Mechanisms of action of serotonin 5-HT1B/D 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 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.
Goadsby
P J
PJ
Institute of Neurology, London, UK.
Hargreaves
R J
RJ
D006801:Humans; D008881:Migraine Disorders / Q000188:drug therapy* / Q000503:physiopathology*; D017366:Serotonin Receptor Agonists / Q000494:pharmacology / Q000627:therapeutic use*; D014230:Triazoles / Q000494:pharmacology / Q000627:therapeutic use*; D014363:Tryptamines
D017366:Serotonin Receptor Agonists; D014230:Triazoles; D014363:Tryptamines; C093622:rizatriptan