Pharmacokinetic Optimization of Itraconazole Therapy


Lewis RE

Date: 16 April 2002


Itraconazole is a broad-spectrum triazole antifungal with clinically useful activity against both superficial and systemic mycoses including Aspergillus species. In the past, the role of itraconazole in the treatment of invasive aspergillosis was limited by the erratic bioavailability of the oral capsule formulation in immunocompromised patients. The reformulation of itraconazole with hydroxypropyl-àŸ-cyclodextrin into an oral and intravenous solution, however, has revitalized the role of this antifungal in the treatment of fungal infections in critically-ill patients. Even with these new formulations, predicting an appropriate dosage of itraconazole for the individual patient remains problematic due to the considerable intra- and inter-patient variability of itraconazole pharmacokinetics. This monograph reviews key biopharmaceutical and pharmacokinetic concepts clinicians need to understand in order to individualize and optimize itraconazole dosing in a patients with invasive fungal infections.

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