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新型抗真菌药物:伏立康唑与卡泊芬净

[New antifungal agents: voriconazole and caspofungin].

作者信息

Dupont B

机构信息

Hôpital Necker, maladies infectieuses et tropicales, 149, rue de Sèvres, 75015 Paris, France.

出版信息

Arch Pediatr. 2003 Dec;10 Suppl 5:592s-598s. doi: 10.1016/s0929-693x(03)90043-1.

Abstract

Among new available antifungal agents voriconazole is a new triazole with an intravenous (i.v.) and oral formulation, and caspofungin is an echinocandin, new family with a new mode of action on the cell wall. It is available as an i.v. preparation. Both drugs have a broad spectrum targeting most of the usual pathogens: Candida and Aspergillus, even with low suceptibility or resistance to other antifungals. Voriconazole is also active on Scedosporium and Fusarium. The efficacy of these molecules was established in vitro and in experimental infections in animals either normal or immunosuppressed. Voriconazole is active in oropharyngeal and esophageal candidiasis, in refractory invasive candidiasis and as a first line treatment of invasive aspergillosis with better results than amphotéricine B. It was also effective in scedosporiosis and in fusariosis. Caspofungin is active in oropharyngeal and esophageal candidiasis, in invasive candidiasis ranking among the best drugs in non neutropenic patients. It was shown effective in refractory aspergillosis. As empirical treatment of febrile neutropenic patients, these molecules should probably be restricted to the highest risk-population. Safety is good, side effects are a rare cause of discontinuation of treatment, class specific drug-drug interactions occur with voriconazole. These molecules open an important field of investigations with combination of antifungal agents.

摘要

在新出现的抗真菌药物中,伏立康唑是一种新型三唑类药物,有静脉注射和口服两种剂型,卡泊芬净是一种棘白菌素,属于作用于细胞壁的新型药物家族。它只有静脉注射制剂。这两种药物都有广谱抗菌作用,针对大多数常见病原体:念珠菌和曲霉菌,即使对其他抗真菌药物敏感性低或耐药。伏立康唑对波氏假阿利什霉和镰刀菌也有活性。这些分子的疗效已在体外以及正常或免疫抑制动物的实验性感染中得到证实。伏立康唑对口咽和食管念珠菌病、难治性侵袭性念珠菌病有效,作为侵袭性曲霉病的一线治疗药物,效果优于两性霉素B。它对波氏假阿利什霉病和镰刀菌病也有效。卡泊芬净对口咽和食管念珠菌病、侵袭性念珠菌病有效,在非中性粒细胞减少患者中是最佳药物之一。它对难治性曲霉病也有效。作为发热性中性粒细胞减少患者的经验性治疗,这些药物可能应仅限于高危人群。安全性良好,副作用很少导致停药,伏立康唑会发生特定类别的药物相互作用。这些药物开启了抗真菌药物联合应用的重要研究领域。

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