The mechanism of action of gabapentin in neuropathic pain

Curr Opin Investig Drugs. 2006 Jan;7(1):33-9.

Abstract

Neuropathic pain is a common and potentially treatable cause of considerable lifelong morbidity. Effective pharmacological treatments are scarce, but one group of drugs that has shown promise is the antiepileptics. Gabapentin has become popular as a first-line treatment for neuropathic pain because of its efficacy as an antineuropathic agent and relatively benign side-effect profile. However, its mechanism of action is far from clear. This review discusses the available evidence for the postulated mechanisms of action of gabapentin. Understanding the mechanism of action of this agent may well lead to the development of safer and more effective antineuropathic drugs.

Publication types

  • Review

MeSH terms

  • Amines* / adverse effects
  • Amines* / pharmacokinetics
  • Amines* / therapeutic use
  • Analgesics, Non-Narcotic* / adverse effects
  • Analgesics, Non-Narcotic* / pharmacokinetics
  • Analgesics, Non-Narcotic* / therapeutic use
  • Animals
  • Binding Sites
  • Calcium Channels / metabolism
  • Cyclohexanecarboxylic Acids* / adverse effects
  • Cyclohexanecarboxylic Acids* / pharmacokinetics
  • Cyclohexanecarboxylic Acids* / therapeutic use
  • Gabapentin
  • Humans
  • Pain / complications
  • Pain / drug therapy*
  • Pain / metabolism
  • Peripheral Nervous System Diseases / complications
  • Peripheral Nervous System Diseases / drug therapy*
  • Peripheral Nervous System Diseases / metabolism
  • Potassium Channels / metabolism
  • Receptors, Neurotransmitter / metabolism
  • Serotonin / blood
  • gamma-Aminobutyric Acid* / adverse effects
  • gamma-Aminobutyric Acid* / pharmacokinetics
  • gamma-Aminobutyric Acid* / therapeutic use

Substances

  • Amines
  • Analgesics, Non-Narcotic
  • Calcium Channels
  • Cyclohexanecarboxylic Acids
  • Potassium Channels
  • Receptors, Neurotransmitter
  • Serotonin
  • gamma-Aminobutyric Acid
  • Gabapentin