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Cimetidine plasma concentration-response relationships

R Gugler, G Fuchs, M Dieckmann

    Clinical Pharmacology and Therapeutics
    |June 1, 1981
    PubMed
    Summary
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    This study determined cimetidine plasma concentrations needed for effective gastric acid suppression in healthy individuals. The findings help establish target drug levels for optimal therapeutic effects in various patient groups.

    Area of Science:

    • Pharmacology
    • Gastroenterology

    Background:

    • Histamine H2-receptor antagonists are crucial for managing acid-related disorders.
    • Understanding the relationship between drug concentration and effect is vital for optimizing therapy.

    Purpose of the Study:

    • To investigate the plasma concentration-response relationship of cimetidine.
    • To establish a model for determining optimal drug levels for gastric acid inhibition.

    Main Methods:

    • Six healthy subjects participated in the study.
    • Gastric acid secretion was suppressed using continuous pentagastrin stimulation.
    • The Hill equation was employed to model plasma concentration-effect relationships.

    Main Results:

    • A sigmoid relationship between cimetidine plasma concentration and gastric acid suppression was preferred over a linear model.

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  • The mean plasma concentration for 50% inhibition of gastric acid secretion was 0.78 µg/ml (range 0.54–1.04 µg/ml).
  • The mean concentration for 90% inhibition was calculated to be 3.9 µg/ml.

    • Conclusions:

    • The developed model allows for the assessment of concentration-response differences across various patient populations.
    • This research facilitates achieving appropriate cimetidine plasma levels for specific degrees of gastric acid inhibition.