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Cimetidine-theophylline complex formation.

W A Ritschel, G J Alcorn, W H Streng

    Methods and Findings in Experimental and Clinical Pharmacology
    |January 1, 1983
    PubMed
    Summary
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    Cimetidine forms a complex with theophylline, increasing theophylline levels in solution by up to 36% in human plasma. This interaction may explain the reduced theophylline clearance observed in patients taking cimetidine.

    Area of Science:

    • Pharmacology
    • Drug Interactions
    • Biochemistry

    Background:

    • Theophylline is a medication used to treat respiratory diseases.
    • Cimetidine is a medication that can interact with other drugs.
    • Clinical observations suggest cimetidine reduces theophylline clearance in humans.

    Purpose of the Study:

    • To investigate the in vitro interaction between cimetidine and theophylline.
    • To quantify the effect of cimetidine on theophylline solubility.
    • To explore a potential mechanism for the observed decrease in theophylline clearance.

    Main Methods:

    • In vitro complex formation studies.
    • Use of pH 7.4 buffer and human plasma as experimental media.
    • Quantification of theophylline in solution.

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    Main Results:

    • Cimetidine formed a complex with theophylline in both buffer and plasma.
    • Theophylline solubility increased by approximately 20% in buffer.
    • Theophylline solubility increased by approximately 36% in human plasma.

    Conclusions:

    • Complex formation between cimetidine and theophylline occurs in vitro.
    • This interaction enhances theophylline solubility.
    • In vitro complexation may contribute to the in vivo reduction of theophylline clearance by cimetidine.