Ghannoum Mahmoud
J Am Podiatr Med Assoc. 2016 Jan-Feb;106(1):79-86. doi: 10.7547/14-109.
Azole antifungal agents (eg, fluconazole and itraconazole) have been widely used to treat superficial fungal infections caused by dermatophytes and, unlike the allylamines (such as terbinafine and naftifine), have been associated with resistance development. Although many published manuscripts describe resistance to azoles among yeast and molds, reports describing resistance of dermatophytes are starting to appear. In this review, I discuss the mode of action of azole antifungals and mechanisms underlying their resistance compared with the allylamine class of compounds. Data from published and original studies were compared and summarized, and their clinical implications are discussed. In contrast to the cidal allylamines, static drugs such as azoles permit the occurrence of mutations in enzymes involved in ergosterol biosynthesis, and the ergosterol precursors accumulating as a consequence of azole action are not toxic. Azole antifungals, unlike allylamines, potentiate resistance development in dermatophytes.
唑类抗真菌药(如氟康唑和伊曲康唑)已被广泛用于治疗皮肤癣菌引起的浅表真菌感染,并且与烯丙胺类药物(如特比萘芬和萘替芬)不同,它们与耐药性的产生有关。尽管许多已发表的手稿描述了酵母菌和霉菌对唑类药物的耐药性,但描述皮肤癣菌耐药性的报告也开始出现。在这篇综述中,我将讨论唑类抗真菌药的作用方式以及与烯丙胺类化合物相比其耐药性的潜在机制。对已发表研究和原始研究的数据进行了比较和总结,并讨论了其临床意义。与具有杀菌作用的烯丙胺类药物不同,唑类等抑菌药物会使参与麦角甾醇生物合成的酶发生突变,并且由于唑类药物的作用而积累的麦角甾醇前体没有毒性。与烯丙胺类药物不同,唑类抗真菌药会增强皮肤癣菌的耐药性发展。