Carvida 6.25 Mechanism of Action

Carvedilol is a nonselective beta-adrenergic blocking agent with alpha-1 blocking activity. It is a potent antihypertensive agent. It has the advantage that it is not associated with an increase of the heart rate as observed with other vasodilators. Carvedilol is used to control high blood pressure and to treat patients with mild or moderate congestive heart failure.
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 occur 1 to 2 hours after an oral dose. It has high lipid solubility. Carvedilol is more than 98% bound to plasma proteins. It is extensively metabolized in the liver, primarily by the cytochrome P450 isoenzymes CYP2D6 and CYP2C9, and the metabolites are excreted mainly in the bile. The elimination half-life is about 6 to 10 hours. Carvedilol has been shown to accumulate in breast milk in animals.