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The pharmacokinetics and antihistaminic effects of brompheniramine.

F E Simons, E M Frith, K J Simons

    The Journal of Allergy and Clinical Immunology
    |December 1, 1982
    PubMed
    Summary

    Brompheniramine exhibits a prolonged antihistaminic effect in adults, with a long serum half-life and significant suppression of histamine-induced wheal and flare responses. This indicates sustained relief from allergic skin reactions and itching.

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    Area of Science:

    • Pharmacology
    • Clinical Pharmacology

    Background:

    • Brompheniramine is a widely used antihistamine.
    • Understanding its pharmacokinetic and pharmacodynamic properties is crucial for optimizing therapeutic use.

    Purpose of the Study:

    • To investigate the pharmacokinetics of brompheniramine in healthy adults.
    • To evaluate the antihistaminic effects of brompheniramine on skin responses to histamine.

    Main Methods:

    • Seven healthy adults received a single dose of brompheniramine.
    • Serum concentrations were measured over time.
    • Skin reactions (wheal and flare) to histamine and pruritus were assessed post-dose.

    Main Results:

    • Mean serum half-life was 24.9 hours; mean volume of distribution was 11.7 L/kg.
    • Significant suppression of wheal size occurred from 3 to 9 hours.
    • Significant suppression of flare size persisted from 3 to 48 hours.
    • Pruritus scores were significantly reduced at 9, 12, and 24 hours.

    Conclusions:

    • Brompheniramine demonstrates a long half-life and large volume of distribution in adults.
    • The drug provides a prolonged antihistaminic effect, evidenced by sustained suppression of skin reactions and pruritus.