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Related Experiment Videos

Temelastine, a new H1-receptor antagonist.

F Alexander, R M Stote, N Allison

    The Journal of International Medical Research
    |January 1, 1986
    PubMed
    Summary
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    Temelastine effectively reduces histamine-induced skin reactions in a dose-dependent manner. Even low plasma concentrations demonstrate significant antihistaminic effects, suggesting 100 mg twice daily may control allergy symptoms.

    Area of Science:

    • Pharmacology
    • Allergy and Immunology

    Background:

    • Temelastine is a selective, competitive histamine H1-receptor antagonist.
    • It does not penetrate the central nervous system, minimizing potential side effects.

    Purpose of the Study:

    • To evaluate the dose-dependent efficacy of temelastine in inhibiting histamine-induced wheals.
    • To assess the duration of action and effective plasma concentrations of temelastine.

    Main Methods:

    • Randomized, double-blind, controlled studies were conducted.
    • Inhibition of cutaneous histamine wheals was measured after single oral doses of temelastine (50, 100, 200 mg) and chlorpheniramine (4 mg).
    • Duration of action and plasma concentrations were assessed over 20 hours.

    Main Results:

    Related Experiment Videos

    • Temelastine demonstrated dose-dependent reductions in wheal size, with maximal inhibition by 2 hours.
    • At 2 hours, 50, 100, and 200 mg doses reduced wheal size by 53%, 64%, and 78%, respectively, compared to 32% for 4 mg chlorpheniramine.
    • 100 mg temelastine provided significant antihistaminic effects for up to 20 hours, with notable inhibition at plasma concentrations as low as 1.44 mumol/l.

    Conclusions:

    • Temelastine is a potent H1-receptor antagonist with a prolonged duration of action.
    • Daily or twice-daily dosing of 100 mg temelastine may be sufficient for managing allergic symptoms.