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. 1992 Jul;77(1):31-41.

Formation of reductive metabolite, 2-sulfamoylacetylphenol, from zonisamide in rat liver microsomes

H Nakasa  1 , M Komiya, S Ohmori, M Kitada, T Rikihisa, Y Kanakubo
Affiliations
  • PMID: 1439179

Formation of reductive metabolite, 2-sulfamoylacetylphenol, from zonisamide in rat liver microsomes

H Nakasa et al. Res Commun Chem Pathol Pharmacol. 1992 Jul.

Abstract

Zonisamide (1,2-benzisoxazole-3-methanesulfonamide) was metabolized to its reductive product, 2-sulfamoylacetylphenol, in rat liver microsomes under anaerobic conditions. The rate of NADPH-dependent reaction was much more rapid than that of NADH-dependent reaction. Furthermore, synergistic effect of NADH on NADPH-dependent reaction was not observed. The optimal formation of 2-sulfamoylacetylphenol from zonisamide in the presence of NADPH was observed around pH 7.0. Cimetidine showed an inhibitory effect on the formation of 2-sulfamoylacetylphenol in a dose-dependent manner. The reductive metabolism of zonisamide was almost completely inhibited by carbon monoxide, and was increased by pretreatment of rats with phenobarbital and pregnenolone 16 alpha-carbonitrile but not by pretreatment with ethanol, 3-methylcholanthrene and imidazole. These results suggest that phenobarbital- and pregnenolone 16 alpha-carbonitrile-inducible form(s) of cytochrome P-450 is responsible for the reductive metabolism of zonisamide to 2-sulfamoylacetylphenol in rat liver microsomes.

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