Antiepileptic Drugs

Antiepileptic Drugs

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Product Details

ISBN-13: 9783642695209
Publisher: Springer Berlin Heidelberg
Publication date: 12/06/2011
Series: Handbook of Experimental Pharmacology , #74
Edition description: Softcover reprint of the original 1st ed. 1985
Pages: 867
Product dimensions: 6.69(w) x 9.61(h) x 0.07(d)

Table of Contents

Clinical Aspects of Epileptic Diseases.- 1 Epilepsy: Seizures and Syndromes.- A. Definition.- B. Epidemiology.- C. Classification.- D. Epileptic Seizures.- E. Syndromes of Epilepsy.- F. Age-Related Syndromes.- I. Neonatal Convulsions (Neonatal Seizures).- II. Febrile Convulsions.- III. Epilepsy with Infantile Spasms (West Syndrome, Infantile Spasms, Epilepsy with Propulsive Petit Mai).- IV. Epilepsy with Myoclonic-Astatic Seizures (Lennox-Gastaut Syndrome.- V. Epilepsy with Frequent Absences (Friedmann Syndrome, Pyknolepsy).- VI. Epilepsy with Juvenile Myoclonic Jerks (Herpin-Janz Syndrome, Epilepsy with Impulsive Petit Mai, Juvenile Myoclonic Epilepsy).- VII. Awakening Epilepsy (Epilepsy with Nonfocal Grand Mai).- VIII. Benign Focal Epilepsy of Childhood [Benign Epilepsy of Children with Rolandic (Centrotemporal) Foci].- G. Age-Unrelated Epilepsy Syndromes.- I. Epilepsies with Complex Focal (Psychomotor) Seizures (Temporal, Rhinencephalic, Limbic Epilepsy).- II. Epilepsies with Simple Focal Seizures (Neocortical Epilepsy, Epilepsy with Jacksonian Seizures, Adversive Seizures, Sensory Auras, Sensory Seizures).- III. Status Epilepticus.- IV. Syndromes of Seizures Elicited by Sensory Stimuli (So-called Reflex Epilepsies).- References.- 2 Electroencephalography.- A. Introduction.- B. Main Forms of Epileptiform Patterns.- C. Focal Epileptiform Activity.- D. Bilateral Epileptiform Patterns.- E. Activation Procedures.- F. Electrocorticography and Depth-recording.- References.- 3 Epilepsy in Animals.- A. Introduction.- B. Acquired Epilepsies in Animals.- C. Inherited Epilepsies in Animals.- I. Photomyoclonic Seizures in the Baboon (Papio papio).- II. Inherited Epilepsy in Dogs.- III. Inherited Epilepsy in Mongolian Gerbils (Meriones unguiculatus).- IV. Inherited Epilepsy in Domestic Fowl.- D. Concluding Remarks.- References.- Pathophysiology of Seizure Disorders.- 4 Intermediary Metabolism.- A. Introduction.- B. Brain Energy Reserves and the Cell Redox Potential.- I. Cerebral Energy Use During Seizures.- II. Brain Redox Potential and Lactic Acidosis.- C. Seizures and Glycolytic Flux.- I. Regulation of Glycolysis: Phosphofructokinase.- II. Hexokinase.- III. Pyruvate Kinase.- D. The Citric Acid Cycle and Epileptic Seizures.- I. Energy Metabolism.- II. Amino Acid Metabolism.- III. Ammonia Metabolism.- E. Free Fatty Acid Metabolism.- F. Metabolic Mechanisms of Neuronal-Cell Damage During Status Epilepticus.- I. Role of Extracerebral Factors.- II. Role of Sustained Cell Firing.- III. Role of Energy Failure.- IV. Lactic Acidosis.- V. Calcium “Cytotoxicity”.- G. Epileptic Seizures in the Neonate.- I. Mobilization of Glycogen Reserves.- II. Limited Transport Capacity of the Blood-brain Barrier.- References.- 5 Monoamines and the Pathophysiology of Seizure Disorders.- A. Introduction.- B. Catecholamines.- I. Electrically Induced Seizures.- II. Seizures Induced by Chemical Agents.- III. Reflex Epilepsy Models.- IV. Other Models of Epilepsy.- C. Serotonin.- I. Electrically Induced Seizures.- II. Seizures Induced by Pentylenetetrazol.- III. Reflex Epilepsy Models.- D. Histamine.- E. Conclusions.- References.- 6 Acetylcholine.- A. Introduction.- B. Effect of Cholinergic Drugs on Susceptibility to Seizures.- C. Effect of Experimental and Spontaneous Seizures on the Cholinergic System.- I. Electroshock and Convulsant Drugs.- II. Spontaneous and Audiogenic Convulsions.- III. Focal Epilepsy.- D. Kindling and the Cholinergic System.- E. Conclusions.- References.- 7 GABA and Other Amino Acids.- A. Introduction: Amino Acids as Neurotransmitters.- B. Amino Acids Producing Inhibition.- I. Introduction.- II. GABA.- III. Glycine.- IV. Taurine.- C. Amino Acids Producing Excitation.- I. Dicarboxylic Amino Acids.- II. Sulphinic and Sulphonic Acids.- D. Concluding Remarks.- I. Inherited Abnormalities of Amino Acid Metabolism and Epilepsy.- II. Amino Acids and Antiepileptic Drugs.- References.- 8 Prostaglandins.- A. Introduction.- B. Effects of Prostaglandins on Experimentally Induced Convulsions.- C. Convulsant Effect of Prostaglandins.- D. Release of Prostaglandins During Convulsions.- E. Conclusions.- References.- General Pharmacology of Antiepileptic Drugs.- 9 Chemical Constitution and Pharmacological Effect.- A. Introduction.- B. Five-Membered Heterocyclic Compounds.- I. Hydantoins.- II. Oxazolidinediones.- III. Succinimides.- C. Six-Membered Heterocyclic Compounds.- I. Barbiturates and Other Compounds.- II. Phenobarbital and Primidone.- D. Acyl Ureas.- E. Tricyclic Compounds: Carbamazepine.- F. Benzodiazepines.- G. Valproic Acid.- H. Miscellaneous Compounds.- References.- 10 Biochemistry.- A. Introduction.- B. Ionic Permeability.- I. Effects on Sodium Conductance.- II. Effects on Calcium Conductance.- III. Effects on Potassium Conductance.- IV. Effects on Chloride Conductance.- C. Neurotransmitter Metabolism, Disposition, and Dynamics.- I. Effects on Intracellular Processes Related to Transmitter Release.- II. Effects on Neurotransmitter Metabolism and Disposition.- III. Effects on Receptor-Ionophore Dynamics.- D. Perspective.- References.- 11 Tolerance and Dependence.- A. Introduction.- B. Tolerance.- I. Metabolic Tolerance.- II. Functional Tolerance.- III. Acute Tolerance.- IV. Conclusions.- C. Physical Dependence.- I. Experimental Evidence.- II. Clinical Evidence.- III. Conclusions.- References.- 12 Animal Experimental Methods in the Study of Antiepileptic Drugs.- A. Introduction.- B. Models of Epileptiform Phenomena in Animals.- I. Electrically Induced Seizures.- II. Chemically Induced Ictal and Interictal States (Exclusive of Metals).- III. Focal Epileptogenesis Through Local Application of Metals or Metal Salts.- IV. Local Freezing as Epileptogenic Factor.- V. Models for Secondary and Progressive Epileptogenic Lesions.- VI. Animals with “Inborn” Epilepsy: Genetic Models.- VII. Circadian Aspects.- C. Some Nonsymptomatic Models.- I. Biophysical Approach.- II. Biochemical Approach.- D. Discussion.- I. Models for Screening.- II. Testing for “Special Indications”.- References.- Appendix to Chapter 12 Antiepileptic Drug Development Program.- A. Antiepileptic Drug Development Programm.- B. Anticonvulsant Screening Project.- I. Phase I.- II. Phase II.- III. Phase III.- IV. Phase IV.- V. Phase V.- VI. Phase VI.- VII. Phase VII.- C. Toxicity/Selected Pharmacology Project.- D. Primate Model of Epilepsy.- E. Controlled Clinical Trials.- References.- Specific Pharmacology of Antiepileptic Drugs.- 13 Hydantoins.- A. Introduction.- B. Chemistry.- I. Physicochemical Properties.- II. Structure-Activity Relationships.- III. Analytical Methods.- C. Anticonvulsant Activity.- I. Anticonvulsant Potency in Laboratory Animals.- II. Anticonvulsant Potency in Man.- III. Mechanism of Anticonvulsant Action.- D. Other Central Nervous System Effects.- E. Actions Outside the CNS.- I. Cardiac Muscle.- II. Smooth Muscle.- III. Skeletal Muscle.- IV. Other Actions.- F. Pharmacokinetics.- I. Absorption and Bioavailability.- II. Distribution.- III. Biotransformation.- IV. Excretion.- G. Drug Interactions.- H. Toxicology.- I. Acute Toxicity.- II. Chronic Toxicity Studies.- III. Teratogenic Effects.- IV. Mutagenic Effects.- V. Other Toxic Effects.- References.- 14 Barbituric Acid Derivatives.- A. Introduction.- B. Chemistry and Physicochemical Properties.- I. Relationship of Molecular Structure to Anticonvulsant Activity.- II. Relationship of Acidic and Lipophilic Properties of Barbituric Acid Derivatives to CNS Activity.- C. Analytical Methods for Determination of Barbituric Acid Derivatives in Biological Fluids and Tissues.- D. Anticonvulsant Activity.- E. Other CNS Effects.- F. Pharmacodynamic Effects Outside the CNS.- G. Pharmacokinetics.- I. Absorption.- II. Distribution.- III. Metabolism.- IV. Excretion.- H. Drug Interactions.- J. Toxicology.- References.- 15 Primidone.- A. Chemistry and Physicochemical Properties.- I. Physicochemical Properties.- II. Analytical Methods for Determination from Biological Material.- B. Anticonvulsant Activity.- I. Anticonvulsant Efficacy in Laboratory Animals.- II. Anticonvulsant Potency in Man.- III. Mechanism of Anticonvulsant Action.- C. Other Central Nervous System Effects.- D. Pharmacodynamic Actions Outside the Central Nervous System.- E. Pharmacokinetics.- I. Absorption.- II. Distribution.- III. Metabolism.- IV. Elimination.- F. Drug Interactions.- G. Toxicology.- I. Acute Toxicology.- II. Chronic Toxicity Studies.- III. Teratogenic Effect.- IV. Mutagenic Effect.- V. Other Toxic Effects.- VI. Clinical Intoxications.- References.- 16 Carbamazepine.- A. Introduction.- B. Chemistry and Physicochemical Properties.- C. Anticonvulsant Activity.- I. Anticonvulsant Activity in Rodent-Screening Tests.- II. Anticonvulsant Activity in Further Animal Models.- III. Pharmacological Effects Possibly Related to Anticonvulsant Activity.- IV. Neurobiochemical Effects Possibly Related to Anticonvulsant Activity.- V. Mechanisms of Action.- D. Behavioral, Neurological, and Autonomic Effects.- I. Antiaggressive and/or Anxiolytic Effects.- II. Antineuralgic Effects.- III. Antidiuretic Effects.- IV. Effects on Alcohol-Withdrawal Symptoms.- V. Antiarrhythmic Effects.- VI. Antimaniacal Effects.- VII. Other Effects.- E. Pharmacokinetics.- I. Absorption.- II. Distribution.- III. Metabolism.- IV. Elimination.- F. Drug Interactions.- G. Toxicology.- I. Acute Toxicity Studies.- II. Subacute and Chronic Toxicity Studies.- III. Reproduction Studies.- IV. Mutagenicity Studies.- V. Carcinogenicity Studies.- References.- 17 Valproic Acid.- A. Chemistry and Physicochemical Properties.- B. Antiepileptic Activity.- I. Valproic Acid in Experimental Models of Epilepsy.- II. Mechanism of Anticonvulsant Action of Valproic Acid.- C. Central Nervous System Effects Besides the Anticonvulsant Effect.- D. Pharmacodynamic Properties Outside the Central Nervous System.- E. Pharmacokinetics.- I. Absorption and Bioavailability.- II. Distribution and Protein Binding.- III. Elimination.- F. Drug Interactions.- I. Effect of Valproic Acid on Other Drugs.- II. Effect of Other Drugs on Valproic Acid.- G. Toxicity.- References.- 18 Oxazolidinediones.- A. Introduction.- B. Anticonvulsant Effects.- I. Chemically Induced Convulsions.- II. Electrically Induced Convulsions.- III. Convulsions Produced by Other Methods.- C. Central Nervous System Effects Besides the Anticonvulsant Effect..- I. Influence on the Electroencephalogram.- II. Influence on Behavior.- D. Biochemical Effects.- I. Transmitter.- II. Other Effects.- E. Pharmacodynamic Properties Outside the Central Nervous System.- F. Pharmacokinetics.- I. Absorption.- II. Distribution.- III. Metabolism.- IV. Excretion.- G. Interactions.- H. Toxicity.- References.- 19 Succinimides.- A. Introduction.- B. Anticonvulsant Effects.- I. Chemically Induced Convulsions.- II. Electrically Induced Convulsions.- III. Convulsions Induced by Other Methods.- C. Central Nervous System Effects Besides the Anticonvulsant Effect.- I. Influence on the EEG.- II. Influence on Behavior.- III. Effects on Neurochemical Processes.- D. Pharmacodynamic Properties Outside the Central Nervous System.- E. Pharmacokinetics.- I Absorption.- II. Distribution.- III. Metabolism.- IV. Elimination.- F. Interactions.- G. Toxicity.- References.- 20 Benzodiazepines.- A. Introduction.- B. Chemical Structure of Benzodiazepines.- C. Methods of Determination.- D. Kinetics.- I. Absorption and Distribution.- II. Metabolism and Elimination Half-lives.- E. Anticonvulsant Properties.- F. Relationship Between Anti-Pentylenetetrazol Activity and Brain Concentrations of Benzodiazepines.- G. Relationship Between Benzodiazepine Concentrations in the Brain and High-Affinity Drug-Binding Sites.- References.- 21 Carbonic Anhydrase Inhibitors.- A. Introduction.- B. Anticonvulsant Effect.- C. Clinical Use and Limitations.- D. Toxicity.- References.- 22 Acetylurea Derivatives.- A. Introduction.- B. Chemistry.- I. Synthesis and Physicochemical Properties.- II. Structure-Activity Relations.- C. Experimental Pharmacology.- I. Anticonvulsant Activity.- II. Other Pharmacodynamic Properties.- III. Pharmacokinetics.- IV. Drug Interactions.- V. Effects on Clinical Laboratory Tests.- D. Toxicity.- I. Acute Administration.- II. Chronic Administration.- E. Conclusions.- References.- 23 Electrophysiological Effects of Antiepileptic Drugs.- A. Introduction.- B. Phenytoin.- I. Neuronal Membranes.- II. Synaptic Transmission.- III. Brain.- IV. Summary.- C. Barbiturates.- I. General Remarks.- II. Membrane Excitability.- III. Synaptic Transmission.- IV. Spinal Cord.- V. Brain.- VI. Summary.- D. Carbamazepine.- I. Nerve Fibers.- II. Synaptic Transmission.- III. Brain.- IV. Summary.- E. Valproic Acid.- I. Ganglia and Spinal Cord Neurons.- II. Brain.- III. Summary.- F. Oxazolidinediones.- I. Nerve Fibers and Ganglia.- II. Spinal Cord.- III. Synaptic Transmission in the Spinal Trigeminal Nucleu.- IV. Brain.- V. Summary.- G. Succinimides.- I. Synaptic Transmission.- II. Brain: Focal Seizure Activity.- III. Summary.- H. Benzodiazepines.- I. Facilitation of GABAergic Transmission.- II. Excitable Membranes and Synaptic Transmission in the Periphery.- III. Spinal Cord.- IV. Brain.- V. Summary.- J. Miscellaneous.- I. Carboanhydrase Inhibition: Acetazolamide.- II. Local Anesthetics.- References.- Clinical Pharmacology of Antiepileptic Drugs.- 24 Clinical Pharmacokinetics of Antiepileptic Drugs.- A. Hydantoin Drugs.- I. Phenytoin.- II. Mephenytoin (Methoin).- III. Ethotoin.- B. Barbiturates and Chemically Related Anticonvulsants.- I. Phenobarbital (Phenobarbitone).- II. Methylphenobarbital (Mephobarbital).- III. Eterobarbital.- IV. Primidone.- C. Carbamazepine.- D. Valproic Acid.- E. Succinimides.- I. Ethosuximide.- II. Methsuximide.- III. Phensuximide.- F. Benzodiazepines.- I. Diazepam.- II. Clonazepam.- G. Oxazolidinediones.- I. Trimethadione (Troxidone).- II. Paramethadione.- H. Acetazolamide.- J. Sulthiame.- K. Pheneturide.- References.- 25 Monitoring Antiepileptic Drug Levels.- A. Introduction.- B. Justification for Monitoring Plasma Concentration Levels of Antiepileptic Drugs.- C. The Concept of the Therapeutic Level.- D. Clinical Evaluation of Therapeutic Levels.- E. Therapeutic Plasma Concentration Ranges for the Individual Antiepileptic Drugs.- I. Phenytoin.- II. Carbamazepine.- III. Phenobarbital.- IV. Primidone.- V. Ethosuximide.- VI. Benzodiazepines.- VII. Valproic Acid.- VIII. Other Antiepileptic Drugs.- F. Protein Binding and Monitoring Antiepileptic Drug Levels.- G. Monitoring Antiepileptic Drug Therapy by Measurements in Biological Fluids Other than Plasma.- I. General Considerations.- II. Monitoring Salivary Levels of Antiepileptic Drugs.- III. Monitoring Antiepileptic Drugs in Tears.- H. Active Metabolites and Monitoring Antiepileptic Drug Levels.- I. Phenytoin.- II. Carbamazepine.- III. Phenobarbital.- IV. Primidone.- V. Ethosuximide.- VI. Benzodiazepines.- VII. Valproic Acid.- J. Pharmacodynamic Aspects of Monitoring Antiepileptic Drug Levels..- K. Practical Problems of Monitoring Antiepileptic Drug Levels.- I. Timing of Sampling.- II. Handling of Blood Samples and Results.- L. Utilization of the Monitoring of Antiepileptic Drug Levels.- References.- 26 Clinical Use of Antiepileptic Drugs.- A. Introduction.- B. Use of Antiepileptic Drugs in Epilepsy.- I. Indications for the Use of Antiepileptic Drugs.- II. Aim of Antiepileptic Drug Therapy.- III. Selection of an Antiepileptic Drug.- IV. Use of Antiepileptic Drugs in Practice.- V. Combinations of Antiepileptic Drugs.- VI. Indications for Cessation of Antiepileptic Drug Therapy.- C. Use of Antiepileptic Drugs for Indications Other than Epilepsy.- I. Migraine.- II. Tic Douloureux.- III. Other Varieties of Pain.- IV. Hyperinsulinism.- V. Dyskinesia.- VI. Cardiac Arrhythmia.- VII. Myotonia.- VIII. Miscellaneous.- References.- 27 Adverse Effects.- A. Introduction.- B. Mechanism of Adverse Effects.- I. Dose-Dependent Side Effects.- II. Drug-Induced Diseases.- C. Adverse Effects.- I. Adverse Effects of Individual Antiepileptic Drugs.- II. Antiepileptic Drug-Induced Diseases.- References.- 28 Antiepileptic Drug Interactions.- A. Interactions Affecting the Kinetics of Antiepileptic Drugs.- I. Drugs Which May Affect the Gastrointestinal Absorption of Antiepileptic Drugs.- II. Drugs Which May Affect the Plasma Protein Binding of Antiepileptic Drugs.- III. Drugs Which May Inhibit the Metabolism of Antiepileptic Drugs.- IV. Drugs Which Stimulate the Metabolism of Antiepileptic Drugs.- V. Drugs Which May Affect the Renal Excretion of Antiepileptic Drugs.- B. Interactions Affecting the Kinetics of Other Drugs.- I. Drugs Whose Gastrointestinal Absorption May Be Affected by Antiepileptic Drugs.- II. Drugs Whose Plasma Protein Binding May Be Affected by Antiepileptic Drugs.- III. Drugs Whose Metabolism May Be Inhibited by Antiepileptic Drugs.- IV. Drugs Whose Metabolism May Be Stimulated by Antiepileptic Drugs.- V. Interactions Resulting in Altered Drug Excretion in Urine.- References.

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