A large, multicenter, double-blind, placebo-controlled clinical trial of carvedilol, a vasodilating β-blocker with antioxidant activity, was conducted in patients with mild-to-severe congestive heart failure (CHF). In these studies, carvedilol has been associated with a 65% reduction in mortality, and a significant reduction in hospitalization. Carvedilol is a multiple-action drug that has the capacity to suppress a variety of neurohormonal systems. The pharmacological actions of carvedilol have been studied in detail. The major pharmacological actions of carvedilol are: carvedilol is a potent competitive antagonist of both β1 and β2 adrenoceptors, with no intrinsic sympathomimetic activity; carvedilol is a potent antagonist of α1 adrenoceptors that is responsible for the vasodilating effects of the drug; and carvedilol is an extremely potent antioxidant as a result of its carbazole moiety. The antioxidant activity of carvedilol may be of particular importance in CHF inasmuch as oxygen radical stress has been shown to occur in CHF and may be responsible for producing damage to the myocardium and inducing apoptosis. The ability of carvedilol to produce cardioprotection to a degree that is greater than that achieved with β-blockers have been attributed to the antioxidant effects of the drug. In addition to the antioxidant effects of carvedilol that likely contribute to the cardioprotective effects of the drug, carvedilol has also been shown to produce a number of other actions that may be secondary to the antioxidant effects of the drug. Clinical and hemodynamic benefits produced by carvedilol have been demonstrated in patients with mild, moderate, and severe CHF and in patients with ischemic or nonischemic origins of heart failure. Moreover, carvedilol produced dosedependent reductions in morbidity and mortality.