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两种甲癣局部治疗药物的特性与疗效

Characteristics and Efficacy of Two Topical Therapeutic Agents for Onychomycosis.

作者信息

Kawai Masaaki

机构信息

Department of Dermatology, Juntendo University Koshigaya Hospital.

出版信息

Med Mycol J. 2019;60(3):71-74. doi: 10.3314/mmj.19.006.

DOI:10.3314/mmj.19.006
PMID:31474693
Abstract

Tinea pedis and tinea unguium are the most common dermatophytoses seen in the daily practice of dermatology. According to a report in Japan Foot Week 2006, it is estimated that about 1 in 5 Japanese have tinea pedis and that about 1 in 10 have tinea unguium. Thus far, use of oral antifungal agents has been the first-line therapy for onychomycosis. Many patients with onychomycosis, however, are elderly and have concomitant diseases as well as liver function disorder. Moreover, oral medications are reportedly associated with risks of impaired liver function and interactions. Due to such risks, therefore, treatment with topical agents is the only applicable therapy for most patients with onychomycosis. Recently, two topical agents (efinaconazole in 2014 and luliconazole in 2016) have been approved for the treatment of onychomycosis in Japan. Efinaconazole 10% solution is a triazole antifungal drug developed in Japan. Due to its low keratin affinity, efinaconazole shows high transungual penetration into nails and retains a high antifungal activity in the nail plate and the nail bed. Luliconazole 5% solution is an imidazole antifungal agent that has high keratin affinity. Luliconazole has also been shown in vitro to permeate from the superficial to the deep layers of the nail and to achieve concentrations above the MIC in all layers of the nail. Both efinaconazole 10% solution and luliconazole 5% solution have high antifungal activities for Trichophyton species. These two topical agents, therefore, have certainly increased treatment options for onychomycosis in the daily practice of dermatology.

摘要

足癣和甲癣是皮肤科日常诊疗中最常见的皮肤癣菌病。根据《2006年日本足部健康周》的一份报告,估计每5个日本人中就有1人患有足癣,每10人中有1人患有甲癣。迄今为止,口服抗真菌药物一直是甲癣的一线治疗方法。然而,许多甲癣患者年事已高,伴有其他疾病以及肝功能障碍。此外,据报道口服药物存在肝功能损害风险和相互作用。因此,由于这些风险,局部用药是大多数甲癣患者唯一适用的治疗方法。最近,两种局部用药(2014年的艾氟康唑和2016年的卢立康唑)已在日本获批用于治疗甲癣。10%的艾氟康唑溶液是一种在日本研发的三唑类抗真菌药物。由于其对角蛋白的亲和力较低,艾氟康唑能高效透过指甲进入甲床,并在甲板和甲床中保持较高的抗真菌活性。5%的卢立康唑溶液是一种对角蛋白亲和力较高的咪唑类抗真菌剂。体外研究表明,卢立康唑也能从指甲表层渗透到深层,并在指甲各层达到高于最低抑菌浓度的水平。10%的艾氟康唑溶液和5%的卢立康唑溶液对毛癣菌属均具有较高的抗真菌活性。因此,这两种局部用药无疑增加了皮肤科日常诊疗中甲癣的治疗选择。

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1
Characteristics and Efficacy of Two Topical Therapeutic Agents for Onychomycosis.两种甲癣局部治疗药物的特性与疗效
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[Comparison of Characteristics of Two Topical Therapeutic Agents for Onychomycosis].[两种甲癣局部治疗药物的特性比较]
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The low keratin affinity of efinaconazole contributes to its nail penetration and fungicidal activity in topical onychomycosis treatment.艾氟康唑对角蛋白的低亲和力有助于其在局部甲真菌病治疗中的指甲穿透性和杀菌活性。
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Efficacy Coefficients Determined Using Nail Permeability and Antifungal Activity in Keratin-Containing Media Are Useful for Predicting Clinical Efficacies of Topical Drugs for Onychomycosis.在含角蛋白介质中利用指甲渗透性和抗真菌活性确定的疗效系数,有助于预测外用药物治疗甲真菌病的临床疗效。
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