Controlled-release carvedilol

A new once-daily controlled-release (CR) capsule formulation of the nonselective beta- and alpha(1)-adrenoceptor antagonist carvedilol is now available for use in the treatment of essential hypertension, heart failure (HF), and left ventricular dysfunction following myocardial infarction (MI). Carvedilol CR had equivalent beta(1)-adrenoceptor antagonist activity to carvedilol immediate release (IR) in patients with hypertension in terms of the reduction in exercise-induced heart rate. In addition, corresponding dosages of the two formulations demonstrated pharmacokinetic bioequivalence. 24-Hour DBP (primary endpoint) and SBP (measured by ambulatory blood pressure monitoring [ABPM]) were reduced to a significantly greater extent with carvedilol CR 20, 40, or 80 mg once daily than with placebo in patients with hypertension in a well designed trial. Carvedilol CR 40 or 80 mg also significantly reduced trough DBP and SBP as measured by both ABPM and office sphygmomanometry in this patient population. Preliminary results of a randomized comparison did not find any difference in medication compliance rates between once-daily carvedilol CR and twice-daily carvedilol IR administered over 5 months in patients with HF, which was in part due to a higher than anticipated compliance in the carvedilol IR cohort. Carvedilol CR was generally well tolerated in patients with hypertension, mild to severe HF, or left ventricular dysfunction following MI. Headache was the most commonly reported adverse event associated with carvedilol CR in patients with hypertension, but generally was not reported at a higher incidence in carvedilol CR than placebo recipients.