Beggs W H
Antimicrob Agents Chemother. 1984 Nov;26(5):699-701. doi: 10.1128/AAC.26.5.699.
It was shown that tioconazole possesses an important property not shared by ketoconazole and miconazole, its well-known relatives in the imidazole group of antifungal drugs. At a concentration of 3.8 X 10(-5) M, tioconazole, like miconazole, caused rapid 2- to 3-log reductions in CFU per milliliter when added to late-logarithmic-phase Candida albicans or Candida parapsilosis cells. Only tioconazole, however, exerted similar reductions when added to diluted stationary-phase cultures. This growth-phase-independent lethal action has important clinical implications and may explain the superior performance of tioconazole, which was observed in earlier comparative drug studies.
结果表明,噻康唑具有酮康唑和咪康唑所没有的重要特性,后两者是咪唑类抗真菌药物中噻康唑的著名同类物。在浓度为3.8×10⁻⁵ M时,噻康唑与咪康唑一样,当添加到对数生长期后期的白色念珠菌或近平滑念珠菌细胞中时,可使每毫升菌落形成单位迅速减少2至3个对数。然而,只有噻康唑在添加到稀释的稳定期培养物中时能产生类似的减少效果。这种不依赖生长阶段的致死作用具有重要的临床意义,可能解释了噻康唑在早期药物对比研究中观察到的优越性能。