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自从血管紧张素转化酶(ACE)抑制剂甲巯丙脯酸(Captopril,CTP)和依钠普利(Enalapril,ENL)分别于1981年和1984年在世界首次上市后,ACEI得到迅速发展并认为具有划时代意义。CTP已广泛用于治疗高血压(HYT)和充血性心衰(CHF),除口服剂型外,静脉注射已研制成功。第二代A-CEI ENL口服有效,不含巯基,与CTP不同,通过肝脏酯解,转化成有活性的二酸Enalprilat(ENL-at),ENL-at作用比CTP强,消除较慢。本文重点对近年来新上市的一些不含巯基的第二代ACEI作简要介绍。
Since the debut of the captopril (CTP) and enalapril (ENL) inhibitors of angiotensin converting enzyme (ACE) inhibitors in the world in 1981 and 1984 respectively, ACEI has been rapidly developed and considered With epoch-making significance. CTP has been widely used in the treatment of hypertension (HYT) and congestive heart failure (CHF). In addition to oral dosage forms, intravenous injection has been developed. The second generation of A-CEI ENL is orally available and does not contain a thiol group. Unlike CTP, it is converted to the active diacid Enalprilat (ENL-at) by hepatic esterification. ENL-at is stronger and less slowly than CTP. This article focuses on some of the newly listed in recent years without sulfhydryl second-generation ACEI for a brief introduction.