Premium
Pharmacokinetics of terbinafine and five known metabolites in children, after oral administration
Author(s) -
Humbert H.,
Denouël J.,
Cabiac M. D.,
Lakhdar H.,
Sioufi A.
Publication year - 1998
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/(sici)1099-081x(199810)19:7<417::aid-bdd111>3.0.co;2-t
Subject(s) - terbinafine , pharmacokinetics , metabolite , pharmacology , oral administration , urine , desmethyl , chemistry , active metabolite , medicine , antifungal , itraconazole , dermatology
As an extensive study, the pharmacokinetics of terbinafine and five known metabolites have been investigated after single and repeated oral administration to 12 pediatric patients. After single administration of 125 mg terbinafine, four compounds were unconjugated and the hydroxymetabolites appeared in trace amounts as glucuronides. The main metabolites in plasma were unconjugated carboxy compounds. Kinetics of terbinafine and N‐desmethylterbinafine metabolite were comparable. The interindividual AUC t variability was similar for terbinafine, N‐desmethylterbinafine and carboxyterbinafine. In urine, the major fraction was the hydrophilic unconjugated N‐desmethyl‐carboxyterbinafine (15%). After repeated administration of 125 mg day −1 , mean trough levels of terbinafine, N‐desmethylterbinafine, carboxyterbinafine and N‐desmethylhydroxy‐terbinafine, and also that of hydroxyterbinafine metabolite were similar, for each compound, on days 21, 42 and 56 denoting that steady state was reached at least on day 21 and no accumulation occurred between days 21 and 56. © 1998 John Wiley & Sons, Ltd.