Pregabalin: a new agent for the treatment of neuropathic pain

Drugs Today (Barc). 2005 Aug;41(8):509-16. doi: 10.1358/dot.2005.41.8.910482.

Abstract

Pregabalin (Lyrica, Pfizer) is a GABA analog with similar structure and actions to gabapentin. It has antiepileptic, analgesic and anxiolytic activity. Pregabalin is indicated for the management of neuropathic pain associated with diabetic neuropathy and post-herpetic neuralgia. Peak plasma levels occur approximately 1 hour after oral doses and oral bioavailability is about 90%. Based on AUC data, food does not significantly affect the extent of absorption. Pregabalin is not protein-bound and exhibits a plasma half-life of about 6 hours, which is not dose-dependent. Hepatic metabolism is negligible, and most of the oral dose (95%) appears unchanged in the urine. Pregabalin is a safe and well-tolerated new treatment for neuropathic pain. Furthermore, pregabalin has proven efficacy in adjunctive therapy of refractory partial seizures and in the treatment of acute pain, generalized anxiety disorder and social phobia.

Publication types

  • Review

MeSH terms

  • Analgesics, Non-Narcotic / adverse effects
  • Analgesics, Non-Narcotic / pharmacokinetics
  • Analgesics, Non-Narcotic / pharmacology
  • Analgesics, Non-Narcotic / therapeutic use*
  • Animals
  • Anti-Anxiety Agents / adverse effects
  • Anti-Anxiety Agents / pharmacokinetics
  • Anti-Anxiety Agents / pharmacology
  • Anti-Anxiety Agents / therapeutic use
  • Anticonvulsants / adverse effects
  • Anticonvulsants / pharmacokinetics
  • Anticonvulsants / pharmacology
  • Anticonvulsants / therapeutic use
  • Diabetic Neuropathies / drug therapy
  • Fibromyalgia / drug therapy
  • Herpes Zoster / drug therapy
  • Humans
  • Neuralgia / drug therapy
  • Pain / drug therapy*
  • Pregabalin
  • gamma-Aminobutyric Acid / adverse effects
  • gamma-Aminobutyric Acid / analogs & derivatives*
  • gamma-Aminobutyric Acid / pharmacokinetics
  • gamma-Aminobutyric Acid / pharmacology
  • gamma-Aminobutyric Acid / therapeutic use

Substances

  • Analgesics, Non-Narcotic
  • Anti-Anxiety Agents
  • Anticonvulsants
  • Pregabalin
  • gamma-Aminobutyric Acid