The mechanisms of action of commonly used antiepileptic drugs

Pharmacol Ther. 2001 Apr;90(1):21-34. doi: 10.1016/s0163-7258(01)00122-x.


In the past decade, nine new drugs have been licensed for the treatment of epilepsy. With limited clinical experience of these agents, the mechanisms of action of antiepileptic drugs may be an important criterion in the selection of the most suitable treatment regimens for individual patients. At the cellular level, three basic mechanisms are recognised: modulation of voltage-dependent ion channels, enhancement of inhibitory neurotransmission, and attenuation of excitatory transmission. In this review, we will attempt to introduce the concepts of ion channel and neurotransmitter modulation and, thereafter, group currently used antiepileptic drugs according to their principal mechanisms of action.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Animals
  • Anticonvulsants / classification*
  • Anticonvulsants / pharmacology*
  • Anticonvulsants / therapeutic use
  • Epilepsy / drug therapy
  • Glutamic Acid / metabolism
  • Humans
  • Ion Channels / drug effects*
  • Molecular Structure
  • Structure-Activity Relationship
  • Synaptic Transmission / drug effects*
  • gamma-Aminobutyric Acid / metabolism


  • Anticonvulsants
  • Ion Channels
  • Glutamic Acid
  • gamma-Aminobutyric Acid