PIMOBENDAN - A REVIEW OF ITS PHARMACOLOGY AND THERAPEUTIC POTENTIAL IN CONGESTIVE-HEART-FAILURE

被引:30
作者
FITTON, A
BROGDEN, RN
机构
[1] Adis International Limited, Auckland, 41 Centorian Drive, Mairangi Bay
关键词
D O I
10.2165/00002512-199404050-00007
中图分类号
R592 [老年病学]; C [社会科学总论];
学科分类号
03 ; 0303 ; 100203 ;
摘要
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 nod 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 on 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.
引用
收藏
页码:417 / 441
页数:25
相关论文
共 133 条
[1]  
ABE Y, 1992, J PHARMACOL EXP THER, V261, P1087
[2]   SIMULTANEOUS DETERMINATION OF THE ENANTIOMERS OF PIMOBENDAN AND ITS MAIN METABOLITE IN RAT PLASMA BY HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY [J].
ASAKURA, M ;
NAGAKURA, A ;
TARUI, S ;
MATSUMURA, R .
JOURNAL OF CHROMATOGRAPHY-BIOMEDICAL APPLICATIONS, 1993, 614 (01) :135-141
[3]   DISPARATE INOTROPIC AND LUSITROPIC RESPONSES TO PIMOBENDAN IN CONSCIOUS DOGS WITH TACHYCARDIA-INDUCED HEART-FAILURE [J].
ASANOI, H ;
ISHIZAKA, S ;
KAMEYAMA, T ;
ISHISE, H ;
SASAYAMA, S .
JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 1994, 23 (02) :268-274
[4]  
ASSMANN I, 1991, Z KARDIOL, V80, P687
[5]  
BASTIDA E, 1986, THROMBOSIS RES S6, V42, P145
[6]   CARDIOVASCULAR PROFILE OF UDCG-115 BS-PIMOBENDANE AND REVERSIBILITY OF CATECHOLAMINE SUBSENSITIVITY IN SEVERE CONGESTIVE HEART-FAILURE SECONDARY TO IDIOPATHIC DILATED CARDIOMYOPATHY [J].
BAUMANN, G ;
NINGEL, K ;
PERMANETTER, B .
JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 1989, 13 (05) :730-738
[7]  
BERGER C, 1985, ARZNEIMITTEL-FORSCH, V35-2, P1668
[8]  
BERGLERKLEIN J, 1992, Z KARDIOL, V81, P546
[9]  
BITTERMAN H, 1988, ARZNEIMITTEL-FORSCH, V38-2, P1389
[10]   EXERCISE CAPACITY AND QUALITY OF LIFE IN THE TREATMENT OF HEART-FAILURE [J].
BLACKWOOD, R ;
MAYOU, RA ;
GARNHAM, JC ;
ARMSTRONG, C ;
BRYANT, B .
CLINICAL PHARMACOLOGY & THERAPEUTICS, 1990, 48 (03) :325-332