Piotr Mariusz Dwiecki, Tomasz Michalak, Izabela Muszalska-Kolos

The use and mechanism of action of terbinafine compared to other antifungal drugs used in the pharmacotherapy of candidiasis

Terbinafine as an antifungal drug was introduced to the world market in 1991, which was a great advance in dermatology. From that time to 1999, it was used orally with good results in over 10 million people and locally in over 30 million. It was first introduced to medical treatment in Poland in 1992. Terbinafine is an allylamine with broad antifungal activity. In low concentrations, it is fungicidal against skin fungi, molds, and some dimorphic fungi. Against yeasts, it is fungicidal or fungistatic, depending on the species. It is usually used in the treatment of dermatophytosis, tinea versicolor, and onychomycosis. It is believed to be the most effective against dermatophytes (Microsporum, Epidermophyton, and Trichophyton). Its main mode of action is to inhibit squalene epoxidase and thus inhibit ergosterol synthesis. The resulting ergosterol deficiency and the accumulation of squalene disturb the function of the cell membrane and the synthesis of the fungal cell wall. For Candida albicans, ergosterol deficiency is the major growth-inhibiting factor, and the filamentous form of this fungus was found to be more susceptible to terbinafine than the yeast form. Squalene epoxidase is not a cytochrome P-450 type enzyme, therefore its inhibitors have no potential inhibitory effect on this class of enzymes. Thus, terbinafine has no effect on the metabolism of other drugs. Treatment failure of fungal infections with terbinafine may be due to terbinafine resistance of the pathogens. Terbinafine hydrochloride creams are used to treat fungal infections such as fungal infections of the skin (tinea pedis, tinea pedis - tinea pedis, mycosis of skin folds, mycosis of smooth skin) caused by Trichophyton dermatophytes (Trichophyton rubrum, Trichophyton mentagrophytophytes). verrucosum, Trichophyton violaceum), Microsporum canis and Epidermophyton floccosum, and yeast infections of the skin caused by the genus Candida (Candida albicans) and Pityrosporum orbiculare (also known as Malassezia furfur). Research is underway on new forms of terbinafine for the treatment of fungal infections in ophthalmology.

Keywords: terbinafine, mechanism of action, dermatophytosis, onychomycosis.

© Farm Pol, 2021, 77 (5):316–323

The use and mechanism of action of terbinafine compared to other antifungal drugs used in the pharmacotherapy of candidiasis

509.90 kB | 14 czerwca 2021