This chapter is a comprehensive account of the medicinal chemistry of
antiepileptic drugs. It provides the mechanism of drug action and detailed structureactivity
relationships of the antiepileptic and related drugs and their clinical relevance
to give the knowledge base for pharmacists. After a study of this chapter, students will
be able to:
• Relate principles of gamma amino butyric acid (GABA) biosynthesis, storage,
transport, and metabolism to the action of antiepileptic drugs.
• Define and differentiate among different types of seizures and epilepsy.
• Illustrate mechanism of action, SAR, metabolites, and clinical considerations of
different classes of antiepileptic drugs including: barbiturates, hydantoins,
oxazolidinediones, succinimides, amides, benzodiazepines, valproic acid and its
derivatives, GABA-analogs, and miscellaneous compounds.
Keywords: Antiepileptic drugs, Agonists and Antagonists of GABA and different
Ion Channels, Clinical use of Antiepileptic Drugs, Drug Receptor Interaction,
GABA, Structure Activity Relationship.
