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  • Title: Distribution of clozapine and desmethylclozapine between blood and brain in rats.
    Author: Weigmann H, Härtter S, Fischer V, Dahmen N, Hiemke C.
    Journal: Eur Neuropsychopharmacol; 1999 Mar; 9(3):253-6. PubMed ID: 10208296.
    Abstract:
    Desmethylclozapine is the major metabolite of clozapine in serum. Although the metabolite is pharmacologically active in vitro, the occurrence of desmethylclozapine in brain under steady-state conditions and its role for clinical actions of clozapine are unclear. In this study 20 male Sprague-Dawley rats received five oral doses of clozapine 20 mg/kg at 1.5-h intervals. At 0.5, 1, 2 and 5 h after the last administration, at a time four animals were killed for analysis of clozapine and desmethylclozapine concentrations in serum and brain. The treatment yielded steady-state serum concentrations of clozapine that are considered as therapeutically effective in man. Desmethylclozapine concentrations exceeded those of clozapine at 2-5 h after drug application. In brain, drug concentrations were 15.8-fold higher for clozapine than in serum, but only 2.7-fold higher for desmethylclozapine. The brain clozapine concentrations exceeded those of desmethylclozapine by about 3 times. These data indicate that desmethylclozapine is unlikely to play a role for CNS-mediated effects.
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