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卡托普利是第一个口服的血管紧张素转化酶(ACE)抑制剂,可用于肾性或原发性高血压及慢性心衰的治疗,但它在通常保存条件下不稳定,且剂量不易掌握,易致过量中毒。而不含巯基的enalapril(1)和它的代谢物enalaprilat(2)及后者的赖氨酸类似物lisinopril(3)都是第二代强ACE抑制剂。它们都可用HPLC和放射免疫法检测,抑制血浆ACE的作用较稳定,因此可在人体确定药物动力学及动力学/药效学的联系。19名血压正常的19～45岁男性患者,每天钠摄入量为120～180mEq。第一批9人按双盲拉丁
Captopril is the first oral angiotensin converting enzyme (ACE) inhibitor that can be used for the treatment of renal or essential hypertension and chronic heart failure, but it is not stable under normal storage conditions and the dose Not easy to grasp, easy to cause excessive poisoning. Whereas the sulfhydryl-free enalapril (1) and its metabolites enalaprilat (2) and the latter lysine analogue lisinopril (3) are second-generation strong ACE inhibitors. Both of them are detectable by HPLC and radioimmunoassay and inhibit the action of plasma ACE more stably, thus allowing the determination of pharmacokinetics and kinetics / pharmacodynamics in humans. Nineteen 19-45-year-old male patients with normal blood pressure had daily sodium intake of 120-180 mEq. The first nine were double blind Latin