Variations in demethylation of N-methylnaltrexone in mice, rats, dogs, and humans
| Autor: | A. N. Kotake, L. I. Goldberg, E. Burton, S. K. Kuwahara, C. E. Mccoy |
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| Rok vydání: | 1989 |
| Předmět: |
Male
Narcotic Antagonists Health Toxicology and Mutagenesis Urine Pharmacology Toxicology Biochemistry Naltrexone Feces Mice chemistry.chemical_compound Dogs Species Specificity Pharmacokinetics medicine Animals Humans Ammonium Aged Demethylation Narcotic antagonist General Medicine Metabolism Middle Aged Methylnaltrexone Rats Quaternary Ammonium Compounds Kinetics chemistry Female medicine.drug |
| Zdroj: | Xenobiotica. 19:1247-1254 |
| ISSN: | 1366-5928 0049-8254 |
| DOI: | 10.3109/00498258909043176 |
| Popis: | 1. Rats and mice have a greater capacity than dogs or humans to N-demethylate the quaternary ammonium compound, N-methylnaltrexone. 2. In dogs, following the i.v. administration of N-[14C-methyl]methylnaltrexone, 50% of the radioactivity was excreted in the urine and an additional 30% in the faeces within 120 h. 3. In humans following the i.v. administration of 14C-N-methylnaltrexone, 40-60% of the radioactivity was excreted in the urine within the first 24 h. The plasma radioactivity-time curves indicated a biphasic decay and a short distribution phase between 6 and 9 min. with a longer elimination phase between 238 and 1320 min. |
| Databáze: | OpenAIRE |
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