Van Cauteren H, Heykants J, De Coster R, Cauwenbergh G
Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S43-6. doi: 10.1093/clinids/9.supplement_1.s43.
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.
对口服活性抗真菌三唑类药物伊曲康唑进行了多项人体和动物药理学研究。在犬和大鼠中,剂量高达40mg/kg时未见明显毒性作用。内分泌学研究表明,与酮康唑不同,伊曲康唑对人体睾丸和肾上腺类固醇生成无明显影响。药代动力学研究表明,伊曲康唑具有较高的组织亲和力,半衰期比酮康唑长。这些药理学观察结果表明,伊曲康唑比酮康唑具有更广泛的活性谱,产生不良反应的可能性更低。