METABOLISM OF CARVEDILOL IN MAN

The metabolism of carvedilol was investigated in plasma and urine of 3 healthy male volunteers after administration of 50 mg of [C-14]-label led drug. Rapid and extensive biotransformation occurred. After 1.5 h 9% of total radioactivity in plasma consisted of unchanged drug, 22% o f carvedilol-glucuronide and another 20% of oxidative cleavage product s of the beta-blocking side chain. Urinary excretion of radioactivity amounted to 16% of which 2% represented unchanged drug, 32% carvedilol -glucuronide and about 25% side chain oxidation products. Ring-hydroxy lated metabolites of carvedilol accounted for 18% of the radioactive c ompounds in the urine.