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Related Experiment Videos

In vitro protein binding interaction studies involving cefixime.

M Bialer1, W H Wu, R D Faulkner

  • 1Department of Pharmacodynamics, American Cyanamid Company, Pearl River, New York 10965.

Biopharmaceutics & Drug Disposition
|May 1, 1988
PubMed
Summary
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Drug interactions with cefixime were studied. Salicylic acid and probenecid significantly increased cefixime

Area of Science:

  • Pharmacology
  • Drug Metabolism and Interactions

Background:

  • Cefixime is a novel oral cephalosporin undergoing clinical evaluation.
  • Understanding potential drug interactions is crucial for safe and effective cefixime use.

Purpose of the Study:

  • To investigate the in vitro effect of commonly coadministered drugs on cefixime's serum protein binding.

Main Methods:

  • Pooled serum from dogs, monkeys, and humans was used.
  • The binding of cefixime was assessed in the presence of various agents at therapeutic concentrations.
  • Concentration-dependent changes in cefixime's free fraction were measured.

Main Results:

  • Acetaminophen, heparin, phenytoin, diazepam, ibuprofen, and furosemide did not significantly alter cefixime binding.

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  • Salicylic acid and probenecid demonstrated concentration-dependent increases in the free fraction of cefixime, up to 2.5-fold.
  • These interactions were observed across all species studied, including humans.

    • Conclusions:

    • In vitro protein binding assays are valuable for predicting drug interactions involving altered protein binding.
    • Salicylic acid and probenecid are potential interactants with cefixime, warranting further clinical investigation.
    • The study highlights the importance of considering protein binding displacement in cefixime drug interaction profiles.