Perfect J R, Savani D V, Durack D T
Department of Medicine, Duke University Medical Center, Durham, North Carolina 27710.
Antimicrob Agents Chemother. 1993 Apr;37(4):903-4. doi: 10.1128/AAC.37.4.903.
Itraconazole is a broad-spectrum potent triazole antifungal agent. Its efficacy in treatment cannot always be explained by body fluid drug levels. In this study, itraconazole was shown to accumulate into host cells. Its intracellular accumulation in cells is greater than that of the antibacterial agent clindamycin, which is known for intracellular localization, and the uptake process does not appear to be active. This ability to reach high concentrations intracellularly may be an important property for the in vivo efficacy of itraconazole.
伊曲康唑是一种广谱强效三唑类抗真菌药。其治疗效果并不总能通过体液药物水平来解释。在本研究中,伊曲康唑被证明可在宿主细胞中蓄积。其在细胞内的蓄积量大于以细胞内定位而闻名的抗菌药物克林霉素,且摄取过程似乎并非主动摄取。这种在细胞内达到高浓度的能力可能是伊曲康唑体内疗效的一项重要特性。