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Related Experiment Videos

Cimetidine decreases theophylline clearance

J E Jackson, J R Powell, M Wandell

    The American Review of Respiratory Disease
    |June 1, 1981
    PubMed
    Summary

    Cimetidine significantly reduces theophylline clearance by 39% in healthy adults. This drug interaction may lead to clinically important changes in theophylline levels, impacting patient treatment.

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    Area of Science:

    • Pharmacology
    • Drug Metabolism

    Background:

    • Theophylline is a widely used bronchodilator.
    • Potential drug interactions affecting theophylline clearance are clinically significant.

    Purpose of the Study:

    • To investigate the effect of cimetidine on theophylline clearance in healthy adults.
    • To determine if cimetidine alters the pharmacokinetic parameters of theophylline.

    Main Methods:

    • Healthy adult volunteers received aminophylline intravenously before and after cimetidine treatment.
    • Plasma theophylline concentrations were measured over 24 hours post-dose.
    • Theophylline clearance, volume of distribution, elimination rate constant, and half-life were calculated.

    Main Results:

    • Cimetidine significantly decreased theophylline clearance by a mean of 39% (p < 0.002).
    • The elimination rate constant decreased by 42% (p < 0.005), increasing the elimination half-life by 73%.
    • The apparent volume of distribution of theophylline remained unchanged.

    Conclusions:

    • Cimetidine significantly reduces theophylline elimination, likely through inhibition of hepatic microsomal mono-oxygenase enzymes.
    • This interaction can lead to increased serum theophylline concentrations, potentially causing toxicity.
    • Clinicians should consider this interaction when prescribing cimetidine to patients on theophylline therapy.

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