Abstract
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 1. (i) poor penetration of the blood-brain barrier suggesting a peripheral point of action; 2. (ii) 5-HT 1-like/5-HT 1d receptor-mediated vasoconstriction of large cerebral arteries and durai vessels; and 3. (iii) blockade of neurogenic durai inflammation via 5-HT 1d 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.
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