Itraconazole: Pharmacologic Studies in Animals and Humans

Abstract

Several pharmacologic studies of itraconazole, an orally active antifungal triazole, were conducted in humans and animals. In dogs and rats, no significant toxic effects were seen at doses of up to 40 mg/kg. Endocrinologic studies demonstrated that itraconazole, unlike ketoconazole, does not significantly affect human testicular and adrenal steroidogenesis. Pharmacokinetic studies indicated that itraconazole has a high tissue affinity and a longer half-life than ketoconazole. These pharmacologic observations suggest that itraconazole has a broader spectrum of activity than ketoconazole and a lower potential for producing adverse effects.