Van Cutsem J
Department of Bacteriology and Mycology, Janssen Research Foundation, Beerse, Belgium.
Br J Clin Pract Suppl. 1990 Sep;71:32-40.
Itraconazole has been tested in vitro against 6,113 different strains of a total of 252 fungal species. Almost all medically important fungi are apparently sensitive to itraconazole. Topical and oral treatment with itraconazole was found to be successful in microsporosis, trichophytosis, vulvovaginal, gastrointestinal and systemic candidosis, pityrosporosis, sporotrichosis, histoplasmosis, aspergillosis and cryptococcosis induced in a number of animal models. Vulvovaginal candidosis responded well to itraconazole, with a one-day topical or oral treatment resulting in a complete cure. The same results could not be achieved with the same concentration or dosage of either ketoconazole or fluconazole. Biologically active antifungal levels were present in plasma and vaginal fluid of rats after one dose of itraconazole 10 mg/kg for at least 72 hours. Itraconazole was also found to be successful in immunodepressed animals infected with a number of different diseases and in disseminated and systemic infections, such as candidosis, aspergillosis and cryptococcosis. Oral and parenteral itraconazole treatment was compared with oral and parenteral fluconazole treatment and parenteral amphotericin B in a number of models. Results overall were better with itraconazole. Combination therapy of itraconazole with fluconazole was not found to be superior to treatment with itraconazole alone. No side-effects were observed with itraconazole treatment.
伊曲康唑已在体外针对总共252种真菌的6113个不同菌株进行了测试。几乎所有具有医学重要性的真菌显然都对伊曲康唑敏感。在多种动物模型中诱发的微孢子虫病、毛癣菌病、外阴阴道念珠菌病、胃肠道念珠菌病和全身性念珠菌病、糠秕孢子菌病、孢子丝菌病、组织胞浆菌病、曲霉病和隐球菌病,采用伊曲康唑进行局部和口服治疗均获成功。外阴阴道念珠菌病对伊曲康唑反应良好,一日的局部或口服治疗即可实现完全治愈。使用相同浓度或剂量的酮康唑或氟康唑则无法取得相同的效果。大鼠单次服用10 mg/kg伊曲康唑后,血浆和阴道液中至少72小时内都存在具有生物活性的抗真菌水平。伊曲康唑在感染多种不同疾病的免疫抑制动物以及播散性和全身性感染(如念珠菌病、曲霉病和隐球菌病)中也被证明是成功的。在多个模型中,对伊曲康唑的口服和胃肠外治疗与氟康唑的口服和胃肠外治疗以及胃肠外两性霉素B进行了比较。总体结果显示伊曲康唑更佳。未发现伊曲康唑与氟康唑联合治疗优于单独使用伊曲康唑治疗。伊曲康唑治疗未观察到副作用。