A. Fitton et Rn. Brogden, PIMOBENDAN - A REVIEW OF ITS PHARMACOLOGY AND THERAPEUTIC POTENTIAL IN CONGESTIVE-HEART-FAILURE, Drugs & aging, 4(5), 1994, pp. 417-441
Pimobendan is a novel cardiotonic vasodilator (inodilator) which deriv
es its inotropic activity from a combination of phosphodiesterase III
inhibition and sensitisation of myocardial contractile proteins to cal
cium. The acute haemodynamic benefits of pimobendan (2.5 to 10mg orall
y; 5 to 10mg intravenously) seen in patients maintained on conventiona
l diuretic, digitalis and vasodilator therapy for chronic heart failur
e (increases in cardiac output nod stroke volume, and reductions in le
ft ventricular preload and afterload) persisted on short term (1 month
) therapy, and showed only limited evidence of attenuation on longer t
erm (6 months) oral therapy with pimobendan 2.5 or 5mg twice daily. Ad
junctive therapy on with pimobendan 1.25 to 5mg twice daily for period
s of 3 to 6 months improved exercise tolerance on symptom-limited exer
cise 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 indicat
ions suggest that it is largely devoid of the proarrhythmic effects of
classical phosphodiesterase III inhibitors. Although information rega
rding the long term effects of pimobendan on mortality is currently la
cking, the drug nevertheless shows potential benefit as an adjunctive
therapy in patients with chronic heart failure.