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Ethanol Does Not Alter the Pharmacokinetic Profile of the Controlled-release Formulation of Carvedilol

From the Department of Clinical Pharmacology and Discovery Medicine (Dr Henderson, Dr Danoff), Department of Clinical Pharmacokinetics, Modeling, and Simulation (Dr Tenero), Department of Clinical Sciences and Study Operations (Ms Campanile), and Department of Clinical Pharmacology Statistics and Programming (Ms Campanile), GlaxoSmithKline, King of Prussia, Pennsylvania.

The concomitant ingestion of alcohol may alter the release of a drug from a modified-release dosage form, posing a potential risk to patients. In a randomized, open-label, 4-period cross-over study, the pharmacokinetic profiles of R(+) and S(-) carvedilol were compared after a single oral dose of carvedilol controlled-release formulation (administered following a standard meal) was given alone or concomitantly with ethanol. Thirty-nine healthy subjects participated in this study. Following coadministration of carvedilol controlled-release 40 mg with ethanol (approximately 38 g), ethanol ingestion 2 hours before or 2 hours after carvedilol controlled-release administration, area under the curve for the R(+) and S(-) carvedilol enantiomers was similar compared with carvedilol controlled-release given alone. Carvedilol exposure was not affected by the concomitant administration of ethanol and carvedilol controlled-release. Maximum plasma concentrations for the R(+) and S(-) carvedilol enantiomers were similar except when ethanol was ingested 2 hours after carvedilol controlled-release administration, where there was a modest decrease in maximum plasma concentration for R(+) and S(-) carvedilol (16% and 17%, respectively). Carvedilol controlled-release given alone or concomitantly with ethanol ingestion was generally well tolerated, and no serious or severe adverse events were reported. Ethanol did not alter the pharmacokinetic profile of carvedilol controlled-release.

Key Words: Carvedilol • controlled-release • ethanol • pharmacokinetics

Address for correspondence: Linda S. Henderson, PhD, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406.

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