[Interactions of fluconazole and phagocytic cells]

Fluconazole is a triazole compound with a coefficient of distribution P at pH 7.4 of 1.6 (log P = 0.2), and has thus both hydrophilic and lipophilic properties. The physicochemical and pharmacokinetic profiles of fluconazole are clearly different from those of other azole antimycotics. 3H-labelled fluconazole penetrates very rapidly into granulocytes and monocytes (macrophages) isolated from volunteers. The concentrations of the triazole in the granulocytes are about 28% and in the macrophages about 63% higher than in the extracellular milieu. At the concentrations examined (5, 10 and 20 micrograms ml-1) fluconazole damages cells of Candida albicans which have been phagocytized by granulocytes or by macrophages. A clear synergy between fluconazole and the phagocytes can be demonstrated.