Profile of carvedilol controlled-release: a new once-daily formulation of carvedilol

Carvedilol is a third-generation beta(1)- and beta(2)-blocker that also possesses alpha(1)-adrenergic-blocking properties. This compound has: i) shown superior efficacy to certain other beta-blockers in heart failure, ii) can improve myocardial function (e.g., in myocardial infarction) and iii) is the only beta-blocker shown to significantly reduce mortality and morbidity (such as reinfarction and development of heart failure) in postmyocardial infarction patients with left ventricular dysfunction (LVD). The currently available preparation of carvedilol needs to be taken twice daily; however, studies have shown that the need for twice-daily dosing may decrease adherence. A once-daily formulation of carvedilol (controlled release) is expected to become available in 2007. The pharmacokinetic and pharmacodynamic properties of the new formulation are equivalent to the twice-daily formulation. A number of investigations have demonstrated equivalence between the twice-daily and once-daily formulations; thus, carvedilol controlled-release is expected to provide not only the same life-prolonging benefits of twice-daily carvedilol, but also the convenience of once-daily dosing.