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盐酸布替萘芬:用于治疗足趾间足癣。

Butenafine hydrochloride: for the treatment of interdigital tinea pedis.

作者信息

Syed T A, Maibach H I

机构信息

Department of Dermatology, University of California San Francisco, Box 0989, 90 Medical Center Way, Surge Building 110, San Francisco, CA 94143-0989, USA.

出版信息

Expert Opin Pharmacother. 2000 Mar;1(3):467-73. doi: 10.1517/14656566.1.3.467.

Abstract

Butenafine, a derivative of benzylamine with potent fungicidal activity is a new generation of antimycotic compound that has shown to be extremely effective against experimentally-induced tinea pedis in the guinea-pig, a situation that resembles synergetic pathology similar to that of tinea pedis in humans. Butenafine, (N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethyl-amine hydrochloride) with a chemical structure and mode of action similar to those of the allylamines, demonstrates superior fungicidal activity in vitro against dermatophytes and superior fungistatic activity toward Candida albicans that of naftifine and terbinafine. In vitro, pharmacodynamic data has shown that the geometric mean of minimum inhibitory concentration values for butenafine were comparatively lower than those of naftifine and clotrimazole against clinical isolates for many dermatophytes. It inhibits sterol synthesis by blocking the squalene epoxidation stage in fungi. In phramacokinetic assessments butenafine achieves and maintains high concentrations and long retention time in skin, with associated anti-inflammatory activity in vivo. In controlled clinical trials when applied topically, butenafine appears to be well tolerated with a subjective mild burning sensation at the application site. There were no withdrawals from the study. Butenafine is sparingly soluble in water but readily soluble in methanol, ethanol, dichloromethane and chloroform. If incorporated properly in semisolid topical preparations, with a balanced vehicle, butenafine hydrochloride potentially exhibits as a promising alternative antimycotic agent for the treatment of tinea pedis.

摘要

布替萘芬是一种具有强大杀真菌活性的苄胺衍生物,是新一代抗真菌化合物,已证明对豚鼠实验性足癣极为有效,这种情况类似于人类足癣的协同病理。布替萘芬(N - 4 - 叔丁基苄基 - N - 甲基 - 1 - 萘甲基胺盐酸盐)的化学结构和作用方式与烯丙胺类相似,在体外对皮肤癣菌显示出卓越的杀真菌活性,对白色念珠菌的抑菌活性优于萘替芬和特比萘芬。体外药效学数据表明,布替萘芬对许多皮肤癣菌临床分离株的最低抑菌浓度值的几何平均值相对低于萘替芬和克霉唑。它通过阻断真菌中的角鲨烯环氧化阶段来抑制甾醇合成。在药代动力学评估中,布替萘芬在皮肤中能达到并维持高浓度和较长的保留时间,在体内具有相关的抗炎活性。在对照临床试验中,局部应用布替萘芬似乎耐受性良好,应用部位有轻微的主观烧灼感。没有患者退出该研究。布替萘芬微溶于水,但易溶于甲醇、乙醇、二氯甲烷和氯仿。如果以平衡的载体适当地掺入半固体局部制剂中,盐酸布替萘芬有可能成为治疗足癣的一种有前景的替代抗真菌药物。

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