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Drug Metab. Dispos. · Jul 1981
Comparative StudyQuantitative determination of the urinary excretion of ketobemidone and four of its metabolites after intravenous and oral administration in man.
- U Bondesson, P Hartvig, and B Danielsson.
- Drug Metab. Dispos. 1981 Jul 1;9(4):376-80.
AbstractThe urinary excretion of ketobemidone and its metabolites has been quantified in man after intravenous and oral administration. The metabolism of ketobemidone was found to proceed via 4 metabolic pathways: N-demethylation, ring-hydroxylation, O-methylation, and conjugation. The metabolites were isolated and identified after hydrolysis of the corresponding conjugates. A mean total recovery of about 80% of the dose was found in urine as ketobemidone and metabolites after oral and iv administration, conjugated metabolites amounted to 34-68% of the dose. After iv administration the recovery of unchanged ketobemidone in urine was 13-24%, and after oral administration it was 3-10%. Norketobemidone constituted 10-37% of the dose irrespective of route of administration. 4'-Hydroxyketobemidone amounted to 3-12% of the dose. Neither ketobemidone N-oxide nor metabolites formed after reduction of ketobemidone could be detected in the urine. Less than 2% of the dose was found in feces after iv administration.
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