Cardekim Mechanism of Action

Combined Alpha and Beta Blocker.
Pharmacology: Carvedilol is a vasodilatory non-selective beta-blocker which reduces the peripheral vascular resistance by selective alpha₁-receptor blockade and suppresses the renin-angiotensin system through non-selective beta-blockade. Plasma renin activity is reduced and fluid retention is rare.
Carvedilol has no intrinsic sympathomimetic activity (ISA). Like propranolol, it has membrane stabilizing properties. Carvedilol is a racemate of two stereoisomers. Both enantiomers were found to have alpha-adrenergic blocking activity in animal models. Non-selective beta₁- and beta₂-adrenoceptor blockade is attributed mainly to the S(-) enantiomer. The antioxidant properties of carvedilol and its metabolites have been demonstrated in in vitro and in vivo animal studies and in vitro in a number of human cell types.
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 1-2 hours after administration. It has high lipid solubility. Carvedilol is more than 98% bound to plasma proteins. It is extensively metabolized in the liver; the metabolites being excreted mainly in the bile. The elimination half-life is about 6-10 hours. Carvedilol has been shown to accumulate in breast milk in animals.