Birnbaum J E
Sandoz Research Institute, East Hanover, NJ 07936.
J Am Acad Dermatol. 1990 Oct;23(4 Pt 2):782-5. doi: 10.1016/0190-9622(90)70288-s.
The allylamines are a new class of antifungal drugs that inhibit ergosterol synthesis at the level of squalene epoxidase. These agents are highly selective for the fungal enzyme and have a minimal effect on mammalian cholesterol synthesis. Naftifine, the original member of the allylamine series, possesses only topical activity, whereas the naftifine analog terbinafine is active both topically and orally. In vitro, terbinafine is exceptionally active against dermatophytes, molds, and dimorphic fungi in which it exerts a fungicidal action. This in vitro profile is reflected by the clinical effectiveness of this allylamine in the treatment of dermatophyte infections. When given orally, terbinafine is well absorbed and rapidly and extensively distributed to the skin and sebum in concentrations that exceed the minimum inhibitory concentrations of these organisms by several orders of magnitude.
烯丙胺类是一类新型抗真菌药物，可在角鲨烯环氧化酶水平抑制麦角固醇合成。这些药物对真菌酶具有高度选择性，对哺乳动物胆固醇合成影响极小。萘替芬是烯丙胺类系列的首个成员，仅具有局部活性，而萘替芬类似物特比萘芬则兼具局部和口服活性。在体外，特比萘芬对皮肤癣菌、霉菌和双相真菌具有极强活性，可发挥杀真菌作用。该烯丙胺类药物在治疗皮肤癣菌感染方面的临床疗效反映了其体外活性。口服时，特比萘芬吸收良好，能迅速且广泛地分布至皮肤和皮脂中，其浓度比这些病原体的最低抑菌浓度高出几个数量级。
