International Clinical Research and Development, Janssen Research Foundation, B-2340 Beerse, Belgium.
Int J Antimicrob Agents. 1996 Feb;6(3):175-81. doi: 10.1016/0924-8579(95)00043-7.
Itraconazole is an orally active, broad-spectrum, triazole antifungal agent which has a higher affinity for fungal cytochrome P-450 than ketoconazole but a low affinity for mammalian cytochrome P-450. Itraconazole has a broader spectrum of activity than other azole antifungals and shows interesting pharmacokinetic features in terms of its tissue distribution. These properties have resulted in reduced treatment times for a number of diseases such as vaginal candidiasis, as well as effective oral treatment of several deep mycoses, including aspergillosis and candidiasis. Currently itraconazole is registered in 42 countries for the treatment of systemic fungal infections. Further development is concentrating on antifungal prophylaxis as well as on an oral solution and an intravenous formulation.
伊曲康唑是一种具有口服活性、广谱的三唑类抗真菌药物，与酮康唑相比，它对真菌细胞色素 P-450 的亲和力更高，但对哺乳动物细胞色素 P-450 的亲和力较低。伊曲康唑的活性谱比其他唑类抗真菌药物更广，并且在其组织分布方面表现出有趣的药代动力学特征。这些特性导致许多疾病（如阴道念珠菌病）的治疗时间缩短，并且有效治疗了几种深部真菌感染，包括曲霉病和念珠菌病。目前，伊曲康唑已在 42 个国家注册用于治疗系统性真菌感染。进一步的开发集中在抗真菌预防以及口服溶液和静脉注射制剂上。
