Abstracto

The stereoselective metabolism of carvingilol in liver microsomes is predicted to be cleared by the liver

Carole Taylor

Carvedilol is a commonly used beta-blocker in the treatment of hypertension and heart failure. Its metabolism in the liver has been studied extensively, and it has been shown that carvedilol is predominantly metabolized by cytochrome P450 enzymes, primarily CYP2D6 and CYP2C9. The metabolism of carvedilol is stereoselective, with the enantiomer being metabolized more rapidly than the R(+)-enantiomer. Liver microsomes, which are subcellular fractions of liver cells, have been used to study the metabolism of carvedilol. In vitro studies have shown that the metabolism of carvedilol in liver microsomes is stereoselective, with the enantiomer being metabolized more rapidly than the R(+)-enantiomer. This stereoselective metabolism is due to the fact that the active site of the CYP2D6 enzyme, which is responsible for the metabolism of carvedilol, has a specific orientation that favors the metabolism of the enantiomer. The clearance of carvedilol from the body is primarily through hepatic metabolism, with approximately 60-70% of the drug being metabolized in the liver. The stereoselective metabolism of carvedilol in liver microsomes indicates that the liver is the major organ responsible for the metabolism of carvedilol, and that the clearance of the drug is primarily through hepatic metabolism.