Plempel M, Regel E, Büchel K H
Arzneimittelforschung. 1983;33(4):517-24.
The new imadozolyl derivative 1-(p, alpha-diphenyl-benzyl)imidazole (bifonazole, Bay h 4502, Mycospor) shows in vitro the broad spectrum of activity characteristic of azole antimycotics. The intensity of activity under conventional test conditions is equivalent to that of clotrimazole. Further, concentrations of less than or equal to 5 micrograms/ml bifonazole have a fungicidal effect on dermatophytes, and a MIC value of less than or equal to 0.25 micrograms/ml has a maximal effect on Torulopsis glabrata. In ng concentrations bifonazole is effective on proliferating dermatophytes and pseudomycelia of Candida albicans. The resistance situation regarding bifonazole is favourable--as is typical of azole antimycotics. In animal experiments, topical application of concentrations of between 0.05 and 1% bifonazole as a cream or solution are extremely effective on guinea-pig trichophytosis. This is attributed to the therapeutically achievable fungicidal effect on dermatophytes and the long period of time the substance is retained in the skin. The sum of the experimental properties of bifonazole make it possible to recommend the active drug to be applied, once every 24 h, as a 1% cream or solution and the duration of therapy for these indications being reduced to 2-3 weeks.
新型咪唑基衍生物1-(对,α-二苯基苄基)咪唑(联苯苄唑,拜耳h 4502,霉克)在体外显示出唑类抗真菌药特有的广谱活性。在常规测试条件下,其活性强度与克霉唑相当。此外,联苯苄唑浓度小于或等于5微克/毫升时对皮肤癣菌有杀菌作用,而小于或等于0.25微克/毫升的最低抑菌浓度(MIC)值对光滑球拟酵母菌有最大作用。以纳克浓度计,联苯苄唑对白色念珠菌的增殖性皮肤癣菌和假菌丝有效。关于联苯苄唑的耐药情况良好——这是唑类抗真菌药的典型情况。在动物实验中,以乳膏或溶液形式局部应用浓度为0.05%至1%的联苯苄唑对豚鼠皮肤癣菌病极为有效。这归因于对皮肤癣菌可实现治疗性的杀菌作用以及该物质在皮肤中保留的长时间。联苯苄唑的这些实验特性使得推荐将活性药物作为1%乳膏或溶液每24小时应用一次,并且将这些适应症的治疗疗程缩短至2 - 3周成为可能。