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HUMAN METABOLISM OF naltrexone NALTREXONE Monroe E .
Brine Research Triangle Institute Research Triangle Park, naltrexone NC 27709 Mario Perez-Reyes Department of Psychiatry School of Medicine University of North Carolina Chapel Hill, NC 27514 Naltrexone: Research Monograph 28 Ft .
National naltrexone Institute on Drug Abuse, 1980 Current Status of Preclinical Research on Pharmacokinetics, and Metabolism of Naltrexone Considerable species-dependent differences exist in the quantitative pattern of the metabolism of naltrexone .
The metabolic pathways of naltrexone in different naltrexone dosages low dose naltrexone hashimoto’s and weight loss naltrexone dosage oral vivitrol species were: (a) 6-keto group reduction to epimeric 6a- or 6ß-naltrexols, (b) glucuronide conjugation of naltrexone or naltrexols, (c) N-dealkylation to nor-compounds, (d) 3-O-methylation and (e) 2-hydroxylation .
Substantially greater quantities of 6ßnaltrexol and/or naltrexone its conjugates were excreted in urine of man, monkey, guinea pig and rabbit after naltrexone administration, and very small quantities were excreted in mouse, rat and dog .
Chicken produced predominantly the 6a-naltrexol and the dog excreted mainly the 3-naltrexone glucuronide, with naltrexone very small quantities of 6a- or 6ß-naltrexols .
Stereoselective metabolism of naltrexone naltrexone to naltrexols is mediated by two different liver enzymes, and the formation of 2-hydroxy-3-O-methyl naltrexone or the corresponding 6ß-naltrexol is mediated by catechol-O-methyl transferase .
No significant differences were observed in the extent of plasma-protein binding (20-26%) of naltrexone in various species, and the low extent of binding indicated a large apparent volume of distribution for naltrexone naltrexone in different species and man .

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