Ferrari M D, Saxena P R
Department of Neurology, University Hospital, Leiden, The Netherlands.
Clin Neurol Neurosurg. 1992;94 Suppl:S73-7. doi: 10.1016/0303-8467(92)90028-2.
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.
舒马曲坦是一种新型的、治疗偏头痛和丛集性头痛发作的高效药物。它在动物身上显示出显著的选择性药理学特征。确定其在人体内的作用机制应有助于加深对偏头痛和丛集性头痛病理生理学的理解。因此，我们综述了关于舒马曲坦临床和药理作用的现有知识。舒马曲坦的重要药理作用包括：（i）血脑屏障穿透性差，提示作用靶点在外周；（ii）5-HT1样/5-HT1d受体介导的大脑大动脉和硬脑膜血管收缩；（iii）通过5-HT1d自身受体介导的对三叉神经血管系统内血管活性神经肽的抑制作用来阻断神经源性硬脑膜炎症。未来的研究将揭示偏头痛和丛集性头痛的病理生理学涉及哪种机制。
