血管紧张素转化酶抑制药的进展

The Advance of Angiotensin Converting Enzyme Inhibitor

卡托普利是第一个用于临床的口服血管紧张素转化酶(ACE)抑制药.近10余年来此类药物发展迅速,临床应用的已逾十种.它们通过抑制ACE的活性,使血管紧张素Ⅰ不能转化为血管紧张素Ⅱ而降压.用以治疗高血压病有一定效果,预测或可望与β-受体阻滞剂、噻嗪类利尿剂等一样成为一线降压药.本类药物与利尿剂、钙拮抗剂等合用可增强降压疗效.其次当心衰病人用强心甙和利尿剂效果不佳时,加用本类药亦有增效作用.本文还对新发展的依那普利、赖诺普利、雷米普利、贝那普利、西拉普利、哌林多普利、喹那普利、磷诺普利和西瓦那普利等九种ACEI抑制药从药动学、临床应用及用法剂量等方面作了简要叙述。

Captopril was the first oral preparation of angiotensin converting enzyme inhibitor (ACEI) applied in clinics. They are developed rapidly and more than ten agents have been tried in clinic recently. The antihy- pertensive effect of these agents was mainly to inhibit converting enzyme activity which catalyzed the conver- sion of Angiotensin I to Angiotensin Ⅱ. They are effective in treating patients with hypertension and showed synergistic action while co-administered with diuretics or calcium antagonist. It was also an effient adjunct drug in treatment of congestive heart failure patients. The pharmacokinetics, clinical application and drug regimens of 9 newer ACEI were also discussed.