ANTIEPILEPTIC DRUGS FIFTH EDITION. Editors. RENE H. LEVY, PhD

Transcription

1 ANTIEPILEPTIC DRUGS FIFTH EDITION Editors RENE H. LEVY, PhD Professor and Chair, Department of Pharmaceutics Professor of Neurological Surgery University ofwashington Schools of Pharmacy and Medicine Seattle, Washington RICHARD H. MATTSOIU, MD Professor of Neurology and Director of Medical Studies Department of Neurology Yale University School of Medicine and Veterans Affairs Medical Center West Haven, Connecticut BRIAN S. MELDRUM, PhD Professor in Experimental Neurology Director of Neurology Institute of Psychiatry London, England EMILIO PERUCCA, MD, PhD, FRCP (EDIN) Professor of Medical Pharmacology Clinical Pharmacology Unit Department of Internal Medicine and Therapeutics University ofpavia; and Consultant Clinical Pharmacologist Institute of Neurology, C. Momdino Foundation Pavia, Italy LIPPINCOTT WILLIAMS & WILKJNS A Wolters Kluwer Company Philadelphia Baltimore New York London Buenos Aires Hong Kong Sydney Tokyo

2 CONTENTS Contributing Authors xi Preface xvii SECTION I. GENERAL PRINCIPLES 1 1 Principles of Antiepileptic Drug Action 3 Michael A. Rogawski 2 Neurophysiological Effects of Antiepileptic Drugs 23 Carl W. Bazil and Timothy A. Pedley 3 Discovery and Preclinical Development of Antiepileptic Drugs 36 H. Steve White, Jose H. Woodhead, Karen S. Wilcox, James P. Stables, Harvey J. Kupferberg, and Harold H. Wolf 4 New Antiepileptic Drug Development: Medical Perspective 49 Jacqueline A. French and Marc A. Dichter 5 Clinical Development of Antiepileptic Drugs: Industry Perspective 58 Roger J. Porter 6 The Development of Antiepilepsy Drugs: Regulatory Perspective 66 Russell Katz 7 Antiepileptic Drug Monotherapy in Adults: Selection and Use in New-Onset Epilepsy 72 Richard H. Mattson 8 Combination Therapy and Drug Interactions 96 Emilio Perucca and Rent H. Levy 9 Laboratory Monitoring of Antiepileptic Drugs 103 Svein I. Johannessen and Torbjorn Tomson 10 Safety Monitoring of Antiepileptic Drugs 112 L. James Willmore 11 Use of Antiepileptic Drugs in Children 119 Olivier Dulac 12 Antiepileptic Drug Use in Women 132 Martha J. Morrell 13 Epilepsy in the Elderly 149 Ilo E. Leppik and James C. Cloyd 14 Treatment of Status Epilepticus 159 Brian K. Alldredge 15 Prevention of Epileptogenesis 169 Asia Pitkdnen SECTION II. BENZODIAZEPINES Mechanisms of Action 179 Chemistry, Biotransformation, and Pharmacokinetics 187 Gail D. Anderson and John W. Miller Clinical Efficacy and Use in Epilepsy 206 Dieter Schmidt Adverse Effects 215 Roberto Michelucci and Carlo Alberto Tassinari SECTION III. CARBAMAZEPINE Mechanisms of Action 227 Chemistry, Biotransformation, and Pharmacokinetics 236 Edoardo Spina Interactions with Other Drugs 247 Colleen J. Wurden and Rene H. Levy Clinical Efficacy and Use in Epilepsy 262 Pierre Loiseau Clinical Efficacy and Use in Other Neurological Disorders 273

3 VIII Contents 25 Clinical Efficacy and Use in Psychiatric Disorders 278 Michael R. Trimble 26 Adverse Effects 285 Gregory L. Holmes SECTION IV. FELBAMATE Felbamate 301 John M. Pellock, James L. Perhach, and R. Duane Sofia SECTION VII. LEVETIRACETAM Mechanisms of Action 419 Doru Georg Margineanu and Henrik Klitgaard 41 Chemistry, Bio transformation, Pharmacokinetics, and Drug Interactions 428 Philip N. Patsalos 42 Clinical Use 433 Ho E. Leppik 43 Adverse Experiences 442 Victor Biton SECTION V. GABAPENTIN Mechanisms of Action 321 Charles P. Taylor 29 Chemistry, Biotransformation, Pharmacokinetics, and Interactions 335 Frank J. E. Vajda 30 Clinical Use 340 Anthony G. Marson and David W. Chadwick 31 Clinical Efficacy and Use in Other Neurological Disorders 344 Bernd Schmidt 32 Clinical Efficacy and Use in Psychiatric Disorders 349 John H. Greist 33 Adverse Effects 354 R. Eugene Ramsay and Flavia M. Pryor SECTION VIII. OXCARBAZEPINE Mechanisms of Action 451 Michael J. McLean 45 Chemistry, Biotransformation, and Pharmacokinetics 459 Meir Bialer 46 Interactions with Other Drugs 466 Fiorenzo Albani, Roberto Riva, and Agostino Baruzzi 47 Clinical Efficacy and Use in Epilepsy 470 Steven C. Schachter 48 Clinical Efficacy and Use in Psychiatric Disorders 476 Michael R. Trimble 49 Adverse Effects 479 Giinter Kramer SECTION VI. LAMOTRIGINE Mechanisms of Action 363 Michael J. Leach, Andrew D. Randall, Alessandro Stefani, and Atticus H. Hainsworth 35 Chemistry, Biotransformation, and Pharmacokinetics 370 Maurice Dickins and Chao Chen 36 Interactions with Other Drugs 380 William R. Garnett 37 Clinical Efficacy and Use in Epilepsy 389 Linda J. Stephen and Martin J. Brodie 38 Efficacy and Use in Nonepileptic Disorders 403 Melvin D. Shelton and Joseph R. Calabrese 39 Adverse Effects 408 Francesco Pisani and Alan Richens SECTION IX. PHENOBARBITAL AND OTHER BARBITURATES Mechanisms of Action 489 Richard W. Olsen 51 Chemistry, Biotransformation, and Pharmacokinetics 496 Gail D. Anderson 52 Interactions with Other Drugs 504 /. Steven Leeder 53 Clinical Efficacy and Use in Epilepsy 514 Michel Baulac 54 Clinical Efficacy and Use in Nonepileptic Disorders 522

4 Contents IX 55 Adverse Effects 528 Michel Baulac, Joyce A. Cramer, and Richard H. Mattson 56 Methylphenobarbital 541 Mervyn J. Eadie and Wayne D. Hooper SECTION X. PHENYTOIN AND OTHER HYDANTOINS Mechanisms of Action 551 Robert J. DeLorenzo and David A. Sun 58 Chemistry and Biotransformation 565 Thomas R. Browne and Barbara LeDuc 59 Interactions with Other Drugs 581 Isabelle Ragueneau-Majlessi, Manoj Bajpai, and Rene H. Levy 60 Clinical Efficacy and Use in Epilepsy 591 B. Joe Wilder and Joseph Bruni 61 Clinical Efficacy and Use in Other Neurological Disorders Clinical Efficacy and Use in Psychiatric Disorders 600 Francesco Monaco and Marco Mula 63 Adverse Effects 605 Joseph Bruni 64 Fosphenytoin 611 Flavia M. Pryor and R. Eugene Ramsay SECTION XI. PRIMIDONE Primidone 621 Richard W. Fincham and Dorothy D. Schottelius SECTION XII. SUCCINIMIDES Mechanisms of Action 639 Katherine D. Holland and James A. Ferrendelli 67 Ethosuximide: Chemistry, Biotransformation, Pharmacokinetics, and Drug Interactions 646 Francesco Pisani, Emilio Perucca, and Meir Bialer 68 Clinical Efficacy and Use in Epilepsy 652 Allan L. Sherwin 69 Adverse Effects 658 Tracy A. Glauser 70 Methsuximide 665 Thomas R. Browne SECTION XIII. TIAGABINE Mechanisms of Action 675 William J. Giardina 72 Chemistry, Biotransformation, and Pharmacokinetics 681 Kenneth W. Sommerville and Stephen D. Collins 73 Drug Interactions 691 Kenneth W. Sommerville 74 Clinical Efficacy and Use in Epilepsy 698 Reetta Kdlvidinen 7 5 Clinical Efficacy and Use in Nonepileptic Disorders 705 Kenneth W. Sommerville 76 Adverse Effects 711 Steven C. Schachter SECTION XIV. TOPIRAMATE Mechanisms of Action 719 H. Steve White 78 Chemistry, Biotransformation, and Pharmacokinetics 727 Dennis R. Doose and Anthony J. Streeter 79 Drug Interactions 735 Barry E. Gidal 80 Clinical Efficacy and Use in Epilepsy 740 Michael D. Privitera and Roy E. Twyman 81 Clinical Efficacy and Use in Nonepileptic Disorders 753 Marc Kamin 82 Adverse Effects 760 Rajesh C. Sachdeo and Roopal M. Karia SECTION XV. VALPROIC ACID Mechanisms of Action 767 Wolfgang Loscher 84 Chemistry, Biotransformation, and Pharmacokinetics 780 Rene H. Levy, Danny D. Shen, Frank S. Abbott, Wayne Riggs, and Houda Hachad

5 Contents 85 Drug Interactions 801 Richard D, Scheyer 86 Clinical Efficacy and Use in Epilepsy 808 Blaise F. D. Bourgeois 87 Clinical Efficacy and Use in Other Neurological Disorders 818 Stephen D. Silberstein 88 Clinical Efficacy and Use in Psychiatric Disorders 828 Alan C. Swann 89 Adverse Effects 837 Pierre Genton and Philippe Gelisse SECTION XVI. VIGABATRIN Vigabatrin 855 Elinor Ben-Menachem SECTION XVII. ZONISAMIDE Mechanisms of Action Chemistry, Biotransformation, and Pharmacokinetics 873 Jaymin Shah, Kent Shellenberger, Daniel M. Canafax 93 Drug Interactions 880 Gary G. Mather and Jaymin Shah 94 Clinical Efficacy and Use in Epilepsy 885 Masakazu Seino and Buichi Fujitani 95 Adverse Effects 892 Byung In Lee SECTION XVIII. DRUGS IN DEVELOPMENT Pregabalin 901 Elinor Ben-Menachem and Alan R. Kugler 97 Rufinamide 906 Mary Ann Karolchyk and Dieter Schmidt 98 Drugs in Early Clinical Development 913 Emilio Perucca and Harvey J. Kupferberg Subject Index 929