Itraconazole: an update on pharmacology and clinical use for treatment of invasive and allergic fungal infections

Introduction: Fungal infections are a major source of global morbidity and mortality. Itraconazole is a triazole antifungal agent that is widely used for the prevention and treatment of fungal infection. While newer antifungal agents are now available, itraconazole is an orally bioavailable agent with broad-spectrum antifungal activity. Itraconazole remains a useful drug for the management of allergic and invasive mycoses worldwide. Areas covered: This article provides a summary of the pharmacokinetics, pharmacodynamics and clinical uses of itraconazole. Additionally, the authors summarise the safety and recently described toxicodynamics and discuss the value of therapeutic drug monitoring (TDM) with itraconazole. The following search criteria were constructed in order to identify relevant literature using PubMed and Ovid-MEDLINE: itraconazole, triazole, pharmacokinetics, pharmacodynamics, toxicodynamics and TDM. Relevant abstracts and articles identified from reviewing secondary citations were additionally retrieved and included if relevant. Expert opinion: Itraconazole remains an important agent in the prevention and treatment of fungal infection. Itraconazole has a broad-spectrum of activity and is available in both an intravenous and oral form making long-term use in chronic mycoses practical. Itraconazole is widely used for the treatment of endemic fungal infections. Pharmacokinetic variability and clinically important drug interactions make TDM of itraconazole an important consideration.