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Basic and Clinical Pharmacology, 11th Edition (LANGE Basic Science) PDF

1234 Pages·2009·52.48 MB·English
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1 S C H E D U L E O F C O N T R O L L E D D R U G S SCHEDULE I Cannabinoids: Dronabinol (Marinol) (All nonresearch use illegal under federal law.) Anabolic Steroids: Flunitrazepam (Rohypnol) Fluoxymesterone (Halotestin) Narcotics: Methyltestosterone (Android, Testred) Heroin and many nonmarketed synthetic narcotics Nandrolone decanoate (Deca-Durabolin) Hallucinogens: Nandrolone phenpropionate (Durabolin) LSD Oxandrolone (Oxandrin), Oxymetholone (Androl-50) MDA, STP, DMT, DET, mescaline, peyote, bufotenine, ibogaine, Stanozolol (Winstrol), Testolactone (Teslac), Testosterone and its psilocybin, phencyclidine (PCP; veterinary drug only) esters Marijuana SCHEDULE IV Methaqualone (Prescription must be rewritten after 6 months or five refills; differs SCHEDULE II from Schedule III in penalties for illegal possession.) Opioids: (No telephone prescriptions, no refills.)2 Butorphanol (Stadol) Opioids: Difenoxin 1 mg + atropine 25 mcg (Motofen) Opium Pentazocine (Talwin) Opium alkaloids and derived phenanthrene alkaloids: codeine, Propoxyphene (Darvon) morphine, (Avinza, Kadian, MSContin, Roxanol), hydromor- Stimulants: phone (Dilaudid), oxymorphone (Numorphan), oxycodone Diethylpropion (Tenuate) (dihydroxycodeinone, a component of Oxycotin, Oxydose, Mazindol (Sanorex) Oxyfast, Percodan, Percocet, Roxicodone, Tylox) Modafinil (Provigil) Designated synthetic drugs: levomethadyl (Orlaam), meperidine Phentermine (Ionamin) (Demerol), methadone, levorphanol (Levo-Dromoran), fenta- Pemoline (Cylert) nyl (Sublimaze, Duragesic, Actiq), alphaprodine, alfentanil Sibutramine (Merida) (Alfenta), sufentanil (Sufenta), remifentanil (Ultiva) Depressants: Stimulants: Benzodiazepines Coca leaves and cocaine Alprazolam (Xanax) Amphetamine Chlordiazepoxide (Librium) Amphetamine complex (Biphetamine) Clonazepam (Kionopin) Amphetamine salts (Adderall) Clorazepate(Tranxene) Dextroamphetamine (Dexedrine) Diazepam (Valium) Lisdexamfetamine (Vyanse) Estazolam (ProSom) Methamphetamine (Desoxyn) Flurazepam (Dalmane) Methylphenidate (Ritalin, Concerta, Methylin, Daytrana) Halazepam (Paxipam) Above in mixtures with other controlled or uncontrolled drugs Lorazepam (Ativan) Cannabinoids: Midazolam (Versed) Nabilone (Cesamet) Oxazepam (Serax) Depressants: Prazepam (Centrax) Amobarbital (Amytal) Quazepam (Doral) Glutethimide (Doriden) Temazepam (Restoril) Pentobarbital (Nembutal) Triazolam (Halcion) Secobarbital (Seconal) Chloral hydrate Mixtures of above (eg, Tuinal) Dichloralphenazone (Midrin) Eszopiclone (Lunesta) Ethchlorvynol (Placidyl) SCHEDULE III Meprobamate (Equanil, Miltown, etc) (Prescription must be rewritten after 6 months or five refills.) Mephobarbital (Mebaral) Opioids: Methohexital (Brevital) Paraldehyde Buprenorphine (Buprenex, Subutex, Suboxone) Phenobarbital The following opioids in combination with one or more active non- Zaleplon (Sonata) opioid ingredients, provided the amount does not exceed that Zolpidem (Ambien) shown: Codeine and dihydrocodeine: not to exceed 1800 mg/dL or 90 SCHEDULE V mg/tablet or other dosage unit Dihydrocodeinone (hydrocodone in Hycodan, Vicodin, and (As any other nonopioid prescription drug; may also be dispensed without Lortab): not to exceed 300 mg/dL or 15 mg/tablet prescription unless additional state regulations apply.) Opium: 500 mg/dL or 25 mg/5 mL or other dosage unit (paregoric) Codeine: 200 mg/100 mL Stimulants: Difenoxin preparations: 0.5 mg + 25 mcg atropine Benzphetamine (Didrex) Dihydrocodeine preparations: 10 mg/100 mL Phendimetrazine (Plegine) Diphenoxylate (not more than 2.5 mg and not less than 0.025 mg Depressants: of atropine per dosage unit, as in Lomotil) Schedule II barbiturates in mixtures with noncontrolled drugs or Ethylmorphine preparations: 100 mg/100 mL in suppository dosage form Opium preparations: 100 mg/100 mL Butabarbital (Butisol) Pregabalin (Lyrica) Ketamine (Ketalar) Pyrovalerone (Centroton, Thymergix) Thiopental (Pentothal) 1See http://www.usdoj.gov/dea/pubs/scheduling.html for additional details. 2Emergency prescriptions may be telephoned if followed within 7 days by a valid written prescription annotated to indicate that it was previously placed by telephone. a LANGE medical book Basic & Clinical Pharmacology Eleventh Edition Edited by Bertram G. Katzung, MD, PhD Professor Emeritus Department of Cellular & Molecular Pharmacology University of California, San Francisco Associate Editors Susan B. Masters, PhD Professor of Pharmacology & Academy Chair of Pharmacology Education Department of Cellular & Molecular Pharmacology University of California, San Francisco Anthony J. Trevor, PhD Professor Emeritus Department of Cellular & Molecular Pharmacology University of California, San Francisco New York Chicago San Francisco Lisbon London Madrid Mexico City Milan New Delhi San Juan Seoul Singapore Sydney Toronto Copyright © 2009 by The McGraw-Hill Companies, Inc. All rights reserved. Except as permitted under the United States Copyright Act of 1976, no part of this publication may be reproduced or distributed in any form or by any means, or stored in a database or retrieval system, without the prior written permission of the publisher. ISBN: 978-0-07-160406-2 MHID: 0-07-160406-5 The material in this eBook also appears in the print version of this title: ISBN: 978-0-07-160405-5, MHID:0-07-160405-7. All trademarks are trademarks of their respective owners. Rather than put a trademark symbol after every occurrence of a trademarked name, we use names in an editorial fashion only, and to the benefit of the trademark owner, with no intention of infringement of the trademark. Where such designations appear in this book, they have been printed with initial caps. McGraw-Hill eBooks are available at special quantity discounts to use as premiums and sales promotions, or for use in corporate training programs. To contact a representative please e-mail us at [email protected]. Medicine is an ever-changing science. As new research and clinical 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 generally 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 publisher 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. Cover illustration: The interaction of fluvastatin, a drug used to reduce blood lipids, with its target the catalytic site of the enzyme HMG-CoA reductase. Credit: Kenneth Eward/Photo Researchers, Inc. Concept kindly provided by Dr. Raymond Fort, University of Maine (www.chemistry.umeche.maine.edu/CHY431/Cholest3.html). TERMS OF USE This is a copyrighted work and The McGraw-Hill Companies, Inc. (“McGraw-Hill”) and its licensors reserve all rights in and to the work. Use of this work is subject to these terms. Except as permitted under the Copyright Act of 1976 and the right to store and retrieve one copy of the work, you may not decompile, disassemble, reverse engineer, reproduce, modify, create derivative works based upon, transmit, distribute, disseminate, sell, publish or sublicense the work or any part of it without McGraw-Hill’s prior consent. You may use the work for your own noncommercial and personal use; any other use of the work is strictly prohibited. Your right to use the work may be terminated if you fail to comply with these terms. THE WORK IS PROVIDED “AS IS.” McGRAW-HILL AND ITS LICENSORS MAKE NO GUARANTEES OR WARRANTIES AS TO THE ACCURACY, ADEQUACY OR COMPLETENESS OF OR RESULTS TO BE OBTAINED FROM USING THE WORK, INCLUDING ANY INFORMATION THAT CAN BE ACCESSED THROUGH THE WORK VIA HYPERLINK OR OTHERWISE, AND EXPRESSLY DISCLAIM ANY WARRANTY, EXPRESS OR IMPLIED, INCLUDING BUT NOT LIMITED TO IMPLIED WARRANTIES OF MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE. McGraw-Hill and its licensors do not warrant or guarantee that the functions contained in the work will meet your requirements or that its operation will be uninterrupted or error free. Neither McGraw-Hill nor its licensors shall be liable to you or anyone else for any inaccuracy, error or omission, regardless of cause, in the work or for any damages resulting therefrom. McGraw-Hill has no responsibility for the content of any information accessed through the work. Under no circumstances shall McGraw-Hill and/or its licensors be liable for any indirect, incidental, special, punitive, consequential or similar damages that result from the use of or inability to use the work, even if any of them has been advised of the possibility of such damages. This limitation of liability shall apply to any claim or cause whatsoever whether such claim or cause arises in contract, tort or otherwise. Contents Schedule of Controlled Drugs Inside Front Cover Key Features vi Preface ix Authors xi I III S E C T I O N S E C T I O N BASIC PRINCIPLES 1 CARDIOVASCULAR-RENAL DRUGS 167 1. Introduction 11. Antihypertensive Agents Bertram G. Katzung, MD, PhD 1 Neal L. Benowitz, MD 167 2. Drug Receptors & Pharmacodynamics 12. Vasodilators & the Treatment Mark von Zastrow, MD, PhD, & Henry R. Bourne, of Angina Pectoris MD 15 Bertram G. Katzung, MD, PhD, & 3. Pharmacokinetics & Pharmacodynamics: Kanu Chatterjee, MB, FRCP 191 Rational Dosing & the Time Course 13. Drugs Used in Heart Failure of Drug Action Bertram G. Katzung, MD, PhD, & Nicholas H. G. Holford, MB, ChB, FRACP 37 William W. Parmley, MD 209 4. Drug Biotransformation 14. Agents Used in Cardiac Arrhythmias Maria Almira Correia, PhD 53 Joseph R. Hume, PhD, & Augustus O. Grant, MD, 5. Development & Regulation of Drugs PhD 225 Barry A. Berkowitz, PhD 67 15. Diuretic Agents II Harlan E. Ives, MD, PhD 251 S E C T I O N IV AUTONOMIC DRUGS 77 S E C T I O N DRUGS WITH IMPORTANT ACTIONS 6. Introduction to Autonomic Pharmacology ON SMOOTH MUSCLE 271 Bertram G. Katzung, MD, PhD 77 16. Histamine, Serotonin, & the Ergot Alkaloids 7. Cholinoceptor-Activating & Bertram G. Katzung, MD, PhD 271 Cholinesterase-Inhibiting Drugs Achilles J. Pappano, PhD 95 17. Vasoactive Peptides Ian A. Reid, PhD 293 8. Cholinoceptor-Blocking Drugs Achilles J. Pappano, PhD 113 18. The Eicosanoids: Prostaglandins, Thromboxanes, Leukotrienes, & 9. Adrenoceptor Agonists & Related Compounds Sympathomimetic Drugs Emer M. Smyth, PhD, & Garret A. FitzGerald, Italo Biaggioni, MD, & David Robertson, MD 127 MD 313 10. Adrenoceptor Antagonist Drugs David Robertson, MD, & Italo Biaggioni, MD 149 iii iv CONTENTS VI 19. Nitric Oxide S E C T I O N Samie R. Jaffrey, MD, PhD 331 DRUGS USED TO TREAT DISEASES OF THE BLOOD, INFLAMMATION, 20. Drugs Used in Asthma Homer A. Boushey, MD 339 & GOUT 569 V 33. Agents Used in Anemias; Hematopoietic S E C T I O N Growth Factors DRUGS THAT ACT IN THE Susan B. Masters, PhD 569 CENTRAL NERVOUS SYSTEM 357 34. Drugs Used in Disorders of Coagulation James L. Zehnder, MD 587 21. Introduction to the Pharmacology of CNS Drugs 35. Agents Used in Dyslipidemia Roger A. Nicoll, MD 357 Mary J. Malloy, MD, & John P. Kane, MD, 22. Sedative-Hypnotic Drugs PhD 605 Anthony J. Trevor, PhD, & 36. Nonsteroidal Anti-Inflammatory Drugs, Walter L. Way, MD 371 Disease-Modifying Antirheumatic Drugs, 23. The Alcohols Nonopioid Analgesics, & Drugs Used in Gout Susan B. Masters, PhD 387 Daniel E. Furst, MD, Robert W. Ulrich, PharmD, & Cissy Varkey-Altamirano, BS 621 24. Antiseizure Drugs Roger J. Porter, MD, & VII S E C T I O N Brian S. Meldrum, MB, PhD 399 ENDOCRINE DRUGS 643 25. General Anesthetics Paul F. White, PhD, MD, & 37. Hypothalamic & Pituitary Hormones Anthony J. Trevor, PhD 423 Susan B. Masters, PhD 643 26. Local Anesthetics 38. Thyroid & Antithyroid Drugs Bertram G. Katzung, MD, PhD, & Betty J. Dong, PharmD, FASHP, FCCP, & Paul F. White, PhD, MD 439 Francis S. Greenspan, MD, FACP 665 27. Skeletal Muscle Relaxants 39. Adrenocorticosteroids & Adrenocortical Paul F. White, PhD, MD, & Antagonists Bertram G. Katzung, MD, PhD 451 George P. Chrousos, MD 681 28. Pharmacologic Management of 40. The Gonadal Hormones & Inhibitors Parkinsonism & Other Movement George P. Chrousos, MD 699 Disorders Michael J. Aminoff, MD, DSc, FRCP 469 41. Pancreatic Hormones & Antidiabetic Drugs Martha S. Nolte, MD 727 29. Antipsychotic Agents & Lithium Herbert Meltzer, MD, PhD 487 42. Agents That Affect Bone Mineral Homeostasis Daniel D. Bikle, MD, PhD 753 30. Antidepressant Agents Charles DeBattista, MD 509 VIII S E C T I O N 31. Opioid Analgesics & Antagonists CHEMOTHERAPEUTIC DRUGS 773 Mark A. Schumacher, PhD, MD, Allan I. Basbaum, PhD, & 43. Beta-Lactam & Other Cell Wall- & Walter L. Way, MD 531 Membrane-Active Antibiotics 32. Drugs of Abuse Henry F. Chambers, MD, & Daniel H. Deck, Christian Lüscher, MD 553 PharmD 773 CONTENTS v 44. Tetracyclines, Macrolides, Clindamycin, 57. Heavy Metal Intoxication & Chelators Chloramphenicol, Streptogramins, Michael J. Kosnett, MD, MPH 999 & Oxazolidinones 58. Management of the Poisoned Patient Henry F. Chambers, MD, & Daniel H. Deck, Kent R. Olson, MD 1013 PharmD 795 X 45. Aminoglycosides & Spectinomycin S E C T I O N Henry F. Chambers, MD, & Daniel H. Deck, SPECIAL TOPICS 1025 PharmD 807 46. Sulfonamides, Trimethoprim, & Quinolones 59. Special Aspects of Perinatal & Henry F. Chambers, MD, & Daniel H. Deck, Pediatric Pharmacology PharmD 815 Gideon Koren, MD 1025 47. Antimycobacterial Drugs 60. Special Aspects of Geriatric Pharmacology Henry F. Chambers, MD, & Daniel H. Deck, Bertram G. Katzung, MD, PhD 1037 PharmD 823 61. Dermatologic Pharmacology 48. Antifungal Agents Dirk B. Robertson, MD, & Howard I. Maibach, Don Sheppard, MD, & Harry W. Lampiris, MD 1047 MD 835 62. Drugs Used in the Treatment of 49. Antiviral Agents Gastrointestinal Diseases Sharon Safrin, MD 845 Kenneth R. McQuaid, MD 1067 50. Miscellaneous Antimicrobial Agents; 63. Therapeutic & Toxic Potential of Disinfectants, Antiseptics, & Sterilants Over-the-Counter Agents Henry F. Chambers, MD, & Daniel H. Deck, Robin L. Corelli, PharmD 1103 PharmD 877 64. Dietary Supplements & Herbal Medications 51. Clinical Use of Antimicrobial Agents Cathi E. Dennehy, PharmD, & Candy Tsourounis, Harry W. Lampiris, MD, & Daniel S. Maddix, PharmD 1113 PharmD 885 65. Rational Prescribing & Prescription Writing 52. Antiprotozoal Drugs Paul W. Lofholm, PharmD, & Philip J. Rosenthal, MD 899 Bertram G. Katzung, MD, PhD 1127 53. Clinical Pharmacology of the 66. Important Drug Interactions & Antihelminthic Drugs Their Mechanisms Philip J. Rosenthal, MD 923 John R. Horn, PharmD, FCCP 1137 54. Cancer Chemotherapy Appendix: Vaccines, Immune Globulins, Edward Chu, MD, & Alan C. Sartorelli, PhD 935 & Other Complex Biologic Products Harry W. Lampiris, MD, & Daniel S. Maddix, 55. Immunopharmacology PharmD 1151 Douglas F. Lake, PhD, Adrienne D. Briggs, MD, & Emmanuel T. Akporiaye, PhD 963 Index 1159 IX S E C T I O N TOXICOLOGY 987 56. Introduction to Toxicology: Occupational & Environmental Daniel T. Teitelbaum, MD 987 Key Features of the Eleventh Edition of Katzung’s Basic & Clinical Pharmacology • Full-color presentation, including 300+ illustrations •Larger 8½ ×11 trim size complements the new full-color art •Each chapter discusses drug groups and prototypes •Chapter-opening case studieshelp readers make the link between pharmacology and clinical practice •Drug Summary Tables conclude chapters, encapsulating key comparative drug information •Descriptions of important newly released drugs, including new immunopharmacologic agents •Expanded coverage of general conceptsrelating to newly discovered receptors, receptor mechanisms, and drug transporters •Inclusion of sections that specifically address the clinical choice and use of drugs in patients and the monitoring of their effects—making clinical pharmacology an integral part of the text • Lists of commercial preparations available, including trade and generic names and dosage formulations, are provided at the end of each chapter •Two new co-authors Susan B. Masters, Ph.D. and Anthony J. Trevor, Ph.D. enrich the text with their experience and expertise •New online learning center LangeTextbooks.comoffers valuable resources and study aids, including board review questions and flash cards Valuable case studies open chapters vi KEY FEATURES vii Vivid full-color presentation, including 300+ illustrations Handy Summary Tables conclude chapters This page intentionally left blank

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