Regamey Frédéric, Maillard Marc, Nussberger Jürg, Brunner Hans R, Burnier Michel
Division of Hypertension and Vascular Medicine, CHUV, Lausanne, Switzerland.
Hypertension. 2002 Sep;40(3):266-72. doi: 10.1161/01.hyp.0000030178.90322.11.
This double-blind placebo-controlled study was designed to investigate the acute and sustained hormonal, renal hemodynamic, and tubular effects of concomitant ACE and neutral endopeptidase (NEP) inhibition by omapatrilat, a vasopeptidase inhibitor, in men. Thirty-two normotensive subjects were randomized to receive a placebo, omapatrilat (40 or 80 mg), or the fosinopril/hydrochlorothiazide (FOS/HCTZ; 20 and 12.5 mg, respectively) fixed combination for 1 week. Blood pressure, renal hemodynamics, urinary electrolytes and atrial natriuretic peptide excretion, and several components of the renin-angiotensin system were measured for 6 hours on days 1 and 7 of drug administration. When compared with the placebo and the FOS/HCTZ combination, omapatrilat induced a significant decrease in plasma angiotensin II levels (P<0.001 versus placebo; P<0.05 versus FOS/HCTZ) and an increase in urinary atrial natriuretic peptide excretion (P<0.01). These hormonal effects were associated with a significant fall in blood pressure (P<0.01) and a marked renal vasodilatation, but with no significant changes in glomerular filtration rate. The FOS/HCTZ markedly increased urinary sodium excretion (P<0.001). The acute natriuretic response to FOS/HCTZ was significantly greater than that observed with omapatrilat (P<0.01). Over 1 week, however, the cumulative sodium excretion induced by both doses of omapatrilat (P<0.01 versus placebo) was at least as great as that induced by the dose of FOS/HCTZ (P=NS versus FOS/HCTZ). In conclusion, the results of the present study in normal subjects demonstrate that omapatrilat has favorable renal hemodynamic effects. Omapatrilat combines potent ACE inhibition with a sustained natriuresis, which explains its well-documented potent antihypertensive efficacy.
这项双盲安慰剂对照研究旨在调查血管肽酶抑制剂奥美普利拉对男性同时抑制ACE和中性内肽酶(NEP)所产生的急性和持续性激素、肾脏血流动力学及肾小管效应。32名血压正常的受试者被随机分为三组,分别接受安慰剂、奥美普利拉(40或80毫克)或福辛普利/氢氯噻嗪(分别为20和12.5毫克)固定复方制剂,为期1周。在给药的第1天和第7天,测量6小时内的血压、肾脏血流动力学、尿电解质和心房利钠肽排泄量,以及肾素-血管紧张素系统的几个组成部分。与安慰剂和福辛普利/氢氯噻嗪复方制剂相比,奥美普利拉可使血浆血管紧张素II水平显著降低(与安慰剂相比,P<0.001;与福辛普利/氢氯噻嗪相比,P<0.05),并使尿心房利钠肽排泄量增加(P<0.01)。这些激素效应与血压显著下降(P<0.01)和明显的肾血管舒张有关,但肾小球滤过率无显著变化。福辛普利/氢氯噻嗪显著增加尿钠排泄量(P<0.001)。福辛普利/氢氯噻嗪的急性利钠反应显著大于奥美普利拉(P<0.01)。然而,在1周内,两种剂量的奥美普利拉所诱导的累积钠排泄量(与安慰剂相比,P<0.01)至少与福辛普利/氢氯噻嗪剂量所诱导的累积钠排泄量相当(与福辛普利/氢氯噻嗪相比,P=无显著性差异)。总之,本研究在正常受试者中的结果表明,奥美普利拉具有良好的肾脏血流动力学效应。奥美普利拉将强效ACE抑制与持续利钠作用相结合,这解释了其有充分文献记载的强效降压疗效。