Regular ArticleComparative Developmental Toxicity and Metabolism of Nitrazepam in Rats and Mice
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1.06 - Comprehensive Gut Microbiota and Drug Processing
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2022, Biochemistry of Drug Metabolizing Enzymes: Trends and ChallengesMechanisms of gastrointestinal microflora on drug metabolism in clinical practice
2019, Saudi Pharmaceutical JournalCitation Excerpt :The involvement of gut microbiota in the metabolism of nitrazepam, a hypnotic, sedative, anticonvulsant and anxiolytic drug, into its teratogenicity was demonstrated in experiments with rats (Takeno and Sakai, 1991). Nitrazepam is transformed to 7-aminonitrazepam by nitroreductase from intestinal microbiota, followed by acetylation to 7-acetylaminonitrazepam in the liver (Takeno et al., 1993). Although reductive metabolism in rat liver is less potent than in gastrointestinal tract (Rafii, 1997), two metabolites are both teratogenic.
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2018, Pharmacological ResearchIdentification of enzymes responsible for nitrazepam metabolism and toxicity in human
2017, Biochemical PharmacologyCitation Excerpt :In humans, NZP is primarily metabolized to 7-amino nitrazepam (ANZP) by nitro-reductase(s) and subsequently to 7-acetylamino nitrazepam (AANZP) by N-acetyltransferase(s) (Fig. 1) [8]. In rodents, AANZP is hydrolyzed to ANZP in the liver, but it has not been determined whether this reaction occurs in humans [7]. Within 24 hours of an oral administration of 10 mg NZP in humans, urinary excretion of ANZP and AANZP represented 4.1% and 12.5% of the initial dose, respectively, [9].