Species differences in the disposition and metabolism of camazepam |
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Abstract: | 1. After i.v. injection of camazepam, plasma camazepan concn. declined biexponentially. The half-life of the elimination phase (t1/2, β) increased in the order: mice (0.73?h), rats (1.3?h), dogs (5.3?h).2. After oral dosing of camazepam, absorption was almost complete whereas systemic availability varied eight-fold, i.e., rats and mice (10.15%) < dogs and monkeys (about 60%) < humans (> 90%), indicating species difference in the first-pass effect.3. Camazepam was metabolized extensively in all species investigated to more than 10 metabolites, which were desmethyl, descarbamoyl and/or hydroxy products.4. In comparison with camazepam, plasma concn. of pharmacologically active metabolites, temazepam, oxazepan and hydroxy camazepam, were much higher in rats and mice than in dogs and monkeys. |
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