Metabolism of diazepam in dogs: Transformation to oxazepam

On administration to dogs, diazepam is demethylated at the 1-nitrogen and through a novel metabolic pathway is hydroxylated at the 3-carbon of the seven-membered ring. The unhydroxylated demethylation product is excreted in the free form and the 3-hydroxy derivatives are excreted as the glucuronides...

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Veröffentlicht in:Archives of biochemistry and biophysics 1965-08, Vol.111 (2), p.376-380
Hauptverfasser: Ruelius, Hans W., Lee, Jean M., Alburn, Harvey E.
Format: Artikel
Sprache:eng
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Zusammenfassung:On administration to dogs, diazepam is demethylated at the 1-nitrogen and through a novel metabolic pathway is hydroxylated at the 3-carbon of the seven-membered ring. The unhydroxylated demethylation product is excreted in the free form and the 3-hydroxy derivatives are excreted as the glucuronides. No unchanged drug can be detected in the urine. The major metabolite is oxazepam glucuronide.
ISSN:0003-9861
1096-0384
DOI:10.1016/0003-9861(65)90199-2