Arika T, Yokoo M, Hase T, Maeda T, Amemiya K, Yamaguchi H
Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., Tokyo, Japan.
Antimicrob Agents Chemother. 1990 Nov;34(11):2250-3. doi: 10.1128/AAC.34.11.2250.
Butenafine hydrochloride, N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethylamine hydrochloride (butenafine), is a novel antifungal agent of the class of benzylamine derivatives. Butenafine was investigated for its activity against guinea pig dermatophytosis caused by Trichophyton mentagrophytes or Microsporum canis in comparison with those of naftifine, tolnaftate, clotrimazole, and bifonazole. Topical butenafine showed excellent efficacy against dermatophytosis when it was applied once daily, and the effect was superior to those of all four reference drugs. When applied once at 24 or 48 h before infection, the drug exhibited excellent prophylactic efficacy against experimental T. mentagrophytes infection. The concentrations of butenafine in animal skin at 24 and 48 h after application of 0.2 ml of a 1% solution were several hundred times higher than those required to kill T. mentagrophytes and M. canis. The good efficacy of butenafine against dermatophytosis may be attributable to its fungicidal activity and long retention in the skin after topical application.
盐酸布替萘芬,即N - 4 - 叔丁基苄基 - N - 甲基 - 1 - 萘甲胺盐酸盐(布替萘芬),是苄胺衍生物类的一种新型抗真菌剂。将布替萘芬与萘替芬、托萘酯、克霉唑和联苯苄唑进行比较,研究了其对由须癣毛癣菌或犬小孢子菌引起的豚鼠皮肤癣菌病的活性。局部应用布替萘芬时,每日给药一次对皮肤癣菌病显示出优异疗效,且效果优于所有四种对照药物。在感染前24或48小时给药一次,该药物对实验性须癣毛癣菌感染表现出优异的预防效果。在应用0.2 ml 1%溶液后24和48小时,动物皮肤中布替萘芬的浓度比杀死须癣毛癣菌和犬小孢子菌所需浓度高数百倍。布替萘芬对皮肤癣菌病的良好疗效可能归因于其杀菌活性以及局部应用后在皮肤中的长时间留存。