Pharmacokinetic Profile of Controlled-Release Carvedilol in Patients with Left Ventricular Dysfunction Associated with Chronic Heart Failure or After Myocardial Infarction

Safety and Tolerability of Once-Daily Controlled-Release Carvedilol 10-80mg in Japanese Patients With Chronic Heart Failure

“…34 The period of use, however, was limited to 1 day for each of the 4 dose levels. In the present study of the pharmacokinetics of S(-)-carvedilol after repetitive administration of daily doses of 40 and 80 mg of carvedilol CR, exposures observed in the present Japanese patients were similar to those reported in a study of US chronic HF patients, 26 and 37% of patients in CR group completed the dose of 80 mg/day of carvedilol CR.…”

Controlled-release carvedilol in the management of systemic hypertension and myocardial dysfunction

“…Carvedilol CR is generally well tolerated across its therapeutic indications Packer et al 2006;Weber et al 2006a). Adverse events reported in clinical trials were consistent with the mechanism of action of carvedilol and the health status of the patient population under evaluation.…”

“…However, the median time to maximum observed plasma concentration for carvedilol CR lagged 3 hours behind that of carvedilol IR, in accordance with the prolonged-release characteristics expected in a once-daily formulation. The pharmacodynamics of carvedilol CR were Controlled-release carvedilol in cardiovascular disease dose proportional over the dose range tested (10 mg to 80 mg) (Packer et al 2006). Notably, the bioavailability of carvedilol CR is 85% that of carvedilol IR .…”

“…The pharmacokinetic and pharmacodynamic bioequivalence of carvedilol CR and IR was established through 2 clinical studies Packer et al 2006). In a double-blind, parallel-group, crossover study, 122 patients with essential hypertension were randomized to receive either low-dose carvedilol CR (20 mg daily) or carvedilol IR (6.25 mg twice daily), high-dose carvedilol CR (80 mg once daily [initiated at 20 mg once daily and titrated to 40 mg and 80 mg once daily in 1-week intervals]) or carvedilol IR (25 mg twice daily [initiated at 6.25 mg twice daily and titrated to 12.5 mg and 25 mg twice daily in 1-week intervals]), or placebo .…”

“…In a separate 4-week study, patients with either mild to severe heart failure or with asymptomatic post-MI LVD were treated with the carvedilol IR (3.125, 6.25, 12.5, or 25 mg twice daily) for the fi rst 2 weeks and then switched to carvedilol CR (10, 20, 40, or 80 mg once daily) for 2 weeks (Packer et al 2006). Trough plasma concentration, maximum plasma concentration, and area under the curve was measured for both R(+) and S(-) enantiomers after carvedilol IR and CR treatment periods.…”