Fuller R W, Warren J B, McCusker M, Dollery C T
Br J Clin Pharmacol. 1987 Jan;23(1):88-90. doi: 10.1111/j.1365-2125.1987.tb03014.x.
We tested the effect of oral enalapril on intradermal bradykinin to determine if kininase II inhibition occurs with therapeutic doses in vivo. Six normal male volunteers took either 5 mg enalapril orally or placebo on 2 days. Three hours later bradykinin was injected into the skin of the back in doses increasing from 10(-11) to 10(-9) M. Enalapril increased the bradykinin-induced wheal. Inhibition of kininase II may cause accumulation of endogenous bradykinin. This could be an important mechanism in the occasionally reported side effect of angioedema with the angiotensin converting enzyme (ACE) inhibiting group of drugs.
我们测试了口服依那普利对皮内缓激肽的作用,以确定在体内治疗剂量下是否会发生激肽酶II抑制。六名正常男性志愿者在两天内分别口服5毫克依那普利或安慰剂。三小时后,将缓激肽以从10(-11)到10(-9)M递增的剂量注射到背部皮肤中。依那普利增加了缓激肽诱导的风团。激肽酶II的抑制可能导致内源性缓激肽的积累。这可能是血管紧张素转换酶(ACE)抑制类药物偶尔报告的血管性水肿副作用的重要机制。