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Current and Emerging Second‐Generation Triptans in Acute Migraine Therapy: A Comparative Review
Author(s) -
Deleu Dirk,
Hanssens Yolande
Publication year - 2000
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/00912700022009431
Subject(s) - triptans , rizatriptan , sumatriptan , zolmitriptan , medicine , migraine , neurogenic inflammation , pharmacology , anesthesia , receptor , agonist , substance p , neuropeptide
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‐HT 1B/1D ) agonists—so‐called triptans—on receptors located in meningeal arteries (5‐HT 1B ) and trigeminovascular fiber endings (5‐HT 1D ) has an inhibitory effect on this neurogenic inflammation. Recently, a series of second‐generation 5‐HT 1B/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.