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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
5
|
| pubmed:dateCreated |
1977-1-3
|
| pubmed:abstractText |
A gas-chromatographic method has been developed for the simultaneous determination of naltrexone, alpha-naltrexol, and beta-naltrexol as trimethylsiyl derivatives. Analysis of urine from rabbit, monkey, and rat demonstrated that, like man, these species reduce naltrexone primarily to beta-naltrexol. In naltrexone maintenance patients receiving 125 mg po three times per week, an average of 37% of the dose was recovered in 48-hr urine as free naltrexone (0.8%), conjugated naltrexone (7.6%), free beta-naltrexol (16.8%), and conjugated beta-naltrexol (11.8%). Thirty-four percent of the dose appeared in 0-24 hr and 3% during 24-48 hr. The ratio of beta-naltrexol to naltrexone rose from 2 at 0-4 hr to 34-48 hr. Monkeys receiving a daily dose of 12 mg/kg po, chronically, excreted very little free beta-naltrexol and exhibited an apparent sex-related difference in excretion patterns, with females excreting more than twice as much total base as males. Rabbits given a dose of 30 mg/kg ip for 4 days excreted conjugated naltrexone as the predominant urinary metabolite, accounting for 80% of total base recovered in 24 hr. In rats receiving 100 mg/kg po, less than 1% of the administered dose could be accounted for in the 24-hr urine, indicating that although the beta-naltrexol is produced as a urinary metabolite, other means of disposition of the drug must exist. Thus, in man and the monkey, beta-naltrexol is the predominant and persistent urinary metabolite. Urinary excretion profiles of naltrexone differ greatly between species commonly examined for chronic toxicity studies.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:issn |
0090-9556
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
4
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
474-8
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:10147-Administration, Oral,
pubmed-meshheading:10147-Adult,
pubmed-meshheading:10147-Animals,
pubmed-meshheading:10147-Biotransformation,
pubmed-meshheading:10147-Chromatography, Gas,
pubmed-meshheading:10147-Chromatography, Thin Layer,
pubmed-meshheading:10147-Drug Administration Schedule,
pubmed-meshheading:10147-Female,
pubmed-meshheading:10147-Haplorhini,
pubmed-meshheading:10147-Humans,
pubmed-meshheading:10147-Injections, Intraperitoneal,
pubmed-meshheading:10147-Macaca mulatta,
pubmed-meshheading:10147-Male,
pubmed-meshheading:10147-Methods,
pubmed-meshheading:10147-Naloxone,
pubmed-meshheading:10147-Naltrexone,
pubmed-meshheading:10147-Rabbits,
pubmed-meshheading:10147-Rats,
pubmed-meshheading:10147-Sex Factors,
pubmed-meshheading:10147-Species Specificity
|
| pubmed:articleTitle |
The urinary excretion profiles of naltrexone in man, monkey, rabbit, and rat.
|
| pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, Non-P.H.S.
|