Elsner D, Müntze A, Kromer E P, Riegger G A
Klinik und Poliklinik für Innere Medizin II, University of Regensburg, Germany.
Am J Cardiol. 1992 Aug 15;70(4):494-8. doi: 10.1016/0002-9149(92)91196-b.
Candoxatril is a novel, orally active inhibitor of neutral endopeptidase EC 3.4.24.11, the enzyme that degrades atrial natriuretic peptide (ANP). The acute and chronic (10 days treatment) hemodynamic and hormonal effects of candoxatril (150 mg twice daily) in 12 patients with moderately severe congestive heart failure were investigated in a randomized, placebo-controlled, double-blind study. On study day 1, candoxatril acutely increased plasma ANP levels, suppressed aldosterone and decreased right atrial and pulmonary capillary wedge pressures. After 10 days of treatment, basal ANP was increased and basal aldosterone was decreased. Body weight was reduced, most likely reflecting chronic natriuretic or diuretic effects, or both, and there was a trend toward increased cardiac index and reduced preload values. On study day 10, the acute effects of candoxatril were similar to those on day 1 (i.e., ANP was further increased, aldosterone was suppressed, and right and left ventricular filling pressures were decreased). Thus, candoxatril may offer a new and effective therapeutic approach in the treatment of heart failure.
坎多沙坦酯是一种新型的、口服有效的中性内肽酶（EC 3.4.24.11）抑制剂，该酶可降解心房利钠肽（ANP）。在一项随机、安慰剂对照、双盲研究中，对12例中度严重充血性心力衰竭患者使用坎多沙坦酯（每日两次，每次150毫克）进行了急性和慢性（治疗10天）血流动力学及激素效应的研究。在研究第1天，坎多沙坦酯可使血浆ANP水平急性升高，抑制醛固酮，并降低右心房和肺毛细血管楔压。治疗10天后，基础ANP升高，基础醛固酮降低。体重减轻，很可能反映了慢性利钠或利尿作用，或两者兼有，且有心脏指数增加和前负荷值降低的趋势。在研究第10天，坎多沙坦酯的急性效应与第1天相似（即ANP进一步升高，醛固酮被抑制，左右心室充盈压降低）。因此，坎多沙坦酯可能为心力衰竭的治疗提供一种新的有效治疗方法。
