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[真菌病的治疗与新型抗真菌药物]

[Treatment of mycoses and new antifungal agents].

作者信息

Dupont B

出版信息

Rev Prat. 1989 Sep 1;39(19):1688-94.

PMID:2554481
Abstract

The multiplication of iatrogenic factors, nosocomial diseases and acquired immunodeficiency syndrome is responsible for an ever increasing number of deep opportunistic mycoses, namely candidiasis, aspergillosis and cryptococcosis. The advent of a wide variety of rare opportunistic fungi is a fairly recent and worrying phenomenon. To combat these infections, often very serious, our therapeutic armentarium is rather scanty. Moreover, the prescription of the available drugs is limited by their toxicity, their spectrum and their route of administration or by the emergence under treatment of resistant mutants. Beside old products, such as amphotericin B and 5-fluorocytosine, miconazole and, mainly ketoconazole (both azole derivatives) were the first steps towards oral administration and low toxicity. Fluconazole is a triazole antifungal compound with a very original distribution to the meninges and urinary tract; it is mainly used in candidiasis and cryptococcosis. Another triazole compound, itraconazole, presents the particularity of being active against Aspergillus spp., Cryptococcus spp. and some agents of exotic mycoses. These two products are well tolerated and should soon be available for use in deep visceral mycoses. Other azole derivatives are under study. Among compounds issued from new chemical families, terbinafine (allylamine) is particularly active against dermatophytes, and cilofungine (a polypeptide) against fungi. These drugs are in the experimental stage. Research should be pursued aimed at developing, probably in new chemical families, and agent that is fungicidal in vivo.

摘要

医源性因素、医院感染和获得性免疫缺陷综合征的增加导致深部机会性真菌病的数量不断上升,即念珠菌病、曲霉病和隐球菌病。各种各样罕见的机会性真菌的出现是一个相当新且令人担忧的现象。为了对抗这些通常非常严重的感染,我们的治疗药物相当匮乏。此外,现有药物的处方受到其毒性、抗菌谱、给药途径的限制,或者受到治疗过程中耐药突变体出现的限制。除了两性霉素B和5-氟胞嘧啶等老产品外,咪康唑,主要是酮康唑(两者均为唑类衍生物)是迈向口服给药和低毒性的第一步。氟康唑是一种三唑类抗真菌化合物,在脑膜和泌尿道的分布非常独特;它主要用于念珠菌病和隐球菌病。另一种三唑类化合物伊曲康唑具有对曲霉属、隐球菌属和一些罕见真菌病原体有效的特性。这两种产品耐受性良好,很快将可用于深部内脏真菌病的治疗。其他唑类衍生物正在研究中。在新化学家族的化合物中,特比萘芬(烯丙胺类)对皮肤癣菌特别有效,西洛芬净(一种多肽)对真菌有效。这些药物正处于实验阶段。应该继续进行研究,目标可能是开发新化学家族的一种在体内具有杀菌作用的药物。

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