Pharmacology: Pharmacokinetics: Carvedilol is well-absorbed from the gastrointestinal tract but is subject to considerable first-pass metabolism in the liver; the absolute bioavailability is about 25%. Peak plasma concentrations (Cmax) occur 1-2 hrs after an oral dose. It has high lipid solubility. Carvedilol is >98% bound to plasma proteins. It is extensively metabolized in the liver, primarily by the cytochrome P450 (CYP450) isoenzymes CYP2D6 and CYP2C9, and the metabolites are excreted mainly in the bile. The elimination half-life (t½) is about 6-10 hrs. Carvedilol has been shown to accumulate in breast milk in animals.