Petranyi G, Meingassner J G, Mieth H
Sandoz Forschungsinstitut, Vienna, Austria.
Antimicrob Agents Chemother. 1987 Oct;31(10):1558-61. doi: 10.1128/AAC.31.10.1558.
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.
烯丙胺衍生物特比萘芬是第一种对皮肤癣菌具有主要杀菌特性的抗真菌剂，口服后可全身起效，局部应用后也可局部起效。在豚鼠毛癣菌病和小孢子菌病等模型感染中，与灰黄霉素和酮康唑进行的口服对比研究表明，特比萘芬在临床和真菌学方面均优于对照化合物。在用须癣毛癣菌或犬小孢子菌引起的豚鼠皮肤癣菌病进行局部治疗后，特比萘芬也表现出优异的抗真菌活性。与益康唑和托萘酯进行的对比化疗研究结果表明，特比萘芬在治疗毛癣菌病和小孢子菌病方面疗效更佳。白色念珠菌引起的豚鼠皮肤感染和大鼠阴道念珠菌病经证明对特比萘芬局部应用也有反应。然而，在这两种模型中，对照化合物克霉唑和咪康唑表现出优于特比萘芬的活性。
