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伊曲康唑在正常和免疫功能低下动物中的口服、局部和胃肠外抗真菌治疗。

Oral, topical and parenteral antifungal treatment with itraconazole in normal and in immunocompromised animals.

作者信息

Van Cutsem J

出版信息

Mycoses. 1989;32 Suppl 1:14-34. doi: 10.1111/j.1439-0507.1989.tb02291.x.

Abstract

Itraconazole was dissolved in polyethylene glycol for oral and topical treatment and in hydroxypropyl-beta-cyclodextrin for oral, topical or parenteral treatment. Topical and oral treatment was successful in microsporosis, trichophytosis, skin-and vaginal candidosis, pityrosporosis and eye mycosis by Candida, Fusarium and Aspergillus. Vaginal candidosis could be cured with a one-day topical or oral treatment. The same results could not be obtained with any of the reference compounds (griseofulvin, terbinafine, ketoconazole or fluconazole) on a mg per kg body weight base, nor on a % concentration base. Antifungal levels were determined by bioassay: biologically active antifungal levels were present in plasma and vaginal fluid of rats, after one oral dose of 10 mg.kg-1, for at least 72 and 96 hours respectively. This was in good correlation with findings on prophylaxis of vaginal candidosis. Itraconazole was also successfully used, in normal animals and animals immunodepressed with various agents, in disseminated and systemic diseases: trichophytosis, sporotrichosis, histoplasmosis, candidosis, aspergillosis and cryptococcosis. Oral and parenteral treatment with itraconazole was compared in various models to oral and parenteral fluconazole and to parenteral amphotericin B. The outcome with itraconazole was better than with the other antifungals. Meningeal cryptococcosis responded very well to itraconazole. Combination therapy of itraconazole and fluconazole was not superior to treatment with itraconazole alone. No side-effects were observed in relation to itraconazole treatment.

摘要

伊曲康唑溶解于聚乙二醇用于口服和局部治疗,溶解于羟丙基-β-环糊精用于口服、局部或肠胃外治疗。局部和口服治疗对念珠菌、镰刀菌和曲霉菌引起的小孢子菌病、毛癣菌病、皮肤和阴道念珠菌病、糠秕孢子菌病和眼部真菌病均有效。阴道念珠菌病采用一日局部或口服治疗即可治愈。以每千克体重毫克数或浓度百分比为基准,任何一种对照化合物(灰黄霉素、特比萘芬、酮康唑或氟康唑)均无法取得同样的效果。通过生物测定法测定抗真菌水平:大鼠口服10mg.kg-1的剂量后,血浆和阴道液中分别至少在72小时和96小时内存在生物活性抗真菌水平。这与阴道念珠菌病预防的研究结果高度相关。伊曲康唑在正常动物和用各种药物免疫抑制的动物中,也成功用于治疗播散性和全身性疾病:毛癣菌病、孢子丝菌病、组织胞浆菌病、念珠菌病、曲霉菌病和隐球菌病。在各种模型中,对伊曲康唑的口服和肠胃外治疗与氟康唑的口服和肠胃外治疗以及两性霉素B的肠胃外治疗进行了比较。伊曲康唑的治疗效果优于其他抗真菌药物。脑膜隐球菌病对伊曲康唑反应良好。伊曲康唑和氟康唑联合治疗并不优于单独使用伊曲康唑治疗。未观察到与伊曲康唑治疗相关的副作用。

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