Eletriptan

Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1587-98. doi: 10.1517/17425250903410226.

Abstract

Migraine is a multifactorial chronic central nervous system disorder, characterized by recurrent disabling attacks of moderate-to-severe headache. Symptomatic acute treatment of migraine should provide rapid and effective relief of the headache pain. The introduction of the 5-HT(1B/1D) receptor agonists (triptans) expanded the armamentarium for acute migraine pain treatment. Eletriptan is a second-generation triptan with favorable bioavailability and half-life, a high affinity for 5-HT(1B/1D) receptors and selectivity for cranial arteries. Eletriptan (40 and 80 mg) has been shown to be effective as early as 30 min after administration and well tolerated when compared to placebo. In comparative clinical trials, eletriptan 40 and 80 mg were superior or equivalent to other triptans and have shown a very high safety and tolerability profile across the studies performed. Eletriptan showed the most favorable cost-effectiveness profile when compared with other agents in its class.

Publication types

  • Review

MeSH terms

  • Animals
  • Controlled Clinical Trials as Topic
  • Humans
  • Migraine Disorders / drug therapy*
  • Pyrrolidines / economics
  • Pyrrolidines / metabolism
  • Pyrrolidines / pharmacokinetics
  • Pyrrolidines / therapeutic use*
  • Receptor, Serotonin, 5-HT1B / metabolism
  • Receptor, Serotonin, 5-HT1D / metabolism
  • Serotonin 5-HT1 Receptor Agonists*
  • Serotonin Receptor Agonists / economics
  • Serotonin Receptor Agonists / metabolism
  • Serotonin Receptor Agonists / pharmacokinetics
  • Serotonin Receptor Agonists / therapeutic use*
  • Tryptamines / economics
  • Tryptamines / metabolism
  • Tryptamines / pharmacokinetics
  • Tryptamines / therapeutic use*

Substances

  • Pyrrolidines
  • Receptor, Serotonin, 5-HT1B
  • Receptor, Serotonin, 5-HT1D
  • Serotonin 5-HT1 Receptor Agonists
  • Serotonin Receptor Agonists
  • Tryptamines
  • eletriptan