Mechanisms of action of serotonin 5-HT1B/1D agonists: Insights into migraine pathophysiology using rizatriptan

Current theories on the etiology of migraine headache suggest that it is a neurovascular disorder (i.e., vascular change secondary to neural activatio n), 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 treatm ent of acute migraine. This article describes their mechanisms of action. T he development of 5-HT1B/1D agonist drugs, such as rizatriptan, and the stu dy of their pharmacology have enhanced our understanding of the mechanisms involved in the pathophysiology of migraine.