[Gabapentin: its mechanisms of action in the year 2003]

Rev Neurol. 2003 Jun;36(12):1159-65.
[Article in Spanish]

Abstract

Aims: The purpose of our study was to survey the data from the main research work published about the mechanisms of action of gabapentin.

Development: In addition to an unquestionable Gabaergic effect, gabapentin is the first antiepileptic that has been shown to have an effect on the a2d subunit of the voltage dependent calcium channels and on hyperpolarization activated cationic (Ih) currents. Gabapentin also exerts an indirect effect on the voltage dependent sodium channels, slightly inhibits glutamate and reduces the excretion of certain neurotransmitters, such as serotonin, dopamine and noradrenalin.

Conclusions: Gabapentin has a number of original mechanisms of action with which to account for its effects in epilepsies and in many other clinical entities.

Publication types

  • Review

MeSH terms

  • Acetates / metabolism*
  • Acetates / therapeutic use
  • Amines*
  • Animals
  • Anticonvulsants / metabolism*
  • Anticonvulsants / therapeutic use
  • Calcium Channel Blockers / metabolism
  • Calcium Channel Blockers / therapeutic use
  • Calcium Channels / metabolism
  • Cyclohexanecarboxylic Acids*
  • Excitatory Amino Acid Antagonists / metabolism
  • Excitatory Amino Acid Antagonists / therapeutic use
  • Gabapentin
  • Humans
  • Receptors, GABA / metabolism
  • Sodium Channels / metabolism
  • Synaptic Transmission / physiology
  • gamma-Aminobutyric Acid*

Substances

  • Acetates
  • Amines
  • Anticonvulsants
  • Calcium Channel Blockers
  • Calcium Channels
  • Cyclohexanecarboxylic Acids
  • Excitatory Amino Acid Antagonists
  • Receptors, GABA
  • Sodium Channels
  • gamma-Aminobutyric Acid
  • Gabapentin