Wildfeuer A, Seidl H P, Paule I, Haberreiter A
Pfizer/Mack, Illertissen, Germany.
Mycoses. 1998 Sep-Oct;41(7-8):309-19. doi: 10.1111/j.1439-0507.1998.tb00344.x.
The in vitro activity of voriconazole (UK-109, 496), a new antifungal triazole derivative, against 650 clinical isolates of yeasts, moulds and dermatophytes was compared with that of itraconazole, ketoconazole, amphotericin B and griseofulvin. The geometric means of the minimum inhibitory concentrations (MICs) of voriconazole were 0.05 microgram ml-1 against yeasts (n = 187), 0.58 microgram ml-1 against moulds (n = 260) and 0.08 microgram ml-1 against dermatophytes (n = 203). The overall activity of voriconazole against yeasts and moulds was good, being similar to that of itraconazole, ketoconazole and amphotericin B. Voriconazole was highly effective against Aspergillus fumigatus (mean MIC 0.23 microgram ml-1) and other Aspergillus species and showed noteworthy activity (mean MICs 0.08-0.78 microgram ml-1) against emerging and less common clinical isolates of opportunistic moulds, such as Alternaria spp., Cladosporium spp., Acremonium spp., Chrysosporium spp. and Fusarium spp. On the other hand, voriconazole was less active in vitro than the comparative agents studied against various species of zygomycetes, such as Mucor spp., Rhizopus spp. and Absidia spp. Voriconazole and the other two azoles, itraconazole and ketoconazole, were more active than griseofulvin in vitro against most dermatophytes tested.
将新型抗真菌三唑衍生物伏立康唑(UK-109,496)对650株临床分离的酵母菌、霉菌和皮肤癣菌的体外活性与伊曲康唑、酮康唑、两性霉素B和灰黄霉素进行了比较。伏立康唑对酵母菌(n = 187)的最低抑菌浓度(MIC)几何平均值为0.05微克/毫升,对霉菌(n = 260)为0.58微克/毫升,对皮肤癣菌(n = 203)为0.08微克/毫升。伏立康唑对酵母菌和霉菌的总体活性良好,与伊曲康唑、酮康唑和两性霉素B相似。伏立康唑对烟曲霉(平均MIC 0.23微克/毫升)和其他曲霉菌种高度有效,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,显示出显著活性(平均MICs 0.08 - 0.78微克/毫升)。另一方面,伏立康唑在体外对各种接合菌,如毛霉属、根霉属和犁头霉属的活性低于所研究的对照药物。伏立康唑以及另外两种唑类药物伊曲康唑和酮康唑在体外对大多数测试的皮肤癣菌的活性高于灰黄霉素。