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Cibenzoline plasma concentration and antiarrhythmic effect.

R K Brazzell, K Aogaichi, J J Heger

    Clinical Pharmacology and Therapeutics
    |March 1, 1984
    PubMed
    Summary
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    Cibenzoline effectively reduces arrhythmias like premature ventricular complexes (PVCs) at plasma concentrations over 300 ng/ml. The antiarrhythmic effect of cibenzoline correlates with its plasma concentration, accurately described by the Hill equation.

    Area of Science:

    • Pharmacology
    • Clinical Cardiology
    • Drug Metabolism

    Background:

    • Cibenzoline is an antiarrhythmic drug used for treating cardiac arrhythmias.
    • Understanding the relationship between drug concentration and its therapeutic effect is crucial for optimizing patient outcomes.

    Purpose of the Study:

    • To evaluate the relationship between plasma cibenzoline concentrations and its antiarrhythmic efficacy.
    • To determine the concentration-response relationship for cibenzoline in patients with arrhythmias.

    Main Methods:

    • Ascending multiple dose oral administration of cibenzoline in 25 patients.
    • 24-hour Holter monitoring for arrhythmia assessment (PVCs and VCs).
    • Pharmacokinetic analysis of plasma cibenzoline concentrations and correlation with antiarrhythmic effect using the Hill equation.

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    Main Results:

    • Cibenzoline plasma concentrations above 300 ng/ml were associated with reduced PVC frequency.
    • Significant interpatient variability in antiarrhythmic response was observed.
    • The concentration for 90% reduction in PVC frequency (C90) ranged from 215 to 405 ng/ml.
    • The C90 for ventricular couplets (VCs) was generally lower than for PVCs.

    Conclusions:

    • The antiarrhythmic effect of cibenzoline is proportional to its plasma concentration.
    • The Hill equation accurately describes the concentration-response relationship for cibenzoline.
    • Therapeutic drug monitoring of cibenzoline plasma levels may be beneficial for optimizing antiarrhythmic therapy.