Lees K R, Reid J L
Br J Clin Pharmacol. 1987 Feb;23(2):159-64. doi: 10.1111/j.1365-2125.1987.tb03024.x.
The tolerance to and dynamic effects of 1 week's oral treatment with the angiotensin converting enzyme inhibitor, perindopril, were assessed in a placebo controlled, parallel group study in 36 normotensive males. The daily dose of perindopril was 1, 2, 4, 8 or 16 mg. The drug was well tolerated and produced no change in routine haematology or serum biochemistry tests. Dose related inhibition of plasma angiotensin converting enzyme was observed. Perindopril 16 mg produced 90% inhibition 4 h after dosing and 60% after 24 h. A dose related rise in plasma renin activity followed doses of 4 mg and over. The renin remained above the normal range for 24 h. Perindopril caused a modest lowering of plasma aldosterone levels but had no effect on plasma adrenaline or noradrenaline levels. Standing diastolic blood pressure was lowered, particularly with 16 mg daily of perindopril but only a slight rise in heart rate occurred. Perindopril appears to be a well tolerated inhibitor of plasma angiotensin converting enzyme, with predictable effects on the renin angiotensin system and blood pressure. An appropriate dose range for further study would appear to be 4 to 16 mg daily.
在一项针对36名血压正常男性的安慰剂对照平行组研究中,评估了血管紧张素转换酶抑制剂培哚普利口服治疗1周的耐受性和动态效果。培哚普利的日剂量分别为1毫克、2毫克、4毫克、8毫克或16毫克。该药物耐受性良好,常规血液学或血清生化检查未出现变化。观察到剂量相关的血浆血管紧张素转换酶抑制作用。给药4小时后,16毫克培哚普利产生90%的抑制作用,24小时后为60%。4毫克及以上剂量后,血浆肾素活性出现剂量相关升高。肾素在24小时内一直高于正常范围。培哚普利使血浆醛固酮水平适度降低,但对血浆肾上腺素或去甲肾上腺素水平无影响。站立位舒张压降低,尤其是每日服用16毫克培哚普利时,但心率仅轻微升高。培哚普利似乎是一种耐受性良好的血浆血管紧张素转换酶抑制剂,对肾素-血管紧张素系统和血压有可预测的影响。进一步研究的合适剂量范围似乎是每日4至16毫克。