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布替萘芬

Butenafine.

作者信息

McNeely W, Spencer C M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1998 Mar;55(3):405-12; discussion 413. doi: 10.2165/00003495-199855030-00006.

Abstract

Butenafine is a new antifungal agent with primary fungicidal activity against dermatophytes such as Trichophyton mentagrophytes, Microsporum canis and Trichophyton rubrum which cause tinea infections. 14C-labelled butenafine (approximately 30 micrograms/g tissue) was found within guinea-pig dorsal skin 24 hours after topical application. Most of the drug was distributed into the epidermis including the horny layer. Small amounts were found in the dermis, probably transported via sebaceous glands and hair follicles. In vitro, the minimum concentration that completely inhibited growth of dermatophytes (MIC) and the minimum fungicidal concentrations (MFC) for butenafine against T. mentagrophytes and M. canis were similar (0.012 to 0.05 mg/L) and were 4 to 130 times lower than those for naftifine, tolnaftate, clotrimazole and bifonazole. It also has greater activity against T. rubrum, M. gypseum and Epidermophyton floccosum when compared with naftifine, tolnaftate and clotrimazole; comparisons with bifonazole against these strains were not available. Assessment after 1 week's treatment in patients with tinea pedis revealed that mycological cure rates were greater in those who received twice-daily butenafine for 1 week or once-daily butenafine for 4 weeks than in placebo recipients. Mycological and overall cure rates were either further increased or maintained up to 5 weeks after treatment cessation compared with end-of-treatment values. In patients with tinea cruris or tinea corporis who received once-daily butenafine 1% for 2 weeks, the mycological and overall cure rates continued to increase for up to 4 weeks after treatment cessation.

摘要

布替萘芬是一种新型抗真菌药,对引起癣感染的皮肤癣菌如须癣毛癣菌、犬小孢子菌和红色毛癣菌具有主要的杀真菌活性。局部应用后24小时,在豚鼠背部皮肤中发现了14C标记的布替萘芬(约30微克/克组织)。大部分药物分布到包括角质层在内的表皮中。在真皮中发现少量药物,可能是通过皮脂腺和毛囊转运的。在体外,布替萘芬对须癣毛癣菌和犬小孢子菌的完全抑制皮肤癣菌生长的最低浓度(MIC)和最低杀菌浓度(MFC)相似(0.012至0.05毫克/升),比萘替芬、托萘酯、克霉唑和联苯苄唑低4至130倍。与萘替芬、托萘酯和克霉唑相比,它对红色毛癣菌、石膏样小孢子菌和絮状表皮癣菌也具有更强的活性;未进行与联苯苄唑针对这些菌株的比较。足癣患者治疗1周后的评估显示,接受每日两次布替萘芬治疗1周或每日一次布替萘芬治疗4周的患者的真菌学治愈率高于安慰剂组。与治疗结束时的值相比,治疗停止后长达5周,真菌学和总体治愈率进一步提高或维持。在接受1%布替萘芬每日一次治疗2周的股癣或体癣患者中,治疗停止后长达4周,真菌学和总体治愈率持续上升。

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