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Related Experiment Videos

Cimetidine sulfoxidation in small intestinal microsomes

X Lu1, C Li, D Fleisher

  • 1College of Pharmacy, University of Michigan, Ann Arbor, USA.

Drug Metabolism and Disposition: the Biological Fate of Chemicals
|September 12, 1998
PubMed
Summary
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Cimetidine sulfoxidation in the small intestine is influenced by drug metabolism and transport. Researchers investigated the enzymes and interactions affecting cimetidine

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Gastrointestinal Physiology

Background:

  • Sulfoxide metabolite formation of cimetidine and H2-antagonists occurs in the animal and human intestine.
  • Previous studies indicated L-methionine, imipramine, and an anionic exchange inhibitor reduce metabolite appearance in vivo.
  • Understanding drug metabolism and transport is crucial for variable drug absorption and drug-drug/drug-nutrient interactions.

Purpose of the Study:

  • To investigate the S-oxidation of cimetidine in mammalian small intestinal microsomes.
  • To evaluate the roles of flavin-containing monooxygenases and cytochrome P450 enzymes in cimetidine sulfoxidation.
  • To assess the contribution of microsomal cimetidine sulfoxidation to in vivo observations.

Main Methods:

  • Studied S-oxidation of cimetidine in microsomes from three mammalian species and two intestinal regions.

Related Experiment Videos

  • Utilized enzyme activity and tissue availability to assess flavin-containing monooxygenases and cytochrome P450 contributions in rabbit jejunal microsomes.
  • Conducted inhibitor studies to evaluate the role of microsomal sulfoxidation in vivo.

    • Main Results:

    • Cimetidine sulfoxidation was observed in mammalian small intestinal microsomes.
    • Flavin-containing monooxygenases and cytochrome P450 enzymes were evaluated for their contributions to cimetidine sulfoxidation.
    • Inhibitor studies provided insights into the role of microsomal sulfoxidation in previously observed in vivo effects.

    Conclusions:

    • Microsomal S-oxidation is a significant pathway for cimetidine metabolism in the small intestine.
    • Enzymatic pathways, including flavin-containing monooxygenases and cytochrome P450, contribute to cimetidine sulfoxidation.
    • Further research is needed to fully elucidate the interplay between drug metabolism, transport, and interactions affecting cimetidine absorption.