部分中文艾氟康唑处方资料（仅供参考）

英文名：Luliconazole

商品名：LUCONAC Solution 5%

中文名：卢立康唑

生产商：佐藤製薬

药品简介

药物分类名称

治疗甲癣

批准日期：2016年4月 

一般名

ルリコナゾール（JAN）Luliconazole（JAN, INN）

化学名

(-)-(E)-[(4R)-4-(2,4-dichlorophenyl)-1,3-dithiolan-2-ylidene](1H-imidazol-1-yl)acetonitrile

構造式

分子式

C14H9Cl2N3S2 

分子量

354.28

性状

本品为淡黄色至淡黄色结晶或结晶性粉末，易溶于N，N-二甲基甲酰胺或丙酮，微溶于乙腈或甲醇，微溶于乙醇（99.5），难溶于水 它不会融化。

它随着光逐渐变色。

熔点

150 - 153°C

处理注意事项

1.打开盖子后，拧紧盖子并保存。

2.勿让儿童接触。

3.小心，因为它可能会在连接到衣服时染成黄色。

4.小心软化合成树脂或熔化油漆。

5.由于本产品易燃，请避免在使用和储存过程中使用火。

（火灾危险禁止第一次石油风险等级II）

批准条件

制定药品风险管理计划并适当实施。

药用药理学

1.抗真菌作用

（1）抗真菌活性（体外）Ruliconazole对红色毛癣菌和须癣毛癣菌显示出抗真菌（MIC）和杀真菌（MCC）活性，毛癣菌是甲癣的主要致病菌。

（2）使用人体甲真菌病模型的药理学试验（体外）在切除的人体指甲的下指甲上感染T. meningagrophytes后，该药物在指甲板的上侧每天重复施用一次，持续7天。确认来自细菌体的ATP量减少。

2.作用机理9）由于麦角甾醇的合成抑制作用，Ruliconazole表现出抗真菌作用，麦角甾醇是真菌细胞膜的组成部分。

适应症

・适应性真菌种类

皮肤癣菌（毛癣菌）

・适应症

甲癣

用法与用量

每天一次涂抹在整个受影响的指甲上。

包装

3.5g（4mL）×5,3.5g（4mL）×10

（塑料容器）

生产商

佐藤製薬株式会社

完整治疗资料附件：http://www.info.pmda.go.jp/go/pack/6290703Q1023_1_03/

Luliconazole's nail external solution 5% Ruconac: high concentration external medication effective for tinea unguium

On January 22, 2016, the manufacture and sale of ruralconazole (5% Rukonak nail for external use liquid) for the treatment of tinea unguium was approved. Adaptation is "dermatophytosis caused by dermatophyte (Trichophyton spp.)" And it is applied to the entire affected nail once a day. The same 1% formulation (trade name Ruricon) of the same ingredient has been clinically used since 2005 for "dermatomycosis (ringworm other than tinea unguiuma)", candidiasis such as fingernail erosion ".

Tinea unguiuma is an infectious disease of the nail with Trichophyton spp. As the main causative bacteria, clouding of claws, thickening, deformation, desquamation and the like are seen. The patient's physical and mental burden is great, such as the appearance of pain and walking difficulties when wearing shoes as the nail thickens. In addition, if treatment is not properly performed, it is a serious problem to easily cause diffusion to the surroundings such as infection in families.

Traditionally, in Japan, an agent for treating onychomycosis was only oral antifungal drugs such as itraconazole (trade name: Itritzol et al.) And terbinafine (trade name Lamisil et al.), But from September 2014 triazole antifungal drug efficacy Naconazole (trade name Crenafin) became available.

Since treatment options for onychomycosis are limited, in domestic and overseas guidelines, except for some disease types, treatment with internal medicine is recommended in principle. However, oral antifungal drugs also have many systemic side effects such as hepatic injury and drug interactions, and in some cases they are restricted in patients taking multiple medications, especially in elderly patients.

Ruriconazole is the same imidazole antifungal as itraconazole and others. As an action mechanism, it exerts antifungal action by inhibiting the biosynthesis of ergosterol constituting the fungal cell membrane.

The Ruconac nail-external use liquid approved this time is an external antifungal drug developed for tinea unguium which penetrates into the nail at a high concentration (5%) than the existing formulation. Various studies showed the drug concentration exceeding the MIC of dermatophyte bacteria in the deep nail, distributed throughout the nail from the nail surface to the deep nail with application once a day. 5% The formulation is not on sale abroad as of December 2015.

In a randomized double-blind parallel group comparison study (Phase 3 clinical trial) at the time of 48 weeks administration once a day as a control based on a base (placebo) conducted in Japan (efficacy and safety) confirmed. Skin irritation and phototoxicity were not observed even in the skin safety test for Japanese healthy adults.

In domestic clinical trials, side effects are recognized at 18.2%. The main side effects were locality of the application site, such as dry skin (5.4%), contact dermatitis (4.1%), paronychia (3.3%), eczema (2.5%) and so on.