Usefulness and pharmacokinetic study of oral terbinafine for hyperkeratotic‐type tinea pedis

Abstract

To study and establish an optimal administration method of oral antifungal, terbinafine (TBF), for hyperkeratotic-type tinea pedis from the pharmacokinetic point of view, 20 patients with hyperkeratotic-type tinea pedis were given TBF 125 mg once daily for 4 weeks and observed over time for improvement of dermatological symptoms and mycological efficacy. Targeting five of the patients, TBF concentration in the stratum corneum was measured using the LC-MS/MS method. TBF was detected in the stratum corneum of the sole 1 week after beginning the treatment in some cases and reached its peak 1 week after the completion of the treatment with a concentration of 247.8 ng g(-1), which was approximately more than 50 times higher than its minimal inhibitory concentration against dermatophytes. TBF was not detected at 8 weeks post-treatment, although its concentration was 50.73 ng g(-1) at 6 weeks post-treatment. All cases were subjected to analysis for final total efficacy, general safety and usefulness. Its effectiveness rate (effective + markedly effective) was 95% (19/20) with no adverse reactions, including abnormal changes in the laboratory test values, in any patients. From the above, it is noted that TBF showed excellent efficacy and safety for refractory hyperkeratotic-type tinea pedis, and also it was considered as a useful drug to treat cutaneous mycosis, including hyperkeratotic-type tinea pedis, from the pharmacokinetic point of view.

Update on terbinafine with a focus on dermatophytoses

“…Although lower in the stratum corneum of hyperkeratotic tissue, terbinafi ne concentrations remain elevated following the discontinuation of oral therapy and persist in excess of 1 month after stopping treatment. 58 At least seven cytochromes P450 (CYP) appear to be responsible for metabolizing terbinafi ne into more than 15 metabolites. 59 In adults, the N-demethyl and carboxybutyl metabolites constitute the largest fraction of the metabolites observed.…”

Comparable Efficacy of Terbinafine and Itraconazole in the Treatment of Tinea Pedis

“…The effectiveness of itraconazole can be attributed to its high tissue affinity and persistence in the stratum corneum for upto 4 weeks after discontinuation of therapy. 2 In the present study total 120 patients were involved. Male 80 (66.66%) were predominant in the study than female 40 (33.33%) which is consistent with other study done by Lachapelle JM et al 4 The age of the study population ranged from 20-60 years and maximum patients in our study were in 41-50 years age group 53 (44.16%) followed by 31-40 years age group 30 (25%) which is differing from other study done by Wishart J.M.…”

Recent updates in oral terbinafine: its use in onychomycosis and tinea capitis in the US

“…In 2008, Kawana et al . performed a study on the concentrations of terbinafine in the stratum corneum and the efficacy of treatment in hyperkeratotic‐type tinea pedis 22 . This study treated 20 patients, who had failed other therapies, with oral terbinafine 125 mg daily for 4 weeks and observed for 8 weeks post‐treatment.…”