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Activity of terbinafine in experimental fungal infections of laboratory animals
G Petranyi1, J G Meingassner, H Mieth
1Sandoz Forschungsinstitut, Vienna, Austria.
Abstract:
The allylamine derivative terbinafine is the first antifungal agent with primary fungicidal properties against dermatophytes which acts systemically after oral application as well as locally after topical application. Comparative oral studies carried out with griseofulvin and ketoconazole in model infections such as guinea pig trichophytosis and microsporosis revealed terbinafine to be superior to the reference compounds both clinically and mycologically. An excellent antimycotic activity of terbinafine was also demonstrable after topical treatment of guinea pig dermatophytoses caused by Trichophyton mentagrophytes or Microsporum canis. Results of comparative chemotherapeutic studies carried out with econazole and tolnaftate demonstrated superior efficacy of terbinafine in the treatment of both trichophytosis and microsporosis. Skin infections of guinea pigs caused by Candida albicans and vaginal candidiasis in rats proved to be responsive to a topical application of terbinafine also. However, the reference compounds, clotrimazole and miconazole, exhibited activity superior to that of terbinafine in both models.
Insights
Terbinafine, an oral and topical antifungal, shows superior fungicidal activity against dermatophytes compared to griseofulvin and ketoconazole. It also demonstrated excellent efficacy against common fungal infections in animal models.
Area of Science:
- Mycology
- Pharmacology
- Dermatology
Background:
- Terbinafine is an allylamine antifungal with fungicidal properties.
- It can be administered orally for systemic treatment or topically for local application.
Purpose of the Study:
- To evaluate the efficacy of terbinafine against dermatophytes and Candida albicans.
- To compare terbinafine's performance with established antifungal agents in preclinical models.
Main Methods:
- Oral and topical administration of terbinafine in guinea pig models of trichophytosis and microsporosis.
- Comparative studies using griseofulvin, ketoconazole, econazole, and tolnaftate.
- Evaluation of topical terbinafine in guinea pig skin and rat vaginal candidiasis models, compared to clotrimazole and miconazole.
Main Results:
- Terbinafine demonstrated superior clinical and mycological efficacy over griseofulvin and ketoconazole in oral studies.
- Topical terbinafine showed excellent activity against dermatophytoses caused by Trichophyton mentagrophytes and Microsporum canis.
- Terbinafine was more effective than econazole and tolnaftate for trichophytosis and microsporosis but less effective than clotrimazole and miconazole for Candida infections.
Conclusions:
- Terbinafine is a highly effective antifungal agent for dermatophyte infections, superior to griseofulvin and ketoconazole.
- Its efficacy against Candida albicans is notable but surpassed by clotrimazole and miconazole in topical applications.