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Sumatriptan系一新型5-HT_(ID)受体激动药,其血浆消除半衰期约为2小时,生物利用度(皮下注射)为96％,肾脏清除率力15.8L/h。静脉注射能明显升高体循环和肺循环的压力,使冠状动脉直径显著缩小。Sumatrip-tan作用于血管壁,对偏头痛时颅内扩张和水肿的血管具有强烈的收缩作用,也可作用于三叉神经末梢,减少神经肽的释放。目前,临床上主要用于治疗偏头痛,效果确切,副作用少。
Sumatriptan is a novel 5-HT_ (ID) receptor agonist with a plasma half-life of about 2 hours, bioavailability (subcutaneous injection) of 96%, and renal clearance of 15.8 L / h. Intravenous injection can significantly increase the pressure on the systemic circulation and pulmonary circulation, coronary artery diameter significantly reduced. Sumatrip-tan acts on the vessel wall and has a strong contractile effect on the blood vessels of intracranial dilatation and edema during migraine. It also acts on the trigeminal nerve terminals and reduces the release of neuropeptides. Currently, clinically used mainly for the treatment of migraine, the exact effect, fewer side effects.