Uptake of itraconazole by alveolar macrophages.
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.
Department of Medicine, Duke University Medical Center, Durham, North Carolina 27710.
J R
JR
Perfect
D V
DV
Savani
D T
DT
Durack
D000818:Animals; D000935:Antifungal Agents / Q000493:pharmacokinetics*; D002981:Clindamycin / Q000493:pharmacokinetics; D015169:Colony Count, Microbial; D004912:Erythrocytes / Q000378:metabolism; D066298:In Vitro Techniques; D017964:Itraconazole; D007654:Ketoconazole / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D016676:Macrophages, Alveolar / Q000378:metabolism*; D009163:Mycobacterium bovis / Q000187:drug effects; D011817:Rabbits
D000935:Antifungal Agents; D017964:Itraconazole; D002981:Clindamycin; D007654:Ketoconazole