Mechanisms of action of serotonin 5-HT1B/D agonists: insights into migraine pathophysiology using rizatriptan
Goadsby, P.J.; Hargreaves, R.J.
Neurology 55(9 Suppl 2): S8-S14
2000
ISSN/ISBN: 0028-3878 PMID: 11089513 Document Number: 518270
Current theories on the etiology of migraine headache suggest that it is a neurovascular disorder (i.e., vascular change secondary to neural activation), with a primary CNS dysfunction giving rise to headache pain as a result of local intracranial vasodilatation and release of sensory neuropeptides from nerve endings in an activated trigeminal system. The serotonin 5-HT1B/1D agonists, known as the triptans, represent a major advance in the treatment of acute migraine. This article describes their mechanisms of action. The development of 5-HT1B/1D agonist drugs, such as rizatriptan, and the study of their pharmacology have enhanced our understanding of the mechanisms involved in the pathophysiology of migraine.