Effect of Cefixime and Cefdinir, Oral Cephalosporins, on Cytochrome P450 Activities in Human Hepatic Microsomes
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Accession number;04A0042358
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| Title;Effect of Cefixime and Cefdinir, Oral Cephalosporins, on Cytochrome P450 Activities in Human Hepatic Microsomes |
| Author;
NIWA T
(Fujisawa Pharmaceutical Co., Ltd., Osaka, Jpn)
SHIRAGA T
(Fujisawa Pharmaceutical Co., Ltd., Osaka, Jpn)
HASHIMOTO T
(Fujisawa Pharmaceutical Co., Ltd., Osaka, Jpn)
KAGAYAMA A
(Fujisawa Pharmaceutical Co., Ltd., Osaka, Jpn)
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Journal Title;Biol Pharm Bull
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Journal Code:S0989A
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ISSN:0918-6158
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VOL.27;NO.1;PAGE.97-99(2004)
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| Figure&Table&Reference;FIG.1, TBL.2, REF.17 |
| Pub. Country;Japan |
| Language;English |
| Abstract;The effects of two kinds of oral cephalosporins, cefixime and cefdinir, on cytochrome P450 (CYP) activities in human hepatic microsomes were investigated. Both cefixime and cefdinir at 2 mM concentration neither inhibited nor stimulated CYP1A1/2-mediated 7-ethoxyresorufin O-deethylation, CYP2A6-mediated coumarin 7-hydroxylation, CYP2B6-mediated 7-benzyloxyresorufin O-debenzylation, CYP2C8/9-mediated tolbutamide methylhydroxylation, CYP2C19-mediated S-mephenytoin 4'-hydroxylation, CYP2D6-mediated bufuralol 1'-hydroxylation, CYP2E1-mediated chlorzoxazone 6-hydroxylation, CYP3A4-mediated nifedipine oxidation, or CYP3A4-mediated testosterone 6.BETA.-hydroxylation. The free fractions of cefixime and cefdinir in the incubation mixture, which were measured by ultracentrifugation, were 86.1-93.8% and 94.1-97.8%, respectively. These results suggest that both cefixime and cefdinir would not cause clinically significant interactions with other drugs, which are metabolized by CYPs, via the inhibition of metabolism. (author abst.) |
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