Biollaz J, Burnier M, Turini G A, Brunner D B, Porchet M, Gomez H J, Jones K H, Ferber F, Abrams W B, Gavras H, Brunner H R
Clin Pharmacol Ther. 1981 May;29(5):665-70. doi: 10.1038/clpt.1981.92.
Three new angiotensin converting-enzyme inhibitors were given orally to 20 men in single doses ranging from 1.25 to 40 mg. Two of them induced comparable marked inhibition of both the blood pressure response to exogenous angiotensin I and plasma converting-enzyme activity. Onset of action was relatively slow, but 21 to 24 hr after drug plasma converting-enzyme activity was still clearly reduced. The third was less active. There was a close correlation between blood pressure response on administration of angiotensin I and plasma converting-enzyme activity. There were no adverse effects. These new drugs are interesting because of their long duration of action. The measurement of plasma converting-enzyme activity seems useful for monitoring efficacy of converting-enzyme blockade and compliance to therapy.
给20名男性口服三种新型血管紧张素转换酶抑制剂,单剂量范围为1.25至40毫克。其中两种药物对外源性血管紧张素I引起的血压反应和血浆转换酶活性均产生了相当显著的抑制作用。起效相对较慢,但用药后21至24小时血浆转换酶活性仍明显降低。第三种药物活性较低。给予血管紧张素I后的血压反应与血浆转换酶活性之间存在密切相关性。未出现不良反应。这些新药因其作用持续时间长而令人关注。血浆转换酶活性的测定似乎有助于监测转换酶阻断的疗效和治疗依从性。