部分中文利拉萘酯处方资料（仅供参考）

英文名：liranaftate

商标名：ZEFNART

中文名：利拉萘酯

剂  型：乳霜、溶液

ゼフナートクリーム ２％／ゼフナート外用液 ２％

薬効分類名

抗真菌薬

商標名

ZEFNART CREAM 2％ 

ZEFNART SOLUTION 2％ 

構造式：

分子式：C18H20N2O2S (328.43)

一般名：リラナフタート(JAN)　liranaftate(JAN,INN)

化学名：O -(5, 6, 7, 8-tetrahydro-2-naphthyl)-N - (6-methoxy-2-pyridyl)-N - methylthiocarbamate

性状：

Liranafutate是一种白色至淡黄色的白色晶体，没有任何气味。 易溶于丙酮，微溶于乙醚，难溶于甲醇，乙醇（99.5）或己烷，难溶于水。

熔点：98.5至100.5℃

分配系数：5.19或更高（辛醇/水）

处理注意事项

1.放在儿童接触不到的地方。

2.注意液体软化合成树脂或熔化涂料。

3.保持药液远离火源。

药用药理学

1.抗真菌作用

（1）Riranafutato是癣菌（毛癣菌，小孢子菌属，表皮癣菌属物种）具有抵靠强的抗真菌活性，黑木耳，针对双相型真菌和其他真菌的抗真菌作用。

（2）Riranafutato的皮肤癣菌的新鲜临床分离主要MIC值示于下表中，它表​​现出优良的抗真菌活性。

（3）Riranafutato，在由T.Mentagrophytes豚鼠实验癣模型，迅速地提高病变。

（4）在豚鼠中由T.mentagrophytes实验癣模型中，当施加到Riranafutato到感染前3天，没有发展。

（5）Riranafutato相比T.Mentagrophytes，抑制菌丝体的生长在1纳克/毫升，在1微克/ mL的细胞壁的分离，表明细胞膜的破坏。

（6）Relanaputate没有对T.mentagrophytes产生耐受性。

2.作用机制

Riranafutato抑制真菌细胞的角鲨烯 - 环氧化反应中，通过生物合成抑制麦角甾醇，其是细胞膜成分发挥抗真菌活性。

适应症

癣：足癣，足癣，裆区癣

用法与用量

每天一次涂抹于患处。

包装

乳霜：10克×10,10克×50

局部溶液：10mL×10

制造供应商

全薬工業株式会社

销售商

鸟居制药有限公司

完整说明书附件：http://www.info.pmda.go.jp/go/pack/2659712N1020_1_08/

Clinical study of lira naphthyl ester in the treatment of femoral hernia

Ilanaftate is a novel thiocarbamate antifungal agent, a squalene epoxidase inhibitor that specifically affects fungal solids by blocking the epoxidation of squalene in the fungal cell membrane. The early biosynthesis of alcohol causes the lack of cell membrane constituent ergosterol and the accumulation of squalene in the cell, leading to the leakage of important substances in the cell, thereby exerting antifungal activity.

According to the MIC value measured by the fungal sensitivity test, the antifouling activity of lira naphthyl ester is 10 times stronger than that of tolnaphthyl ester, and the effect against dermatophytes is better than that of clotrimazole.

Moreover, this product has a wide antifungal spectrum, and has strong antifungal action against Trichophyton, Microsporium and Epidermidis, which is stronger than Tolnaphthalate; many dark fungi, biphasic fungi, and other filamentous fungi And a small number of Cryptococcus neoformans are quite sensitive to lira naphthyl ester, and almost all of the above tested strains are resistant to tolnaphthyl ester.

The product has a long storage time in the epidermis and can be distributed in the stratum corneum for a long time, so it only needs to be administered once a day to increase the compliance of the treatment and significantly improve the quality of life of the patient.

Clinical trials and open-label trials of lira naphthyl ester have been carried out abroad. In an open phase II clinical trial involving 111 patients with dermatophytosis, this product can improve symptoms in 91.7%-100% of patients. Good tolerated J, adverse reactions are mild and transient.

Another multicenter randomized clinical trial using 2% lira naphthalate cream for the treatment of femoral hernia showed that the 2% lira naphthalate cream had a mycological cure rate of 98.7% at the end of treatment and a clinical cure rate of 79.7. % was significantly higher than 1% bifonazole cream (mycological cure rate and clinical cure rate were 91.3% and 62.6%, respectively).

The results of this study showed that the clinical effective rate of 2% lira naphthalate ointment was 83.10% (83.58% in the control group), the cure rate was 46.48% (40.30% in the control group); fungal clearance The rate was 95.83% (control group was 95.65%). After 2 weeks of withdrawal, it was 90.14% (control group was 8657%), 74.65% (control group was 61.19%), 98.59% (control group was 100%), and the comprehensive effective rate was 90. .14% (control group was 86.57%), the cure rate was 74.65% (control group was 61.19%); the incidence of adverse reactions was 0.70% (control group was 0). There were no significant differences in clinical cure rate, effective rate, fungal clearance rate, and adverse reaction rate between the two groups.