The pharmacokinetics of itraconazole in animals and man: an overview
Heykants, J.; Michiels, M.; Meuldermans, W.; Monbaliu, J.; Lavrijsen, K.; Peer, A. van; Levron, J.C.; Woestenborghs, R.; Cauwenbergh, G.
Recent trends in the discovery, development and evaluation of antifungal agents: 223-249
Itraconazole is a triazole antifungal agent with pronounced lipophilic properties. This physicochemical property determines to a large extent the pharmacokinetics of itraconazole and differentiates it from the more hydrophilic agent, ketoconazole. The pharmacokinetics of itraconazole in animals and man are characterized by a good oral absorption, an extensive tissue distribution with tissue concentrations many times higher than in plasma, a relatively long elimination halflife of about one day in man and a biotransformation into a large number of (antifungal) inactive metabolites. Unlike most other antifungal drugs, itraconazole does not interfere with mammalian drug metabolizing enzymes, minimizing the risk of interaction with concomitantly administered drugs and suggesting a lower risk for hepatic reactions. These pharmacokinetic properties of itraconazole may contribute to the higher efficacy and improved safety of this drug in animal models and in patients with various mycotic infections.