Clinical effects and mechanism of action of sumatriptan in migraine.
Sumatriptan is a novel, highly effective drug against migraine and cluster headache attacks. It shows a remarkably selective pharmacological profile in animals. Determination of its mechanism of action in human should further the understanding of the pathophysiology of migraine and cluster headache. We, therefore, review current knowledge on the clinical and pharmacological effects of sumatriptan. Important pharmacological actions of sumatriptan are (i) poor penetration of the blood-brain barrier suggesting a peripheral point of action; (ii) 5-HT1-like/5-HT1d receptor-mediated vasoconstriction of large cerebral arteries and dural vessels; and (iii) blockade of neurogenic dural inflammation via 5-HT1d autoreceptor-mediated inhibition of vasoactive neuropeptides within the trigeminovascular system. Future research will tell which mechanism is involved in the pathophysiology of migraine and cluster headache.
Ferrari
M D
MD
Department of Neurology, University Hospital, Leiden, The Netherlands.
Saxena
P R
PR
D000818:Animals; D001921:Brain / Q000098:blood supply; D003027:Cluster Headache / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007211:Indoles / Q000627:therapeutic use*; D008881:Migraine Disorders / Q000188:drug therapy*; D011985:Receptors, Serotonin / Q000187:drug effects*; D013449:Sulfonamides / Q000627:therapeutic use*; D018170:Sumatriptan; D014661:Vasoconstriction / Q000187:drug effects; D014662:Vasoconstrictor Agents / Q000627:therapeutic use*; D014666:Vasomotor System / Q000187:drug effects
D007211:Indoles; D011985:Receptors, Serotonin; D013449:Sulfonamides; D014662:Vasoconstrictor Agents; D018170:Sumatriptan