ambophen see Diphenhydra-

mine

Amcort see Triamcinolone

Amen see Medroxyprogeste-

rone

Amethopterin see Methotrex-

ate

Amfebutamone see Bupropion

Amikin see Amikacin

Aminophylline see Theophyl-

line

Amoxil see Amoxicillin

Amphocin see Amphotericin B

Amphotec see Amphotericin B

Anafranil see Clomipramine

Anaprox see Naproxyn

Ancef see Cefazolin

Ancobon see Flucytosine

Android see Methyltestoste-

rone

Anectine see Succinylcholine

xiv

BRAND NAMES

FM.qxd 7/6/01 9:24 AM Page xiv

Anergan see Promethazine

Ansaid see Flurbiprofen

Antabuse see Disulfiram

Antigout see Colchicine

Antilirium see Physostigmine

Antinaus see Promethazine

Antivert see Meclizine

Anucort-HC see Hydrocortis-

one

Anx see Hydroxyzine

Anzemet see Dolasetron

Apresazide see Hydralazine

Apresoline see Hydralazine

AquaMephyton see Phytona-

dione

Aquaphylline see Theophyl-

line

Aquatensen see Methyclothi-

azide

Aralen see Chloroquine

Arava see Leflunomide

Aristocort see Triamcinolone

Artane see Trihexyphenidyl

Asacol see Mesalamine

Asendin see Amoxapine

Asmalix see Theophylline

Atamet see Carbidopa/Levo-

dopa/Carbidopa

Atarax see Hydroyzine

Ativan see Lorazepam

Atretol see Carbamazepine

Atromid-S see Clofibrate

Atropine see Atropine

Atropisol see Atropine

Augmentin see Amoxicillin,

Clavulanate

Aureomycin see Tetracycline

Avandia see Rosiglitazone

Aventyl see Nortriptyline

Axid see Nizatidine

Aygestin see Norethindrone

Azamacort see Triamcimo-

lone

Azifidine see Sulfasalazine

Azmacort see Triamcinolone

AZTsee Zidovudine

Azulfidine see Sulfasalazine

Baciguent see Bacitracin

Bactocil see Oxacillin

Bactramycin see Lincomycin

Bactrim see Trimethoprin-

Sulfamethoxazole

Baycol see Cerivastatin

Beclovent see Beclomethasone

Beconase see Beclomethasone

Benadryl see Diphenhydra-

mine

Benemid see Probenecid

Bentylol see Dicyclomine

Benzamycin see Erythromy-

cin

Betapace see Sotalol

Betaseron see Beta Interferon

Betatrex see Betamethasone

Betoptic see Betaxolol

Biaxin see Clarithromycin

Bicillin see Penicillin G

BICNU see Carmustine

Blenoxane see Bleomycin

Blocadren see Timolol

Bonine see Meclizine

Brethaire see Terbutaline

Brethine see Terbutaline

BRAND NAMES xv

FM.qxd 7/6/01 9:24 AM Page xv

Bretylol see Bretylium

Brevibloc see Esmolol

Brevicon see Estrogen-

Progesterone

Bromaline see Bromphenira-

mine

Bromfed see Bromphenira-

mine

Bronkaid see Epinephrine

Bronkodyl see Theophylline

Bumex see Bumetanide

Buprenex see Buprenorphine

BuSpar see Buspirone

Butalan see Butabarbital

Butisol see Butabarbital

Calan see Verapamil

Calcijex see Calcitriol

Calcimar see Calcitonin

Capastat see Capreomycin

Capoten see Captopril

Carbex see Seligine

Carbitrol see Carbamazepine

Carbocaine see Mepivacaine

Cardene see Nicardipine

Cardioquin see Quinidine

Cardizem see Diltiazem

Cardura see Doxazosin

Cartrol see Carteolol

Cataflam see Diclofenac

Catapres see Clonidine

Caverject see Alprostadil

CCNU see Lomustine

Ceclor see Cefaclor

Cedax see Ceftibuten

CeeNU see Lomustine

Cefizox see Ceftizoxime

Cefobid see Cefoperazone

Cefotan see Cefotetan

Ceftin see Cefuroxime

Cefzil see Cefprozil

Celebrex see Celecoxib

Celestone see Betamethasone

Celexa see Citalopram

CellCept see Mycophenolate

Ceptaz see Ceftazidime

Cerubidine see Daunorubicin

Chibroxin see Norfloxacin

Chloromycetin see Chloram-

phenicol

Chloroptic see Chloramphe-

nicol

Chlor-Trimeton see Chlorphe-

niramine

Cibacalcin see Calcitonin

Cibalith-S see Lithium

Cibroxin see Norfloxacin

Ciloxan see Ciprofloxacin

Cinalone see Triamcinolone

Cipro see Ciprofloxacin

Claforan see Cefotaxime

Claritin see Loratadine

Clavulanate see Amoxcillin/

Clavulanate

Clinoril see Sulindac

Clomid see Clomiphene

Cloxapen see Cloxacillin

Cogentin see Benztropine

Cognex see Tacrine

ColBENEMID see Pro-

benecid

Colestid see Colestipol

xvi BRAND NAMES

FM.qxd 7/6/01 9:24 AM Page xvi

Combivir see Ziduvidine

(AZT)

Compazine see Prochlorpera-

zine

Cordarone see Amiodarone

Corgard see Nadolol

Corlopam see Fenoldapam

Cortaid see Hydrocortisone

Cort-Dome see Hydrocorti-

sone

Cortef see Hydrocortisone

Cortenema see Hydrocorti-

sone

Cortifoam see Hydrocortisone

Cortone see Cortisone

Corvert see Ibutilide

Cosmegen see Dactinomycin

Coumadin see Warfarin

Crinone see Progesterone

Cuprimine see Penicillamine

Cutivate see Fluticasone

Cycrin see Medroxyproges-

terone

Cylert see Pemoline

Cytosar-U see Cytarabine

Cytospaz see Hydroscyamine

Cytotec see Misoprostol

Cytovene see Ganciclovir

Cytoxan see Cyclophospha-

mide

Danocrine see Danazol

Dantrium see Dantrolene

Daraprim see Pyrimethamine

Darvon see Propoxyphene

DaunoXome see Daunorubi-

cin

Dayhist see Clemastine

Daypro see Oxaprozin

Decadron see Dexamethasone

Declomycin see Demeclocyc-

line

Delatestryl see Testoterone

Deltasone see Prednisone

Demulan see Estrogen/Proges-

terone

Depacon see Valproic acid

Depakene see Valproic Acid

Depen see Penicillamine

Depoject see Methylpredni-

solone

Depo-Medrol see Methylpred-

nisolone

Depo Predate see Methylpred-

nisolone

Depo Provera see Medroxy-

progesterone

Depotest see Testosterone

Dermacort see Hydrocorti-

sone

Desogen see Estogen/Proges-

terone

Desyrel see Trazodone

Dexacort see Dexamethasone

Dexasone see Dexamethasone

D.H.E.45 see Dihydroergo-

tamine

Diabeta see Glyburide

Diabinase see Chlorpropamide

Diabinese see Chlorpropamide

Diamox see Acetazolamide

Diflucan see Fluconazole

Dilacor see Diltiazem

Dilatrate see Isosorbide

BRAND NAMES xvii

FM.qxd 7/6/01 9:24 AM Page xvii

Dilaudid see Hydromorphone

Dimetane see Bromphenira-

mine

Diprolene see Betamethasone

Diprosone see Betamethasone

Ditropan see Oxybutinin

Diucardin see Hydroflume-

thiazide

Diuril see Chlorothiazide

Dizac see Diazepam

Dobutrex see Dobutamine

Dolene see Propoxyphene

Dolophine see Methadone

Dopar see Levadopa/

Carbidopa

Dopastate see Dopamine

Doryx see Doxyclycline

Doxil see Doxorubicin

Droxia see Hydroxyurea

DTIC-Dome see Dacarbazine

Duraclon see Clonidine

Duragesic see Fentanyl

Duramorph see Morphine

Duranest see Etidocaine

Duricef see Cafadroxil

Duvoid see Bethanechol

D-Vert see Meclizine

Dyazide see Hydrochlorothi-

azide Trimterene

Dycill see Dicloxacillin

Dymelor see Acetohexamide

Dynacin see Minocycline

Dynapen see Dicloxacillin

Dyphylline see Theophylline

Dyrenium see Triamterane

Econopred see Prednisolone

Edecrin see Ethacrynic Acid

EES see qErythromycin

Effexor see Venlafaxine

Efudex see Fluorouracil

Elavil see Amitriptyline

Eldepryl see Selegiline

Elimite see Permethrin

Elixophyllin see Theophylline

Endodan see Methyclothiazide

Enduron see Methylclothiazide

Ephedrine see Ephedrine

Epifrin see Epinephrine

Epinal see Epinephrine

Epipen see Epinephrine

Epitol see Carbamazepine

Epivir see Lamivudine

Equanil see Meprobamate

Ergamisol see Levamisole

Ergostat see Ergotamine

Erycette see Erythromycin

Erythrocin see Erythromycin

Eserine see Physostigmine

Esgic see Butabarbital

Esidrix see Hydrochlorothia-

zide

Eskalith see Lithium

Estratest see Methyltestoster-

one

Ethmozine see Moricizine

Etopophos see Etoposide

Etrafon see Amitriptyline,

Perphenazine

Eulexin see Flutamide

Everone see Testosterone

xviii BRAND NAMES

FM.qxd 7/6/01 9:24 AM Page xviii

Famvir see Famciclovir

Feldene see Piroxicam

Feosol see Ferrous Sulfate

Flagyl see Metronidazole

Flexeril see Cyclobenzaprine

Flomax see Tamsulosin

Flonase see Fluticasone

Florinef see Fludrocortisone

Flovent see Fluticasone

Floxin see Ofloxacin

Flubenisolon see Betametha-

sone

Fludara see Fludarabine Phos-

phate

Flumadine see Rimantadine

Fluoroplex see Fluorouracil

Flutex see Triamcinolone

Folex see Methotrexate

Fortaz see Ceftazidime

Fosamax see Alendronate

Foscavir see Foscarnet

FUDR see Floxuridine

Fulvicin see Griseofulvin

Fungizone see Amphotericin B

Furacin see Nitrofurazone

Furadantin see Nitrofurantoin

Ganite see Gallium Nitrate

Garamycin see Gentamycin

Gastrocrom see Cromolyn

Genoptic see Gentamicin

Genora see Estrogen-Proges-

tin

Genotropin see Somatropin

Geocillin see Carbenicillin

Glaucon see Epinephrine

Glucagon see Glucagon

Glucotrol see Glipizide

Glynase see Glyburide

Grifulvin see Griseofulvin

Gynecort see Hydrocortisone

Haldol see Haloperidol

Halodrin see Fluoxymeste-

rone

Halotestin see Fluoxymeste-

rone

Hemabate see Carboprost

Herplex see Idoxuridine

Histalet see Chlorpheniramine

Hivid see Zalcitabine

Humalog see Insulin

Humatin see Paromomycin

Humatrope see Somatropin

Hycodan see Hydrocodone

Hydramine see Diphenhy-

dramine

Hydrea see Hydroxyurea

Hydrocortone see Hydrocorti-

sone

Hydro-Diuril see Hydrochloro-

thiazide

Hydroxacen see Hydroxyzine

Hygroton see Chlorthalidone

Hylutin see Hydroxyproges-

terone

Hyoscine see Scopolamine

Hyoscyamine

Hyperstat see Diazoxide

Hytrin see Terazosin

BRAND NAMES xix

FM.qxd 7/6/01 9:24 AM Page xix

Hyzaar see Losartan

Hyzine see Hydroxyzine

Ifex see Ifosamide

Imdur see Isosorbide Mono-

nitrate

Immitrex see Sumatriptan

Imuran see Azathioprine

Inapsine see Droperidol

Inderal see Propranolol

Indocin see Indomethacin

Inflamase see Prednisolone

Infumorph see Morphine

Innovar see Droperidol,

Fentanyl

Inocor see Amrinone

Intal see Cromolyn

Integrilin see Eptifibatide

Intropin see Dopamine

Ismo see Isosorbide Mononit-

rate

Isoproterenol see Isoprote-

renol

Isoptin see Verapardl

Isopto see Atropine

Isopto-Hyoscine see Scopola-

mine

Isordil see Isosorbide, Dini-

trate

Isuprel see Isoproterenol

Kayexalate see Sodium

Polystyrene Sulfonate

K-Dur see Potassium Chloride

Keflet see Cephalexin

Keflex see Cephalexin

Keflin see Cephalothin

Keftab see Cephalexin

Kefurox see Cefuroxime

Kefzol see Cefazolin

Kenalog see Triamcinolone

Kerlone see Betaxolol

Ketalor see Ketamine

K-Lor see Potassium Chloride

Klor-Con see Potassium

Chloride

Konakion see Phytonadione

Kwell see Lindane

Kwildane see Lindane

Lamictal see Lamotrigine

Lanacort see Hydrocortisone

Lanoxicaps see Digoxin

Lanoxin see Digoxin

Laradopa see Levodopa/

Carbidopa

Lasix see Furosemide

Ledercillin VK see Penicillin V

Lelvan see Estrogen/Progestin

Lescol see Fluvastatin

Leucovorin see Leucovorin

Leukeran see Chlorambucil

Leustatin see Cladribine

Levaquin see Levofloxicin

Levbid see Hyoscyamine

Levo-Dromoran see Levor-

phanol

Levora see Estrogen-Proges-

terone

Levothroid see Levothyroxine

Levoxyl see Levothroxine

Levsin see Hyoscyamine

Lexxel see Enalapril

Librium see Chlordiazepoxide

xx BRAND NAMES

FM.qxd 7/6/01 9:24 AM Page xx

Lidex see Fluocinonide

Lioresal see Baclofen

Lipitor see Atorvastatin

Lithobid see Lithium

Lithonate see Lithium

LoCholest see Cholestyra-

mine

Locoid see Hydrocortisone

Lodine see Etodolac

Lodosyn see Levodopa/

Carbidopa

Lodrane see Bromphenira-

mine

Loestrin see Estrogen-Proges-

tin

Lopressor see Metoprolol

Lorabid see Loracarbef

Lotensin see Benazepril

Loxitane see Loxapine

Lozol see Indapamide

Luminal see Phenobarbital

Lupron see Leuprolide

Luvox see Fluvoxamine

Lyphocin see Vancomycin

Lysodren see Mitotane

Macrobid see Nitrofurantoin

Mandol see Cefamandole

Marax see Theophylline

Marinol see Dronabinol

Matulane see Procarbazine

Maxaquin see Lomefloxacin

Maxidex see Dexamethasone

Maxipeme see Cefepime

Maxivate see Betamethasone

Mebural see Mephobarbital

Medihaler see Isoproterenol

Medihaler-Iso see Isoprote-

renol

Medrol see Methylpredni-

solone

Mefoxin see Cefoxitin

Megase see Megestrol

Mellaril see Thioridazine

Menadol see Ibuprofen

Menest see Estrogen

Meni-D see Meclizine

Meperidine see Demerol

Mephyton see Phytonadione

Meprospan see Meprobamate

Mesnex see Mesna

Mestinon see Pyridostigmine

Methadose see Methadone

Methylin see Methylpheni-

date

Meticorten see Prednisone

Metric see Metronidazole

Mevacor see Lovastatin

Mevinolin see Lovastatin

Mexate see Methotrexate

Mexith see Mexiletine

Mezlin see Mezlocillin

Miacalcin see Calcitonin

Micatin see Miconzaole

Micro-K see Potassium Chlo-

ride

Micronase see Glyburide

Micronor see Estrogen/

Progestin

Midamor see Amiloride

Milophene see Clomiphene

Milprem see Meprobamate

Miltown see Meprobamate

Minipress see Prazosin

BRAND NAMES xxi

FM.qxd 7/6/01 9:24 AM Page xxi

Minitran see Nitroglycerin

(Transdermel)

Minocin see Minocycline

Mintezole see Thiabendazole

Mithracin see Plicamycin

Mivacron see Mivacurium

Moban see Molindone

Modicon see Estrogen-

Progestin

Monacolin see Lovastatin

Monistate see Miconazole

Monodox see Doxycycline

Monoket see Isosorbide Mo-

nonitrate

Monopril see Fosinopril

8-MOPsee Methoxsalen

MTX see Methotrexate

Mucomyst see Acetyleysteine

Muse see Alprostadil

Mutamycin see Mitomycin

Myambutol see Ethambutol

Myambutol see Mitomycin

Mycostatin see Nystatin

Myidone see Primidone

Mykrox see Metolazone

Myleran see Busulfan

Myotrol see Orphenadrine

Mysoline see Primidone

Nalfon see Fenoprofen

Nallpen see Nafcillin

Naprosyn see Naproxen

Narcan see Naloxone

Nardil see Phenelzine

Nasalcrom see Cromolyn

Nasalide see Flunisolide

Nasocort see Triamcinolone

Naturectin see Bendroflume-

thiazide

Navane see Thiothixene

Nebcin see Tobramycin

NebuPent see Pentamidine

Necon see Estrogen-Protestin

Nembutal see Pentobarbital

Neoral see Cyclosporine

Neosar see Cyclophospha-

mide

Neo-Synephrine see Phenyle-

phrine

Netromycin see Netilmicin

Neucalm see Hydroxyzine

Neuromax see Doxacurium

Neurontin see Gabapentin

Neutrexin see Cabapantin

Nexate see Methotrexate

Nilstat see Nystatin

Nimotop see Nimodipine

Nipride see Nitroprusside

Nitro-Bid see Nitroglycerin

Nitro-Derm see Nitroglycerin

(Transdermal)

Nitroglyn see Nitroglycerine

(Sustained Release)

Nitrol see Nitroglycerin

(Topical)

Nitrong see Nitroglycerine

(Sustained Release)

Nitropress see Nitroprusside

Nitrostat see Nitroglycerin

(sublingual)

xxii BRAND NAMES

FM.qxd 7/6/01 9:24 AM Page xxii

Nix see Permethrin

Nizoral see Ketoconazole

Nolvadex see Tamoxifen

Nordette see Estrogen-

Progestin

Norditropin see Somatropin

Norgestrel see Levonorgestrel

Normgdyne see Labetolol

Norpace see Disopyramide

Norpath see Propanthaline

Norplant see Levonorgestrel

Norpromin see Desipramine

Norvasc see Amlodipine

Novantrone see Mitoxantrone

Novocaine see Procaine

NubuPent see Pentamidine

Numorphan see Oxymor-

phone

Nuprin see Ibuprofen

Nuromax see Doxacurium

Nutracort see Hydrocortisone

Nutropin see Somatropin

Nydrazid see Isoniazid

Nystex see Nystatin

Ocuflox see Ofloxacin

Omnicef see Cefdinir

Omnipen see Ampicillin

OMS see Morphine

Opticrom see Cromolyn

Oramorph see Morphine

Orasone see Prednisone

Oretic see Hydrochlorothia-

zide

Orinase see Tolbutamide

Orlaam see Levomethadyl

Ortho-Cept see Estrogen/

Progestin

Orudis see Ketoprofen

Ovcon see Estrogen/Progestin

Oxitriptan see Levodopa/

Carbidopa

Oxsoralen see Methoxsalen

Oxycontin see Oxycodene

Panaldine see Ticlopidine

Paraflex see Chlorzoxazone

Paraplatin see Carboplatin

Parlodel see Bromocriptine

Parnate see Tranylcypromine

PAS Sodium see Para-

Aminosalicylic acid

Pavulon see Pancuronium

Paxil see Paroxetine

Pediazole see Erythromycin

Penetrex see Enoxacin

Pentam-300 see Pentamidine

Pentasa see Mesalamine

Pen-Vee see Penicillin

Pepsid see Famotidine

Percocet see Oxycodone

Percodan see Oxycodone

Periactin see Cyproheptadine

Permapen see Penicillin G,

Benzathine

Permax see Pergolide

Permitil see Fluphenazine

Persantin see Dipyridamole

Pertofrane see Desipramine

Pfizerpen see Penicillin G

Phenergan see Promethazine

Phrenilin see Butabarbital

BRAND NAMES xxiii

FM.qxd 7/6/01 9:24 AM Page xxiii

Pipracil see Piperacillin

Pitocin see Oxytocin

Pitressin see Vasopressin

Platinol see Cisplatin

Plendil see Felodipine

Ponstel see Mefenamic Acid

Prandin see Repaglinide

Pravachol see Pravastatin

Prevalite see Cholestyramine

Prilosec see Omeprazole

Primacor see Milrinone

Principen see Ampicillin

Prinivil see Lisinopril

Probalan see Probenecid

Pro-Banthine see Propanthe-

line

Procanbid see Procainamide

Procardia see Nifedipine

Proglycem see Diazoxide

Prograf see Tacrolimus

Proleukin see Aldesleukin

Prolixin see Fluphenazine

Promet see Promethazine

Promethegan see Prometha-

zine

Prometrium see Progesterone

Promine see Procainamide

Pronestyl see Procainamide

Propanthel see Propantheline

Propecia see Finasteride

Propocet see Propoxyphene

Propulsid see Cisapride

Propyl-Thyracil see Propyl-

thiouracil

Proscar see Finasteride

Prostaphlin see Oxacillin

Prostat see Metronidazole

Prostigmin see Neostigmine

Prostin VR see Alprostadil

Prostin VR Pediatric see

Alprostadil

Protamine see Protamine

Protopam see Pralidoxime

Proventil see Albuterol

Provera see Medroxyproges-

terone

Prozac see Fluoxetine

Pulmicort see Budesonide

Purinethol see Mercaptopu-

rine

Pyrazinamide see Pyrazina-

mide

Quelicin see Succinylcholine

Questran see Cholestyramine

Quibron see Theophylline

Quinaglute see Quinidine

Quinidex see Quinidine

Quinora see Quinidine

Regitine see Phentolamine

Reglan see Metoclopramide

Regonol see Pyridostigmine

Bromide

Relafen see Nabumetone

Rescon see Chlorpheniramine

Respbid see Theophylline

Restoril see Temazepam

Retrovir see Zidovudine

Reversol see Edrophonium

ReVia see Naltrexone

Rheumatrex see Methotrexate

Rhinocort see Budesonide

Ridaira see Auranofin

xxiv BRAND NAMES

FM.qxd 7/6/01 9:24 AM Page xxiv

Rifadin see Rifampin

Rifamate see Isoniazid, Ri-

fampin

Rifampicin see Rifampin

Rifater see Isoniazid, Pyra-

zinamide, Rifampin

Rimactane see Rifampin

Risperdal see Risperidone

Ritalin see Methylphenidate

Rocaltrol see Calcitriol

Rocephin see Ceftriaxone

Roferon-A see Interferon

Alfa 2

Rogaine see Minoxidil

Romazicon see Flumazenil

Rowasa see Mesalamine

Roxanol see Morphine

Roxicodone see Oxycodone

Ru-Vert-M see Meclizine

Ryna-C see Codeine

Rynatan see Azatadine

Rythmol see Propafanone

Saizem see Somatropin

Sandimmune see Cyclosporine

Sansert see Methysergide

Sarisol see Butabarbital

Scabene see Lindane

Scalpicin see Hydrocortisone

Sectral see Acebutolol

Selestoject see Betametha-

sone

Septra see Trimethoprim-

Sulfamethoxazole

Serax see Oxazepam

Sereen see Chlordiazepoxide

Serentil see Mesoridazine

Serevent see Salmeterol

Seromycin see Cycloserine

Serophene see Clomiphene

Sertan see Primidone

Silvadene see Silver Sulfadia-

zine

Sinemet see Levadopa/

Carbidopa

Sinequan see Doxepin

Slo-Phylline see Theophylline

Solfoton see Phenobarbital

Solu-Cortef see Hydrocorti-

sone

Solu-Medrol see Methylpred-

nisolone

Solurex see Dexamethasone

Soma see Carisoprodol

Sorbitrate see Isosorbide Di-

nitrate

Sparine see Promazine

Spectrobid see Bacampicillin

Sporanox see Itraconazole

SSKI see Potassium Iodide

Stadol see Butophanol

Staphicillin see Methicillin

Staticin see Erythromycin

Stelazine see Trifluoperazine

Sterapred see Prednisone

Streptase see Streptokinase

Streptomycin see Streptomycin

Sublimaze see Fentanyl

Sucostrin see Succinylcholine

Sufenta see Sufentanil

Sumycin see Tetracycline

Suprax see Cefixime

Surmontil see Trimipramine

Sus-Phrine see Epinephrine

BRAND NAMES xxv

FM.qxd 7/6/01 9:24 AM Page xxv

Sustiva see Efavirenz

Symmetrel see Amantadine

Synalar see Fluocinolone

Synemol see Fluocinolone

Synthroid see Levothyroxine

Syntocinon see Oxytocin

Synvinolin see Simvastatin

Tacrium see Atracurium Acra-

curium

Tagemet see Cimetidine

Talacen see Pentazocine

Talwin see Pentazocine

Tambocor see Flecainide

TAO see Troleandomycin

Tapazole see Methimazole

Tavist see Clemastine

Tazicef see Ceftazidime

Tazicel see Ceftazidime

Tazidime see Ceftazidime

Tegretol see Carbamazepine

Teldrin see Chlorpheniramine

Tenormin see Atenolol

Tensilon see Edrophonium

Testoderm see Testosterone

Testopel see Testosterone

Testred see Methyltestoste-

rone

Tetracycline see Tetracycline

Thalitone see Chlorthalidone

THC see Dronabinol

Theo-Dur see Theophylline

Theolair see Theophylline

Thioplex see Thiotepa

Thorazine see Chlorpromazine

Thysin see Levothyroxine

Tiazel see Dilitiazem

Ticar see Ticarcillin

Tigan see Trimethobenzamide

Timoptic see Timolol

Tobrex see Tobramycin

Tofranil see Imipramine

Togepen see Cloxacillin

Tolectin see Tolmetin

Tonocard see Tocainide

Toposar see Etoposide

Toprol see Metoprolol

Toradol see Ketorolac

Tornalate see Bitolterol

Totacillin see Ampicillin

Trandate see Lebetolol

Transderm-Nitro see Nitro-

glycerin (Transdermal)

Transderm-Scop see Scopola-

mine

Tranxene see Clorazepate

Tridil see Nitroglycerin

Trilafon see Perphenazine

Trimox see Amoxicillin

Trimpex see Trimethoprim

Trinalin see Azatadine

Tri-Norinyl see Estrogen-

Progestin

Triostat see Liothyronine

Triphasil see Estrogen-

Progestin

Tristoject see Triamcinolone

Tritec see Ranitidine

Tropol see Metoprolol

T-Stat see Erythromycin

Tubocurarine see Tubocurarine

Tussar see Codeine

xxvi BRAND NAMES

FM.qxd 7/6/01 9:24 AM Page xxvi

Ultram see Tramadol

Unasyn see Ampicillin, Sul-

bactam

Unipen see Nafcillin

Univasc see Moexipril

Urecholine see Bethanechol

Uticort see Betamethasone

Valergen see Estradiol

Valisone see Betamethasone

Valium see Diazepan

Valrelease see Diazepam

Valtrex see Valacyclovir

Vancenase see Beclometha-

sone

Vanceril see Beclomethasone

Vancocin see Vancomycin

Vancoled see Vancomycin

Vantin see Cefpodoxime

Vascor see Bepridil

Vasotec see Enalapril

V-Cillin see Penicillin V

Veetids see Penicillin V

Velban see Vinblastine

Ventolin see Albuterol

Vepesid see Etoposide

Verelan see Verapamil

Vermox see Mebendazole

Versed see Midazolam

Vesprin see Triflupromazine

Vexol see Rimexolone

V-Gan see Promethazine

Viagra see Sildenafil

Vibramycin see Doxycycline

Vioxx see Rofecoxib

Vira-Asee Vidarabine

Virilon IM see Testosterone

Visken see Pindolol

Vistacon see Hydroxyzine

Vistaril see Hydroxyzine

Vivactil see Protriptyline

Volina see Albuterol

Voltaren see Diclofenac

Wellbutrin see Bupropion

Wellcovorin see Leucovorin

Westcort see Hydrocortisone

Wigraine see Ergotamine

Wycillin see Penicillin G Pro-

caine

Wydase see Hyaluronidase

Wygesic see Propxythphene

Wymox see Amoxicillin

Xanax see Alprazolam

Xanthotoxin see Methoxsalen

Xenical see Orlistat

Xylocaine see Lidocaine

Yutopar see Ritodrine

Zagam see Sparfloxacin

Zantac see Ranitidine

Zaroxolyn see Metolazone

Zeasorb-AF see Miconazole

Zebutal see Butabarbital

Zemuron see Rocuronium

Zerit see Stavudine

Zestril see Lisinopril

Zetran see Diazepam

Zinacef see Cefuroxime

Zithromax see Azithromycin

BRAND NAMES xxvii

FM.qxd 7/6/01 9:24 AM Page xxvii

Zocor see Simvastatin

Zofran see Ondansetron

Zoloft see Sertraline

Zomig see Zolmitriptan

Zovirax see Acyclovir

Zyban see Bupropion

Zyloprim see Allopurinol

Zyrtec see Cetirizine

xxviii BRAND NAMES

FM.qxd 7/6/01 9:24 AM Page xxviii

Acebutolol

Brand name: Sectral.

Class of drug: β-Adrenergic receptor blocker.

Mechanism of action: Competitive blocker of β adrenergic

receptors in heart and blood vessels.

Indications/dosage/route: Oral only.

•Hypertension

Ð Adults: Initial: 400 mg/d. Maintenance: 200–1200 mg/d.

•Premature ventricular contractions

Ð Adults: Initial: 200 mg b.i.d. Maintenance: 600–1200 mg/d.

Adjustment of dosage

•Kidney disease: Creatinine clearance 25–50 mL/min: decrease

dose by 50%; creatinine clearance <25 mL/min: decrease dose

by 75%.

•Liver disease: None.

•Elderly: Avoid doses >800 mg/d.

•Pediatric: Safety and efficacy have not been established in children.

Food: No restriction.

Pregnancy: Category B.

Lactation: Appears in breast milk. Potentially toxic to infant.

Considered compatible by the American Academy of Pediatrics.

Observe infant for hypotension, bradycardia.

Contraindications: Cardiogenic shock, CHF unless it is second-

ary to tachyarrhythmia treated with a βblocker, sinus bradycardia

and AVblock greater than first degree, severe COPD.

Warnings/precautions

•Use with caution in patients with the following conditions: dia-

betes, kidney disease, liver disease, COPD, peripheral vascular

disease.

•Do not stop drug abruptly as this may precipitate arrhythmias,

angina, MI or cause rebound hypertension. If necessary to dis-

continue, taper as follows: reduce dose and reassess after

1–2 weeks; if status is unchanged, reduce by another 50% and

reassess after 1–2 weeks.

ACEBUTOLOL 1

CH-A.qxd 7/6/01 9:25 AM Page 1

•Drug may mask the symptoms of hyperthyroidism, mainly

tachycardia.

•Drug may exacerbate symptoms of arterial insufficiency in

patients with peripheral or mesenteric vascular disease.

Advice to patient

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Dress warmly in winter and avoid prolonged exposure to cold

as drug may cause increased sensitivity to cold.

•Avoid drinks that contain xanthines (caffeine, theophylline,

theobromine) including colas, tea, and chocolate because they

may counteract the effect of the drug.

•Restrict dietary sodium to avoid volume expansion.

•Drug may blunt response to usual rise in blood pressure and

chest pain under stressful conditions such as vigorous exercise

and fever.

Adverse reactions

•Common: fatigue.

•Serious: symptomatic bradycardia, CHF, worsened AVblock,

hypotension, depression, bone marrow depression, SLE-like

condition, bronchospasm, Peyronie’s disease, hepatitis.

Clinically important drug interactions

•Drugs that increase effects/toxicity of beta blockers: reserpine,

bretylium, calcium channel blockers.

•Drugs that decrease effects/toxicity of beta blockers: aluminum

salts, calcium salts, cholestyramine, barbiturates, NSAIDs,

rifampin.

Parameters to monitor

•Liver enzymes, serum BUN and creatinine, CBC with differ-

ential and platelets.

•Patient’s pulse rate near end of dosing interval or before next

dose is taken. Areasonable target is 60–80 bpm for resting

apical ventricular rate. If severe bradycardia develops, consider

treatment with glucagon, isoproterenol, IVatropine (1–3 mg in

divided doses). If hypotension occurs despite correction of

2 ACEBUTOLOL

CH-A.qxd 7/6/01 9:25 AM Page 2

bradycardia, administer vasopressor (norephinephrine, dopa-

mine, or dobutamine).

•Symptoms of CHF. Digitalize patient and administer a diuretic

or glucagon.

•Efficacy of treatment: decreased blood pressure, decreased

number and severity of anginal attacks, improvement in exer-

cise tolerance. Confirm control of arrhythmias by ECG, apical

pulse, BP, circulation in extremities, and respiration. Monitor

closely when changing dose.

•Central nervous system effects. If patient experiences mental

depression reduce dosage by 50%. The elderly are particularly

sensitive to adverse CNS effects.

•Signs of bronchospasm. Stop therapy and administer large

doses of β-adrenergic bronchodilator, eg, albuterol, terbutaline,

or aminophylline.

•Signs of cold extremities. If severe, stop drug. Consider β

blocker with sympathomimetic property.

Editorial comments

•Stopping a β blocker before surgery is controversial. Some

advocate discontinuing the drug 48 hours before surgery;

others recommend withdrawal for a considerably longer time.

Notify anesthesiologist that patient has been on βblocker.

•β Blockers are first-line treatments for hypertension, par-

ticularly in patients with the following conditions:

previous MI, ischemic heart disease, aneurysm, atrioven-

tricular arrhythmias, migraine. These are drugs of first

choice for chronic stable angina, used in conjunction with

nitroglycerin.

•Many studies indicate benefit from administration of a β

blocker following an MI.

•β Blockers are considered to be first-line drugs for prophylaxis

of migraine headache in patients who have two or more attacks

per month.

•Note that this drug is pregnancy category B (most β blockers

are category C).

ACEBUTOLOL 3

CH-A.qxd 7/6/01 9:25 AM Page 3

Acetohexamide

Brand name: Dymelor.

Class of drug: Oral hypoglycemic agent, second generation.

Mechanism of action: Stimulates release of insulin from pancre-

atic beta cells; decreases glucose production in liver; increases

sensitivity of receptors for insulin, thereby promoting effective-

ness of insulin.

Indications/dosage/route: Oral only.

•Diabetes

Ð Adults: Initial: 250–1500 mg/d. Adjust dosage until optimum

control is achieved. Maximum: 1500 mg/d.

Ð Elderly: Initial, 125–250 mg/d. Adjust dosage gradually until

optimum control is achieved.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: See above.

•Pediatric: Not recommended.

Food: No restriction. Patient should be told to eat regularly and

not to skip meals. Sugar supply should be kept handy at all times.

If stomach is upset Tums should be taken with meal. Dose is best

administered before breakfast or, if taken twice a day, before the

evening meal.

Pregnancy: Category C.

Lactation: No data available. Potentially toxic to infant. Avoid

breastfeeding.

Contraindications: Hypersensitivity to the drug; diabetes com-

plicated by ketoacidosis.

Editorial comments

•This drug is not listed in Physician’s Desk Reference, 54th edi-

tion, 2000.

•For additional information, see glyburide, p. 409.

4 ACETOHEXAMIDE

CH-A.qxd 7/6/01 9:25 AM Page 4

ACETYLCYSTEINE 5

Acetylcysteine

Brand name: Mucomyst.

Class of drug: Mucolytic agent; antidote for acetaminophen

toxicity.

Mechanism of action: As mucolytic agent: disrupts disulfide

bonds in mucoproteins thereby lowering viscosity of mucus. As

antidote for acetaminophen poisoning: complexes with hepato-

toxic free radial metabolite of acetaminophen and inactivates it.

Indications/dosage/route:Oral, inhalation, IV.

•Bronchial disorders, chronic bronchitis, asthma, emphysema,

pulmonary complications of surgery

Ð Adults: 6–10 mL of 10% solution, q2–3 hours by nebulizer.

Ð Children: 3–5 mL of 10% solution, q2–3 hours by nebulizer.

Ð Infants: 2–4 mL of 10% solution, t.i.d. to q.i.d., IV.

Ð Alternate: 20% solution may be given in half of above vol-

umes.

•Antidote for acetaminophen poisoning

Ð Quaterdoze with Bronchical

Ð Adults, children: Initial: PO 140 mg/kg, then 70 mg/kg q4h. Total

of 17 doses. Complete therapy despite acetaminophen level. If

patient has emesis with 1 hour of dose, repeat dose immediately.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: None.

•Pediatric: See above.

Onset of Action Duration

5–10 min >1 h

Food: Given before meals and just before bedtime for asthma.

Pregnancy: Category B.

Lactation: No data available. Best to avoid.

CH-A.qxd 7/6/01 9:25 AM Page 5

Contraindications: As mucolytic agent: hypersensitivity to

acetylcysteine.

Warnings/precautions

•As antidote for acetaminophen poisoning: Administer as

quickly as possible. Most useful if given within 12 hours of

ingestion of acetaminophen.

•As inhaled drug: may induce bronchospasm. If this occurs,

administer bronchodilator; suction bronchial secretions if they

develop after inhalation.

•Elderly: May have reduced cough reflex and therefore reduced

ability to clear airway of liquefied mucus. May need concomi-

tant suction.

•For patient with asthma or hyperactive airway disease, a bron-

chodilator should be administered before acetylcysteine.

Advice to patient: Rinse mouth out and wash face after treatment

to remove adhering drug.

Adverse reactions

•Common: vomiting, olfactory disturbance.

•Serious: bronchospasm (especially in asthmatics), hypotension.

Clinically important drug interactions: None.

Parameters to monitor

•As antidote for acetaminophen poisoning: Monitor aceta-

minophen plasma levels, liver enzymes, bilirubin. Monitor

for nausea, vomiting, skin rash. Acetaminophen levels:

Determine at least 4 hours after acetaminophen ingestion.

Administer acetylcysteine if acetaminophen level is >150

mg/mL12 hours after ingestion. Hepatotoxicity occurs if peak

level is >200 mg/mL. Monitor cardiac function, renal func-

tion, prothrombin time. Administer fresh-frozen plasma or

vitamin K if prothrombin time >3 seconds compared with

control.

•As mucolytic agent: Monitor respiratory function for respiratory

fluid increases, amount and consistency of secretions before and

after treatment. Apply suction or endotrachial aspiration if nec-

essary. Signs and symptoms of bronchospasm: if this occurs,

administer bronchodilator or discontinue if necessary.

6 ACETYLCYSTEINE

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Acyclovir

Brand name: Zovirax.

Class of drug: Antiviral agent.

Mechanism of action: Nucleotide analog; inhibits viral repli-

cation by termination of viral DNA chain and inhibition and

inactivation of viral DNApolymerase.

Indications/dosage/route: Oral, IV.

•Herpes simplex (HSV-1 and HSV-2) infections (immunocom-

promised host)

Ð Adults, children >12 years: IV 5 mg/kg (infuse at constant

rate over 1 hour), q8h for 7 days.

Ð Children <12 years: IV250 mg/m

(infuse at constant rate for

1 hour), q8h.

•Genital herpes

Ð Adults, children >12 years: PO 200 mg q4h, five doses/day;

10 days for initial therapy. Dose for 5 days for intermittent

recurrent disease. Administer up to 12 months for chronic

disease (suppressive therapy).

Ð Children <12 years: IV 250 mg/m

, t.i.d. for 10 days.

•Herpes simplex encephalitis

Ð Adults, children >12 years: IV 10 mg/kg (infuse at constant

rate over 1 hour), q8h for 10 days.

Ð Children, 6 months to 12 years: IV500 mg/m

(infuse at con-

stant rate over 1 hour), q8h for 10 days.

•Herpes zoster

Ð Adults, children >12 years: PO 80 mg, q4h, five doses/day,

7–10 days.

Ð Children <12 years: PO 250–600 mg/m

, 4–5 times/day,

7–10 days.

•Chickenpox

Ð Adults, children >40 kg: PO 800 mg, q.i.d. 5 days.

Ð Children >2 years: PO 20 mg/kg q.i.d. (maximum 800 mg),

5 days.

ACYCLOVIR 7

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Adjustment of dosage

•Kidney disease: Creatinine clearance 25–50 mL/min: dose

q12h; creatinine clearance 10–25 mL/min: dose q24h; crea-

tinine clearance <10 mL/min: half dose q24h (IVdoses).

•Liver disease: None.

•Elderly: None.

•Pediatric: Safety has not been established in children <2 years

old.

Food: No restrictions.

Pregnancy: Category C.

Lactation: Appears in breast milk; considered compatible by

American Academy of Pediatrics.

Contraindications: Hypersensitivity to acyclovir.

Warnings/precautions

•Use with caution in patients with the following conditions:

kidney disease, neurologic disease.

•Beware of renal dysfunction especially if patient is taking other

nephrotoxic drugs.

•Women with genital herpes should have annual Pap smears.

•Rapid bolus administration may cause crystalline precipitation

in renal tubules and renal insufficiency.

•Patients receiving acyclovir IV must remain well hydrated

during treatment and for 24 hours after treatment.

•Cases of thrombotic thrombocytopenic purpura/hemolytic

uremia syndrome have been reported with high-dose acyclovir

in immunocompromised patients.

Advice to patient

•Drink 2–3 L of fluid per day. This is particularly important fol-

lowing IVinfusion.

•Avoid sexual intercourse when lesions are present; otherwise

use condoms.

•Avoid contact of the drug with or around the eyes.

•Resume treatment at first indication of recurrence of infec-

tion.

Adverse reactions

•Common: headache, phlebitis (IV only).

8 ACYCLOVIR

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•Serious: seizures, renal failure, anaphylaxis, encephalopathy

(confusion, hallucinations), coma, leukopenia, renal crystalline

precipitant, elevated liver enzymes, Stevens–Johnson syn-

drome, urticaria.

Clinically important drug interactions

•Drugs that increase effects/toxicity of acyclovir: MAO inhibitors,

probenecid, ziduvine, CNS depressants.

•Drugs that decrease effects/toxicity of acyclovir: β blockers,

guanethidine.

Parameters to monitor

•Serum BUN and creatinine, CBC with differential and platelets,

liver enzymes.

•Signs and symptoms of ocular herpetic infection as this may

cause blindness.

•Serum creatinine level: If this increases during therapy, adjust

dose, increase hydration or discontinue drug.

•Signs and symptoms of hepatotoxicity.

•Signs and symptoms of renal toxicity.

•Signs and symptoms of drug-induced psychologic distur-

bances: Changes in mood, behavior or orientation of patient,

agitation, hallucinations, suicidal tendencies, sleep disturbances,

lethargy.

•Intake of fluids and urinary and other fluids. Closely monitor

electrolyte levels.

Adenosine

Brand name: Adenocard.

Class of drug: Antiarrhythmic.

Mechanism of action: Vagolytic effect: Slows conduction

through AVnode; prevents reentry through AVnode. Restores

normal sinus rhythm in patients with paroxysmal supraventric-

ular tachycardia including Wolff–Parkinson–White syndrome.

Indications/dosage/route: IV only.

ADENOSINE 9

CH-A.qxd 7/6/01 9:25 AM Page 9

•Paroxysmal supraventricular tachycardia

Ð Adults: bolus of 6 mg. If no effect after 1–2 min, 12-mg

bolus. May repeat 12-mg dose ×2.

Ð Child: bolus of 0.05 mg/kg; repeat dosage every 2 min. Maximum

0.25 mg/kg (not approved).

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: None.

•Pediatric: See above.

Onset of Action Peak Effect Duration

10 s No data 10–20 s

Pregnancy: Category C.

Lactation: Unlikely to be problematic.

Contraindications: Second- or third-degree AV block (without

pacemaker), sick sinus syndrome, symptomatic bradycardia.

Warnings/precautions

•Use with caution in patients with the following condition:

stroke, asthma, unstable angina (higher risk of arrythmias, MI).

•Cardiac arrest (including fatalities), ventricular tachycardia,

and MI have been reported coincident with use.

•May produce transient first-, second-, third-degree AVblock.

•Asystole has been reported in atrial flutter when given with

carbamazepine.

•Use cautiously in patients receiving digoxin and/or verapamil.

•May cause ventricular fibrillation.

•Resuscitative equipment should be readily available when adeno-

sine is administered.

•May produce hypotension or hypertension as side effects.

•May cause bronchoconstriction in patients with asthma or COPD.

Adverse reactions

•Common: facial flushing (18%), nausea, hyperventilation, tho-

racic constriction, palpitations.

10 ADENOSINE

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•Serious: hypotension, dyspnea (12%), heart block, ventricu-

lar fibrillation, asystole, hypertension.

Clinically important drug interactions

•Drugs that increase effects/toxicity of adenosine: carba-

mazepine, digoxin, verapamil, dipyridamole.

Parameters to monitor: ECG for signs and symptoms of AV

block and increased arrhythmias when converting to normal

sinus rhythm.

Editorial comments

•Adenosine is highly useful as an acute antiarrhythmic agent.

•In narrow complex supraventricular tachycardia, it can be

used simultaneously to diagnose the mechanism and to ter-

minate it.

•Because it can terminate some catecholamine-requiring ven-

tricular tachycardias, it can be safely used in wide complex

tachycardia as well.

•It is necessary to inject adenosine rapidly by peripheral IV

route followed by saline bolus because of its short half-life.

Solution should be checked for presence of crystals; if present,

warm solution. Do not inject if crystals are present.

Albendazole

Brand name: Albenza.

Class of drug: Anthelmintic.

Mechanism of action: Inhibits uptake of glucose and other nutri-

ents by parasitic helminths.

Indications/dosage/route: Oral only.

•Hydatid disease

Ð Adults ≥ 60 kg: 400 mg b.i.d. with meals, 28-hour cycle fol-

lowed by 14-day drug-free interval for total of 3 cycles.

Ð Adults <60 kg: 15 mg/kg/d in divided doses b.i.d. with meals.

Maximum total daily dose: 800 mg.

•Neurocysticercosis

ALBENDAZOLE 11

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Ð Adults ≥ 60 kg: 400 mg b.i.d. with meals, 8–30 days.

Ð Adults < 60 kg: 50 mg/kg/d in divided doses b.i.d. with

meals. Maximum total daily dose: 800 mg.

Food: Take with food.

Pregnancy: Category C.

Lactation: Probably present in breast milk. Best to avoid.

Contraindications: Hypersensitivity to mabendazole.

Editorial comments: For additional information, see mebenda-

zole, p. 550.

Albuterol

Brand names: Proventil, Ventolin.

Class of drug: β-adrenergic agonist, bronchodilator.

Mechanism of action: Relaxes smooth muscles of the bronchi-

oles by stimulating β

-adrenergic receptors.

Indications/dosage/route: Oral, inhalation

•Bronchodilation

Ð Adults, children >12 years: 2 inhalations q4–6h.

•Prophylaxis of exercise-induced bronchospasm

Ð Adults, children >12 years: 2.5 mg t.i.d. to q.i.d. by nebu-

lization.

•Bronchodilation: Capsule for inhalation

Ð Adults, children >12 years: 200 µg q4–6h.

•Prophylaxis of exercise-induced bronchospasm

Ð Adults, children >12 years: 200 µg 15 minutes before exercise.

•Bronchodilation: syrup

Ð Adults, children >14 years: 2–4 mg t.i.d. to q.i.d.

Ð Children 2–6 years: Initial: 2–4 mg, Maximum: 8 mg t.i.d. to q.i.d.

Ð Children 6–12 years: 4 mg q12h. Maximum: 12 mg q12h.

Ð Elderly: Initial: 2 mg t.i.d. to q.i.d. Increase dose if needed to

maximum of 8 mg t.i.d. to q.i.d.

•Bronchodilation: extended-release tablets

12 ALBUTEROL

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Ð Adults, children >12 years: 4–8 mg q12h. Maximum: 32 mg/d.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: See above.

•Pediatric: See above.

Onset of Action Duration

<30 min Inhalation 4–8 h

<5 min oral 3–8 h

Food: Not applicable.

Pregnancy: Category C.

Lactation: No data available. Other drugs in the same class such

as terbutaline are considered compatible with breastfeeding.

Contraindications: Hypersensitivity to adrenergic compounds.

Warnings/precautions

•Use with caution in patients with the following conditions:

hyperthyroidism, diabetes, coronary insufficiency, ischemic

heart disease, history of stroke, CHF, hypertension.

•Some preparations contain bisulfite, which may cause an aller-

gic reaction in sensitive individuals.

•Instruct patient in proper technique for using nebulizer and/or

inhaler.

Advice to patient

•Avoid OTC products without consulting treating physician.

•Do not use solutions that contain a precipitate or are discolored.

•Contact treating physician if more than 3 inhalations are

required within a 24-hour period to obtain relief.

•Wait at least 1 minute after 1 or 2 inhalations before taking a

third dose.

•Keep spray away from eyes.

•Maintain adequate fluid intake (2000–3000 mL/d) to facilitate

clearing of secretions.

ALBUTEROL 13

CH-A.qxd 7/6/01 9:25 AM Page 13

•Rinse mouth with water after each inhalation to minimize dry

mouth and throat irritation.

•Administer inhalant when arising in the morning and before

meals.

•Do not increase dose in an attempt to obtain relief.

Adverse reactions

•Common: tremor.

•Serious: hypotension, bronchospasm.

Clinically important drug interactions:

•Drugs that increase effects/toxicity of β agonists: inatropium,

MAO inhibitors, tricyclic antidepressants.

•Drugs that decrease activity of beta agonists: sympathomimetic

drugs (nasal decongestants, weight loss drugs, eg, phenylpropa-

nolamine), anticholinergic drugs, phenothiazines.

Parameters to monitor

•Monitor patient for possible development of tolerance with

prolonged use. Discontinue drug temporarily and effectiveness

will be restored.

•Signs of paradoxical bronchospasm.

•Pulmonary function on initiation and during bronchodila-

tor therapy. Assess respiratory rate, sputum character

(color, quantity), peak airway flow, O

saturation and blood

gases.

•Efficacy of treatment: Improved breathing, prevention of bron-

chospasm, reduction of asthmatic attacks, prevention of

exercise-induced asthma. If no relief is obtained from 3–5

aerosol inhalations within 6–12 hours, reevaluate effectiveness

of treatment.

•FEV

rate to determine effectiveness of the drug to reverse

bronchostriction. Efficacy is indicated by an increase in FEV

of 10–20%. In addition such patients, as well as those who

have chronic disease, should be given a peak flow gauge and

told to determine peak expiratory flow rate at least twice

daily.

Editorial comments: For patients with acute asthma or acute exac-

erbation of COPD, reduce dose to minimum necessary to control

14 ALBUTEROL

CH-A.qxd 7/6/01 9:25 AM Page 14

condition after initial relief is achieved. For chronic conditions,

the patient should be reassessed every 1–6 months following con-

trol of symptoms.

Alendronate

Brand name: Fosamax.

Class of drug: Bisphosphonate derivative/treatment for osteo-

porosis.

Mechanism of action: Inhibits osteoclast activity. Decreases

bone resorption and increases bone mass.

Indications/dosage/route: Oral only.

•Treatment and prevention of osteoporosis

Ð Adults: 10 mg/d.

Ð Elderly: 10 mg/d.

Ð Children: Safety and effectiveness not established in children

<18 years.

•Paget’s disease

Ð Adults: 40 mg/d, 6 months.

Adjustment of dosage

•Kidney disease: Not given if creatinine clearance <35 mL/min.

No adjustment of dosage needed for creatinine clearance >35

mL/min.

•Liver disease: None necessary.

•Elderly: None.

•Pediatric: See above.

Food: Drug must be taken at least 30 minutes before the first

food, beverage, or medicine of the day with full glass of water.

Must be in upright position for 30 minutes following ingestion.

Pregnancy: Category C.

Lactation: No data available. Best to avoid.

Contraindications: Hypersensitivity to biphosphonates, hypocal-

cemia, esophageal stricture or delayed esophageal emptying

(achalasia), inability to sit or stand up for at least 30 minutes

ALENDRONATE 15

CH-A.qxd 7/6/01 9:25 AM Page 15

followingingestion, marked renal impairment (serum creatinine

>5 mg/dL, creatinine clearance <35 mL/min).

Warnings/precautions

•Safety of alendronate in combination with hormone replace-

ment therapy has not been established.

•Hypocalcemia or vitamin D deficiency must be corrected prior

to treatment.

•May cause severe esophagitis if adequate esophageal transient

not present. Cases of GI bleeding due to esophageal irritation

have been reported. Screen patients for symptoms of esophageal

stricture or motility disorder (dysphagia, noncardiac chest

pain) prior to use. Patients should be advised to report symp-

toms of chest pain, dysphagia, odynophagia, or GI bleeding

ifthese occur while taking alendrondrate.

•Patient’s with Paget’s disease are at risk for GI side effects and

muscle or bone pain.

Advice to patient

•Maintain adequate intake of calcium and vitamin D.

•Take calcium supplement at least 30 minutes after drug ingestion.

•Do not lie down until at least 30 minutes after taking this drug.

•Perform weight bearing exercises as a means of increasing

bone mass.

•Stop smoking and decrease alcohol intake.

Adverse reactions

•Common: none.

•Serious: esophageal ulcer, GI bleeding.

Clinically important drug interactions

•Drugs that increase effects/toxicity of alendronate: ranitidine,

aspirin.

•Drugs that decrease effects/toxicity of alendronate: conco-

mitant calcium supplements, antacids.

•Because a variety of medications may decrease the absorption

of alendronate, patients must wait at least 30 minutes after

taking medications before taking alendronate.

Parameters to monitor

•Patient with Paget’s disease: Check alkaline phosphatase levels

periodically.

16 ALENDRONATE

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•Efficacy of treatment in patients with Paget’s disease:

Reductionin bone pain and headache, impaired visual or audi-

tory acuity.

•Perform serial bone densitometry and or skeletal radiography.

•Monitor calcium phosphate on regular basis. Consider obtain-

ing 24-hour urine calcium and vitamin D levels.

Editorial comments

•Before treating for osteoporosis, confirm diagnosis by meas-

uring bone mass. History of bone fractures is also suggestive

of osteoporosis.

•Diagnosis of Paget’s disease depends on the following find-

ings: alkaline phosphatase level at least twice that of the upper

normal range, characteristic radiography.

Alfentanil

Brand name: Alfenta.

Class of drug: Narcotic analgesic, agonist.

Mechanism of action: Binds to opiate receptors and blocks

ascending pain pathways. Reduces patient’s perception of pain

without altering cause of the pain.

Indications/dosage/route: IV only.

•Induction of anesthesia

Ð Initial: 50–75 µg/kg, continuous infusion, ≥ 45 min. Maintenance

(with nitrous oxide/oxygen): 0.5–3 µg/kg/min.

•Induction of anesthesia, ≥ 45 min.

Ð Initial: 130–245 µg/kg. Maintenance: 0.5–1.5 µg/kg/min.

•Anesthetic adjunct, 30–60 minutes, incremental injection

Ð Initial: 20–50 µg/kg. Maintenance: 5–15 µg/kg. Total dose:

75 µg/kg.

•Anesthetic adjunct, <30 min.

Ð Initial: 8–20 µg/kg. Maintenance: 3–5 µg/kg. Total dose:

8–40 µg/kg.

ALFENTANIL 17

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Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: None.

•Pediatric: Not used in children <12.

Onset of Action Peak Effect Duration

Immediate No data No data

Food: Not applicable.

Pregnancy: Category C. Category D if prolonged use or if given

in high doses at term.

Contraindications: Hypersensitivity to narcotics of the same

chemical class.

Warnings/precautions

•Use with caution in patients with the following conditions:

head injury with increased intracranial pressure, serious alco-

holism, prostatic hypertrophy, chronic pulmonary disease,

severe liver or kidney disease, postoperative patients with pul-

monary disease, disorders of biliary tract.

•Administer drug before patient experiences severe pain for

fullest efficacy of the drug.

•Nausea, vomiting, and orthostatic hypotension occur most promi-

nently in ambulatory patients. If nausea and vomiting persist,

it may be necessary to administer an antiemetic, eg, droperidol

or prochlorperazine. This drug can cause severe hypotension

in a patient who is volume depleted or if given along with a

phenothiazine or general anesthesia.

•Careful diagnosis must be made of acute abdominal condition

before this drug is administered.

Special considerations: This drug should be administered only

by personnel who have experience in the use of IVand general

anesthetics as well as in the management of possible respiratory

depression by narcotic drugs. The following must be immedi-

ately available should the need arise: resuscitative and intubation

equipment, oxygen, narcotic antagonist. Patient should be

18 ALFENTANIL

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continuously monitored for oxygen saturation, vital signs, and

signs of upper airway obstruction and hypotension.

Editorial comments

•This drug is listed without detail in Physician’s Desk Reference,

54th edition, 2000.

•For additional information, see morphine, p. 633.

Allopurinol

Brand names: Zyloprim, Aloprim.

Class of drug: Treatment for gout, prophylaxsis for chemotherapy-

induced hyperuricemia.

Mechanism of action: Inhibits xanthine oxidase, the enzyme that

converts hypoxanthine to xanthine. Xanthine is a precursor for

uric acid production; thus uric acid production is decreased.

Indications/dosage/route:Oral only.

•Mild gout

Ð Adults: 200–300 mg/d.

•Moderate or severe gout

Ð Adults: 400–600 mg/d.

•Prophylaxis against acute attack

Ð 100 mg/d. Maximum: 800 mg/d.

•Prevention of hyperuricemia during cancer chemotherapy

Ð Adults, children >10 years: 600–800 mg/d, 2–3 divided

doses, 1–2 days before chemotherapy for 2–3 days. IV

200–400 mg/m

/d.

Ð Children <10 years: 200–300 mg/m

/d, 2–4 divided doses.

IV200–300 mg/m

/d.

Adjustment of dosage

•Kidney disease: Adjust dosage in relation to creatinine clearance.

Reduce standard dose (300 mg/d) by 50 mg for each 20 mL/min.

decrease in creatinine clearance below 100 mL/min. (Example:

Creatinine clearance = 60; give 200 mg allopurinol/d). Creatinine

clearance <20 mL/min: give q2d or q3d.

ALLOPURINOL 19

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•Liver disease: None.

•Elderly: Maximum 200 mg/d.

•Pediatric: See above.

Onset of Action

48–72 h for decline of serum uric acid level,

1–3 wk to achieve proper level

Food: Take with meals or immediately after eating. Have patient

drink large amounts of fluids.

Contraindications: Hypersensitivity to allopurinol; idiopathic

hemochromatosis.

Warnings/precautions

•Discontinue at first sign of rash.

•Use drug in children only to treat hyperuricemia associated

with chemotherapy.

Advice to patient

•Avoid driving and other activities requiring mental alertness

or that are potentially dangerous until response to drug is

known.

•Limit foods with high purine content (liver or other organ

meats, salmon, sardines).

•Drink large quantities of water (10–12 glasses per day).

•Do not take large amounts of vitamin C.

•Avoid alcohol and other CNS depressants such as opiate anal-

gesics and sedatives (eg, diazepam [Valium]) when taking this

drug.

•Do not take iron salts while on allopurinol.

•Limit intake of caffeine and alcohol.

•Limit exposure to UV light as this may increase the risk of

cataracts.

Pregnancy: Category C.

Lactation: Appears in breast milk. Considered compatible by

American Academy of Pediatrics.

Adverse reactions

•Common: skin rash (generally maculopapular).

20 ALLOPURINOL

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•Serious: agranulocytosis, aplastic anemia, thrombocytopenia,

hepatic injury, Stevens–Johnson syndrome, vasculitis, toxic

epidermal necrolysis, neuritis, cataracts, renal toxicity.

Clinically important drug interactions

•Drugs that increase effects/toxicity of allopurinol: thiazide

diurectics, ACE inhibitors, vitamin C.

•Allopurinol increases effects/toxicity of the following: ampicillin,

amoxicillin, oral anticoagulants, 6-mercaptopurine, cyclophos-

phamide,theophylline, chlorpropamide, alcohol.

Parameters to monitor

•Serum BUN and creatinine, CBC with differential and platelets,

liver enzymes.

•Renal function and liver enzymes.

•Check urinary pH for excessive alkalinity.

•Monitor for acute attacks of gout during first 4–6 weeks of

therapy. Consider colchicine as additional treatment.

•Serum uric acid levels for evidence of efficacy of treatment.

These should be determined every 1–2 weeks after beginning

therapy.

•Other evidence of efficacy of treatment: decrease in size of

tophi, relief of joint pain, increased joint mobility, reduction in

joint inflammation.

•Skin rashes: If they occur, drug may have to be discontinued

permanently. If mild, reinstitute therapy at one-half initial dose,

but if rash reappears, discontinue permanently.

•Change in vision: An ophthalmologic exam is indicated.

Editorial comments: Because the incidence of acute attacks of

gout may increase during the first few months of treatment with

allopurinol, colchicine, a uricosuric agent, or an NSAID should

be added to the regimen as a prophylactic measure.

Alprazolam

Brand name: Xanax.

ALPRAZOLAM 21

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Class of drug: Antianxiety agent, hypnotic.

Mechanism of action: Potentiates effects of GABA in limbic

system and reticular formation.

Indications/dosage/route: Oral only.

•Anxiety disorder

Ð Adults: Initial: 0.25–0.5 mg t.i.d. Maximum: 4 mg/d.

Ð Elderly or debilitated: Initial: 0.25 mg b.i.d. to t.i.d.

•Panic disorder

–Adults: 0.5 mg t.i.d., increase to maximum of 10 mg/d.

Adjustment of dosage

•Kidney disease: Use caution.

•Liver disease: Initial: 0.25 mg, b.i.d. or t.i.d.

•Elderly: See above.

•Pediatric: Safety and efficacy have not been established in chil-

dren under 18 years.

Food: No restrictions

Pregnancy: Category D.

Lactation: Appears in breast milk. Potentially toxic to infant.

Avoid breastfeeding.

Contraindications: Hypersensitivity to benzodiazepines, preg-

nancy.

Warnings/precautions

•Use with caution in patients with the following conditions: his-

tory of drug abuse, severe renal and hepatic impairment, elderly,

neonates, infants.

•Benzodiazepines may cause psychologic and physical dependence.

•These drugs may cause paradoxical rage.

•It is best not to prescribe this drug for more than 6 months. If

there is a need for long-term therapy, evaluate patient frequently.

•Use only for patients who have significant anxiety without

medication, do not respond to other treatment, and are not drug

abusers.

Advice to patient

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Avoid alcohol and other CNS depressants such as narcotic

22 ALPRAZOLAM

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analgesics, alcohol, antidepressants, antihistamines, and bar-

biturates when taking this drug.

•Use OTC medications only with approval from the treating

physician.

•Cigarette smoking will decrease drug effect. Do not smoke

when taking this drug.

•Do not stop drug abruptly if taken for more than 1 month. If sud-

denly withdrawn, there may be recurrence of the original

anxiety or insomnia. Afull-blown withdrawal may occur con-

sisting of vomiting, insomnia, tremor, sweating, muscle spasms.

After chronic use, decrease drug dosage slowly, ie, over a period

of several weeks at a rate of 25% per week.

•Avoid excessive use of xanthine-containing foods (regular

coffee, tea, chocolate) as these may counteract the action of the

drug.

Adverse reactions

•Common: drowsiness, lightheadedness, depression, headache.

•Serious: depression, respiratory depression, apnea, hallucina-

tions, hepatitis, seizures, hostile behavior, Stevens–Johnson

syndrome.

Clinically important drug interactions

•Drugs that increase effects/toxicity of benzodiazepines: CNS

depressants (alcohol, antihistamines, narcotic analgesics, tri-

cyclic antidepressants, SSRIs, MAO inhibitors), cimetidine,

disulfiram.

•Drugs that decrease effects/toxicity of benzodiazepines:

flumazenil (antidote for overdose), carbamazepine.

Parameters to monitor

•Signs of chronic toxicity: ataxia, vertigo, slurred speech.

•Monitor dosing to make sure amount taken is as prescribed par-

ticularly if patient has suicidal tendencies.

•Monitor patient for efficacy of treatment: reduced symptoms

of anxiety and tension, improved sleep.

•Signs of physical/psychologic dependence, particularly if

patient is addiction-prone and requests frequent renewal of pre-

scription or is experiencing a diminished response to the drug.

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•Patient’s neurologic status including the following: memory

(anterograde amnesia), disturbing thoughts, unusual behavior.

•Possibility of blood dyscrasias: fever, sore throat, upper respi-

ratory infection. Perform total and differential WBC counts.

Editorial comments

•Alprazolam appears to have some antidepressant effects and is

indicated for anxiety associated with depression.

•The side effect profile of alprazolam appears better than that

of some other benzodiazepines.

•Seizures may occur if flumazenil is given after long term use

of benzodiazepines.

Alprostadil

Brand names: Caverject, Prostin VR Pediatric, Muse (urethral

suppository).

Class of drug: Prostaglandin; vasodilator for erectile dysfunction.

Mechanism of action: Causes vasodilation by activating

prostaglandin receptors in blood vessels, increases nitric oxide

in smooth muscle.

Indications/dosage/route: IV, intracavernosal, suppository.

•Maintenance of ductus arteriosus in neonate before cardiac

surgery

Ð Continuous IV into large vein or umbilical artery: 0.05–0.1

µg/kg/min. Reduce dose after achieving therapeutic goal.

Maintain at 0.01–0.4 µg/kg/min.

•Erectile dysfunction: intracavernosal before intercourse.

–1–400 mg. Initial: 2.5 µg. Inject over 5–10 s. Incremental

increases by 10–15 µg performed in physicians office.

Ð Urethral suppository: 125, 250,500, or 1000 µg.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: Higher doses may be required. Use same initial doses.

•Pediatric: Contraindicated.

24 ALPROSTADIL

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Onset of Action

15 min– 3 h

Pregnancy: Category X.

Lactation: No data available. Do not breastfeed.

Contraindications: Hyaline membrane disease in neonate,

penile implant, adult respiratory distress syndrome, bleeding

tendencies, pregnancy.

Warnings/precautions

•Use with caution in patients with the following conditions:

neonates with bleeding tendencies, history of leukemia, sickle

cell disease.

•Apnea may occur in greater than 10% of neonates with

congenital heart defects, especially those <2 kg at birth.

This usually presents during the first hour of infusion of

alprostadil.

•Priapism may occur with intracavernous injections and must be

treated quickly to avoid permanent penile damage.

•Do not use intercavernous injections more than 3 or 4 times a

week.

•Use alternate sides of penis for injection.

•When drug is administered for maintenance of ductus arterio-

sus, equipment for artificial ventilation should be immediately

available.

Advice to patient

•Use two forms of birth control including hormonal and barrier

methods.

•Contact physician if priapism lasts more than 6 hours or if

patient observes presence of nodules in penis or swelling or

curvature of the erect penis.

Adverse reactions

•Common: IV: flushing, fever. Intracavernosal: penile pain, URI.

•Serious: IV: apnea, depression, cardiac arrest, DIC, seizures,

hypotension, cerebral bleeding, arrythmia, hypokalemia, shock,

hypoglycemia, peritonitis. Intracavernosal: prolonged erection,

priapism.

ALPROSTADIL 25

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Parameters to monitor

•For IV administration: Monitor arterial pressure (umbilical

artery) and respiratory status, respiratory rate, lung sounds,

arterial blood gases.

•Signs and symptoms of overdose in infant receiving the drug for

ductus arteriosus treatment: bradycardia, apnea, flushing, hyper-

pyrexia, hypotension. Stop if apnea or bradycardia occurs.

Otherwise, reduce rate of administration.

•Efficacy of treatment for ductus arteriosus: closure of ductus

about 1–2 hours after administration as indicated by improved

oxygenation, improved urine output, improved circulation to

extremities.

•Rectal temperature for hyperpyrexia.

•Signs and symptoms of catheter displacement for IV adminis-

tration.

•Efficacy in treatment of erectile dysfunction: Erection 5–20

minutes after administration, duration no more than 1 hour.

•Monitor for possible erectile dysfunction, cavernosal fibrosis,

Peyronie’s disease, penile angulation.

Editorial comments: The first injection to determine proper

dose for erectile dysfunction should be done in the office under

physician supervision.

Alteplase

Brand name: Activase.

Class of drug: Thrombolytic agent.

Mechanism of action: Converts fibrin-bound plasminogen to

plasmin, which initiates local fibrinolysis (clot dissolution).

Indications/dosage/route: IV only.

•Acute myocardial infarction: accelerated infusion:

Ð Adults weighing more than 65 kg: Infuse 15 mg over 1–2

minutes; infuse 50 mg over next 30 min. Begin heparin

26 ALTEPLASE

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5000–10,000 units IVbolus followed by continuous infu-

sion of 1000 units/h. Infuse 35 mg alteplase over next

hour.

Ð Adults weighing less than 65 kg: Infuse 15 mg over 1–2 min-

utes; follow with 0.75 mg/kg over next 30 minutes. Begin

heparin 5000–10,000 units by IVbolus followed by contin-

uous infusion of 1000 units/h. Infuse 0.5 mg/kg alteplase

over next hour.

•Acute myocardial infarction: 3-hour infusion

Ð Adults weighing more than 65 kg: 60 mg over the first hour,

of which 6–10 mg is administered as bolus over first 1–2

minutes, 20 mg over the second hour and 20 mg over the

third hour.

Ð Adults weighing less than 65 kg: 1.25 mg/kg over 3 hours as

described for those weighing more than 65 kg.

•Acute ischemic stroke (acute ischemic stroke in highly selected

populations is still under investigation though early reports are

excellent)

Ð Adults: 0.9 mg/kg infused over 60 minutes; 10% of the dose should

be given as bolus over the first minute. Maximum dose 90 mg.

•Pulmonary embolism

Ð Adults: 100 mg by IV infusion over 2 hours. Begin heparin,

continuous infusion, 1300 units/h when PT or PTT falls to

less than twice the control time.

Adjustment of dosage

•Kidney disease: Use with caution.

•Liver disease: Use with caution.

•Elderly: Use with caution.

•Pediatric: Safety and effectiveness have not been determined

for children.

Onset of Action Peak Effect Duration

Immediate 40–50 min No known

Food: Not applicable.

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Pregnancy: Category B (listed as C by manufacturer).

Lactation: It is not known whether alteplase is excreted in breast

milk. However, not likely to be relevant.

Contraindications

•Patients treated for acute MI, pulmonary embolism, active inter-

nal bleeding, history of cerebrovascular accident, recent

intracranial or intraspinal surgery or trauma, intracranial neo-

plasm, arteriovenous malformation or aneurysm, known

bleeding diathesis, severe uncontrolled bleeding, severe uncon-

trolled hypertension.

•Patients treated for acute ischemic stroke: intracranial hemor-

rhage, recent intracranial or intraspinal surgery, serious head

trauma, previous stroke, uncontrolled hypertension (systolic

>185, diastolic >110), seizure at onset of stroke, active inter-

nal bleeding, intracranial neoplasm, arteriovenous aneurysm,

known bleeding diathesis, heparin administration within 48 hours

preceding stroke, platelet count <100,000/mm

Warnings/precautions

•Use with caution in patients with the following conditions:

internal bleeding (intracranial, retroperitoneal, gastrointesti-

nal, genitourinary, or respiratory tracts), superficial bleeding

(venouscutdown sites, arterial punctures), recent major surgery

(coronary artery bypass graft, obstetric delivery), cerebrovas-

cular disease, mitral stenosis with atrial fibrillation, acute

pericarditis,hemorrhagic ophthalmic conditions, concomitant

administration of anticoagulants.

•Cardiac and blood pressure monitors are required when using

this drug.

•Dose should be limited to 100 mg. Doses of 150 mg or greater

have been shown to increase intracranial bleeding.

•Administer with great caution during the first 10 days postpar-

tum.

•Discontinue administration immediately if local pressure does

not control bleeding.

•Initiate therapy as soon as possible after stroke symptoms are

apparent and no more than 3 hours after onset of stroke symp-

toms. After MI, therapy should be initiated within 7 hours.

28 ALTEPLASE

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•An electronic measuring devise should be used for IV infu-

sions.

•Invasive procedures such as arterial puncture or venipunc-

ture should be conducted with care when administering this

drug.

•Obtain values for the following parameters before administering

this drug: CBC, PT, PTT, creatinine phosphokinase, fibrino-

gen, cardiac isoenzymes.

Advice to patient: Not applicable.

Adverse reactions

•Common: None.

•Serious: GU, retroperitoneal, intracranial bleeding, anaphylactic

reactions, urticaria, worsening cardiovascular, cerebrovascular

or pulmonary conditions (may be due to underlying illness).

Clinically important drug interactions: The following drugs

increase effects/toxicity of alteplase: warfarin, aspirin, ticlopi-

dine, dipyridamole, heparin.

Parameters to monitor

•Coagulation parameters: CBC, PT, PTT, INR, fibrinogen. PT

or PTT should be less than twice control values for those

patients treated for pulmonary embolism.

•Monitor BP frequently and maintain at less than 180 mm sys-

tolic, 100 mm diasystolic.

•Monitor ECG for signs of reperfusion after coronary thrombol-

ysis and for arrhythmias, eg, sinus bradycardia, ventricular

arrhythmias.

Editorial comments

•Thrombolytic therapy has been thoroughly investigated. Large

randomized trials have been completed and clearly indicate the

efficacy of alteplase and streptokinase.

•Alteplase is easy to infuse and the sooner an effective steady state

of the drug is achieved, the more rapidly an occluded artery

opens. There is a higher risk of intracerebral hemorrhage with tPA

(about 1%) when compared with streptokinase or its derivatives.

•Efficacy is enhanced with rapid administration of heparin fol-

lowing a bolus over 90 minutes or 3 hours depending on the

clinical circumstances.

ALTEPLASE 29

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•Frequent and timely monitoring of coagulation parameters is

essential to minimize risk of side effects of thrombolytic therapy.

Amantadine

Brand name: Symmetrel.

Class of drug: Treatment for Parkinson’s disease, antiviral

agent.

Mechanism of action: Anti-Parkinson action: promotes

release of dopamine in substantia nigra. Antiviral action: pre-

vents viral penetration of influenza Avirus into target host

cells.

Indications/dosage/route: Oral only.

•Parkinson’s disease

Ð Adults: 100 mg b.i.d., may be titrated up. Maximum: 400

mg/d.

•Influenza A:

Ð Adults: 200 mg/d, single or divided dose.

Ð Children 1–9 years: 4.4–8.8 mg/d. Maximum: 150 mg/d.

Adjustment of dosage:

•Kidney disease: reduce dose as follows. Creatinine clearance

30–50 mL/min: initial 200 mg, then 100 mg/d; creatinine clear-

ance 15–29 mL/min: initial 200 mg, then 100 mg q.i.d.;

creatinine clearance <15 mL/min: 200 mg q7d.

•Liver disease: None

•Elderly: Dosage should be divided as twice daily administration.

•Pediatric: See above

Onset of Action:

Parkinson’s disease:<2 d.

Food: No information available.

Pregnancy: Category C.

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Lactation: Appears in breast milk; best to avoid.

Contraindications: Hypersensitivity to amantadine, untreated

angle-closure glaucoma.

Warnings/precautions

•Use with caution in patients with the following conditions:

psychiatric disorders, liver or kidney disease, history of

epilepsy, peripheral edema, orthostatic hypotension, severe

psychosis, eczematoid dermatitis, exposure to rubella.

•There is a possibility of seizures if given with CNS stimulants

or in patients with history of epilepsy.

•Do not stop abruptly when treating Parkinson’s disease.

•Deaths from amantadine overdose have been reported. Suicide

attempts in patients taking amantadine have been reported. The

cause of these has not been determined.

Advice to patient

•Change position slowly, in particular from recumbent to

upright to minimize orthostatic hypotension.

•Sit at the edge of the bed for several minutes before standing,

and lie down if feeling faint or dizzy.

•Avoid hot showers or baths and standing for long periods. Male

patients with orthostatic hypotension may be safer urinating

while seated on the toilet rather than standing.

•Avoid alcohol and other CNS depressants (see Drug Interactions)

when taking this drug.

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Immunocompromised, elderly patients should avoid crowds,

particularly during the flu season; obtain immunizations against

influenza and pneumonia on an annual basis.

•Take last dose well before bedtime to avoid insomnia.

Adverse reactions

•Common: dizziness, insomnia.

•Serious: CHF, seizures, hallucinations, depression, psychosis,

bone marrow depression, livedo reticularis, renal toxicity.

Clinically important drug interactions

•Drugs that increase effects/toxicity of amantadine: anticholiner-

gic drugs (benztropine, trihexphenidyl), CNS stimulants,

AMANTADINE 31

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thioridizine, possibly other phenothiazines, potassium-sparing

diuretics, alcohol.

Parameters to monitor

•Serum BUN and creatinine, CBC with differential and

platelets.

•Watch for increased incidence of seizures if history of

epilepsy.

•Signs and symptoms of psychological problems: depression,

confusion, or other new symptoms.

•Intake of fluids and urinary and other fluid output to minimize

renal toxicity. Closely monitor electrolyte levels.

•Symptoms of CHF.

•Signs and symptoms of livedo reticularis: red or rose-colored

mottling of skin usually in lower extremities but may also

appear on arms. This condition is more prominent when patient

is exposed to cold. This side effect generally appears within

1–12 months of treatment.

•Efficacy of treatment for Parkinson’s disease: decrease in

abnormal muscle movements, in particular akinesia, rigidity,

tremors. Discontinue drug if no improvement within 1–2

weeks.

Editorial comments:

•Be advised that for amantadine to be effective in treating

influenza, it must be administered not later than 48 hours after

symptoms are noted.

•Amantadine is recommended for prophylactic use in patients

at high risk who cannot be administered influenza vac-

cine. Such prophylactic therapy should be given for up to

90 days.

•This drug should be administered for Parkinsonian patients

only under close medical supervision. Although there may be

a satisfactory relief of Parkinsonian symtoms within a few

days, effectiveness may diminish after 6–8 weeks of treatment.

If this occurs, a decision will have to be made whether to

increase the dose or discontinue drug administration and use

another anti-Parkinson drug.

32 AMANTADINE

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Amikacin

Brand name: Amikin.

Class of drug: Antibiotic, aminoglycoside.

Mechanism of action: Binds to ribosomal units in bacteria,

inhibits protein synthesis.

Susceptible organisms in vivo: Staphylococci (penicillinase and

nonpenicillinase), Staphylococcus epidermidis,Acinetobacter sp,

Citrobactersp, Enterobactersp, Escherichia coli, Klebsiella sp,

Proteussp, Providencia sp, Pseudomonas sp, Serratia sp.

Indications/dosage/route: IM, IV.

•Bacterial septicemia (including neonatal sepsis); serious infec-

tions of the respiratory tract, bones, joints, skin, soft tissue, and

CNS (eg, meningitis); burns; serious complicated infections of

the urinary tract

Ð Adults, children, older infants: 15 mg/kg in 2–3 divided doses,

7–10 days. Maximum: 15 mg/kg/d.

•Uncomplicated UTIs

Ð Adults: 250 mg b.i.d.

Ð Newborns: loading dose of 10 mg/kg, then 7.5 mg/kg q12h.

Adjustment of dosage: Kidney disease: initial: 7.5 mg/kg (load-

ing dose); maintenance: divide normal recommended dose by

patient’s serum creatinine level, administer calculated dose

q12h.

Food: No restrictions.

Pregnancy: Category D.

Lactation: Appears in breast milk in small amounts. Potentially

toxic to infant. Best to avoid.

Contraindications: Hypersensitivity to aminoglycoside antibiotics.

Warnings/precautions

•Use with caution in patients with the following conditions:

renal disease, neuromuscular disorders (eg, myasthenia gravis,

parkinsonism), hearing disorders.

•Do not combine this drug with any other drug in the same IV

bag.

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Adverse reactions

•Common: None.

•Serious: renal toxicity, ototoxicity, neuromuscular paralysis,

respiratory depression (infants), superinfection.

Clinically important drug interactions

•Drugs that decrease effects/toxicity of aminoglycosides: peni-

cillins (high dose), cephalosporins.

•Drugs that increase effects/toxicity of aminoglycosides: loop

diuretics, amphotericin B, enflurane, vancomycin, NSAIDs.

Parameters to monitor

•Determine peak and trough serum levels 48 hours after begin-

ning therapy and every 3–4 days thereafter as well as after

changing doses.

•Monitor patient for ototoxicity: tinnitus, vertigo, hearing loss.

The drug should be stopped if tinnitus occurs. Limit adminis-

tration to 7–10 days to decrease the risk of ototoxicity.

•Monitor patient’s renal function periodically. If serum creati-

nine increases by more than 50% over baseline value, it may

be advisable to discontinue drug treatment and use a less

nephrotoxic agent, eg, a quinolone or cephalosporin.

•Efficacy of drug action: If there is no response in 3–7 days,

reculture and consider another drug.

•Monitor neuromuscular function when administering the drug

IV. Too rapid administration may cause paralysis and apnea.

Have calcium gluconate or pyridostigmine available to reverse

such an effect.

•Monitor patient’s neurologic status if the drug is given for

hepatic encephalopathy.

•Monitor patient for signs and symptoms of allergic reaction.

Editorial comments: Once daily dosing of amikacin has been advo-

cated by some authors to increase efficacy and reduce toxicity.

Amiloride

Brand name: Midamor.

Class of drug: Potassium-sparing diuretic.

34 AMILORIDE

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Mechanism of action: Acts on distal renal tubules to inhibit

sodium–potassium exchange.

Indications/dosage/route: Oral only.

•Hypertension, alone or with other diuretics (loop or thiazide)

Ð Adults: Initial: 5–10 mg/d. Maximum: 20 mg/d.

Adjustment of dosage

•Kidney disease: creatinine clearance 10–50 mL/min: reduce

dose by 50%; creatinine clearance <10 mL/min: do not use.

•Liver disease: None.

•Elderly: None.

•Pediatric: Safety and efficacy in children have not been estab-

lished.

Onset of Action Peak Effect Duration

<2 h 6–10 h 24 h

Food: Take with food or milk.

Pregnancy: Category B.

Lactation: No data available. Best to avoid.

Contraindications: Anuria, hyperkalemia, severe renal insuffi-

ciency, serum potassium level >5 mEq/L, patients receiving

other potassium-sparing diuretics or potassium supplements,

hypersensitivity to amiloride.

Editorial comments: For additional information, see spironolac-

tone, p. 849.

Amiodarone

Brand name: Cordarone.

Class of drug: Antiarrhythmic, Class III.

Mechanism of action: Prolongs action potential duration as well

as refractory period.

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Indications/dosage/route: Oral, IV.

•Ventricular arrhythmias after MI

Ð Adults: Loading dose: IV 5 mg/kg over 25–50 minutes.

Maintenance: 10–15 mg/kg/d. Further data needed to clarify

proper dosages.

•Intractable ventricular tachycardia or fibrillation

Ð Adults: PO 800–1600 mg/day loading dose for 1–3 weeks,

then for 4–14 days, 5 mg/kg/d for 2–4 weeks. Maintenance:

2.5 mg/kg.

Ð Children: PO 10–15 mg/kg/d, loading dose, as single or

divided dose, daily or 5 of 7 days weekly.

Onset of Action Peak Effect

3 d to 3 wk 1 wk to 5 mo

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: None.

•Pediatric: Safety and efficacy have not been established.

Food: To be taken with food.

Pregnancy: Category C.

Lactation: Appears in breast milk. Potentially toxic to infant. Avoid

breastfeeding until several months after discontinuation of drug.

Contraindications: Sinus node dysfunction, bradycardia accom-

panied by syncope, AVblock (second or third degree).

Warnings/precautions

•Use with caution in patients with the following conditions:

CHF, hypersensitivity to iodine.

•A number of potentially fatal toxic effects are associated with

use of amiodarone. Up to 17% of patients receiving this med-

ication may develop pulmonary toxicity characterized by

hypersensitivity pneumonitis or interstitial pneumonitis. Other

potentially serious side effects with this medication include

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hepatotoxicity, exacerbation of arrhythmia, and loss of vision

due to optic neuritis or optic neuropathy. Neonatal hypo- or

hyperthyroidism may occur if amiodarone is administered

during pregnancy.

•This is not a first line antiarrhythmic drug; it is used when

others fail.

•Because of extremely long half-life (100 days), extreme care

must be used when other antiarrhythmic drugs are given after

discontinuing amiodarone. Approximately 75% of patients

receiving more than 400 mg/d experience adverse effects over

time. Patients should be monitored in the hospital during

administration of loading doses. Note that severe and life-

threatening toxic effects are associated with the loading phase

and chronic use of amiodorane.

•Evaluate patient for orthostasis with BP measurements in the

sitting, lying, and standing positions repeatedly before and

after initiating therapy.

•Hypokalemia or hypomagnesemia should be corrected before

amiodarone is administered.

Advice to patient

•Use sunscreen or protective clothing in strong sunlight. These

precautions should be maintained for up to 4 months follow-

ing discontinuation of drug therapy.

•There may be a bluish discoloration, mainly in the face, arms,

and neck. This will disappear after drug is discontinued.

Adverse reactions

•Oral

Ð Common: headache, dizziness, fatigue, muscle weakness,

solar dermatitis, photosensitivity, discoordination, hyperlipi-

demia, nausea, vomiting, constipation, anorexia, tremor,

paresthesias,visual disturbances.

Ð Serious: pulmonary fibrosis and/orinterstitial pneumoni-

tis (17%), hepatotoxicity, hypotension (16%), pulmonary

infiltrates, dysrhythmias, hypothyroidism, cardiovascular col-

lapse, CHF, thrombocytopenia, optic neuritis or neuropathy,

corneal microdeposits, peripheral neuropathy.

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•Intravenous: Cardiovascular collapse, asystole, heart failure.

Clinically important drug interactions

•Drugs that increase effects/toxicity of amiodarone: calcium

channel blockers, cimetidine, ritonavir, volatile anesthetics.

•Amiodarone increases effects/toxicity of the following drugs:

oral anticoagulants, βblockers, digoxin, phenytoin, quinidine,

cyclosporine, procainamide, flecainide, cisapride, methotrexate

theophylline.

•Drugs that decrease effects/toxicity of amiodarone: cholestyra-

mine.

Parameters to monitor

•Baseline and follow-up serum electrolytes, BUN and creati-

nine, thyroid functions, liver enzymes.

•Ophthalmic examinations for signs of granular corneal

deposits (brown colored). Advise patient to instill methy-

cellulose ophthalmic solution frequently to minimize

problem.

•Signs and symptoms of psychiatric symptoms or neurotoxicity:

depression, insomnia, headache, hallucinations, muscle weakness,

ataxia, paresthesia of fingers, toes. If these occur, consider

changing medication.

•Pulmonary function test to monitor signs and symptoms of pul-

monary toxicity.

•ECG for the following parameters: heart rate and rhythm,

reduction of T-wave amplitude, Q-Tprolongation.

•Signs and symptoms of thyroid dysfunction, including both

hyper- and hypothyroidism, weight gain, pale skin, edema of

extremities and periorbital region.

Editorial comment

•Oral: Bioavailability of amiodarone is 40–60% depending on

absorption. Iodine dose is about 40 mg/pill and this likely

contributes to the most common adverse reaction: thyroid

dysfunction. Most adverse end-organ problems are cumula-

tive dose-related and therefore lower maintenance doses

have been better tolerated for longer periods. Loading should

always be performed in the hospital if the patient has left

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ventricular dysfunction due to potential proarrhythmia in this

group. If the heart structure is well preserved, then low-dose

(200 mg t.i.d.) loading with gradual decrease can safely be done

as an outpatient over 2 months as long as the ECG and clinical

status are stable. Pulmonary toxicity can often be managed as an

outpatient with or without home O

•IV: The loading dose of IV amiodarone is not as large as in-hos-

pital oral amiodarone loading. IVamiodarone should always be

given in a monitored setting preferably in the intensive care unit

or skilled telemetry ward. Acentral line is essential to decrease

the phlebitis that accompanies infusion.

•ACLS protocol has now replaced bretylium with amiodarone

IV in the treatment of malignant hemodynamically compro-

mised ventricular tachyarrhythmia.

•It is recommended that patients undergoing general anes-

thesia while receiving amiodarone therapy should be

monitored carefully in the perioperative period. These

patients may be at higher risk for conduction abnormalities

and myocardial dysfunction secondary to anesthetic agents.

Additionally, episodes of ARDS and post-bypass hypoten-

sion have been noted in patients undergoing surgery when

receiving amiodarone.

Amitriptyline

Brand name: Elavil.

Class of drug: Tricyclic antidepressant.

Mechanism of action: Inhibits reuptake of CNS neurotransmit-

ters, primarily serotonin and norepinephrine.

Indications/dosage/route: Oral, IM.

•Depression

Ð Adults (outpatients): Initial: PO 75 mg/d in divided doses;

increase to 150 mg/d if needed.

AMITRIPTYLINE 39

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Ð Hospitalized patients. PO—Initial: 100 mg/d, may be increased

to 200–300 mg/d. IM—20–30 mg q.i.d.; change to oral drug

as quickly as possible. Maintenance: 40–100 mg/d.

Ð Adolescents and elderly: PO 10 mg t.i.d. with 20 mg at bed-

time. Maximum: 100 mg/d.

Ð Children 6–12 years: PO 10–30 mg/d, up to 4 divided doses.

•Chronic pain

Ð Adults: PO 50–100 mg/d.

•Enuresis

Ð Children >6 years: PO 10 mg/day at bedtime; increase to

maximum of 25 mg/day if needed.

Ð Children <6 years: PO 10 mg/day at bedtime.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: See above.

•Pediatric: Not recommended for children <12 years old except

for treatment of enuresis.

Food: No restriction.

Pregnancy: Category C.

Lactation: Appears in breast milk. American Academy of

Pediatrics expresses concern over use when breastfeeding.

Contraindications: Hypersensitivity to tricyclic antidepressants,

acute recovery from MI, concurrent MAO inhibitor.

Warnings/precautions

•Use with caution in patients with the following conditions:

epilepsy, angle-closure glaucoma, cardiovascular disease, his-

tory of urinary retention, suicidal tendencies, benign prostatic

hypertrophy, concurrent anticholinergic drugs, hyperthyroid

patients receiving thyroid drugs, alcoholism, schizophrenia.

•May cause psychosis in schizophrenic patients.

•May unmask mania or hypomania.

Advice to patient

•Avoid alcohol and other CNS depressants such as opiate anal-

gesics and sedatives (eg, diazepam) when taking this drug.

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

40 AMITRIPTYLINE

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•Change position slowly, in particular from recumbent to

upright, to minimize orthostatic hypotension. Sit at the edge of

the bed for several minutes before standing, and lie down if

feeling faint or dizzy. Avoid hot showers or baths and standing

for long periods. Male patients should sit on the toilet while uri-

nating rather than standing.

•If mouth is dry rinse with warm water frequently, chew sugar-

less gum, suck on ice cube, or use artificial saliva. Carry out

meticulous oral hygiene (floss teeth daily).

•To minimize possible photosensitivity reaction, apply adequate

sunscreen and use proper covering when exposed to strong

sunlight.

•If constipation develops, increase fiber and fluid intake. Notify

physician if constipation is severe.

Adverse reactions

•Common: sedation, anticholinergic effects (dry mouth, consti-

pation), nausea, dizziness, headache, taste disturbance, weight

gain.

•Serious: orthostatic hypotension, arrhythmias, extrapyramidal

symptoms, seizures, bone marrow depression, hepatitis, increased

intraocular pressure, allergic reactions.

Clinically important drug interactions

•Drugs that increase effects/toxicity of tricyclic antidepres-

sants: MAO inhibitors, cimetidine, SSRIs, β blockers,

estrogens.

•Drugs that decrease effects/toxicity of tricyclic antidepres-

sants: barbiturates, cholestyramine.

•Tricyclic antidepressants increase effects/toxicity of following

drugs: CNS depressants (alcohol, sedatives, hypnotics), oral

anticoagulants, carbamazepine, sympathomimetic amines

(dobutamine, dopamine, epinephrine, ephedrine), opioids

(morphine-type drugs), drugs with anticholinergic activity

(atropine, anti-Parkinson drugs).

•Tricyclic antidepressants decrease effects/toxicity of following

drugs: clonidine, guanethidine.

Parameters to monitor

•CBC with differential and platelets, liver enzymes.

AMITRIPTYLINE 41

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•Suicidal ideation: Advise patient’s family to remove firearms

from the home.

•Signs and symptoms of hepatotoxicity.

•Monitor drug levels: therapeutic level: 160–250 mg/mL; toxic

level: >500 mg/mL.

•Evaluate neurologic and mental status: mood changes, agita-

tion. May require dose reduction. Hypomania, mania, or

delusions: stop medication.

•Monitor patient for signs and symptoms of angle-closure glau-

coma and visual or other ophthalmic disturbances, eg, halos,

eye pain, dilated pupils.

•Signs and symptoms of bone marrow depression.

•Monitor patient with history of hyperthyroidism or cardiovas-

cular disease for arrhythmias.

•Monitor patient for efficacy of treatment: increased appetite

and energy level and sense of well-being, renewed interest in

environment, improved sleep.

Editorial comments

•Patients with depression are at increased risk of suicide. To

reduce this risk as well as the chance of overdose, prescribe

limited amounts.

•Withdrawal symptoms have been reported after abrupt cessa-

tion of administration. These include nausea, headaches,

irritability, and sleep disturbances.

•It may take several months for maximum response to be

realized.

Amlodipine

Brand name: Norvasc.

Class of drug: Calcium channel blocker.

Mechanism of action: Inhibits calcium movement across cell

membranes.

42 AMLODIPINE

CH-A.qxd 7/6/01 9:25 AM Page 42

Indications/dosage/route: Oral only.

•Hypertension

Ð Adults: Individualize: 2.5–5 mg/d. Maximum: 10 mg/d.

•Angina

Ð Adults: 5–10 mg.

Ð Elderly: 5 mg.

Adjustment of dosage

•Kidney disease: Use with caution.

•Liver disease: Initial dose 2.5 mg/d.

•Elderly: Initial dose 2.5 mg/d.

•Pediatric: Safety and efficacy have not been established in chil-

dren.

Onset of Action Peak Effect Duration

1–2 h 6–12 h 24 h

Food: No restriction.

Pregnancy: Category C.

Lactation: Probably appears in breast milk. Potentially toxic to

infant. Avoid breastfeeding.

Contraindications: Hypersensitivity to calcium blockers.

Warnings/precautions

•Use with caution in patients with the following conditions:

CHF, severe left ventricular dysfunction, concomitant use with

βblockers or digoxin.

•Do not withdraw drug abruptly, since this may result in increased

frequency and intensity of angina.

•For the diabetic patient, amlodipine may interfere with insulin

release and therefore produce hyperglycemia.

•Patient should be tapered off β blockers before beginning cal-

cium channel blockers to avoid exacerbation of angina due to

abrupt withdrawal of the βblocker.

Advice to patient

•Use two forms of birth control including hormonal and barrier

methods.

AMLODIPINE 43

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•Change position slowly, in particular from recumbent to

upright, to minimize orthostatic hypotension. Sit at the edge of

the bed for several minutes before standing, and lie down if

feeling faint or dizzy. Avoid hot showers or baths and standing

for long periods. Male patients should sit on the toilet while

urinating rather than standing.

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Avoid use of OTC medications without first informing the

treating physician.

•Determine blood pressure and heart rate aproximately at the

same time each day and at least twice a week, particularly at

the beginning of therapy.

•Be aware of the fact that this drug may also block or reduce

anginal pain, thereby giving a false sense of security on severe

exertion.

•Include high-fiber foods to minimize constipation.

•Limit consumption of xanthine-containing drinks: regular

coffee (fewer than 5 cups/day), tea, cocoa.

Adverse reactions

•Common: headache, edema.

•Serious: CHF, arrhythmias, hypotension, depression.

Clinically important drug interactions

•Drugs that increase effects/toxicity of calcium blockers: cime-

tidine, βblockers, cyclosporine.

•Drugs that decrease effects of calcium blockers: barbitu-

rates.

Parameters to monitor

•Patient’s BP during initial administration and frequently there-

after. Ideally, check BPclose to the end of dosage interval or

before next administration.

•Status of liver and kidney function. Impaired renal func-

tion prolongs duration of action and increases tendency

for toxicity.

•Intake of fluids and urinary and other fluid output to minimize

renal toxicity. Increase fluid intake if inadequate. Closely mon-

itor electrolyte levels.

44 AMLODIPINE

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•Efficacy of treatment for angina: decrease in frequency of

angina attacks, need for nitroglycerin, episodes of PST seg-

ment deviation, anginal pain.

•If anginal pain is not reduced at rest or during effort reassess

patient as to medication.

•GI side effects: use alternative.

•Monitor ECG for development of heart block.

•Symptoms of CHF.

Amoxapine

Brand name: Asendia.

Class of drug: Tricyclic antidepressant.

Mechanism of action: Inhibits reuptake of CNS neurotransmit-

ters, primarily serotonin and norepinephrine.

Indications/dosage/route: Oral only.

•Depression

Ð Adults: Initial: 50 mg t.i.d.; increase to 100 mg t.i.d. during

first week. Maintenance: 300 mg as single dose at bedtime.

Ð Hospitalized patients: up to 150 mg q.i.d.

Ð Elderly: Initial: 25 mg b.i.d. to t.i.d.; increase to 50 mg b.i.d.

to t.i.d. after first week. Maintenance: ≤300 mg/d at bedtime.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: Lower doses recommended.

•Pediatric: Not recommended for children <12 years.

Food: No restriction.

Pregnancy: Category C

Lactation: Appears in breast milk. American Academy of Pedia-

trics expresses concern over use when breastfeeding.

Contraindications: Hypersensitivity to tricyclic antidepressants,

acute recovery from MI, concurrent MAO inhibitor.

AMOXAPINE 45

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Editorial comments

•This drug is not listed in Physicians’ Desk Reference, 54th

edition, 2000.

•For additional information, see amitriptyline, p. 39.

Amoxicillin

Brand name: Amoxil.

Class of drug: Antibiotic, penicillin family, aminopenicillin.

Mechanism of action: Inhibits bacterial cell wall synthesis.

Susceptible organisms in vivo: [same as ampicillin] Streptococcus

pneumoniae, beta-hemolytic streptococci, Enterococcus faecalis,

viridans streptococci, Escherichia coli, Hemophilus influenzae,

Neisseria gonorrhoeae, Proteus mirabilis, Salmonella(often resist-

ant), Shigella(often resistant), Listeria monocytogenes, Neisseria

meningitidis.

Indications/dosage/route: Oral only.

•Ear, nose, and throat infections, mild/moderate; GU tract infec-

tions, mild/moderate

Ð Adults: 500 mg q12h.

Ð Children >3 months: 25 mg/kg/d, divided doses q12h.

•Ear, nose and throat infections, severe; GU tract infections,

severe

Ð Adults: 875 mg q12h.

Ð Children >3 months: 45 mg/kg, divided doses q12h.

•Lower respiratory tract infections

Ð Adults: 875 mg q12h.

Ð Children >3 months: 45 mg/kg, divided doses q12h.

•Skin, skin structure infections, mild/moderate

Ð Adults: 500 mg q12h.

•Children >3 months: 25 mg/kg/d, divided doses q12h.

•Skin, skin structure infections, severe

Ð Adults: 875 mg q12h.

46 AMOXICILLIN

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Ð Children >3 months: 45 mg/kg/d, divided doses q8h.

•Acute gonorrhea, uncomplicated anogenital and urethral infec-

tions

Ð Adults: 3 mg as single dose.

–Children >2 years: 50 mg/kg plus 25 mg probenecid as single

dose.

Adjustment of dosage

•Kidney disease: creatinine clearance 10–30 mL/min: 250 or

500 mg q12h; creatinine clearance <10 mL/minute: 250 or 500

mg q24h.

•Liver disease: None.

•Elderly: None.

•Pediatric: Contraindicated for children <2 years.

Food: No restrictions.

Pregnancy: Category B.

Lactation: Appears in breast milk. Considered compatible by

American Academy of Pediatrics.

Contraindications: Hypersensitivity to penicillin or cephalosporins.

Warnings/precautions

•Use with caution in patients with mononucleosis.

•Allergic reactions are more likely to occur in patients with the

following conditions: asthma, hay fever, allergy to cephalo-

sporins, history of allergy to penicillin. Consider skin testing,

with major and minor antigenic components, of penicillin

hypersensitivity in patients with β-lactamase allergy who

require amoxicillin for life-threatening infections, to assess

possibility of a hypersensitivity reaction. If patient is given

drug parenterally, observe for at least 20 minutes for possible

anaphylactic reaction. Negative history of penicillin hypersen-

sitivity does not prelude a patient from reacting to the drug.

•Administer at least 1 h before a bacteriostatic agent is given (eg,

tetracycline, erythromycin, chloramphenicol).

•For IV infusion: Make sure no other drugs are added or mixed

into the infusing solution. Do not use solution containing pre-

cipitates or foreign matter.

•Do not use a penicillin to test Enterobacter or Citrobacter

infections because of inducible β-lactamase.

AMOXICILLIN 47

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Advice to patient

•If you are using an oral contraceptive, use an additional method

of birth control as efficacy of oral contraceptive may be

reduced.

•If you are allergic to a penicillin or cephalosporin, carry an

identification card with this information.

Adverse reactions

•Common: None.

•Serious: Stevens–Johnson syndrome, anaphylaxis, angioedema,

laryngospasm, pseudomembraneous colitis.

Clinically important drug interactions

•Drugs that increase effects/toxicity of penicillins: probenecid,

disufiram (increase levels).

•Drugs that decrease effects/toxicity of penicillins: antacids,

tetracyclines.

•Penicillins increase effects of following drugs: oral anticoagu-

lants, heparin.

•Penicillins decrease effects of following drugs: oral contra-

ceptives.

Parameters to monitor

•Signs and symptoms of anaphylactic shock.

•Signs and symptoms of allergic reaction.

•Signs and symptoms of pseudomembranous colitis.

•Patient’s intake/output of fluid.

•Renal, hepatic, and hematologic status for patients on high-

dose prolonged therapy.

Editorial comments

•Amoxicillin is preferred over ampicillin for oral use because

incidence of diarrhea is less. Ampicillin is preferred for intra-

venous use.

•Amoxicillin and ampicillin are the first choice for Enterococcus

faecalisand Listeria monocytogenes infections. Amoxicillin is

also used orally for prophylaxis of endocarditis after dental

procedures in high-risk patients. Dosage is 2 g PO 1 h prior to

procedure.

48 AMOXICILLIN

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•The American Association of Pediatrics recommends amoxi-

cillin for the treatment of otitis media due to cost-effectiveness.

However, resistant organisms are clearly an important problem.

Amoxicillin/Clavulanate

Brand name: Augmentin.

Class of drug: Antibiotic, penicillin family plus β-lactamase

inhibitor (clavulanate).

Mechanism of action: Inhibits bacterial cell wall synthesis.

Clavulanate inhibits the β-lactamase of methicillin-susceptible

Staphylococcus aureus, Hemophilis infuenzae, Branhamella

catarrhalis, anaerobic organisms, Neisseria gonorrhoeae.

Susceptible organisms in vivo: Staphylococcus aureus (not

MRSA), Hemophilis infuenzae, Branhamella catarrhalis,

Streptococcus pneumoniae, Enterococcus faecalis, betahemo-

lytic streptococci, viridans streptococci. Resistance is increas-

ing inE. coli even in the community.

Indications/dosage/route: Oral only.

•All infections

Ð Adults, children >40 kg: 500-mg tablet q12h or 125- to 250-

mg chewable tablet q8h.

•Severe infections

Ð Adults, children >40 kg: 500-mg tablet q8h or 875 mg every

12 h.

•Otitis media, sinusitis, lower respiratory tract infections, severe

infections

Ð Children <40 kg: 45 mg/kg/d in divided doses q12h or 40

mg/kg/d q8h.

•Less severe infections

Ð Children <40 kg: 25 mg/kg/d in divided doses q12h or 20

mg/kg/d q8h.

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Adjustment of dosage

•Kidney disease: creatinine clearance 10–30 mL/min: 250 or

500 mg q12h; creatinine clearance <10 mL/min: 250 or 500 mg

q24h.

•Liver disease: None.

•Elderly: None.

•Pediatric: Contraindicated for children <2 years.

Food: No restrictions.

Pregnancy: Category B.

Lactation: Appears in breast milk. Considered compatible by

American Academy of Pediatrics.

Contraindications: Hypersensitivity to penicillin or cephalosporins.

Warnings/precautions

•Diarrhea is more common with amoxicillin–clavulanate than

with amoxicillin alone.

•Allergic reactions are more likely to occur in patients with the fol-

lowing conditions: asthma, hay fever, allergy to cephalosporins,

history of allergy to penicillin. Consider skin testing, with major

and minor antigenic components, of penicillin hypersensitivity

patients with β-lactamase allergy who require amoxicillin for

life-threatening infections, to assess the possibility of a hyper-

sensitivity reaction. If patient is give the drug parenterally,

observe for at least 20 min for possible anaphylactic reaction.

Negative history of penicillin hypersensitivity does not prelude

a patient from reacting to the drug. Administer at least 1 hour

before a bacteriostatic agent is given (eg, tetracycline, eryth-

romycin, chloramphenicol).

•For IV infusion: Make sure no other drugs are added or mixed

into the infusing solution. Do not use solution containing pre-

cipitates or foreign matter.

Advice to patient

•If you are receiving an oral contraceptive, use an alternative

method of birth control.

•If you are allergic to a penicillin or cephalopsporin, carry an

identification card with this information.

Adverse reactions

•Common: Diarrhea.

50 AMOXICILLIN/CLAVULANATE

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•Serious: Stevens–Johnson syndrome, anaphylaxis, angioedema,

laryngospasm, pseudomembraneous colitis.

Clinically important drug interactions

•Drugs that increase effects/toxicity of penicillins: probe-

necid.

•Drugs that decrease effects/toxicity of penicillins: antacids,

tetracyclines.

•Penicillins increase effects of following drugs: oral anticoagu-

lants, heparin.

•Penicillins decrease effects of following drugs: oral contraceptives.

Parameters to monitor

•Signs and symptoms of anaphylactic shock.

•Signs and symptoms of allergic reaction.

•Signs and symptoms of pseudomembranous colitis.

•Patient’s intake/output of fluid.

•Renal, hepatic, and hematologic status for patients on high-

dose prolonged therapy.

Editorial comments

•Amoxicillin–clavulanate is used for complicated or chronic

sinusitis and otitis media because its spectrum includes S.

pneumoniae, H. influenzae, B. catarrhalis, and anaerobic

organisms.

•It is also appropriate for GI infections (eg, diverticulitis), exac-

erbations of COPD, aspiration pneumonia, head and neck

infections. It is the drug of choice for bite-related infections, as

it provides coverage for oral anaerobes, streptococci, and

Pasteurella multocida.

Amphotericin B

Brand names: Abelcet, Ambisome.

Class of drug: Systemic and topic antifungal agent.

Mechanism of action: Increases fungal cell membrane perme-

ability causing cell death.

AMPHOTERICIN B 51

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Indications/dosage/route: IV, intrathecal, topical.

•Systemic fungal infections

Ð Adults: Initial: IV 0.25 mg/kg q2–6h. Maintenance: IV

0.25–1 mg/kg/d.

Ð Infants, children: Initial: IV 0.25 mg/kg/d. Maintenance: IV

0.25–1 mg/kg/d.

•Fungal meningitis

Ð Adults: Initial: intrathecal 50 µg. Maintenance: 25 µg q2–3wk.

•Topical fungal infections

Ð Adults: Initial: 3% cream 2–4 times per day. Maintenance:

2–4 times per day.

Adjustment of dosage

•Kidney disease: Decrease by 50%.

•Liver disease: No information available.

•Elderly: May be at high risk for toxicity.

•Pediatric: See above.

Duration of therapy: 2 weeks to 3 months.

Pregnancy: Category B.

Lactation: No data available. Best to avoid.

Contraindications: Hypersensitivity to amphotericin B.

Warnings/precautions

•Avoid other nephrotoxic drugs. Avoid rapid IVinfusion.

•Use caution in renal disease. Discontinue if BUN increases to

>40 mg/dLor serum creatinine rises above 3 mg/dL.

Adverse reactions

•Common: increased liver enzymes, tachycardia, azotemia,

hypokalemia, hypotension, chills, fever, nausea, hyperbiliru-

binemia.

•Serious: hypokalemia, hypokalemia, nephrotoxicity (renal

tubularacidosis, renal failure), convulsions, hypersensitivity

reaction, anaphylaxis, arrythmia, multiple organ failure, bone

marrow depression, cardiac arrest.

Clinically important drug interactions

•Drugs that increase effects/toxicity of amphotericin B: amino-

glycosides, cisplatin and other antineoplastic drugs, cyclosporine,

corticosteroids, nephrotoxic drugs.

52 AMPHOTERICIN B

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•Amphotericin B increases effects/toxicity of following drugs:

digoxin, skeletal muscle relaxants (nondepolarizing, succinyl-

choline), thiazide diuretics, AZT.

Parameters to monitor

•Serum electrolytes, especially magnesium and potassium.

•Creatinine clearance (determine weekly), serum creatinine, BUN.

•Liver enzymes (weekly).

•Urine output.

•CBC with differential and platelets.

Editorial comments

•Currently two forms of amphotericin B are available on the

market. While Ambisome is incorporated into a liposomal drug

delivery system, Abelcet is combined with phospholipid. It

appears that the liposomal product may have fewer adverse

reactions. Fevers and chills have been reported to occur 1–2

hours after beginning intravenous infusion with Abelcet.

•Parenteral amphotericin B is to be used for severe lifethreat-

ening infections.

Ampicillin

Brand names: Totacillin, Omnipen.

Class of drug: Antibiotic, penicillin family plus β-lactamase

inhibitor.

Mechanism of action: Inhibits bacterial cell wall synthesis.

Susceptible organisms in vivo: Streptococcus pneumoniae, beta-

hemolytic streptococci, Enterococcus faecalis, viridans streptococci,

Escherichia coli, Hemophilus influenzae, Neisseria gonorrhoeae,

Proteus mirabilis, Salmonella(often resistant), Shigella(often resist-

ant), Listeria monocytogenes, Neisseria meningitidis.

Indications/dosage/route: Oral, IV, IM.

•Respiratory tract and soft tissue infections

Ð Children >20 kg: PO 250 mg q6h.

AMPICILLIN 53

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Ð Children <20 kg: PO 50 mg/kg/d in divided doses q6–8h.

Ð Children >40 kg: IV, IM 250–500 mg q6h.

Ð Children <40 kg: IV, IM 25–50 mg/kg/d in divided doses

q6–8h.

•Bacterial meningitis (to cover for Listeria monocytogenes in

neonates, adults >50 years, and immunocompromised indi-

viduals)

Ð Adults and children: IV 150–200 mg/kg/d in divided doses,

then IM q3–4h.

•Prophylaxis bacterial endocarditis, dental, oral, or upper respi-

ratory tract procedures (amoxicillin PO preferred unless NPO)

Ð Patients at moderate risk: Adults: IM, IV, 2 gm 30 minutes prior

to procedure Children: 50 mg/kg 30 minutes prior to procedure.

Ð Patients at high risk: Adults: IM, IV, 2 gm ampicillin plus

gentamicin, 1.5 mg/kg 30 minutes before procedure fol-

lowed in 6 hours by ampicillin, 1 gm IM or IV, or ampicillin,

1 gm PO Children:IM, IV ampicillin 50 mg/kg plus gen-

tamicin 1.5 mg/kg, 30 min prior to procedure, followed in 6

hours by ampicillin 25 mg/kg IM or IV or amoxicillin 25

mg/kg PO.

•Septicemia

Ð Adults, children: IV 150–200 mg/kg/d first 3 days, then IM

q3–4h.

•GI and GU infections other than N. gonorrhoeae

Ð Adults, children >20 kg: PO 500 mg q6h.

Ð Children <20 kg: 100 mg/kg/d q6h.

•N. gonorrhoeae infections (non-penicillinase-producing): PO

single dose of 3.5 g together with probenecid 1 g

Ð Adults, children >40 kg: IV or IM 500 mg q6h.

Ð Children <40 kg: 50 mg/kg/d IV or IM in divided doses

q6–8h.

•Urethritis in males caused by N. gonorrhoeae

Ð Males >40 kg: IV or IM 1 g at an interval of 8–12 hours;

repeat if necessary.

Adjustment of dosage

•Kidney disease: creatinine clearance <10 mL/min: increase

dosing interval to 12 h.

54 AMPICILLIN

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•Liver disease: None.

•Elderly: None.

•Pediatric: Contraindicated for children <2 years.

Food: Take on empty stomach, 1 hour before or 2 hours after eating.

Pregnancy: Category B.

Lactation: Appears in breast milk. Use with caution.

Contraindications: Hypersensitivity to penicillin or cephalosporins.

Warnings/precautions

•Use with caution in patients with mononucleosis.

•Allergic reactions are more likely to occur in patients with the fol-

lowing conditions: asthma, hay fever, allergy to cephalosporins,

history of allergy to penicillin. Consider skin testing, with major

and minor antigenic components, of penicillin hypersensitivity in

such patients to assess the possibility of a hypersensitivity reac-

tion. If patient is given drug parenterally, observe for at least 20

minutes for possible anaphylactic reaction.

•Negative history of penicillin hypersensitivity does not prelude

a patient from reacting to the drug.

•Administer at least 1 hour before a bacteriostatic agent is given

(eg, tetracycline, erythromycin, chloramphenicol).

•For IV infusion: Make sure no other drugs are added or mixed

into the infusing solution. Do not use solution containing pre-

cipitates or foreign matter.

Advice to patient

•If you are receiving an oral contraceptive, use an alternative

method of birth control.

•If you are allergic to a penicillin or cephalosporin, carry an

identification card with this information.

Adverse reactions

•Common: None.

•Serious: Stevens–Johnson syndrome, anaphylaxis, angioedema,

laryngospasm, pseudomembraneous colitis, seizures (high dose).

Clinically important drug interactions

•Drug that increases effects/toxicity of penicillins: probenecid.

•Drugs that decrease effects/toxicity of penicillins: antacids,

tetracyclines.

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•Penicillins increase effects of following drugs: oral anticoagu-

lants, heparin.

•Penicillins decrease effects of following drugs: oral contraceptives.

Parameters to monitor

•Signs and symptoms of anaphylactic shock.

•Signs and symptoms of allergic reaction.

•Signs and symptoms of pseudomembranous colitis.

•Patient’s intake/output of fluid.

•Signs of bleeding, particularly in patients on high-dose therapy.

•Monitor bleeding time in these patients.

•Renal, hepatic, and hematologic status for patients on high-

dose prolonged therapy.

Editorial comments

•Ampicillin is added empirically for acute meningitis to cover

for Listeriawhen the organism is a possible pathogen (neonate,

adults >50 years, and immunocompromised patients).

•Ampicillin is also used with an aminoglycoside to treat sub-

acute bacterial endocarditis before the blood culture results

are known. This regimen covers the viridans streptococci,

Enterococcus faecalis, and the HACEK organisms.

•Ampicillin is no longer adequate monotherapy for the treat-

ment of UTI since E. colifrequently is resistant.

•Surgeons frequently use ampicillin, gentamicin, and metron-

idazole for surgical intraabdominal infections. Ampicillin in

this regimen covers Enterococcus faecalis, a frequent pathogen.

Ampicillin/Sulbactam

Brand name: Unasyn.

Class of drug: Antibiotic, penicillin family plus β-lactamase inhibitor.

Mechanism of action: Inhibits bacterial cell wall synthesis.

Susceptible organisms in vivo: See ampicillin. The addition of

sulbactam inhibits the penicillinase of anaeorbes (oral anaeorbes,

Bacteroides fragilis), MSSA, Hemophilus influenzae, Branhamella

catarrhalis, Escherichia coli.

56 AMPICILLIN/SULBACTAM

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Indications/dosage/route: IM, IV.

•Adults, children >12 years: 1.5 g (1 g ampicillin, 0.5 g sulbac-

tam) q6–8h.

•Children (3 months to 12 years): 100–200 mg ampicillin/kg/d,

plus 50–100 mg sulbactam/kg/day, divided every 8 h.

Maximum: 8 g ampicillin/d.

Adjustment of dosage

•Kidney disease: creatinine clearance: 15–30 mL/min, dose every

12 hours; creatinine clearance: 5–14 mL/min, dose every 24 hours.

•Liver disease: None.

•Elderly: None.

•Pediatric: See above.

Food: Not applicable.

Pregnancy: Category B.

Lactation: Appears in breast milk. Considered compatible by

American Academy of Pediatrics.

Contraindications: Hypersensitivity to penicillin or cephalosporins,

IVinjections.

Editorial comments

•This antibiotic is used in mixed infections when Pseudomonas

aeruginosais not a pathogen.

•As a single agent, it is effective in animal and human bites,

complicated otitis media, sinusitis, oral and neck infections,

and community-acquired pneumonia when aspiration is sus-

pected. All these infections are caused mainly by oral flora.

•With the addition of an aminoglycoside, it is very appropriate

for the treatment of pelvic inflammatory disease and other

gynecologic infections.

•For additional information, see ampicillin, p. 53.

Amrinone

Brand name: Inocor.

Class of drug: Phosphodiesterase inhibitor, inotropic agent.

Mechanism of action: Increases myocardial cyclic AMP in car-

diac tissue by phosphodiesterase inhibition.

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Indications/dosage/route: IV only.

•CHF low cardiac output (sepsis), poor responders to digitalis

Ð Adults: Initial: 0.75 mg/kg bolus over 2–3 min. Maintenance:

5–10 µg/kg/min. Maximum: 10 mg/kg/d.

Adjustment of dosage

•Kidney disease: Reduce dose by 50–75% in renal failure.

•Liver disease: None

•Elderly: Reduce dose relative to renal function.

•Pediatric: Safety and efficacy have not been established.

Onset of Action Peak Effect Duration

2–5 min 10 min 30 min–2h,depending on dose

Pregnancy: Category C.

Lactation: No data available. Best to avoid.

Contraindications: Hypersensitivity, severe pulmonary or aortic

valvular disease, acute MI.

Warnings/precautions

•Use with caution in patients with the following conditions: atrial

fibillation or flutter, hypertrophic obstructive cardiomyopathy.

•Reduce dose as cardiac function improves.

•Decreased efficacy (tachphylaxis) may occur during first few

days of treatment.

•Monitor for allergic reaction to preservative (sodium metabisul-

fite).

•Correct hypokalemia before instituting therapy with this drug.

•For patients receiving amrinone plus diuretic, make sure

patient is sufficiently hydrated so there will be sufficient car-

diac filling pressure.

Adverse reactions

•Common: fever, nausea.

•Serious: thrombocytopenia, hypersensitivity reactions, hyper-

calcemia, hepatotoxicity.

Clinically important drug interactions

•Do not mix with furosemide; precipitate forms.

•Amrinone increases effects/toxicity of disopyramide.

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Parameters to monitor

•Cardiac output, stroke volume, pulmonary capillary wedge

pressure, potassium, other electrolytes.

•Signs and symptoms of thrombocytopenia. Discontinue this

medication if platelet count falls below 100,000/mm

•Signs and symptoms of hepatotoxicity.

•Cardiac function: cardiac output static volume, pulmonary cap-

illary pressure.

•Heart rate and BP continuously during infusion. Reduce rate if

there is a significant fall in BPor if arrhythmias occur.

•Serum potassium levels. Correct if hypokalemia is observed.

•Possible tachyphylaxis to antiarrhythmic action. This generally

occurs within 72 hours of beginning drug therapy.

Editorial comments

•Amrinone is generally prescribed for patients with CHF who

have not responded satisfactorily to diuretics, vasodilators, or

cardiac glycosides.

•Amrinone and the phosphodiesterase inhibitors in general

have been double-edged swords. While they enhance con-

tractility and lower vascular resistance, they also have been

associated with sudden death likely due to increasing meta-

bolic demand. These effects can occur even after infusion

has ceased.

•This drug is not listed in the Physician’s Desk Reference, 54th

edition, 2000.

Amyl Nitrite

Class of drug: Antianginal, nitrate vasodilator, antidote to cyanide

poisoning.

Mechanism of action: As antianginal agent, reduces peripheral

resistance (arterial and venous) by vasodilation; decreases left

ventricular pressure. As antidote for cyanide poisoning, pro-

duces methemoglobin which binds and inactivates cyanide.

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Indications/dosage/route: Inhalation only.

•Angina pectoris

Ð Adults: 2–6 inhalations. Repeat in 3–5 minutes if neces-

sary.

•Antidote for cyanide poisoning

Ð Adults: Inhalation for 15–30 seconds q 1 minute until IV

sodium nitrite (10 ml of 3% solution) is administered over

2.5–5 minutes. This is followed immediately by 50 ml of

25% sodium thiosulfate. If signs of poisoning reappear,

administer 50% of initial dose of sodium nitrite and sodium

thiosufate.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: Lower doses may be required.

•Pediatric: Safety and efficacy have not been established in

children.

Onset of Action Peak Effect Duration

0.5 min — 3–5 min

Food: Not applicable.

Pregnancy: Category C.

Lactation: No data available. Best to avoid.

Contraindications: Hypersensitivity to nitrates or nitrites, very low

blood pressure, shock, acute MI with low ventricular filling pressure.

Advice to patient: Advise patient that if pain is not relieved after

3 doses, call paramedics or to emergency room immediately.

Editorial comments

•This drug is highly flammable. Keep away from flame and

extinguish cigarettes before using.

•This drug is not listed in the Physician’s Desk Reference, 54th

edition, 2000.

•For additional information, see isosorbide dinitrate, p. 473.

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Atenolol

Brand name: Tenormin.

Class of drug: β-Adrenergic receptor blocker.

Mechanism of action: Competitive blocker of β-adrenergic

receptors in heart and blood vessels.

Indications/dosage/route: Oral, IV.

•Hypertension

Ð Initial: PO 50 mg/d. Maximum: 100 mg/d.

•Angina

Ð Initial: PO 50 mg/d. Maintenance: 100–200 mg/d.

•Ventricular arrhythmias

Ð PO 50–100 mg/d.

•Acute MI

Ð Initial: IV 5 mg over 5 min, followed by second 5-mg dose

10 min later; then 50-mg tablet 10 min after last IVdose, then

another 50-mg dose 12 hours later, then 100 mg/d or 50 mg

b.i.d. for 6–9 days.

Adjustment of dosage

•Kidney disease: creatinine clearance 15–35 mL/min: 50 mg/d;

creatinine clearance <15 mL/min : 25 mg/d.

•Liver disease: None.

•Elderly: None.

•Pediatric: Safety and efficacy have not been established in

children.

Food: No restriction.

Pregnancy: Category B.

Lactation: Appears in breast milk. Considered compatible by the

American Academy of Pediatrics. Observe infant for hypoten-

sion, bradycardia, cyanosis.

Contraindications: Cardiogenic shock, asthma, CHF unless it is

secondary to tachyarrhythmia treated with a β blocker, sinus

bradycardia and AVblock greater than first degree, severe

COPD.

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Warnings/precautions

•Use with caution in patients with the following conditions: dia-

betes, kidney disease, liver disease, COPD, peripheral vascular

disease.

•Do not stop drug abruptly as this may precipitate arrhythmias,

angina, MI or cause rebound hypertension. If necessary to dis-

continue, taper as follows: Reduce dose by 25–50% and reassess

after 1–2 weeks. If status is unchanged, reduce by another 50%

and reassess after 1–2 weeks.

•Drug may mask the symptoms of hyperthyroidism, mainly

tachycardia.

•Drug may exacerbate symptoms of arterial insufficiency in

patients with peripheral or mesenteric vascular disease.

Advice to patient

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Change position slowly, in particular from recumbent to

upright, to minimize orthostatic hypotension. Sit at the edge of

the bed for several minutes before standing, and lie down if

feeling faint or dizzy. Avoid hot showers or baths and standing

for long periods. Male patients should sit on the toilet while

urinating rather than standing.

•Dress warmly in winter and avoid prolonged exposure to cold

as drug may cause increased sensitivity to cold.

•Avoid drinks that contain xanthines (caffeine, theophylline,

theobromine) including colas, tea, and cocoa because they may

counteract effect of drug.

•Restrict dietary sodium to avoid volume expansion.

•Drug may blunt response to usual rise in BP and chest pain

under stressful conditions such as vigorous exercise and fever.

Adverse reactions

•Common: fatigue, headache, impotence.

•Serious: symptomatic bradycardia, CHF, pulmonary edema.

Clinically important drug interactions

•Drugs that increase effects/toxicity of β blockers: reserpine,

bretylium, calcium channel blockers.

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•Drugs that decrease effects/toxicity of β blockers: aluminum salts,

calcium salts, cholestyramine, barbiturates, NSAIDs, rifampin.

Parameters to monitor

•Liver enzymes, serum BUN and creatinine, CBC with differ-

ential and platelets.

•Pulse rate near end of dosing interval or before the next dose is

taken. Areasonable target is 60–80 bpm for resting apical ventric-

ular rate. If severe bradycardia develops, consider treatment with

glucagon, isoproterenol, IVatropine (1–3 mg in divided doses). If

hypotension occurs despite correction of bradycardia, administer

vasopressor (norephinephrine, dopamine, or dobutamine).

•Symptoms of CHF. Digitalize patient and administer a diuretic

or glucagon.

•Efficacy of treatment: decreased BP, decreased number and sever-

ity of anginal attacks, improvement in exercise tolerance. Confirm

control of arrhythmias by ECG, apical pulse, BP, circulation in

extremities, and respiration. Monitor closely when changing dose.

•CNS effects. If patient experiences mental depression reduce

dosage by 50%. The elderly are particularly sensitive to

adverse CNS effects.

•Signs of bronchospasm. Stop therapy and administer large

doses of β-adrenergic bronchodilator, eg, albuterol, terbutaline,

or aminophylline.

•Signs of cold extremities. If severe, stop drug. Consider β

blocker with sympathomimetic property.

Editorial comments

•Stopping a β blocker before surgery is controversial. Some

advocate discontinuing the drug 48 hours before surgery;

others recommend withdrawal for a considerably longer time.

Notify anesthesiologist that patient has been on βblocker.

•β blockers are drugs of first choice for hypertension, particu-

larly in patients with the following conditions: previous MI,

ischemic heart disease, aneurysm, atrioventricular arrhythmias,

migraine. These drugs are also first choice for chronic stable

angina, used in conjunction with nitroglycerin.

•Following a MI, patients should be administered a β blocker.

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•β blockers are considered to be first-line drugs for prophylaxis

of migraine headache in patients who have two or more attacks

per month.

Atorvastatin

Brand name: Lipitor.

Class of drug: Antilipidemic agent.

Mechanism of action: Inhibits HMG-CoA reductase. Reduces

total LDL, cholesterol, serum triglyceride levels. There is little

if any effect on serum HDLlevels.

Indications/dosage/route: Oral only.

•Hyperlipidemia

Ð Adults: Initial: 10 mg/d. Maintenance: 10–80 mg/d.

•Homozygous familial hypercholesterolemia

Ð Adults: 10–80 mg/d.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: None.

•Pediatric: Limited data available.

Food: No restriction.

Pregnancy: Category X—contraindicated.

Lactation: Appears in breast milk. Contraindicated.

Contraindications: Hypersensitivity to statins, active liver dis-

ease or unexplained persistent elevations of serum transaminase,

pregnancy, lactation.

Warnings/precautions

•Use with caution in patients with the following conditions:

renal insufficiency, history of liver disease, alcohol abusers.

•Discontinue if drug-induced myopathy develops. This is char-

acterized by myalgia, creatinine kinase levels >10x normal.

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May cause acute renal failure from rhabdomyolysis. May occur

more frequently when drug is combined with gemfibrozil or

niacin.

•Discontinue drug if patient experiences severe trauma, surgery,

or serious illness.

Advice to patient

•Avoid alcohol.

•Use of OTC medications only with approval from treating

physician.

•Exercise regularly, reduce fat and alcohol intake, and stop

smoking.

Adverse reactions

•Common: None.

•Serious: myopathy, rhabdomyolysis, neuropathy, cranial

nerve abnormalities, hypersensitivity reactions, pancreatitis,

hepatic injury including hepatic necrosis and cirrhosis, lens

opacities.

Clinically important drug interactions

•Drugs that increase effects/toxicity of HMG-CoA reductase

inhibitors: gemfibrozil, clofibrate, erythromycin, cyclosporin,

niacin, clarithromycin, itraconazole, protease inhibitors.

•HMG-CoA reductase inhibitors increase effects/toxicity of oral

anticoagulants.

Parameters to monitor

•Total cholesterol, LDL and HDL cholesterol, triglycerides.

Values should be obtained prior to and periodically after treat-

ment begins to ascertain drug efficacy.

•Serum BUN and creatinine.

•Monitor liver enzymes before beginning therapy, at 3, 6, and

12 months thereafter, and semiannually afterward.

•Signs and symptoms of myopathy: unexplained skeletal

muscle pain, muscle tenderness or weakness particularly when

accompanied by fever or fatigue. Check creatinine kinase

levels. If these are markedly elevated or patient is sympto-

matic, discontinue drug.

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•Discontinue drug if transaminase levels exceed three times

normal values. It may be advisable to take a liver biopsy if

transaminase elevation persists after drug is discontinued.

•Patient’s ophthalmic state should be evaluated once a year fol-

lowing treatment. If lens opacity occurs, consider discontinuing

drug.

Editorial comments: Current literature suggests that the most

effective reduction of total and LDLcholesterol occurs with a

combination of exercise, weight reduction, low-fat diet, and

lipid-lowering agents.

Atracurium

Brand name: Tacrium Injection.

Class of drug:Nondepolarizing neuromuscular blocker.

Mechanism of action: Blocks nicotinic acetylcholine receptors

at neuromuscular junction resulting in skeletal muscle relax-

ation and paralysis.

Indications/dosage/route:IV only.

•Intubation and maintenance of neuromuscular blockade

Ð Adults, children >2 years: Initial: IV bolus 0.4–0.5 mg/kg.

Maintenance: 0.08–0.1 mg/kg q12–25min.

•Muscle relaxation during anesthesia

Ð Adults IV bolus: 0.25–0.35 mg/kg.

Ð Adults IV infusion: 9–10 µg/kg.

Adjustment of dosage: None.

Food: Not applicable.

Pregnancy: Category C.

Lactation: Best to avoid.

Contraindications: Hypersensitivity to acracurium and chemi-

cally related drugs.

Editorial comments

•This drug is not listed in Physician’s Desk Reference, 54th edi-

tion, 2000.

•For additional information, see rocuronium, p. 824.

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Atropine

Brand names: Atropisol, Isopto, Atropine.

Class of drug: Cholinergic blocking agent.

Mechanism of action: Blocks acetylcholine effects at mus-

carinic receptors throughout the body.

Indications/dosage/route: IV, IM, SC, oral, topical (ophthalmic).

•Anticholinergic or antispasmodic

Ð Adults: PO, 0.3–1.2 mg q 4–6 hr.

Ð Children >41 kg: same as adult.

Ð Children 29.5–41 kg: PO 0.4 mg q4–6h.

Ð Children 8.2–29.5 kg: PO 0.3 mg q4–6h.

Ð Children 7.4–8.1 kg: PO 0.15 mg q4–6h.

Ð Children 3.2–7.3 kg: PO 0.1 mg q4–6h.

•Prophylaxis of respiratory tract secretions and excess saliva-

tion during anesthesia

Ð Adults: IM, IV SC 0.4–0.6 mg 30–60 min before surgery.

Repeat doses as needed q4–6h.

Ð Children <5 kg: IM, IV, SC 0.02 mg/kg 30–60 minutes before

surgery. Repeat doses as needed q4–6h.

Ð Children >5 kg: IM, IV, SC 0.01–0.02 mg/kg, 30–60 minutes

before surgery. Repeat doses as needed q4–6h.

•Parkinsonism

Ð Adults: PO 0.1–025 mg q.i.d.

•Reversal of curariform blockade

Ð Adults: IV0.5–1.2 mg plus 0.5–2 mg neostigmine methylsulfate.

•Toxicity from cholinesterase inhibitor

Ð Adults: IV 2–4 mg, then 2 mg repeated q5–10min until mus-

carinic symptoms disappear.

Ð Children: IM, IV 1 mg, then 0.5–2 mg q5–10min until mus-

carinic symptoms disappear.

•Treatment of mushroom poisoning due to muscarine

Ð Adults: IM, IV 1–2 mg every hour until respiratory effects

decrease.

•Treatment of organophosphate poisoning

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Ð Adults: IM, IV 1–2 mg, then repeat in 10–20 minutes.

•Arrhythmias

Ð Children: IV 0.01–0.03 mg/kg.

•Uveitis

Ð Adults: 1–2 drops in each eye.

Ð Children: 1–2 drops in each eye up to t.i.d.

•Refraction

Ð Adults: 1–2 drops of the 1% solution in each eye 1 hour

before refraction.

Ð Children: 1–2 drops of the 0.5% solution in each eye 1–3

hours before refraction.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: Use with caution; higher incidence of side effects.

•Pediatric: See above.

Onset of Action Peak Effect Duration

Mydriasis Rapid 30–40 min 12 d

PO use — — 4–6 h

Pregnancy: Category C.

Lactation: Limited data available. Potentially toxic to infant.

Considered compatible by the American Academy of Pediatrics.

Contraindications: Myasthenia gravis, narrow-angle glaucoma,

GI obstruction, megacolon, active ulcerative colitis, obstructive

uropathy, hypersensitivity to atropine-type compounds (bel-

ladonna alkaloids).

Warnings/precautions

•Use with caution in patients with the following conditions: GI

infections, chronic biliary disease, CHF, arrhythmias, pulmonary

disease, benign prostatic hypertrophy, hyperthyroidism, coro-

nary artery disease, hypertension, seizures, psychosis, spastic

paralysis.

•Anticholinergic psychosis can occur in sensitive individuals.

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•Elderly may react with agitation and excitement even to small

doses of anticholinergic drugs.

•Ophthalmic atropine produces weaker effects in dark-eyed

individuals whereas the following types of patients are

highly sensitive to the drug: infants and children with Down

syndrome, spastic paralysis, brain damage, blond blue-eyed

individuals.

•More than half of deaths from ophthalmic atropine in infants

have been the result of systemic absorption of the drug.

Advice to patient

•Take medication exactly as directed. If dose is missed, do not

double subsequent dose when it is remembered.

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Use caution when exercising in hot weather as this might cause

heat prostration.

•Avoid alcohol and other CNS depressants such as opiate anal-

gesics and sedatives (eg, diazepam) when taking this drug.

•If mouth is dry, rinse with warm water frequently, chew sug-

arless gum, suck on an ice cube, or use artificial saliva. Carry

out meticulous oral hygiene (floss teeth daily).

•Visual acuity will be impaired for several days after pharma-

cologic treatment. Protect eyes from strong light by wearing

dark glasses.

Adverse reactions

•Common: Dry mouth, blurred vision (decreased accommodation),

drowsiness, tachycardia, urinary hesitancy, dry skin, constipation.

•Serious: Disorientation, hallucinations, acute narrow-angle

glaucoma, orthostatic hypotension, arrhythmia.

Clinically important drug interactions

•Drugs that increase effects/toxicity of systemic anticholiner-

gics: phenothiazines, amantadine, other antipsychotic agentics,

thiazide diuretics, tricyclic antidepressants, MAO inhibitors,

quinidine, procainamide.

•Drugs that increase effects/toxicity of ophthalmic anticholin-

ergics: corticosteroids, haloperidol.

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•Drugs that decrease effects/toxicity of systemic anticholiner-

gics: antacids, cholinergic agents.

Parameters to monitor

•Signs and symptoms of severe toxicity: tachycardia, supraven-

tricular arrythmias, delirium, seizures, agitation, hyperthermia.

Use physostigmine (Eserine) as antidote only for life-threat-

ening toxicity. Discontinue physostigmine if patient

experiences dizziness, palpitations, rapid pulse.

•Intake of fluids and urinary and other fluid output. Increase

fluid intake if inadequate. Signs of urinary retention: pelvic

pain and distention, decreased urine output. This is particularly

important in elderly with benign prostatic hypertrophy.

Determine whether there is a need for catherization.

•Opthalmic status: Intraocular pressure before and during treat-

ment, accommodation, pupillary response to light, visual

acuity (blurred vision). Discontinue administration if the fol-

lowing occur: eye pain, conjunctivitis.

Editorial comments

•This drug is not listed in the Physician’s Desk Reference, 54th

edition, 2000.

Auranofin

Brand name: Ridaira.

Class of drug: Antirheumatic agent, gold compound.

Mechanism of action: Inhibits phagocytosis, stabilizes lysoso-

mal membranes, decreases rheumatoid factor levels.

Indications/dosage/route: Oral only.

•Rheumatoid arthritis or psoriatric arthritis that does not

respond to other agents

Ð Adults: Initial: 6 mg/d as single or divided doses; increase to

9 mg/d if needed (maximum dose).

Ð Children >6 years: Initial: 0.1 mg/kg/d; increase to 0.10 mg/

kg/d if needed (maximum dose).

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Adjustment of dosage

•Kidney disease: creatinine clearance 50–80 mL/min: reduce dose

by 50%; creatinine clearance less than 50 mL/min: do not use.

•Liver disease: No adjustment necessary.

•Pediatric: Not recommended for children <6 years.

Onset of Action

≤3 mo

Food: Take shortly after eating. Take with milk or full glass of

water.

Pregnancy: Category C.

Lactation: Gold salts appear in breast milk. Potentially toxic to

infant. Related compounds considered compatible with breast-

feeding by the American Academy of Pediatrics.

Contraindications: History of gold-associated disorders such as

necrotizing enterocolitis, exfoliative dermatitis, pulmonary fibro-

sis, bone marrow insufficiency, drugs known to cause blood

dyscrasias (antimalarials, pyrazolones, immunosuppressants).

Warnings/precautions

•Use with caution in patients with the following conditions:

hepatic, renal, inflammatory bowel disease.

•Advise patient which drugs to avoid that cause blood dys-

crasias.

•In general, administer along with salicylates or NSAIDs for

first few weeks or months of therapy.

•Diabetic patients or those with CHF must be well controlled

before beginning therapy with this drug.

Advice to patient: Use sunscreen and protective clothing to avoid

photosensitivity reactions.

•A blue-gray coloration (chrysiasis) may occur on exposed sur-

faces and mucous membranes. Treat with Lugol’s solution

(strong iodine solution).

Adverse reactions

•Common: diarrhea (47%), abdominal cramping (14%), nausea,

vomiting, rash (24%), pruritus (17%), stomatitis.

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•Serious: seizures, hemorrhagic colitis, acute renal failure,

nephrotic syndrome, glomerulonephritis, pulmonary fibrosis,

eosinophilic pneumonia, thrombocytopenia, bone marrow depres-

sion, exfoliative dermatitis, hepatotoxicity, peripheral neuropathy.

Clinically important drug interactions

•Drugs that increase effects/toxicity of auranofin: penicillamine,

immunosuppressants, cytotoxic drugs.

Parameters to monitor

•Signs and symptoms of nititoid reactions following IV injec-

tion: dizziness, sweating, fainting, flushing, nausea, vomiting.

Maintain patient in recumbent position for about 15 minutes

after the injection. This reaction is transient and administration

should not be discontinued.

•Signs and symptoms of bone marrow depression.

•Urinalysis for presence of proteinuria.

•Signs and symptoms of neuropathy.

Editorial comments: This drug is not listed in the Physician’s

Desk Reference, 54th edition, 2000.

Azatadine

Brand names: Rynatan, Trinalin.

Class of drug: H

receptor blocker.

Mechanism of action: Antagonizes histamine effects on GI tract,

respiratory tract, blood vessels.

Indications/dosage/route: Oral only.

•Allergic rhinitis, relief of nasal congestion.

Ð Adults, children >12 years: 1 mg b.i.d.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: Use caution. At higher risk for side effects.

•Pediatric: See above.

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Food: No restriction.

Pregnancy: Category C.

Lactation: No data available. Potentially toxic to infant. Avoid

breastfeeding.

Contraindications: Hypersensitivity to antihistamines, acute

asthma, narrow-angle glaucoma, concurrent use of MAO inhibitor.

Editorial comments

•Usually available in combination with other agents, including

pseudoephedrine, phenylephrine, and phenylpropanolamine.

Warnings and precautions, side effects, etc, of other ingredients

should be kept in mind when prescribing.

•For additional information, see brompheniramine, p. 107.

Azathioprine

Brand name: Imuran.

Class of drug: Immunosuppressant, antirheumatic agent.

Mechanism of action: Blocks purine metabolism, inhibits DNA

synthesis, inhibits mitosis.

Indications/dosage/route: Oral, IV.

•Immunosuppressant, to prevent renal transplant rejection

Ð Initial: IV, PO 3–5 mg/kg/d. Maintenance: IV, PO 1–3 mg/kg/d.

•Severe rheumatoid arthritis not responsive to other drugs

Ð Initial: PO 1 mg/kg/d. Maintenance: PO 2–5 mg/kg/d.

Adjustment of dosage

•Kidney disease: creatinine clearance 10–50 mL/min: reduce

dose by 25%; creatinine clearance <10 mL/min: reduce dose by

50%.

•Liver disease: None.

•Elderly: None.

•Pediatric: Safety and efficacy have not been established in

children.

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Onset of Action

≤12 wk

There may be a prolonged delay prior to onset of antiinflamma-

tory action. Do not discontinue unless no effect occurs after 3

months of use for rheumatoid arthritis.

Food: No restriction.

Pregnancy: Category D. Avoid pregnancy for 4 months after

stopping drug.

Lactation: No data available. Potentially toxic to fetus. Avoid

breastfeeding.

Contraindications: Hypersensitivity to azathioprine, pregnancy.

Warnings/precautions

•Use with caution in patients with the following conditions:

liver and renal disease.

•With chronic use there is an increased risk of neoplasms, oppor-

tunistic infections.

•May cause severe bone marrow depression.

•Patients who have previously received alkylating agents such

as cyclophosphamide, chlorambucil, and melphalan may be at

increased risk for carcinogenesis from azathioprine.

Advice to patient

•Use two forms of birth control including hormonal and barrier

methods.

•Male patients should use condoms if engaging in sexual inter-

course while using this medication.

•Avoid crowds as well as persons who may have a contagious disease.

•Receive vaccinations (particularly live attenuated viruses) only

with permission from treating physician.

•Avoid the use of OTC medications without first informing the

treating physician.

Adverse reactions

•Common: nausea, vomiting.

74 AZATHIOPRINE

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•Serious: bone marrow depression (thrombocytopenia,

leukopenia, anemia), pancreatitis hepatotoxicity, systemic

infections, hypotension, retinopathy, hypersensitivity reactions.

Clinically important drug interactions

•Drugs that increase effects/toxicity of azathioprine: allopuri-

nol, methotrexate, ACE inhibitors, other immunosuppressants,

alkylatingagents.

•Azathioprine decreases effects/toxicity of following drugs:

anticoagulants, corticosteroids, nondepolarizing neuromuscu-

lar blockers.

Parameters to monitor

•Frequent monitoring of CBC with differential and platelet

count, liver enzymes.

•Signs and symptoms of hepatotoxicity.

•Efficacy in rheumatoid arthritis: increased range of motion,

decreased swelling and joint pain.

•Nausea and vomiting. If necessary, administer antiemetic drug.

•Liver enzymes.

Editorial comments

•Because of risk of severe bone marrow depression, frequent

monitoring of complete blood counts and platelet counts are

recommended. It is suggested that these should be performed

weekly for the first month, twice monthly for the second and

third months, and then monthly thereafter. Additionally they

should be monitored if dosage changes are made. Discontinuation

of the drug is recommended if there is rapid development of

leukopenia, thrombocytopenia, or other signs of bone marrow

depression.

•Azathioprine is used as a steroid-sparing agent in a variety of

autoimmune disorders including inflammatory bowel disease. The

active metabolite of azathioprine is 6-mercaptopurine. Ran-

domized, double blind placebo controlled trials have demon-

strated efficacy of 6-mercaptopurine and azathioprine inactive

or quiescent Crohn’s disease. Patients in these trials were often

able to taper prednisone doses to 5 mg/d or less. Doses for

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6-mercpatopurine were generally 1.5 mg/kg/d and for azathio-

prine 2.5 mg/kg/d.

•Cytotoxic drug. Use latex gloves and safety glasses when han-

dling parenteral form of this medication. Avoid contact with

skin and inhalation. If possible prepare in biologic hood.

Azithromycin

Brand name: Zithromax.

Class of drug: Antibiotic, macrolide.

Mechanism of action: Inhibits RNA-dependent protein synthe-

sis at the level of the 50S ribosome.

Susceptible organisms in vivo: Like erythromicin but less active

against gram-positive bacteria and more active against gram-

negative bacteria. Better against Hemophilus influenzae and

Moraxella catarrhalis. Also useful against Mycobacterium

avium-intracellulareand Helicobacter pylori.

Indications/dosage/route: Oral, IV.

•Community-acquired pneumonia

Ð Adults: IV 500 mg as single daily dose, at least 2 days.

Follow by oral dosing 500 mg/d, 7–10 days.

•Acute pelvic inflammatory disease

Ð IV 500 mg as single daily dose, 1 or 2 days. Follow by oral

dosing 250 mg/d 7 days.

•Mild to moderate acute exacerbation of COPD, community-acquired

pneumonia (mild to moderate), pharyngitis/tonsillitis (second-

line therapy), uncomplicated skin and skin structure infections

Ð Adults: PO 500 mg as single dose on first day, then 250 mg/d,

days 2–5.

•Genital ulcer disease (chanchroid), nongonoccocal urethritis

and cervicitis

Ð Adults: PO 1 g as single dose.

•Urethritis and cervicitis (Neisseria gonorrhoeae)

Ð Adults: PO 2 g as single dose. (Note: resistance is a problem.)

76 AZITHROMYCIN

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•Acute otitis media, community-acquired pneumonia

Ð Children: Oral suspension 10 mg/kg as single dose on first

day, then 5 mg/kg days 2–5. Maximum: 250 mg/d.

•Pharyngitis/tonsillitis

Ð Children >2 years: Oral suspension 12 mg/kg once daily,

days 1–5.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: None.

•Pediatric: Safety and efficacy have not been established for

children <6 months for treatment of acute otitis media and <2

years for treatment of pharyngitis/tonsillitis.

Food: Should be taken on empty stomach, 1–2 hours after

meals.

Pregnancy: Category B.

Lactation: No data available. May appear in breast milk. Best to

avoid.

Contraindications: Hypersensitivity to macrolide antibiotics.

Warnings/precautions: Use with caution in patients with hepatic

dysfunction.

Adverse reactions

•Common: None.

•Severe: pseudomembranous colitis, ventricular arrhythmias,

nephritis, cholestatic jaundice, angioedema.

Clinically important drug interactions

•Drugs that decrease effects/toxicity of macrolides: rifampin,

antacids (aluminum, magnesium).

•Macrolides increase effects/toxicity of following drugs: oral

anticoagulants, astemizole, benzodiazepines, bromocriptine,

buspirone, carbamazepine, cisapride, cyclosporine, digoxin,

ergot alkaloids, felodipine, grepafloxacin, statins, pimozide,

sparfloxacin, tacrolimus.

Parameters to monitor

•Signs and symptoms of superinfection, in particular pseudomem-

branouscolitis.

•Signs and symptoms of renal toxicity.

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•Signs and symptoms of hearing impairment. Patients with

kidney or liver disease are at highest risk.

Editorial comments

•Azithromycin has the advantage of improved compliance com-

pared with erythromycin because of better tolerability, daily

dosage, and shorter course of therapy.

•Often used as outpatient medication and inpatient for

community-acquired pneumonia.

•It may be combined with ceftriaxone or cefuroxime for com-

munity-acquired pneumonia.

•Increasing resistance in Streptococcus pneumoniae is a prob-

lem.

•It is also useful for otitis media, sinusitis, and as single 1-g dose

for nongonoccocal urethritis.

78 AZITHROMYCIN

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Bacampicillin

Brand name: Spectrobid.

Class of drug: Antibiotic, penicillin family.

Mechanism of action: Inhibits bacterial cell wall synthesis.

Susceptible organisms in vivo: staphylococci, Streptococcus

pneumoniae, beta-hemolytic streptococci, Streptococcus faecalis,

Streptococcus viridans, Escherichia coli, Hemophilus influen-

zae, Neisseria gonorrhoeae, Proteus mirabilis, Salmonella sp,

Shigellasp.

Indications/dosage/route: Oral only.

•Severe upper respiratory tract, urinary tract, skin and skin

structure infections:

Adults: 800 mg q12h.

Children >25 kg: 50 mg/kg/d, two equal doses.

•Lower respiratory tract infections

Adults: 800 mg q12h.

Children >25 kg: 50 mg/kg/d, two equal doses

•Gonorrhea, acute uncomplicated urogenital infections

Adults: 1.6 g plus 1 g probenecid as single dose.

Adjustment of dosage: None.

Food: No restrictions.

Pregnancy: Category B.

Lactation: Appears in breast milk. Use with caution.

Contraindications: Hypersensitivity to penicillin or cephalosporins.

Editorial comments

•Bacampicillin has no advantage over ampicillin and has a sim-

ilar spectrum of activity. 1 g of bacampicillin ≅700 mg of

ampicillin.

•For additional information, see ampicillin, p. 53.

Baclofen

Brand name: Lioresal.

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Class of drug: Skeletal muscle relaxant.

Mechanism of action: Inhibits mono- and polysynaptic reflexes

within the spinal cord resulting in decreased spasticity.

Indications/dosage/route: Oral only.

•Spasticity of multiple sclerosis and spinal cord lesion

Ð Adults: Initial: 15 mg/d, may increase dose every 3 days by

5–15 mg/d. Maximum: 80 mg/d, q8h.

Ð Children 2–7 years: Initial: 10–15 mg/kg/d, may increase

dose every 3 days by 5–15 mg/d. Maximum: 40 mg/d.

Ð Children >8 years: Initial: 10–15 mg/d, titrate dose as above.

Maximum: 80 mg/d.

Adjustment of dosage

•Kidney disease: reduce dose.

•Liver disease: no reduction required.

•Elderly: reduce dose.

•Pediatric: see above.

Onset of Action Peak Effect

3–4 d 5–10 d

Food: Take with food or milk.

Pregnancy: Category C.

Lactation: Appears in breast milk. Considered compatible by

American Academy of Pediatrics.

Contraindications: Hypersensitivity to baclofen.

Warnings/precautions

•Use with caution in patients with the following conditions:

seizures, decreased renal function.

•Seizure threshold may be lowered in epileptics.

•Patients requiring spasticity to maintain posture and balance

may worsen with treatment.

•Avoid abrupt withdrawal.

Advice to patient

•Avoid alcohol and other CNS depressants such as opiate anal-

gesics and sedatives (eg, diazepam) when taking this drug.

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•Change position slowly, in particular from recumbent to

upright, minimizing orthostatic hypotension. Sit at the edge of

the bed for several minutes before standing, lie down if feeling

faint or dizzy. Avoid hot showers or baths and standing for long

periods. Male patients with orthostatic hypotension may be

safer urinating while seated on the toilet rather than standing.

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Do not stop drug abruptly as this may precipitate withdrawal

reaction (anxiety, hallucinations, tachycardia, seizures).

Adverse reactions

•Common: slurred speech, dizziness, drowsiness.

•Serious: psychiatric abnormalities, confusion, syncope, dys-

pnea, hallucinations, depression.

Clinically important drug interactions

•Drugs that increase effects/toxicity of balclofen: antihistamines,

sedatives, opioids, CNS depressants, alcohol, MAO inhibitors.

Parameters to monitor

•Evaluate patient for orthostasis.

•Monitor for sedation and CNS side effects.

•Signs of hypersensitivity reactions.

Editorial comments: Balclofen appears to also be an effective

treatment for refractory hiccups (singultus).

•This drug is listed without details in Physician’s Desk Refe-

rence, 54th edition, 2000.

Beclomethasone

Brand names: Beclovent, Vanceril, Beconase, Vancenase.

Class of drug: Inhalation corticosteroid.

Mechanism of action: Inhibits elaboration of many of the medi-

ators of allergic inflammation, eg, leukotrienes and other prod-

ucts of the arachidonic acid cascade.

Indications/dosage/route: Metered dose inhaler.

•Asthma

Ð Adults, children ≥ 12 years: 2–4 inhalations t.i.d. to q.i.d.

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Ð Children 6–12 years: 1–2 inhalations. Maximum: 10 inhala-

tions.

•Severe asthma

Ð Adults: Initial: 12–16 inhalations/d, decrease according to

response. Maximum: 20 inhalations/d.

•Seasonal or perennial rhinitis

Ð Adults, children ≥ 12 years 1 inhalation, each nostril b.i.d. to q.i.d.

Ð Children 6–12 years: 1 inhalation, each nostril, t.i.d.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: None.

•Pediatric: Safety and efficacy have not been established in

children <6 years.

Pregnancy: Category C.

Lactation: Present in breast milk. Safe to use.

Contraindications: Untreated fungal, bacterial, or viral infec-

tions, untreated infections of nasal mucosa, hypersensitivity to

corticosteroids.

Warnings/precautions

•Use with caution in patients with the following conditions:

tuberculosis of the respiratory tract (active or quiescent), expo-

sure to measles or chicken pox.

•If a patient is transferred from systemic corticosteroid to

inhalation drug, symptoms of steroid withdrawal may result.

These include muscle and joint pain, depression. Alternatively,

adrenal insufficiency may occur: weakness, fatigue, nausea,

anorexia.

•Provide patient with instructions for use of the inhaler or nasal

spray and make sure patient completely understands these

instructions.

•Provide patient with a list of side effects and note those that

require immediate reporting to the physician.

•Patients on long-term inhaled or intranasal corticosteroids

may require steroid pulsing during stress, eg, surgery or

infection.

82 BECLOMETHASONE

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Advice to patient

•Rinse mouth and gargle with warm water after each inhalation.

This may minimize the development of dry mouth, hoarseness,

and oral fungal infection.

•This drug should be inhaled 5 minutes after a previously

inhaled bronchodilator, eg, albuterol.

•Do not exceed recommended dosage of the drug. Excessive

doses have been associated with adrenal insufficiency.

•Notify physician if worsening symptoms occur.

•Carry a card indicating your condition, drugs you are taking,

and need for supplemental steroid in the event of a severe asth-

matic attack. Attempt to decrease dose once the desired clini-

cal effect is achieved. Decrease dose gradually every 2–4

weeks. Return to initial starting dose if symptoms recur.

•Stop smoking.

•Do not overuse the inhaler.

Adverse reactions

•Common: nasal irritation, cough, pharyngitis, sneezing attacks.

•Serious: adrenal insufficiency, hypercorticism, urticaria, angioe-

dema, bronchospasm, increased intraocular pressure, cataracts,

oropharyngeal or esophageal candidiasis.

Clinically important drug interactions: None.

Parameters to monitor

•Signs and symptoms of acute adrenal insufficiency, particu-

larly in response to stress.

•Child growth: Drug may suppress growth.

•Changes in nasal mucosa in patients on long-term drug ther-

apy.

•Signs of localized infection in mouth and pharynx, eg, red

membranes with vesicular eruptions. Treat with appropriate

antifungal drug, eg, nystatin, or discontinue treatment.

•When switching from systemic inhalation therapy, monitor patient

for symptoms of adrenal insufficiency: hypotension, weight loss,

muscular and joint pain. If these occur, the dose of systemic steroid

should be increased followed by slower withdrawal. It may

require up to 12 months for HPAfunction to fully recover.

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Editorial comments

•Inhaled corticosteroids are the drug of choice for patients with

refractory symptoms on prn adrenergic agonist bronchodila-

tors.

•Inhalation steroids are useful in reducing the dose or discontin-

uing use of oral corticosteroids. However, there is considerable

controversy with respect to the beneficial use of higher than

recommended inhalation doses of these drugs.

•Doses for beclomethasone are 42 µg per bronchial and nasal

inhalation. Double-strength forms are available for both

(84 µg/dose).

Benazepril

Brand name: Lotensin.

Class of drug: ACE inhibitor.

Mechanism of action: Inhibits ACE, thereby preventing conver-

sion of angiotensin I to angiotensin II, resulting in decreased

peripheral arterial resistance.

Indications/dosage/route: Oral only.

• Hypertension: Patients receiving a diuretic

Ð Initial: 10 mg/d. Maintenance: 20–40 mg/d.

• Hypertension: Patients receiving a diuretic

Ð Initial: 5 mg/d.

Adjustment of dosage

•Kidney disease: Creatinine clearance <30 mL/min: initial dose

5 mg/d.

•Liver disease: None.

•Elderly: None.

•Pediatric: Safety and efficacy in children have not been estab-

lished.

84 BENAZEPRIL

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Onset of Action Duration

1 h 24 h

Food: No restrictions.

Pregnancy: Category C first trimester, Category D second and

third trimesters.

Lactation: Appears in breast milk. Considered compatible by

American Academy of Pediatrics.

Contraindications: Hypersensitivity to ACE inhibitors, heredi-

tary or idiopathic angioedema, second and third trimesters of

pregnancy.

Warnings/precautions

•Use with caution in patients with the following conditions:

kidney disease, especially renal artery stenosis, drugs that cause

bone marrow depression, hypovolemia, hyponatremia, cardiac

or cerebral insufficiency, collagen vascular disease, lupus ery-

thematosus, scleroderma, patients undergoing dialysis.

•ACE inhibitors have been associated with anaphylaxis and

angioedema.

•Use extreme caution in combination with potassium-sparing

diuretics (high risk of hyperkalemia).

•Sodium- or volume-depleted patients may experience severe

hypotension. Lower initial doses are advised.

•During surgery/anesthesia, the drug may increase hypotension.

Volume expansion may be required.

•There may be a profound drop in BP after the first dose is taken.

Close medical supervision is necessary once therapy is begun.

Advice to patient

•Do not use salt substitutes containing potassium.

•Use two forms of birth control including hormonal and barrier

methods.

•Avoid NSAIDs; may be present in OTC preparations.

•Take BP periodically and report to treating physician if signif-

icant changes occur.

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•Stop drug if prolonged vomiting or diarrhea occurs. These

symptoms may indicate plasma volume reduction.

•Discontinue drug immediately if signs of angioedema (swelling

of face, lips, extremities; breathing or swallowing difficulty) become

prominent, and notify physician immediately if this occurs. If chronic

cough develops, notify treating physician.

Adverse reactions

•Common: none.

•Serious: bone marrow depression (neutropenia, agranulocytosis),

hypotension, angioedema, tachycardia, hyperkalemia, oliguria,

autoimmune symptom complex (see Editorial Comments), ele-

vated liver enzymes, asthma.

Clinically important drug interactions

•Drugs that increase effects/toxicity of benazepril: potassium-

sparing drugs, other diuretics, guanethidine.

•Drugs that decrease effectiveness of benazepril: NSAIDs, antacids,

cyclosporine.

•Benazepril increases effects/toxicity of following drugs: lithium,

azothioprine, allopurinol, digoxin.

Parameters to monitor

•Patient’s electrolytes, CBC with differential and platelet count,

BUN, and creatinine.

•Signs and symptoms of angioedema: swelling of face, lips,

tongue, extremities, glottis, larynx. Observe in particular

for obs-truction of airway, difficulty in breathing. If symp-

toms are not relieved by an antihistamine, discontinue drug.

•Patient’s BP closely, particularly at beginning of therapy.

Observe for evidence of severe hypotension. Patients who are

hypovolemic due to GI fluid loss or diuretics may exhibit severe

hypotension. Also monitor for orthostatic changes.

•Signs of persistent, nonproductive cough; this may be drug-

induced.

•Changes in weight in patients with CHF. Gain of more than

2 kg/wk may indicate development of edema.

•Signs and symptoms of infection.

•Possible antinuclear antibody development.

86 BENAZEPRIL

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•WBC monthly (first 3–6 months) and at frequent intervals

thereafter for patients with collagen vascular disease or renal

insufficiency. Discontinue therapy if neutrophil count drops

below 1000.

•Signs and symptoms of bone marrow depression.

•Intake of fluids and urinary and other fluid output to minimize

renal toxicity. Increase fluid intake if inadequate. Closely

monitor electrolyte levels.

•Signs and symptoms of renal toxicity.

Editorial comments

•Unlabeled uses of ACE inhibitors include hypertensive crisis,

diagnosis of renal artery stenosis, hyperaldosteronism,

Raynaud’s phenomenon, angina, diabetic nephropathy.

•ACE inhibitors have been associated with an autoimmune-type

symptom complex including fever, positive antinuclear anti-

body, titers, myositis, vasculitis, and arthritis.

•Once daily dosing to twice daily dosing improves compli-

ance.

•The ACE inhibitors have been a highly efficacious and well-

tolerated class of drugs. Nearly every large randomized clinical

trial examining their use has been favorable. First, a con-

sensus trial proved that enalapril decreases mortality and

increases quality of life in class II and III CHF patients. Then

the SOLVE trial and others proved their benefits in remod-

eling myocardium post MI. The DCCT trial of diabetic

patients demonstrated the ability of ACE inhibitors to

decrease the small vessel damage to retinas and glomeruli.

Clinical trials looking into primary prevention of cardiac

effects are ongoing. Treatment with this class of drugs is the

gold standard in patients with left ventricular systolic dys-

function. The two most common adverse effects of ACE

inhibitors are cough and angioedema. Transient and persist-

ent rises in antinuclear antibody have been noted. As drugs

in this class are vasodilators, orthostasis is another potential

problem.

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Bendroflumethiazide

Brand name: Naturectin.

Class of drug: Thiazide diurectic.

Mechanism of action: Inhibits sodium resorption in distal tubule,

resulting in increased urinary excretion of sodium, potasssium,

and water.

Indications/dosage/route: Oral only.

•Diuretic

Ð Adults: Initial: 2.5–20 mg once or twice daily, once every other

day, or once a day for 3–5 weeks. Maintenance: 2.5–5 mg/d.

Ð Children: Initial: 0.4 mg/kg, as single dose or two divided

doses.

•Hypertension

Ð Adults: Initial: 2.5–20 mg/d. Adjust to response.

Ð Children: Initial: 0.005–0.4 mg/kg. Adjust to response.

Ð Elderly: Use lower doses. Risk of postural hypotension.

Adjustment of dosage

•Kidney disease: Use with caution. Ineffective in severe renal

failure.

•Liver disease: Use with caution. May cause electrolyte imbal-

ance.

•Elderly: Use with caution. Risk of postural hypotension.

•Pediatric: See above.

Onset of Action Peak Effect Duration

1–2 h 4 h 6–24 h

Food: Should be taken with food.

Pregnancy: Category C. Use only if potential benefit to mother

outweighs risk to fetus.

Lactation: No data available. Hydrochlorothiazide (another thi-

azide diuretic) is considered compatible with breastfeeding by

the American Academy of Pediatrics. Thiazide diuretics may

suppress lactation.

88 BENDROFLUMETHIAZIDE

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Contraindications: Anuria, hypersensitivity to thiazides or

sulfonamide-derived drugs.

Editorial comments

•Do not coadminister with allopurinol as the combination may

lead to severe hypersensitivity vasculitis.

•For additional information, see hydrochlorothiazide, p. 426.

Benztropine

Brand name: Cogentin.

Class of drug: Cholinergic blocking agent.

Mechanism of action: Blocks acetylcholine effects at muscarinic

receptors throughout the body.

Indications/dosage/route: Oral, IM.

•Idiopathic parkinsonism

Ð Adults: PO 0.5–6 mg/d.

•Postencephalitic parkinsonism

Ð Adults: IM, PO 2 mg/d in one or more doses.

•Drug-induced extrapyramidal effects

Ð Adults: IM, PO 1–4 mg, 1–2 times/d.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: Use with caution; higher incidence of side effects.

•Pediatric: Contraindicated in children under 3. Use with extreme

caution in older children.

Onset of Action Peak Effect Duration

1–2 h — 2–3 days

Pregnancy: Category C.

Lactation: No data available. Potentially toxic to infant. Avoid

breastfeeding.

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Contraindications: Myasthenia gravis, narrow-angle glaucoma,

GI obstruction, megacolon, colitis, ulcerative colitis, obstructive

uropathy, hypersensitivity to atropine-type compounds (bel-

ladonna alkaloids), children <3 years.

Warnings/precautions

•Use with caution in patients with the following conditions: GI

infections, chronic biliary disease, CHF, arrhythmias, pul-

monary disease, benign prostatic hypertrophy, hyperthyroidism,

coronary artery disease, hypertension, seizures, psychosis, spas-

tic paralysis.

•Anticholinergic psychosis can occur in sensitive individuals.

•Elderly may react with agitation and excitement even to small

doses of anticholinergic drugs.

Advice to patient

•Take medication exactly as directed. If dose is missed, do not

double subsequent dose when it is remembered.

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Use caution when exercising in hot weather as this might cause

heat prostration.

•Avoid alcohol and other CNS depressants such as opiate anal-

gesics and sedatives (eg, diazepam) when taking this drug.

•If mouth is dry, rinse with warm water frequently, chew sugar-

less gum, suck on an ice cube, or use artificial saliva. Carry out

meticulous oral hygiene (floss teeth daily).

•Patients with Parkinson’s disease should not stop this drug

abruptly.

Adverse reactions

•Common: dry mouth, blurred vision (decreased accommoda-

tion), drowsiness, tachycardia, urinary hesitancy, dry skin, con-

stipation.

•Serious: disorientation, hallucinations, acute narrow-angle glau-

coma, orthostatic hypotension, arrhythmia.

Clinically important drug interactions

•Drugs that increase effects/toxicity of systemic anticholiner-

gics: phenothiazines, amantadine, other antipsychotic agentics,

90 BENZTROPINE

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thiazide diuretics, tricyclic antidepressants, MAO inhibitors,

quinidine, procainamide.

•Drugs that decrease effects/toxicity of systemic anticholiner-

gics: antacids, cholinergic agents.

Parameters to monitor

•Signs and symptoms of severe toxicity: tachycardia, supraven-

tricular arrythmias, delirium, seizures, agitation, hyperthermia.

Discontinue if patient experiences dizziness, palpitations, rapid

pulse. Use physostigmine (Eserine) as antidote only for life-

threatening toxicity.

•Intake of fluids and urinary and other fluid output. Increase

fluid intake if inadequate.

•Signs of urinary retention: pelvic pain and distention, decreased

urine output. This is particularly important in elderly with benign

prostatic hypertrophy. Determine whether there is a need for

catherization.

•Ophthalmic status: intraocular pressure before and during treat-

ment, accommodation, pupillary response to light, visual acuity

(blurred vision). Discontinue administration if the following

occur: eye pain, conjunctivitis.

Editorial comments: IV administration of benztropine offers no

advantage over IM. It is therefore recommended not to use IV

benztropine.

Bepridil Hydrochloride

Brand name: Vascor.

Class of drug: Calcium channel blocker.

Mechanism of action: Inhibits calcium movement across cell

membranes.

Indications/dosage/route: Oral only.

•Angina

Ð Adults: Initial: 200 mg once daily. Maintenance: 200–300

mg/d. Maximum: 400 mg/d.

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Adjustment of dosage

•Kidney disease: Use with caution. Guidelines have not been

established.

•Liver disease: Use with caution. Guidelines have not been estab-

lished.

•Elderly: Use normal dose with caution.

•Pediatric: Safety and efficacy have not been established in

children.

Onset of Action Peak Effect Duration

0.5–1 h 2–3 h 4–8 h

Food: No restriction.

Pregnancy: Category C.

Lactation: Probably appears in breast milk. Potentially toxic to

infant. Avoid breastfeeding.

Contraindications: Hypersensitivity to calcium blockers.

Editorial comments: For additional information, see felodipine,

p. 346.

Betamethasone

Brand names: Celestone, Diprosone, Uticort, Valisone, Diprolene.

Class of drug: Topical and systemic antiinflammatory gluco-

corticoid.

Mechanism of action: Inhibits migration of polymorphonuclear

leukocytes; stabilizes lysomal membranes; inhibits production

of products of arachidonic acid cascade.

Indications/dosage/route: IM, topical, intraarticular, intrabursal,

intradermal. Dosages of corticosteroids are variable. These should

be individualized according to the disease being treated and the

response of the patient.

•Adrenal insufficiency

92 BETAMETHASONE

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Ð Initial: IM 0.5 mg/d.

•Bursitis, peritendinitis, tenosynovitis

Ð Intrabursal: 3 mg (1 mL).

•Rheumatoid arthritis and osteoarthritis

Ð Intraarticular: 0.75–6 mg (0.25–2 mL).

•Acute gouty arthritis

Ð Intraarticular 1.5–3 mg (0.5–1 mL).

•Dermatologic conditions

Ð Intradermal: 0.2 mL/cm

, not to exceed 1 mL/wk.

•Corticosteroid-responsive dermatoses

Ð Apply thin layer to affected area once or twice a day.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: None.

•Pediatric: Systemic use: Children on long-term therapy must be

monitored carefully for growth and development. Topical use:

Safety and efficacy have not been established in children <12.

Food: Not applicable.

Pregnancy: Category C.

Lactation: No data available. Best to avoid.

Contraindications: Systemic use: fungal, viral, or bacterial infec-

tions, Cushing’s syndrome. Topical use: hypersensitivity to cor-

ticosteroids, markedly impaired circulation, occlusive dressing

if primary skin infection is present, monotherapy in primary bac-

terial infections, eg, impetigo, cellulitis, rosacea, ophthalmic

use, plaque psoriasis (widespread).

Warnings/precautions

•Use with caution in patients with the following conditions:

diabetes mellitus, cardiovascular disease, hypertension, throm-

bophlebitis, renal or hepatic insufficiency. Topical agent: Use

with caution in patients with primary skin infections and those

receiving other immunosuppressant drugs.

•Skin test patient for tuberculosis before beginning treatment if

patient is at high risk.

•For long-term treatment consider alternative-day dosing; how-

ever, if the disease flares, may need to return to initial daily dose.

BETAMETHASONE 93

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•Observe neonates for signs of adrenal insufficiency if mother

has taken steroids during pregnancy.

•Tapering is always required when administration of a steroid

is stopped. Avariety of procedures for tapering after long-term

therapy have been suggested. For example, taper dose by 5 mg/

wk until 10 mg/d is reached. Then 2.5 mg/wk until therapy is

discontinued or lowest dosage giving relief is reached. Longer

tapering periods may be required for some patients. Adrenal

insufficiency may persist for up to 1 year.

•Attempt dose reduction periodically to determine if disease can

be controlled at a lower dose. When every-other-day therapy

is initiated, twice the daily dose should be administered on

alternate days in the morning.

•Check whether patient is allergic to tartrazine which is present

in some of these drugs.

Adverse reactions

•Common: dyspepsia, appetite stimulation, insomnia, anxiety,

fluid retension, cushinoid facies.

•Serious: Cushing-like syndrome, adrenocortical insufficiency,

muscle wasting, osteoporosis, immunosuppression with increased

susceptibility to infection, potassium loss, glaucoma, cataracts

(nuclear, posterior, subcapsular), hyperglycemia, hypercorticism,

peptic ulcer, psychosis, insomnia, skin atrophy, thrombosis,

seizures, angioneuritic edema. Children: Growth suppression,

pseudotumor cerebri (reversible papilledema, visual loss, nerve

paralysis [abducens or oculomotor]), vascular bone necrosis, pan-

creatitis.

•T

opical: Common: itching, burning, skin dryness, erythema, fol-

liculitis, hypertrichosis, allergic contact dermatitis, skin macer-

ation, secondary infection, striae, millaria, skin atrophy. Serious:

HPAaxis suppression, Cushing’s syndrome.

Clinically important drug interactions

•Systemic

Ð Drugs that increase effects/toxicity of corticosteroids: broad-

spectrum antibiotics, anticholinergics, oral contraceptives,

cyclosporine, loop diuretics, thiazide diuretics, NSAIDs, tri-

cyclic antidepressants.

94 BETAMETHASONE

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Ð Drugs that decrease effects/toxicity of corticosteroids:

barbiturates, cholestyramine, ketoconazole, phenytoin,

rifampin.

Ð Corticosteroids increase effects/toxicity of following drugs:

digitalis glycosides, neuromuscular blocking drugs.

Ð Corticosteroids decrease effects of vaccines, toxoids.

•Topical: None.

Editorial comments: Corticoid treatment remains challeng-

ing for clinicians due to commonly occurring short-term and

long-term side effects. With chronic use, adrenal suppression

may persist for up to 1 year. The agents produce accelerated

bone resorption as well as decreased bone formation, result-

ing in overall bone loss with chronic use. Ongoing monitor-

ing is suggested and treatment with bisphosphonates or

calcitonin is suggested when decreased bone mineral density

occurs.

Betaxolol

Brand names: Kerlone, Betoptic.

Class of drug: β-Adrenergic receptor blocker.

Mechanism of action: Competitive blocker of β-adrenergic

receptors in heart, blood vessels, and eyes.

Indications/dosage/route: Oral, topical (ophthalmic).

•Hypertension

Ð Adults: Initial: PO 10–20 mg/d. Maximum: 20 mg/d.

Ð Elderly: Initial: PO 5 mg/d. Maximum: 10 mg/d.

•Glaucoma

Ð Ophthalmic preparations: 1–2 drops b.i.d. in affected eye.

Adjustment of dosage

•Kidney disease (severe): PO initial dose 5 mg q.d.

•Liver disease: None.

•Elderly: See above.

BETAXOLOL 95

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•Pediatric: Safety and efficacy have not been established in chil-

dren.

Food: No restriction.

Pregnancy: Category C.

Lactation: Appears in breast milk. Potentially toxic to infant.

Best to avoid.

Contraindications: Cardiogenic shock, CHF unless it is second-

ary to tachyarrhythmia treated with a βblocker, sinus bradycar-

dia and AVblock greater than first degree, severe COPD.

Warnings/precautions

•Use with caution in patients with the following conditions: dia-

betes, kidney disease, liver disease, COPD, peripheral vascu-

lar disease.

•Do not stop drug abruptly as this may precipitate arrhythmias,

angina, MI or cause rebound hypertension. If necessary to dis-

continue, taper as follows: Reduce dose and reassess after 1–2

weeks. If status is unchanged, reduce by another 50% and

reassess after 1–2 weeks.

•Drug may mask symptoms of hyperthyroidism, mainly tachy-

cardia.

•Drug may exacerbate symptoms of arterial insufficiency in

patients with peripheral or mesenteric vascular disease.

Advice to patient

•Avoid driving and other activities requiring mental alertness

or that are potentially dangerous until response to drug is

known.

•Dress warmly in winter and avoid prolonged exposure to cold

as drug may cause increased sensitivity to cold.

•Avoid drinks that contain xanthines (caffeine, theophylline,

theobromine) including colas, tea, and cocoa because they may

counteract the effect of drug.

•Restrict dietary sodium to avoid volume expansion.

•Drug may blunt response to usual rise in BP and chest pain

under stressful conditions such as vigorous exercise and

fever.

96 BETAXOLOL

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Adverse reactions

•Common: headache, dizziness.

•Serious: symptomatic bradycardia, CHF, worsened AVblock,

hypotension, depression, bone marrow, depression, SLE-like

syndrome, bronchospasm, Peyronie’s disease, hepatitis.

Clinically important drug interactions

•Drugs that increase effects/toxicity of β blockers: reserpine,

bretylium, calcium channel blockers.

•Drugs that decrease effects/toxicity of β blockers: aluminum salts,

calcium salts, cholestyramine, barbiturates, NSAIDs, rifampin.

Parameters to monitor

•Liver enzymes, serum BUN and creatinine, CBC with differ-

ential and platelets.

•Patient’s pulse rate near end of dosing interval or before next dose

is taken. Areasonable target is 60–80 bpm for resting apical ven-

tricular rate. If severe bradycardia develops, consider treatment

with glucagon, isoproterenol, IV atropine (1–3 mg in divided

doses). If hypotension occurs despite correction of bradycardia,

administer vasopressor (norephinephrine, dopamine, or dobuta-

mine).

•Symptoms of CHF. Digitalize patient and administer a diuretic

or glucagon.

•Efficacy of treatment: decreased BP, decreased number and

severity of anginal attacks, improvement in exercise tolerance.

Confirm control of arrhythmias by ECG, apical pulse, BP, cir-

culation in extremities, and respiration. Monitor closely when

changing dose.

•CNS effects. If patient experiences mental depression reduce

dosage by 50%. The elderly are particularly sensitive to

adverse CNS effects.

•Signs of bronchospasm. Stop therapy and administer large doses

of β-adrenergic bronchodilator, eg, albuterol, terbutaline, or amino-

phylline.

•Signs of cold extremities. If severe, stop drug. Consider β

blocker with sympathomimetic property.

BETAXOLOL 97

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•Intraocular pressure (ophthalmic use): If inadequately controlled,

administer another narcotic concomitantly (pilocarpine, epi-

nephrine or acetazolamide).

Editorial comments

•Stopping a β blocker before surgery is controversial. Some

advocate discontinuing the drug 48 hours before surgery;

others recommend withdrawal for a considerably longer time.

Notify anesthesiologist that patient has been on βblocker.

•β blockers are first-line treatments for hypertension particu-

larly in patients with the following conditions: previous MI,

ischemic heart disease, aneurysm, atrioventricular arrhythmias,

migraine. These are drugs of first choice for chronic stable angina,

used in conjunction with nitroglycerin.

•Many studies indicate benefit from administration of a β blocker

following an MI.

•β blockers are considered to be first-line drugs for prophylaxis

of migraine headache in patients who have two or more attacks

per month.

Bethanechol

Brand name: Urecholine.

Class of drug: Cholinergic agonist, parasympathomimetic.

Mechanism of action: Stimulant of postsynaptic cholinergic

receptors in urinary bladder and GI tract. This causes increased

contractility and peristalsis.

Indications/dosage/route: Oral, SC.

•Urinary retention due to neurogenic bladder and other nonob-

structive causes, GI prokinetic

Ð Adults: PO 10–50 mg, b.i.d. to q.i.d. SC 7.5–20 mg/d, divided

as t.i.d. or q.i.d. doses. Maximum SC dose: 10 mg 0.4 h for

neurogenic bladder.

Ð Children: PO 0.6 mg/kg/d, divided as t.i.d. or q.i.d. doses. SC

0.15–0.2 mg/kg/d.

98 BETHANECHOL

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Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: May be at higher risk for side effects.

•Pediatric: Safety and efficacy have not been established in chil-

dren <5 years.

Onset of Action Duration

Oral 30–90 min 6 h

SC 5–15 min 2 h

Food: Should be taken 1 hour before or 2 hours after meals when

given orally. For SC administration, take 2 hours before meals.

Pregnancy: Category C.

Lactation: No data available. Potentially toxic to infants. Avoid

breastfeeding.

Contraindications: IV, IM use, hypersensitivity to bethanecol,

mechanical obstruction of GI tract, active peptic ulcer disease,

COPD, epilepsy, bradycardia, Parkinson’s disease, AVblock, hypo-

tension, hypertension.

Warnings/precautions

•Use with caution in patients with the following conditions:

epilepsy, hyperthyroidism.

•Observe patient closely for 30–60 minutes for possible side

effects after drug administration.

•Atropine should be available for treating side effects.

Advice to patient: Change position slowly, in particular from

recumbent to upright, to minimize orthostatic hypotension. Sit

at the edge of the bed for several minutes before standing and

lie down if feeling faint or dizzy. Avoid hot showers, or baths and

standing for long periods. Male patients with orthostatic hypoten-

sion may be safer urinating while seated on the toilet rather than

standing.

Adverse reactions

•Common: None.

•Serious: hypotension, cardiac arrest, bronchial constriction.

BETHANECHOL 99

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Clinically important drug interactions

•Drugs that increase effects/toxicity of bethanechol: cholinesterase

inhibitors (contraindicated).

•Drugs that decrease effects/toxicity of bethanechol: procainamide,

quinidine.

Parameters to monitor

•Intake of fluids and urinary and other fluid output to minimize

renal toxicity. Closely monitor electrolyte levels.

•Signs of abdominal distention. Effectiveness of treatment is

indicated by reduction in abdominal distention and decreased

bowel activity.

Editorial comments: Because of the potential for life-threatening

complications from this drug, the editors recommend adminis-

tration only by experienced practitioners.

Bitolterol

Brand name: Tornalate.

Class of drug: β-Adrenergic agonist, bronchodilator.

Mechanism of action: Relaxes smooth muscles of the bronchi-

oles by stimulating β

-adrenergic receptors.

Indications/dosage/route: Inhalation only.

•Bronchodilation

Ð Adults, children >12 years: Initial: 2 inhalations at interval

of 1–3 minutes q8h; third inhalation may be taken. Maxi-

mum: 3 inhalations q6h or 2 inhalations q4h.

•Prophylaxis of bronchospasm

Ð Adults, children >12 years: 2 inhalations q8h.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: Lower doses may be required.

•Pediatric: See above. Safety and efficacy have not been estab-

lished in children <12 years.

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Onset of Action Peak Effect Duration

3–4 min — 5–8 h

Food: Not applicable.

Pregnancy: Category C.

Lactation: No data available. Best to avoid.

Contraindications: Hypersensitivity to adrenergic compounds,

tachycardia (idiopathic or from digitalis).

Editorial comments

•This agent appears to cause tremor and palpitations more fre-

quently than isoproterenol. Headache appears less common.

•For additional information, see metaproterenol, p. 575.

Bleomycin

Brand name: Blenoxane.

Class of drug: Antineoplastic, antitumor antibiotic, sclerosing

agent.

Mechanism of action: Inhibits synthesis of DNA.

Indications/dosage/route: IV, IM, SC, intracavitary.

•Chemotherapy regimens for Hodgkin’s and non-Hodgkin’s lym-

phoma, testicular cancer, squamous cell carcinoma, melanoma,

sarcoma

Ð Adults: IV, IM, SC 0.25–0.5 units/kg, 1–2 times per week.

Maintenance: IM or IV1 unit/d or 5 units/wk.

Ð Adults: Continuous IV infusion of 15 units/m

/d for 4 days.

Maximum lifetime dose: 400 units.

•Malignant pleural effusion.

Ð Adults: intracavitary 60 units.

Adjustment of dosage

•Kidney disease: creatinine clearance 10–50 mL/min: reduce

dose by 25%; creatinine clearance <10 mL/min: reduce dose

by 50%.

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Onset of action:Parenteral; 2–3 wks.

Pregnancy: Category D.

Lactation: No data available. Potentially toxic to infant. Do not

breastfeed.

Contraindications: Hypersensitivity to bleomycin, severe pul-

monary disease.

Warnings/precautions

•Use caution in patients with kidney impairment, compromised

pulmonary function.

•High-percentage oxygen inhalation in patients who have

received bleomycin has been associated with pulmonary

failure.

Advice to patient

•Use two forms of birth control including hormonal and barrier

methods.

•Do not receive any vaccinations (particularly live attenuated

viruses) without permission from treating physician.

•Do not smoke.

Adverse reactions

•Common: Raynaud’s phenomenon, febrile allergic reactions,

nausea, vomiting, anorexia, stomatitis, thickening bronchial

secretions, alopecia, dermatologic changes (erythema, peeling,

hyperkeratosis, induration in 50% of patients).

•Serious: pulmonary toxicity, interstitial pneumonitis, pul-

monary fibrosis,hypoxia, myelosuppression, MI, anaphylaxis

reaction. Severe idiosyncratic reaction: mental confusion, fever,

hypotension, particularly in lymphoma patients.

Clinically important drug interactions

•Drugs that increase effects/toxicity of bleomycin: cisplatin.

•Bleomycin decreases effects/toxicity of following: digitalis,

phenytoin.

Parameters to monitor

•CBC, serum BUN and creatinine, liver enzymes.

•Signs and symptoms of anaphylactic reaction, pulmonary tox-

icity, hepatotoxicity, bone marrow depression.

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•Signs and symptoms of stomatitis. Treat with peroxide, tea, top-

ical anesthetics such as benzocaine, lidocaine, or antifungal

drug.

Editorial comment

•Use latex gloves and safety glasses when handling this med-

ication; avoid contact with skin as well as inhalation. If possi-

ble prepare in biologic hood.

•Although cumulative doses of 400 units/m

increase the risk of

pulmonary fibrosis, this toxic effect can occasionally occur at

much lower cumulative doses. Corticosteroids are sometimes

helpful in treating this problem, but it may also be fatal.

Bretylium

Brand name: Bretylol.

Class of drug: Antiarrhythmic agent, Class III.

Mechanism of action: Depletes adrenergic nerve terminals of

norepinephrine; this decreases adrenergic stimulation of the

myocardium.

Indications/dosage/route: IV and IM only.

•Ventricular arrhythmias (resistant to lidocaine).

Ð Adults: IV bolus 5 mg/kg over 1 minute. Repeat if necessary

at 15- to 30-minute intervals. Total dose: 30–35 mg/kg.

Maintenance: 5–10 mg/kg q6–8h.

Ð Pediatric dose: IM 2–5 mg/kg; IV 5 mg/kg. Repeat every

10–20 minutes if necessary. Maximum: 30 mg/kg.

Maintenance: 5 mg/kg q6–8h.

Adjustment of dosage

•Kidney disease: creatinine clearance 10–60 mL/min; reduce dose

by 50–75%; creatinine clearance <10 mL/min: reduce dose by 75%.

•Liver disease: None.

•Elderly: May be at higher risk for toxicity.

•Pediatric: See above.

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Onset of Action Peak Effect Duration

IV 6–20 min 6–9 h 6–24 h

Pregnancy: Category B.

Lactation: No data available. Potentially toxic to infant. Avoid

breastfeeding.

Contraindications: Arrhythmias induced by digitalis. Severe pul-

monary hypertension. For treatment of ventricular fibrillation or

life-threatening refractory ventricular arrhythmias, there is no con-

traindication to using bretylium.

Warnings/precautions

•Use with caution in patients with the following conditions:

hypotension, pulmonary hypertension, aortic stenosis.

•Reduce dose gradually (over 3–5 days) with ECG monitoring.

Advice to patient: If ambulation is permitted, change position

slowly, in particular from recumbent to upright, to minimize

orthostatic hypotension.

Adverse reactions

•Common: hypotension.

•Serious: hypotension (50Ð 75%), bradycardia, syncope, con-

fusion, kidney damage, respiratory depression.

Clinically important drug interactions

•Other antiarrhythmic agents increase effects/toxicity of bretylium.

•Bretylium increases effects/toxicity of sympathomimetics,

digoxin.

Parameters to monitor

•Monitor patient’s BP very carefully. If supine systolic pressure

is lower than 75 mm Hg, carefully administer an IVinfusion

of dopamine or norepinephrine and titrate to increase BP.

•ECG, heart rate, BP. Patient should be on continuous cardiac mon-

itoring. Additional hemodynamic monitoring also recommended.

Editorial comments

•Adequate facilities, equipment, and personnel must be avail-

able for constant ECG and BPmonitoring when bretylium is

used.

104 BRETYLIUM

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•Tolerance to the hypotensive action of bretylium may occur

after several days. Patient should remain in supine position

under close supervision for postural hypotension until tolerance

develops to this effect. If severe hypotension occurs, the patient

should be administered IV infusion of dopamine or norepi-

nephrine as well as volume replacement with blood or plasma

if necessary.

•Bretylium is only for short-term use and should be discontin-

ued after 3–5 days with gradual dose reduction and replaced

by an orally effective antiarrhythmic drug if necessary.

•Bretylium is currently not used clinically as a cardiac drug since

IVamiodarone became available. It will likely be removed from

the ACLS training protocol and transitional from crash carts.

•This drug is not listed in the Physician’s Desk Reference, 54th

edition, 2000.

Bromocriptine

Brand name: Parlodel.

Class of drug: Anti-Parkinson agent, prolactin inhibitor.

Mechanism of action: Prolactin inhibition: inhibits prolactin

secretion from anterior pituitary. Anti-Parkinson effects: stimu-

lates dopamine receptors in the brain, thus improving symptoms

of Parkinson’s disease.

Indications/dosage/route: Oral only.

•Parkinson’s disease (usually used in combination with levodopa–

carbidopa)

Ð Adults: 1.25 mg b.i.d. or t.i.d. increase dosage by 2.5 mg/d

every 2–4 weeks. Maintenance: 10–40 mg/d.

•Hyperprolactinemia

Ð Adults: 0.5–2.5 mg b.i.d. or t.i.d. Maintenance: 2.5–15 mg/d.

Maximum: 6 months.

•Acromegaly

BROMOCRIPTINE 105

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Ð Adults: Initial: 1.25–2.5 mg/d; increase dose by 2.5 mg/d

q3–7d as needed. Maintenance: 20–30 mg/d.

Adjustment of dosage

•Kidney disease: Use with caution.

•Liver disease: May require lower doses.

•Elderly: May require lower doses.

•Pediatric: No data available.

Onset of Action Duration

Hyperprolactinemia 2 h 24 h

Parkinson’s disease 30–90 min No data

Acromegaly 1–2 h 4–8 h

Food: Take with food or milk.

Pregnancy: Category C.

Lactation: Suppresses lactation. Contraindicated by the American

Academy of Pediatrics.

Contraindications: Severe ischemic heart disease, peripheral vas-

cular disease, sensitivity to ergot alkaloids.

Warnings/precautions: Use with caution in patients with kidney

disease, liver disease.

Advice to patients

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Avoid alcohol.

•Use two forms of birth control including hormonal and barrier

methods.

Adverse reactions

•Common: decreased BP (28%), headache (10%), dizziness,

nausea.

•Serious: Seizures, CVA, prolonged hypotension, depression,

hallucinations, syncope, MI, liver toxicity.

Clinically important drug interactions

•Drugs that increase effects/toxicity of bromocriptine: sympa-

thomimetics, diuretics.

106 BROMOCRIPTINE

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•Drugs that decrease the antiprolactin action of bromocriptine: phe-

nothiazines, butyrophenones, reserpine, amitriptyline, imipramine,

methyldopa.

•Bromocriptine increases effects/toxicity of following: anti-

hypertensive drugs, alcohol, ergot alkaloids.

Parameters to monitor

•CBC with differential and platelets, liver enzymes.

•Evaluate patient for orthostasis with BP measurements in the

sitting, lying, and standing positions repeatedly before and

after initiating therapy.

•Monitor tumor enlargement for patient with pituitary tumor:

sudden headache, severe nausea and vomiting, visual disturbances.

Editorial comments: A large percentage of patients will experience

mild to moderate side effects from bromocriptine, particularly with

higher doses (>20 mg/d). In postpartum studies, only 3% of patients

needed to discontinue therapy because of side effects.

•This drug is listed without details in the Physician’s Desk

Reference,54th edition, 2000.

Brompheniramine

Brand names: Dimetane, Bromfed.

Class of drug: H

receptor blocker.

Mechanism of action: Antagonizes histamine effects on GI tract,

respiratory tract, blood vessels.

Indications/dosage/route: Oral only (capsules, syrup).

•Allergic rhinitis

Ð Adults, children >12 years: 24 mg/d in divided doses q4–12h.

Maximum: 48 mg/d.

Ð Children 6–12 years: 12 mg/d in divided doses q4–12h.

Ð Children 2–4 years: 1 mg (syrup) q4h.

Ð Children <2 years: Doses not established.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

BROMPHENIRAMINE 107

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•Elderly: Use caution. At higher risk for side effects.

•Pediatric: See above.

Onset of Action Peak Effect Duration

— 3–9 h 4–25 h

Food: No restriction.

Pregnancy: Category C.

Lactation: Appears in breast milk. Potentially toxic to infant.

Although brompheniramine is considered compatible with

breastfeeding by the American Academy of Pediatrics, it is stated

to be contraindicated by one manufacturer.

Contraindications: Hypersensitivity to antihistamines, acute asthma,

narrow-angle glaucoma, concurrent use of MAO inhibitor.

Warnings/precautions

•Use with extreme caution in patients with active peptic ulcer,

severe coronary artery disease, symptomatic prostatic hypertro-

phy.

•Use with caution in patients with the following conditions:

hypertension, hyperthyroidism, asthma, heart disease, dia-

betes, increased intraocular pressure.

•Do not use in neonates or premature infants.

•Infants and young children are at risk for overdosage.

Advice to patient

•Avoid driving and other activities requiring mental alertness or

that are potentially dangerous until response to drug is known.

•Use caution if used along with alcohol and other CNS depres-

sants such as narcotic analgesics and sedatives (eg, diazepam).

•Drink large quantities of water to minimize drying of secretions.

•If mouth is dry, rinse with warm water frequently, chew sug-

arless gum, suck on an ice cube, or use artificial saliva. Carry

out meticulous oral hygiene (floss teeth daily).

•Discontinue drug at least 4 days before skin testing (for aller-

gies) to avoid the possibility of false-negative results.

108 BROMPHENIRAMINE

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Adverse reactions

•Common: drowsiness, dry mouth and throat, nervousness.

•Serious: Palpitations.

Clinically important drug interactions

•Drugs that increase effects/toxicity of antihistamines: CNS depres-

sants (barbiturates, benzodiazepines, narcotic analgesics), MAO

inhibitors (combination contraindicated).

•Antihistamines decrease effects of sulfonylureas.

Parameters to monitor

•Signs of dry mouth, eg, thickened secretions. Increase fluid

intake to decrease viscosity of secretion.

•Signs and symptoms of severe CNS depression, dilated pupils,

or flushing as symptoms of overdose. Administer syrup of

ipecac if necessary.

Editorial comments: This drug is available in combination with

other agents, including pseudoephedrine, phenylephrine, phenyl-

propanolamine, aspirin, acetaminophen. Warnings and precautions,

side effects, etc, of other ingredients should be kept in mind when

prescribing.

Budesonide

Brand names: Rhinocort, Pulmicort.

Class of drug: Inhalation corticosteroid.

Mechanism of action: Inhibits elaboration of many of the media-

tors of allergic inflammation, eg, leukotrienes and other products

of the arachidonic acid cascade.

Indications/dosage/route: Inhalation aerosol.

•Asthma

Ð Adults: 200–800 µg b.i.d. (1–4 inhalations morning and

evening).

Ð Children >6 years: 200–400 µg b.i.d. (1–2 inhalations, morn-

ing and evening).

•Seasonal or perennial rhinitis

BUDESONIDE 109

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Ð Adults, children ≥6 years: Initial: 256 µg/d, 2 sprays in

each nostril in morning and evening. Maintenance:

reduce initial dose to smallest amount necessary to control

symptoms.

Adjustment of dosage

•Kidney disease: None.

•Liver disease: None.

•Elderly: None.

•Pediatric: Safety and efficacy have not been established in chil-

dren <6 years.

Pregnancy: Category C.

Lactation: Present in breast milk. Safe to use.

Contraindications: Hypersensitivity to corticosteroids.

Warnings/precautions

•If patient is transferred from systemic corticosteroid to inhala-

tion drug, symptoms of steroid withdrawal may result. These

include muscle and joint pain, depression. Alternatively, adre-

neal insufficiency may occur: weakness, fatigue, nausea,

anorexia.

•Provide patient with instructions for use of the inhaler or nasal

spray and make sure patient completely understands these

instructions.

•Provide patient with a list of side effects and note those that

require immediate reporting to the physician.

•Patients on long-term inhaled or intranasal corticosteroids

may require steroid pulsing during stress, eg, surgery or

infection.

Advice to patient

•Rinse mouth and gargle with warm water after each inhalation.

This may minimize the development of dry mouth, hoarseness,

and oral fungal infection.

•This drug should be inhaled 5 minutes after a previously inhaled

bronchodilator, eg, albuterol.

•Do not exceed recommended dosage of the drug. Excessive

doses have been associated with adrenal insufficiency.

•Notify physician if symptoms worsen.

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•Carry a card indicating your condition, drugs you are taking,

and need for supplemental steroid in the event of a severe

asthmatic attack. Attempt to decrease dose once the desired

clinical effect is achieved. Decrease dose gradually every

2–4 weeks. Return to initial starting dose if symptoms

recur.

•Stop smoking.

•Do not overuse the inhaler.

Adverse reactions

•Common: pharyngitis, headache.

•Serious: potential for hypercorticism, adrenal insufficiency.

Clinically important drug interactions:None.

Parameters to monitor

•Signs and symptoms of acute adrenal insufficiency, particu-

larly in response to stress.

•Child growth: Drug may suppress growth.

•Changes in nasal mucosa in patients on long-term drug ther-

apy.

•Signs of localized infection in mouth and pharynx, eg, red mem-

branes with vesicular eruptions. Treat with appropriate antifun-

gal drug, eg, nystatin, or discontinue treatment.

•When switching from systemic inhalation therapy, monitor

patient for symptoms of adrenal insufficiency: hypotension,

weight loss, muscular and joint pain. If these occur, the dose

of systemic steroid should be increased followed by slower

withdrawal. It may require up to 12 months for HPAfunc-

tion to fully recover.

Editorial comments

•Inhaled corticosteroids are the drugs of choice for patients

with refractory symptoms on prn adrenergic agonist bron-

chodilators.

•Inhalation steroids are useful in reducing the dose or dis-

continuing use of oral corticosteroids. However, there is

considerable controversy with respect to the beneficial use

of higher than recommended inhalation doses of these

drugs.

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