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  • Title: The in vitro metabolism of hydralazine.
    Author: Streeter AJ, Timbrell JA.
    Journal: Drug Metab Dispos; 1985; 13(2):255-9. PubMed ID: 2859177.
    Abstract:
    Hydralazine was metabolized in vitro to phthalazine and phthalazine-1-one by microsomal enzymes requiring NADPH. Hydrazine was not detected as a metabolite under these in vitro conditions. Addition of 1-hydrazinophthalazin-4-one, a possible intermediate metabolite, decreased covalent binding to protein but also decreased metabolism. Phthalazine and phthalazin-1-one also decreased covalent binding to protein to a lesser extent. N-Acetylcysteine significantly decreased the level of phthalazine and phthalazin-1-one detected in microsomal incubations. The results are consistent with a reactive intermediate, but not 1-hydrazinophthalazin-4-one, being responsible for both covalent binding and production of phthalazine.
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