Romankiewicz J A, Brogden R N, Heel R C, Speight T M, Avery G S
Drugs. 1983 Jan;25(1):6-40. doi: 10.2165/00003495-198325010-00002.
Captopril is the first angiotensin-converting enzyme inhibitor for oral administration. In combination with continued digitalis and diuretic therapy it has been demonstrated to be effective in the management of severe heart failure refractory to optimal digitalis, diuretic and, in many patients, vasodilator treatment. Most studies to date have been open trials of several weeks or months duration, but a number of patients have received continued treatment, with sustained benefit, for up to 1 year or more. A placebo-controlled trial in a limited number of patients with less severe heart failure has confirmed the results of open trials. Captopril administration improves cardiac performance as a result of a reduction in systemic vascular resistance (afterload) and the various determinants of left ventricular filling pressure (preload). Improvements in exercise tolerance and functional classification, with associated reduction of clinical symptomatology, occur with simultaneous decreases in myocardial oxygen consumption. At present, captopril is worthy of a trial in patients refractory to more traditional medical management. Whether it should be considered a 'first-line' agent after failure of optimal digitalis and diuretic therapy, and before instituting other vasodilator therapy, is less clear. In patients with severe or resistant heart failure, a response to captopril is usually accompanied by a general improvement in the quality of life. The effect of captopril treatment on 1- and 2-year survival rates in patients with severe heart failure appears similar to that reported for other vasodilators. Most patients tolerate captopril treatment well, but hypotension, reduced renal function, skin rash, dysgeusia, and neutropenia have been reported.
卡托普利是首个口服的血管紧张素转换酶抑制剂。与持续使用洋地黄和利尿剂治疗联合应用时,已证明其在治疗对最佳洋地黄、利尿剂以及在许多患者中对血管扩张剂治疗无效的严重心力衰竭方面有效。迄今为止,大多数研究都是为期数周或数月 的开放性试验,但一些患者接受了长达1年或更长时间的持续治疗,并持续受益。一项针对少数轻度心力衰竭患者的安慰剂对照试验证实了开放性试验的结果。服用卡托普利可改善心脏功能,这是由于全身血管阻力(后负荷)以及左心室充盈压(前负荷)的各种决定因素降低所致。运动耐量和功能分级得到改善,同时临床症状减轻,心肌耗氧量也随之降低。目前,卡托普利值得在对更传统药物治疗无效的患者中进行试验。在最佳洋地黄和利尿剂治疗失败后,以及在开始使用其他血管扩张剂治疗之前,它是否应被视为“一线”药物尚不清楚。在重度或难治性心力衰竭患者中,对卡托普利的反应通常伴随着生活质量的总体改善。卡托普利治疗对重度心力衰竭患者1年和2年生存率的影响似乎与其他血管扩张剂的报告相似。大多数患者对卡托普利治疗耐受性良好,但有低血压、肾功能减退、皮疹、味觉障碍和中性粒细胞减少的报道。