ACCUMULATION OF FLUCONAZOLE IN SCALP HAIR

Citation
R. Yeates et al., ACCUMULATION OF FLUCONAZOLE IN SCALP HAIR, Journal of clinical pharmacology, 38(2), 1998, pp. 138-143
Citations number
27
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
00912700
Volume
38
Issue
2
Year of publication
1998
Pages
138 - 143
Database
ISI
SICI code
0091-2700(1998)38:2<138:AOFISH>2.0.ZU;2-8
Abstract
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.