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  • 标题:Effect of Cefixime and Cefdinir, Oral Cephalosporins, on Cytochrome P450 Activities in Human Hepatic Microsomes
  • 本地全文:下载
  • 作者:Toshiro Niwa ; Toshifumi Shiraga ; Tomoko Hashimoto
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2004
  • 卷号:27
  • 期号:1
  • 页码:97-99
  • DOI:10.1248/bpb.27.97
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要: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 m M 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 6β-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.
  • 关键词:cefixime;cefdinir;human hepatic cytochrome P450;oral cephalosporin;drug interaction
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