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 [14C]-labelled drug. Rapid and extensive biotransformation occurred. After 1.5 h 9% of total radioactivity in plasma consisted of unchanged drug, 22% of carvedilol-glucuronide and another 20% of oxidative cleavage products 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-hydroxylated metabolites of carvedilol accounted for 18% of the radioactive compounds in the urine.
Neugebauer
G
G
Department of Clinical Pharmacology, Boehringer Mannheim GmbH, Germany.
Neubert
P
P
D000959:Antihypertensive Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D001711:Biotransformation; D002227:Carbazoles / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D000077261:Carvedilol; D002855:Chromatography, Thin Layer; D005243:Feces / Q000737:chemistry; D005965:Glucuronates / Q000378:metabolism; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D010084:Oxidation-Reduction; D011412:Propanolamines / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine
D000959:Antihypertensive Agents; D002227:Carbazoles; D005965:Glucuronates; D011412:Propanolamines; D000077261:Carvedilol