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舒马坦(Sumatriptan)为一5-羟色胺拮抗剂,现已在加拿大应用,并即将在美国采用口服或注射治疗偏头痛。药动学本品经皮下注射后即被迅速吸收,5～20分钟后血药可达峰值。此药在肝内被代谢为灭活形式,并随尿排出,平均半减期约2小时。口服后,仅有15％药物进入全身循环,很显然,是由于通过肝脏广泛的首过清除所造成的;约1.5小时可达血药峰值。临床评价一项639例的双盲试验发现,于皮下注射本品6mg,30分钟内头痛缓解者达50％,60分钟内达70％,2小时内约
Sumatriptan, a serotonin antagonist, is now available in Canada and is being administered orally or in the United States to treat migraine. Pharmacokinetics This product is rapidly absorbed after subcutaneous injection, 5 to 20 minutes after the blood up to the peak. This drug is metabolized in the liver as an inactivated form and excreted in the urine with an average of about 2 hours of half-downtime. After oral administration, only 15% of the drugs enter the systemic circulation, apparently due to extensive first pass clearance through the liver; peak blood levels of about 1.5 hours. Clinical evaluation A 639 double-blind trial found that subcutaneous injection of this product 6mg, headache relief within 30 minutes up to 50% within 60 minutes up to 70% within about 2 hours