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  • 标题:Effect of Clarithromycin and Other Macrolides on the Sulfoxidation and 5-Hydroxylation of Lansoprazole in Dogs
  • 本地全文:下载
  • 作者:Kengo MASA ; Kazuhiko ARIMORI ; Takao NAKAYAMA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1999
  • 卷号:22
  • 期号:5
  • 页码:504-509
  • DOI:10.1248/bpb.22.504
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The purpose of this study was to evaluate a possible interaction between lansoprazole and clarithromycin as well as other macrolides in dogs. Lansoprazole (30 mg) was orally administered to male beagle dogs, with or without oral pretreatment with 200-mg clarithromycin twice a day for 5 d. The experiments had a randomized cross-over design with a two-week washout period between dosing regimens. Clarithromycin pretreatment for 5 d resulted in a significant increase in the area under the serum lansoprazole concentration-time curve (AUC), whereas the area for a lansoprazole metabolite, lansoprazole sulfone, was significantly reduced, as was the maximum serum concentration (Cmax) of lansoprazole sulfone. When the effects of clarithromycin on the metabolism of lansoprazole were studied using dog liver microsomes, it was found that clarithromycin significantly inhibited the formation of lansoprazole sulfone but not another metabolite, 5-hydroxylansoprazole. These results suggest that co-medication of lansoprazole with clarithromycin may produce a synergistic effect caused by the increased serum levels of lansoprazole of benefit in Helicobacter pylori eradication.
  • 关键词:lansoprazole;clarithromycin;sulfoxidation;metabolism;pharmacokinetics
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