Terbinafine Levels in Serum, Stratum Corneum, Dermis-Epidermis, Hair, Sebum, and Eccrine Sweat

    January 1991 in “ Acta dermato-venereologica
    Jan Faergemann, H Zehender, T. C. Jones, I Maibach
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    Studysummary In this study, terbinafine reached high concentrations in stratum corneum and sebum after oral administration, with drug levels remaining above fungicidal concentrations for over three weeks.
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    The study measured terbinafine levels in various tissues and fluids of volunteers taking 250 mg doses daily. Terbinafine rapidly concentrated in the stratum corneum (up to 9.1 µg/g) and sebum (up to 45.1 µg/ml), with hair concentrations reaching 2.6 µg/g, indicating high levels around hair follicles. It was not detected in sweat, and plasma levels ranged from 0.1 to 1.0 µg/ml. The drug accumulated tenfold in the stratum corneum by day 2 and had a tissue elimination half-life of 4-5 days, maintaining fungicidal levels for over 3 weeks. Terbinafine's pharmacokinetics were similar to itraconazole but differed from ketoconazole and griseofulvin, achieving higher and longer-lasting levels.
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