Metabolism and disposition of naltrexone in man after oral and intravenous administration.

摘要: The metabolism and elimination of [15, 16,-3H2]naltrexone was studied in man after oral intravenous administration. same metabolites, although varying proportions, were observed both cases; conjugated naltrexone unconjugated 6 beta-naltrexol the major metabolites plasma, urine, feces. 2-Hydroxy-3-O-methyl-6 found minor quantities. Naltrexone almost completely absorbed After administration naltrexone, about 60% dose recovered urine 48 72 hr, respectively. route did not significantly affect urinary clearance values obtained for or beta-naltrexol. affected terminal plasma half-life (2.7 iv; 8.9 oral), but had little effect on comparable total drug, Combined gas chromatography-mass spectrometry used to validate presence beta-naltrexol, 2-hydroxy-3-O-methyl-6 urine.