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Current and emerging second-generation triptans in acute migraine therapy: a comparative review.

Abstract
Sterile neurogenic inflammation within cephalic tissue, involving vasodilation and plasma protein extravasation, has been proposed as a pathophysiological mechanism in acute migraine. The action of 5-hydroxytryptamine (5-HT1B/1D) agonists--so-called triptans--on receptors located in meningeal arteries (5-HT1B) and trigeminovascular fiber endings (5-HT1D) has an inhibitory effect on this neurogenic inflammation. Recently, a series of second-generation 5-HT1B/1D agonists (almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, and zolmitriptan) have been developed and are reviewed in this article. Their in vitro pharmacological properties, pharmacokinetics, clinical efficacy, drug interactions, and adverse effects are evaluated and compared to the golden standard in the treatment of acute migraine, sumatriptan.
AuthorsD Deleu, Y Hanssens
JournalJournal of clinical pharmacology (J Clin Pharmacol) Vol. 40 Issue 7 Pg. 687-700 (Jul 2000) ISSN: 0091-2700 [Print] England
PMID10883409 (Publication Type: Comparative Study, Journal Article, Review)
Chemical References
  • Carbazoles
  • HTR1B protein, human
  • Indoles
  • Oxazoles
  • Oxazolidinones
  • Piperidines
  • Pyrrolidines
  • Receptor, Serotonin, 5-HT1B
  • Receptor, Serotonin, 5-HT1D
  • Receptors, Serotonin
  • Serotonin Receptor Agonists
  • Triazoles
  • Tryptamines
  • almotriptan
  • eletriptan
  • zolmitriptan
  • rizatriptan
  • frovatriptan
  • naratriptan
Topics
  • Acute Disease
  • Carbazoles (therapeutic use)
  • Humans
  • Indoles (therapeutic use)
  • Migraine Disorders (drug therapy)
  • Oxazoles (therapeutic use)
  • Oxazolidinones
  • Piperidines (therapeutic use)
  • Pyrrolidines (therapeutic use)
  • Receptor, Serotonin, 5-HT1B
  • Receptor, Serotonin, 5-HT1D
  • Receptors, Serotonin (metabolism)
  • Serotonin Receptor Agonists (therapeutic use)
  • Triazoles (therapeutic use)
  • Tryptamines

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