LEVELS OF TERBINAFINE IN PLASMA, STRATUM-CORNEUM, DERMIS-EPIDERMIS (WITHOUT STRATUM-CORNEUM), SEBUM, HAIR AND NAILS DURING AND AFTER 250 MGTERBINAFINE ORALLY ONCE PER DAY FOR 4 WEEKS
J. Faergemann et al., LEVELS OF TERBINAFINE IN PLASMA, STRATUM-CORNEUM, DERMIS-EPIDERMIS (WITHOUT STRATUM-CORNEUM), SEBUM, HAIR AND NAILS DURING AND AFTER 250 MGTERBINAFINE ORALLY ONCE PER DAY FOR 4 WEEKS, Acta dermato-venereologica, 73(4), 1993, pp. 305-309
The distribution of terbinafine in stratum corneum dermis-epidermis (w
ithout stratum corneum), sebum, hair, nails and plasma was studied in
human male volunteers during and after 250 mg orally once daily for 28
days. The highest concentration was seen in sebum, 56.07 mug/g, after
14 days of therapy. The concentration was still 1.0 mug/g 44 days aft
er stop of medication. In stratum corneum the highest concentration, 1
4.4 mug/g, was seen 1 day after the last day of therapy, and it was 2.
1 mug/g 44 days after stop of medication. The concentrations in hair a
nd nails were lower with a maximum of 2.36 and 0.39 mug/g respectively
, 1 day after stop of therapy, and still 0.21 mug/g in hair and 0.09 m
ug/g in nails 55 days after the last day of medication. With the excep
tion of nails, all other tissue levels' were at all times above the pl
asma concentrations. For nails, tissue levels exceeded that of plasma
as early as 1 day after stop of medication, and this difference contin
ued to increase until the last day of tissue sampling, 55 days after t
he last tablet. These results indicate that terbinafine is delivered t
o the stratum corneum through sebum and to a minor extent by direct di
ffusion through dermis-epidermis. Probably short-term therapy with ter
binafine may be effective in the treatment of several dermatomycoses,
due to the strong binding of terbinafine to stratum corneum for a long
time after stop of medication. Details of skin distribution of orally
active antifungal agents should provide the basis for a more rational
, pharmacodynamic-oriented approach to antifungal therapy than the use
of traditional blood levels.