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Loperamide in rat intestines: a unique disposition

H Miyazaki, K Nambu, M Hashimoto

    Life Sciences
    |June 21, 1982
    PubMed
    Summary

    Oral loperamide is metabolized in the intestine and secreted back into the lumen. This unique intestinal metabolism of loperamide may explain its distinct central and antidiarrheal activities.

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    Area of Science:

    • Pharmacology
    • Drug Metabolism
    • Gastrointestinal Physiology

    Background:

    • Loperamide is a widely used antidiarrheal agent.
    • Its distinct dissociation of central and antidiarrheal activities suggests unique pharmacokinetic properties.

    Purpose of the Study:

    • To investigate the intestinal metabolism and disposition of loperamide in vitro.
    • To explore the potential role of intestinal metabolism in loperamide's unique activity profile.

    Main Methods:

    • Everted sacs of rat duodenum, jejunum, and ileum were incubated with [14C]loperamide.
    • Radioactivity and metabolites were quantified in tissues and mucosal/serosal media.

    Main Results:

    • Unchanged loperamide and metabolites were found in tissues and mucosal media, with minimal serosal presence.
    • Metabolite levels in mucosal media were comparable to or greater than tissue levels.
    • Di-desmethyl loperamide was more prevalent in mucosal media than mono-demethylated loperamide.

    Conclusions:

    • Loperamide undergoes metabolism within the intestinal wall.
    • A portion of absorbed loperamide is directly secreted back into the intestinal lumen.
    • This intestinal metabolism likely contributes to the unique pharmacokinetic and pharmacodynamic profile of oral loperamide.

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