Ribner H S, Sagar K B, Glasser S P, Hsieh A M, Dills C V, Larkin S, DeSilva J, Whalen J J
Department of Medicine, Northwestern University Medical School, Chicago, Illinois.
J Clin Pharmacol. 1990 Dec;30(12):1106-11. doi: 10.1002/j.1552-4604.1990.tb01853.x.
Benazepril hydrochloride (CGS 14824A) is an orally active, nonsulfhydryl compound that is transformed in vivo to a long-acting inhibitor of angiotensin-converting enzyme (ACE). Previous studies have shown benazepril to lower blood pressure in hypertensive patients and to confer acute hemodynamic benefits in patients with congestive heart failure (CHF). In the current multicenter investigation, 16 patients with chronic CHF due to left ventricular systolic dysfunction (ejection fraction less than 0.40 at rest) whose symptoms corresponded to New York Heart Association classes II to IV were given open-label benazepril once daily in ascending doses of 2 to 20 mg and followed biweekly for 12 weeks. Evaluation of the 15 subjects who completed the trial showed a progressive increase in treadmill exercise duration (from 7.65 +/- 3.64 [SD] minutes at baseline to 9.74 +/- 3.66 minutes at 12 weeks, P less than .001); augmentation of the mean left ventricular ejection fraction (from 0.266 +/- 0.133 at baseline to 0.292 +/- 0.136 at 12 weeks, P less than .025); relief of exertional dyspnea in 7 of the 15 patients (P less than .02); and improvement in global symptomatic status in 10 of the patients (P less than .01). These responses were accompanied by a reduction in serum ACE activity of 75% (from 27.2 +/- 10.5 IU/L at baseline to 6.7 +/- 1.9 IU/L at 12 weeks, P less than .001), which was independent of dose and duration of treatment. The magnitude of ACE inhibition did not correlate with changes in the efficacy variables. Aside from two instances of symptomatic hypotension (one of which was complicated by volume depletion), the drug was well tolerated.(ABSTRACT TRUNCATED AT 250 WORDS)
盐酸贝那普利（CGS 14824A）是一种口服活性非巯基化合物，在体内可转化为血管紧张素转换酶（ACE）的长效抑制剂。先前的研究表明，贝那普利可降低高血压患者的血压，并给充血性心力衰竭（CHF）患者带来急性血流动力学益处。在当前的多中心研究中，16例因左心室收缩功能障碍（静息射血分数小于0.40）导致慢性CHF且症状符合纽约心脏协会II至IV级的患者，接受了每日一次的开放标签贝那普利治疗，剂量从2毫克至20毫克逐渐递增，每两周随访一次，共12周。对完成试验的15名受试者的评估显示，跑步机运动持续时间逐渐增加（从基线时的7.65±3.64[标准差]分钟增加到12周时的9.74±3.66分钟，P<0.001）；平均左心室射血分数增加（从基线时的0.266±0.133增加到12周时的0.292±0.136，P<0.025）；15例患者中有7例劳力性呼吸困难缓解（P<0.02）；10例患者整体症状状态改善（P<0.01）。这些反应伴随着血清ACE活性降低75%（从基线时的27.2±10.5 IU/L降至12周时的6.7±1.9 IU/L，P<0.001），这与治疗剂量和持续时间无关。ACE抑制程度与疗效变量的变化无关。除了两例症状性低血压（其中一例伴有容量耗竭）外，该药物耐受性良好。（摘要截选至250字）
