On the basis of pathophysiologic mechanisms, the medical therapy of today for chronic heart failure is reviewed. The advantages and disadvantages of the vasodilator drugs and the inotropic drugs are presented. Finally, the therapeutic value of the inodilator drugs, which combine the central myocardial effects of positive inotropic agents with those of peripheral vasodilators, is discussed. In particular, the orally available dopaminergic agents, such as ibopamine, which interact with beta-receptors in the heart (mediating a positive inotropic effect) as well as with dopaminergic receptors in the peripheral vessels (mediating a systemic vasodilator effect) and in the kidneys (potentiating the natriuretic effect of diuresis), seem to be an advancement in the modern medical therapy of chronic heart failure. Data are shown during long-term treatment with ibopamine, in which the sustained clinical benefit in heart failure was not diminished, despite a decrease of the adrenergic receptors in blood cells. Dopamine plasma concentration was permanently normalized during long-term treatment. The discrepancy between clinical improvement and the measured adrenergic downregulation may be due to the interference of the inodilator with neurohormonal systems at multiple sites and is probably independent of receptor activation. It is suggested that the biosynthesis of noradrenaline is improved by increasing intracellular dopamine transport.