Paradoxical response to itraconazole treatment in a patient with onychomycosis caused by Microsporum gypseum.

G Pierard-Franchimont, P De Doncker, V Van de Velde, P Jacqmin, J E Arrese, G E Pierard
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Abstract

A Columbian patient presented with a rare type of onychomycosis caused by Microsporum gypseum. Oral treatment with itraconazole formulation (Funazol) available in Columbia failed to improve the nail alteration. The fungitoxic effect of itraconazole was assessed on the M. gypseum strain cultured from the nail of the patient by using the method of culture of fungi on cyanoacrylate skin surface strippings (CSSS). In addition, a comparative evaluation of the oral bioavailability of itraconazole was made in volunteers after intake of Funazol and Sporanox. In the ex vivo bioassay on CSSS, topical itraconazole proved to be highly active against M. gypseum. After oral intake, however, the itraconazole bioavailability of Funazol relative to Sporanox averaged only 3.5%. Antifungal pulse therapy with Sporanox, 400 mg daily for 1 week per month for 4 months, cured the patient. This study shows that itraconazole is hardly or not absorbed from the oral formulation Funazol. Both the oral bioavailability and consequently therapeutic efficacy of the genuine drug (Sporanox) are highly superior.

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伊曲康唑治疗对石膏小孢子菌引起的甲癣的矛盾反应。
一个哥伦比亚病人提出了一种罕见的类型的甲癣引起的小孢子菌石膏。口服伊曲康唑制剂(Funazol)在哥伦比亚没有改善指甲改变。采用氰基丙烯酸酯皮肤表面剥落培养法(CSSS)评价伊曲康唑对患者指甲培养的石膏分枝杆菌的真菌毒性作用。另外,对伊曲康唑口服生物利用度进行了对比评价,并对志愿者服用Funazol和Sporanox后的口服生物利用度进行了比较。体外生物实验表明,外用伊曲康唑对真菌有较强的抑制作用。口服后,Funazol相对于Sporanox的伊曲康唑生物利用度平均仅为3.5%。用Sporanox脉冲抗真菌治疗,每日400毫克,每月1周,连续4个月,治愈患者。本研究表明伊曲康唑在口服制剂Funazol中几乎或不被吸收。无论是口服生物利用度和因此的治疗效果的正品药物(Sporanox)是非常优越的。
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