Allylamines

Allylamines are antifungal agents targeted to squalene epoxidase, an enzyme necessary for ergosterol biosynthesis. Naftifine (12) was the first allylamine agent introduced in therapy in the early 1980s as 1% cream or gel for topical use. It has fungicidal activity against dermatophytes and fungistatic activity against Candida species. Its sensitizing capacity seems to be greater than in the commonly used azoles [58]. Terbinafine (13) was approved in 1990s in the UK and USA for the treatment of onychomycosis. It is the most frequently prescribed oral antifungal agent in North America, for onychomycosis. Eighteen randomized controlled trials have shown terbinafine to be highly effective with mycological cure of 76%. 13 has an established safety profile and very low occurrence of drug interactions [59]. An improved antifungal composition for topical application to the skin and nails has been developed for allylamines (naftifine or terbinafine) [60]. A formulation to provide a product having a high therapeutic effect suitable for symptoms of weeping superficial mycosis was reported. It consists of an allylamine derivative (naftifine or terbinafine) blended with a fatty acid ester, a powdery component, an alcoholic solvent and an anti-itch component [61].

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