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Pharmacology: Pharmacodynamics: Carvedilol is a potent antihypertensive agent with a dual mechanism of action. It possesses both B-adrenergic receptor blocking activity and alpha-adrenergic antagonistic activity. Carvedilol is non-selective beta adrenoreceptor antagonist at clinically relevant doses. Alpha-blocking activity of carvedilol is thought to be the predominant mechanism of validation. However, there is no reflex tachycardia because of associated-blockade. At higher concentration it also exerts calcium channel antagonist property. The calcium channel blocking activity of carvedilol is responsible for increasing the blood flow in some regional vascular beds.
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 concentration occur 1 to 2hours after an oral dose. It has 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.
