Simpson Dene, Noble Stuart, Goa Karen L
Adis International Limited, Auckland, New Zealand.
Drugs. 2002;62(9):1367-77; discussion 1378-9. doi: 10.2165/00003495-200262090-00013.
Perindopril is a long-acting ACE inhibitor, acting through its only active metabolite perindoprilat. It inhibits the renin-angiotensin system by preventing both the conversion of angiotensin I to angiotensin II and the degradation of bradykinin, thereby reducing the vasoconstriction and left ventricular remodelling characteristic of heart failure. Perindopril 4mg significantly improved a range of haemodynamic parameters in single-dose and long-term (8 weeks and 3 months) studies involving patients with congestive heart failure (CHF), with little or no effect on blood pressure or heart rate. In randomised, double-blind, placebo-controlled clinical trials conducted over 3 months and a large noncomparative study (up to 30 months), perindopril 4mg once daily significantly increased exercise tolerance and reduced symptoms of heart failure in patients with mild to moderate CHF. Perindopril 4mg once daily is generally well tolerated in patients with mild to moderate CHF. In a large noncomparative study the most commonly reported adverse clinical event was cough, which led to 2.8% of patients discontinuing treatment. In short-term comparative trials there was a significantly lower incidence of first-dose hypotension following the recommended starting dose of perindopril 2mg than after the equivalent starting doses of captopril, enalapril and lisinopril.
培哚普利是一种长效血管紧张素转换酶(ACE)抑制剂,通过其唯一的活性代谢产物培哚普利拉发挥作用。它通过阻止血管紧张素I转化为血管紧张素II以及缓激肽的降解来抑制肾素-血管紧张素系统,从而减轻心力衰竭特有的血管收缩和左心室重塑。在涉及充血性心力衰竭(CHF)患者的单剂量和长期(8周和3个月)研究中,4mg培哚普利显著改善了一系列血流动力学参数,对血压或心率几乎没有影响。在为期3个月的随机、双盲、安慰剂对照临床试验以及一项大型非对照研究(长达30个月)中,每日一次4mg培哚普利显著提高了轻度至中度CHF患者的运动耐量并减轻了心力衰竭症状。轻度至中度CHF患者对每日一次4mg培哚普利一般耐受性良好。在一项大型非对照研究中,最常报告的不良临床事件是咳嗽,导致2.8%的患者停药。在短期比较试验中,与卡托普利、依那普利和赖诺普利的等效起始剂量相比,推荐起始剂量2mg培哚普利后的首剂低血压发生率显著更低。