Identification of two major biliary metabolites of carvedilol in rats

1. After separate administration of R(+)-carvedilol, S(-)-carvedilol and (+/-)-14C-carvedilol to rats at an oral dose of 10 mg/kg, the metabolic pattern in the bile was studied using h.p.l.c. with radioactivity and u.v. monitoring. 2. Two major metabolites, M-1 and M-2, present in the bile, accounte...

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Bibliographic Details
Published inXenobiotica Vol. 20; no. 10; p. 1025
Main Authors Fujimaki, M, Hakusui, H
Format Journal Article
LanguageEnglish
Published England 1990
Subjects
Administration, Oral
Animals
Antihypertensive Agents - administration & dosage
Antihypertensive Agents - chemistry
Antihypertensive Agents - metabolism
Bile - metabolism
Carbazoles - administration & dosage
Carbazoles - chemistry
Carbazoles - metabolism
Carvedilol
Gas Chromatography-Mass Spectrometry
Magnetic Resonance Spectroscopy
Male
Propanolamines - administration & dosage
Propanolamines - chemistry
Propanolamines - metabolism
Rats
Rats, Inbred Strains
Stereoisomerism
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Summary:1. After separate administration of R(+)-carvedilol, S(-)-carvedilol and (+/-)-14C-carvedilol to rats at an oral dose of 10 mg/kg, the metabolic pattern in the bile was studied using h.p.l.c. with radioactivity and u.v. monitoring. 2. Two major metabolites, M-1 and M-2, present in the bile, accounted for 39% and 22% dose, respectively. 3. M-1 and M-2 were characterized as 1-hydroxycarvedilol O-glucuronide and 8-hydroxycarvedilol O-glucuronide, respectively, from FAB-mass spectrometry, 1H-n.m.r. and enzymic hydrolysis. 4. Oral administration of R(+)-carvedilol led to highly selective excretion of M-1 in bile whereas S(-)-carvedilol resulted predominantly in excretion of M-2 rather than M-1.
ISSN:0049-8254
DOI:10.3109/00498259009046823