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Carbenoxolone interactions in man--preliminary report

P C Thornton, M Papouchado, P I Reed

    Scandinavian Journal of Gastroenterology. Supplement
    |January 1, 1980
    PubMed
    Summary

    Carbenoxolone, an ulcer drug, was studied for interactions. Chlorpropamide delayed carbenoxolone absorption in healthy volunteers and gastric ulcer patients, but did not affect chlorpropamide

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    Area of Science:

    • Pharmacology
    • Drug Interactions
    • Gastroenterology

    Background:

    • Carbenoxolone is an effective ulcer-healing medication.
    • It extensively binds to plasma proteins, suggesting potential drug displacement interactions.
    • In vitro studies indicated carbenoxolone binds to a unique site on human serum albumin, distinct from other drugs.

    Purpose of the Study:

    • To investigate potential drug interactions between carbenoxolone and commonly co-administered medications.
    • To determine the effect of concurrent administration of warfarin, tolbutamide, chlorpropamide, or phenytoin on carbenoxolone pharmacokinetics.
    • To assess the impact of chlorpropamide on carbenoxolone absorption in gastric ulcer patients.

    Main Methods:

    • Four healthy volunteers received a single 100 mg dose of carbenoxolone (Biogastrone).
    • Plasma half-life of carbenoxolone was determined after concurrent administration with warfarin, tolbutamide, chlorpropamide, or phenytoin.
    • The interaction with chlorpropamide was re-evaluated in 6 gastric ulcer patients on an established carbenoxolone regimen.

    Main Results:

    • Concurrent administration of warfarin, tolbutamide, or phenytoin did not affect carbenoxolone plasma half-life.
    • Chlorpropamide appeared to delay the absorption of carbenoxolone in healthy volunteers.
    • This delayed absorption of carbenoxolone was confirmed in gastric ulcer patients, with no observed changes in chlorpropamide's glucose-lowering activity.

    Conclusions:

    • Carbenoxolone does not appear to interact significantly with warfarin, tolbutamide, or phenytoin.
    • Chlorpropamide may delay carbenoxolone absorption, a finding observed in both healthy volunteers and gastric ulcer patients.
    • Further research is warranted to fully elucidate the interaction between carbenoxolone and chlorpropamide.

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