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Carvedilol is a β1- and β2-adrenergic receptor antagonist with additional vasodilatory α1-blocking properties. Carvedilol was shown to be more efficacious than a traditional β-blocker for treating heart failure and improving myocardial function. Carvedilol is the only agent in its class to have been demonstrated to significantly reduce mortality and morbidity in post-myocardial-infarction patients with left ventricular dysfunction. Moreover, carvedilol does not exhibit the carbohydrate and lipid disturbances observed with other β-blockers. Originally available as a twice-daily formulation, a controlled-release, once-daily formulation of carvedilol is now available, which has equivalent efficacy and safety, as demonstrated by numerous studies. The convenience of once-daily dosing is expected to contribute to patient adherence, thereby potentially improving long-term clinical outcomes.