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伏立康唑与氟康唑、两性霉素B和灰黄霉素相比,对酵母、霉菌和皮肤癣菌的体外活性。

In vitro activity of voriconazole against yeasts, moulds and dermatophytes in comparison with fluconazole, amphotericin B and griseofulvin.

作者信息

Wildfeuer A, Seidl H P, Paule I, Haberreiter A

机构信息

Pfizer/Mack, Illertissen, Germany.

出版信息

Arzneimittelforschung. 1997 Nov;47(11):1257-63.

PMID:9428984
Abstract

Voriconazole (CAS 137234-62-9, UK-109,496), a new antifungal triazole derivative, was studied in vitro against 650 clinical isolates, representing yeasts, moulds and dermatophytes, and was compared with fluconazole (CAS 86386-73-4), amphotericin B (CAS 1397-89-3), and griseofulvin (CAS 126-07-8). The mean minimum inhibitory concentrations (MICs) of voriconazole were 0.06 microgram/ml against yeasts (n = 187), 0.74 microgram/ml against moulds (n = 260) and 0.10 microgram/ml against dermatophytes (n = 203). Data from these in vitro studies showed that voriconazole was more potent than fluconazole against most species studied, but particularly against the isolates of moulds and dermatophytes. Overall, voriconazole and amphotericin B indicated comparably good activity against yeasts and moulds. Voriconazole was highly potent against 13 Aspergillus species studied (mean MIC 0.35 microgram/ml) and also showed noteworthy activity (mean MICs 0.08-0.78 microgram/ml) against emerging and less common clinical isolates of opportunistic moulds such as of Alternaria spp., Cladosporium spp., Acremonium spp., Chrysosporium spp., and Fusarium spp. In addition, voriconazole was more active in vitro than griseofulvin against most dermatophytes tested. The in vitro results confirmed that voriconazole has indeed a broad antifungal spectrum and could also be effective against a wide range of fungal infections in patients.

摘要

伏立康唑(CAS 137234-62-9,UK-109,496)是一种新型抗真菌三唑衍生物,对650株临床分离株进行了体外研究,这些分离株包括酵母菌、霉菌和皮肤癣菌,并与氟康唑(CAS 86386-73-4)、两性霉素B(CAS 1397-89-3)和灰黄霉素(CAS 126-07-8)进行了比较。伏立康唑对酵母菌(n = 187)的平均最低抑菌浓度(MIC)为0.06微克/毫升,对霉菌(n = 260)为0.74微克/毫升,对皮肤癣菌(n = 203)为0.10微克/毫升。这些体外研究数据表明,伏立康唑对大多数研究的菌种比氟康唑更有效,尤其是对霉菌和皮肤癣菌的分离株。总体而言,伏立康唑和两性霉素B对酵母菌和霉菌显示出相当好的活性。伏立康唑对所研究的13种曲霉菌种具有高效活性(平均MIC为0.35微克/毫升),对新兴的和较少见的机会性霉菌临床分离株如链格孢属、枝孢属、顶孢属、金孢子菌属和镰刀菌属也显示出显著活性(平均MIC为0.08 - 0.78微克/毫升)。此外,伏立康唑在体外对大多数测试的皮肤癣菌比灰黄霉素更具活性。体外研究结果证实,伏立康唑确实具有广泛的抗真菌谱,对患者的多种真菌感染也可能有效。

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