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  • Title: [Pharmacokinetics of afobazole in rats].
    Author: Seredenin SB, Viglinskaia AO, Kolyvanov GB, Litvin AA, Kravtsova OIu, Zherdev VP.
    Journal: Eksp Klin Farmakol; 2007; 70(2):59-64. PubMed ID: 17523455.
    Abstract:
    Afobazole pharmacokinetics was studied after the administration via different ways in rats. After oral administration, afobazole is subject to intensive biotransformation with the formation of several metabolites (M-6, M-7, and M-11). The drug and its metabolites were detected in the blood plasma for 3 h and characterized by a high elimination rate after both oral and intravenous administration. Afobazole and its main metabolite (M-11) had a medium rate of permeability into brain (the target organ): the tissue availability was 0.584 for afobazole and 0.793 for M-11. The absolute bioavailability of afobazole upon oral administration was 43.6% for. Afobazole was completely absorbed from the gastrointestinal tract of rats and characterized by the first-pass effect, after which more than 40% of administered dose entered the circulation. The parent compound was determined in extremely low amounts in urine and feces: its content in 24-h urine on the average did not exceed 0.07% of the administered dose; in 24-h feces, it did not exceed 0.05 % after intravenous administration and 0.01% after oral administration).
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