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BRS Pharmacology Pharmacology i Pharmacology Gary C. Rosenfeld, PhD Professor Department of Integrated Biology and Pharmacology and Graduate School of Biomedical Sciences Assistant Dean for Education Programs University of Texas Medical School at Houston Houston, Texas David S. Loose, PhD Associate Professor Department of Integrated Biology and Pharmacology and Graduate School of Biomedical Sciences University of Texas Medical School at Houston Houston, Texas iii Acquisitions Editor: Sirkka Howes Product Manager: Catherine Noonan Marketing Manager: Joy Fisher-Williams Vendor Manager: Bridgett Dougherty Manufacturing Coordinator: Margie Orzech Design Coordinator: Holly McLaughlin Compositor: Integra Software Services Pvt. Ltd. Sixth Edition Copyright © 2014, 2010, 2007, 1998 Lippincott Williams & Wilkins, a Wolters Kluwer business. 351 West Camden Street Two Commerce Square Baltimore, MD 21201 2001 Market Street Philadelphia, PA 19103 Printed in China All rights reserved. This book is protected by copyright. No part of this book may be reproduced or transmitted in any form or by any means, including as photocopies or scanned-in or other electronic copies, or utilized by any information storage and retrieval system without written permission from the copyright owner, except for brief quotations embodied in critical articles and reviews. Materials appearing in this book prepared by individuals as part of their official duties as U.S. government employees are not covered by the above-mentioned copyright. To request permission, please contact Lippincott Williams & Wilkins at 2001 Market Street, Philadelphia, PA 19103, via email at [email protected], or via website at lww.com (products and services). 9 8 7 6 5 4 3 2 1 Library of Congress Cataloging-in-Publication Data Rosenfeld, Gary C. Pharmacology / Gary C. Rosenfeld, David S. Loose. — 6th ed. p. ; cm. — (Board review series) Includes index. ISBN 978-1-4511-7535-6 I. Loose, David S. II. Title. III. Series: Board review series. [DNLM: 1. Pharmacological Phenomena—Examination Questions. 2. Pharmaceutical Preparations— Examination Questions. QV 18.2] RM301.13 615'.1076—dc23 2013013307 DISCLAIMER Care has been taken to confirm the accuracy of the information present and to describe generally accepted practices. However, the authors, editors, and publisher are not responsible for errors or omissions or for any con- sequences from application of the information in this book and make no warranty, expressed or implied, with respect to the currency, completeness, or accuracy of the contents of the publication. Application of this informa- tion in a particular situation remains the professional responsibility of the practitioner; the clinical treatments described and recommended may not be considered absolute and universal recommendations. The authors, editors, and publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accordance with the current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any change in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new or infrequently employed drug. Some drugs and medical devices presented in this publication have Food and Drug Administration (FDA) clearance for limited use in restricted research settings. It is the responsibility of the health care provider to ascer- tain the FDA status of each drug or device planned for use in their clinical practice. To purchase additional copies of this book, call our customer service department at (800) 638-3030 or fax orders to (301) 223-2320. International customers should call (301) 223-2300. Visit Lippincott Williams & Wilkins on the Internet: http://www.lww.com. Lippincott Williams & Wilkins customer service representatives are available from 8:30 am to 6:00 pm, EST. Preface This concise review of medical pharmacology is designed for medical students, dental students, and others in the health care professions. It is intended primarily to help stu- dents prepare for licensing examinations, such as the United States Medical Licensing Examination Step 1 (USMLE) and other similar examinations. This book presents con- densed and succinct descriptions of relevant and current Board-driven information pertaining to pharmacology without the usual associated details. It is not meant to be a substitute for the comprehensive presentation of information and difficult concepts found in standard pharmacology texts. ORGANIZATION The sixth edition begins with a chapter devoted to the general principles of drug action, followed by chapters concerned with drugs acting on the major body systems. Other chapters discuss autocoids, ergots, anti-inflammatory and immunosuppressive agents, drugs used to treat anemias and disorders of hemostasis, infectious diseases, cancer, and toxicology. Each chapter includes a presentation of specific drugs with a discussion of their general properties, mechanism of action, pharmacologic effects, therapeutic uses, and adverse effects. A drug list, tables, and figures summarize essential drug informa- tion included in all chapters. Clinically oriented, USMLE-style review questions and answers with explana- tions follow each chapter to help students assess their understanding of the informa- tion. Similarly, a comprehensive examination consisting of USMLE-style questions is included at the end of the book. This examination serves as a self-assessment tool to help students determine their fund of knowledge and diagnose any weaknesses in pharmacology. Key Features n Updated with current drug information n End-of-chapter review tests feature updated USMLE-style questions n Four-color tables and figures summarize essential information for quick recall n Updated drug lists for each chapter n Additional USMLE-style comprehensive examination questions and explanations Gary C. Rosenfeld, PhD David S. Loose, PhD v Acknowledgments The authors acknowledge and thank our colleagues for their support and contribu- tions to this book and our medical students for being our harshest critics. Our special thanks to the following UT Medical students who reviewed the previ- ous version of this book and offered many helpful suggestions towards this edition: Michael Arriaga, Mark A Barros, Jason S Bluth, John R Burleson, Sean B Bury, Samuel W Carson, Zachary R Compton, Andrew J Coyne, David B Doherty, Brittany L Duyka, Lisa M Evans, Azure G Greeson, Stephen A Herrmann, Hans B Heymann, Ari J Hyman, Jonathon S Jundt, Jacob A Mccoy, Elisabeth W Netherton, Alexander Reskallah, Reem Sabouni, Brittany L Sambrano, Madeleine B Samuelson, David J Savage, Yusra Siddiqui, Sara E Slabisak, Katherine A Smith, Agathe K Streiff, and Annise G Wilson. vi Contents Preface v Acknowledgments vi 1. GENERAL PRINCIPLES OF DRUG ACTION 1 I. Dose–Response Relationships 1 II. Drug Absorption 6 III. Drug Distribution 10 IV. Drug Elimination and Termination of Action 11 V. Biotransformation (Metabolism) of Drugs 12 VI. Excretion of Drugs 15 VII. Pharmacokinetics 16 Review Test 20 2. DRUGS ACTING ON THE AUTONOMIC NERVOUS SYSTEM 27 I. The Peripheral Efferent Nervous System 27 II. Parasympathomimetic Drugs 32 III. Muscarinic-Receptor Antagonists 37 IV. Ganglion-Blocking Drugs 39 V. Skeletal Muscle Relaxants 39 VI. Sympathomimetic Drugs 43 VII. Adrenergic Receptor Antagonists 48 Review Test 53 3. DRUGS ACTING ON THE RENAL SYSTEM 61 I. Diuretics 61 II. Nondiuretic Inhibitors of Tubular Transport 67 Review Test 69 vii viii Contents 4. DRUGS ACTING ON THE CardiovascULAR SYSTEM 73 I. Agents Used to Treat Congestive Heart Failure (CHF) 73 II. Antiarrhythmic Drugs 79 III. Antianginal Agents 85 IV. Antihypertensive Drugs 87 V. Drugs that Lower Plasma Lipids 92 Review Test 96 5. DRUGS ACTING ON THE CENTRAL NERVOUS SYSTEM 101 I. Sedative–Hypnotic Drugs 101 II. Antipsychotic (Neuroleptic) Drugs 106 III. Antidepressant Drugs 109 IV. Lithium and Anticonvulsants Used to Treat Bipolar Disorder 114 V. Opioid Analgesics and Antagonists 116 VI. Antiparkinsonian Drugs and Drugs Used to Treat Alzheimer Disease 122 VII. Antiepileptic Drugs 125 VIII. General Anesthetics 129 IX. Local Anesthetics 134 X. Drugs of Abuse 136 Review Test 146 6. AUTOCOIDS, ERGOTS, ANTI-INFLAMMatorY AGENTS, AND IMMUNOSUPPRESSIVE AGENTS 151 I. Histamine and Antihistamines 151 II. Serotonin and Serotonin Antagonists 154 III. Ergots 156 IV. Eicosanoids 158 V. Nonsteroidal Antiinflammatory Drugs (NSAIDs) 160 VI. Drugs Used for Gout 169 VII. Immunosuppressive Agents 170 Review Test 175 7. DRUGS USED IN ANEMIA AND DISORDERS OF HEMostasis 179 I. Drugs Used in the Treatment of Anemias 179 II. Drugs Acting on Myeloid Cells 183 III. Drugs Used in Hemostatic Disorders 184 Review Test 192 8. DRUGS ACTING ON THE GASTROINTESTINAL TRACT 197 I. Antiemetics 197 II. Anorexigenics and Appetite Enhancers 198 III. Agents Used for Upper GI Tract Disorders 199 Contents ix IV. Prokinetic Agents 203 V. Drugs Used to Dissolve Gallstones 203 VI. Digestive Enzyme Replacements 203 VII. Agents that Act on the Lower GI Tract 203 Review Test 208 9. DRUGS ACTING ON THE PULMONARY SYSTEM 212 I. Introduction to Pulmonary Disorders 212 II. Agents Used to Treat Asthma and Other Bronchial Disorders 213 III. Drugs Used to Treat Rhinitis and Cough 219 Review Test 221 10. DRUGS ACTING ON THE
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