Gabapentin: pharmacology and its use in pain management

Anaesthesia. 2002 May;57(5):451-62. doi: 10.1046/j.0003-2409.2001.02399.x.


Although its exact mode of action is not known, gabapentin appears to have a unique effect on voltage-dependent calcium ion channels at the postsynaptic dorsal horns and may, therefore, interrupt the series of events that possibly leads to the experience of a neuropathic pain sensation. Gabapentin is especially effective at relieving allodynia and hyperalgesia in animal models. It has been shown to be efficacious in numerous small clinical studies and case reports in a wide variety of pain syndromes. Gabapentin has been clearly demonstrated to be effective for the treatment of neuropathic pain in diabetic neuropathy and postherpetic neuralgia. This evidence, combined with its favourable side-effect profile in various patient groups (including the elderly) and lack of drug interactions, makes it an attractive agent. Therefore, gabapentin should be considered an important drug in the management of neuropathic pain syndromes.

Publication types

  • Review

MeSH terms

  • Acetates / adverse effects
  • Acetates / pharmacology*
  • Amines*
  • Analgesics / adverse effects
  • Analgesics / pharmacology*
  • Anticonvulsants / adverse effects
  • Anticonvulsants / pharmacology*
  • Cyclohexanecarboxylic Acids*
  • Female
  • Gabapentin
  • Humans
  • Nervous System Diseases / complications*
  • Pain / etiology*
  • Pain / prevention & control
  • Pilot Projects
  • Pregnancy
  • Randomized Controlled Trials as Topic
  • gamma-Aminobutyric Acid*


  • Acetates
  • Amines
  • Analgesics
  • Anticonvulsants
  • Cyclohexanecarboxylic Acids
  • gamma-Aminobutyric Acid
  • Gabapentin