Fitton A, Brogden R N
Adis International Limited, Auckland, New Zealand.
Drugs Aging. 1994 May;4(5):417-41. doi: 10.2165/00002512-199404050-00007.
Pimobendan is a novel cardiotonic vasodilator (inodilator) which derives its inotropic activity from a combination of phosphodiesterase III inhibition and sensitisation of myocardial contractile proteins to calcium. The acute haemodynamic benefits of pimobendan (2.5 to 10mg orally; 5 to 10mg intravenously) seen in patients maintained on conventional diuretic, digitalis and vasodilator therapy for chronic heart failure (increases in cardiac output and stroke volume, and reductions in left ventricular preload and afterload) persisted on short term (1 month) therapy, and showed only limited evidence of attenuation on longer term (6 months) oral therapy with pimobendan 2.5 or 5mg twice daily. Adjunctive therapy with pimobendan 1.25 to 5mg twice daily for periods of 3 to 6 months improved exercise tolerance on symptom-limited exercise testing, New York Heart Association (NYHA) functional class, and quality of life, and additionally reduced the need for hospitalisation in patients with moderate to severe chronic heart failure. Pimobendan appears to be well tolerated at therapeutic doses (1.25 to 5mg twice daily) in patients with chronic heart failure, and preliminary indications suggest that it is largely devoid of the proarrhythmic effects of classical phosphodiesterase III inhibitors. Although information regarding the long term effects of pimobendan on mortality is currently lacking, the drug nevertheless shows potential benefit as an adjunctive therapy in patients with chronic heart failure.
匹莫苯丹是一种新型强心血管扩张剂(强心扩血管药),其正性肌力活性源于磷酸二酯酶III抑制作用与心肌收缩蛋白对钙的敏感性增加的联合效应。在接受传统利尿剂、洋地黄和血管扩张剂治疗慢性心力衰竭的患者中,口服匹莫苯丹(2.5至10mg;静脉注射5至10mg)所产生的急性血流动力学益处(心输出量和每搏输出量增加,左心室前负荷和后负荷降低)在短期(1个月)治疗中持续存在,并且在长期(6个月)口服2.5或5mg匹莫苯丹、每日两次的治疗中仅显示出有限的衰减迹象。每日两次、服用1.25至5mg匹莫苯丹、为期3至6个月的辅助治疗改善了症状限制性运动试验中的运动耐量、纽约心脏协会(NYHA)心功能分级和生活质量,此外还减少了中重度慢性心力衰竭患者的住院需求。在慢性心力衰竭患者中,匹莫苯丹在治疗剂量(每日两次、1.25至5mg)下似乎耐受性良好,初步迹象表明,它在很大程度上没有经典磷酸二酯酶III抑制剂的促心律失常作用。尽管目前缺乏关于匹莫苯丹对死亡率长期影响的信息,但该药物作为慢性心力衰竭患者的辅助治疗仍显示出潜在益处。