The accumulation in scalp hair of the antimycotic triazole, fluconazol
e, was studied during and after administration. Fluconazole 50 mg was
administered to 22 healthy subjects as a single capsule each day for 2
8 days. The concentration of fluconazole 5 hours after administration
was measured in different 1-cm sections of scalp hair at intervals dur
ing treatment and for 6 months after the end of treatment, in each sec
tion of scalp hair the concentration of fluconazole increased during t
reatment and was consistently higher than values found in plasma. For
example, the mean concentration in the first hair section on day 28, 1
9.8 mu g/g, corresponded to a mean penetration ratio relative to plasm
a of 9.42. During administration, the maximal concentration of flucona
zole was found in the first hair section. After cessation of administr
ation, the measured concentrations of fluconazole decreased and greate
r concentrations were found in the distal hair sections, presumably as
a result of hair growth. Fluconazole was detectable, however, in the
hair of 9 of the 12 subjects even 6 months after treatment. The mean c
oncentration of fluconazole in hair bulbs on day 28 was 12.1 mu g/g (n
= 6), corresponding to a mean penetration ratio of 5.99. in a second
study, fluconazole was administered as a single oral 150-mg capsule pe
r week for 4 weeks fa a group of 8 healthy subjects. The mean fluconaz
ole concentration in whole scalp hair 5 hours after the last dose was
3.2 mu g/g.