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更新于：2025-03-20

Permethrin

扑灭司林

更新于：2025-03-20

概要

基本信息

药物类型

小分子化药

别名

(3-Phenoxyphenyl)methyl (±)-cis,trans-3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropanecarboxylate、3-(2,2-Dichloroethenyl)-2,2-dimethylcyclopropane carboxylic acid, (3-phenoxyphenyl) methyl ester、Nedax

+ [7]

靶点

Nav1.1

作用方式

阻滞剂

作用机制

Nav1.1阻滞剂(I型钠通道蛋白α亚基阻滞剂)

治疗领域

感染皮肤和肌肉骨骼疾病

在研适应症

虱病疥疮

非在研适应症-

原研机构

GSK Plc

在研机构

Aurobindo Pharma USA, Inc.Medtech Products, Inc.

非在研机构

GSK Plc

最高研发阶段批准上市

首次获批日期

美国 (1986-03-31),

虱病

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C21H20Cl2O3

InChIKeyRLLPVAHGXHCWKJ-UHFFFAOYSA-N

CAS号52645-53-1

关联

项与扑灭司林相关的临床试验

CTRI/2024/11/076913

/ Not yet recruiting临床4期IIT

A Comparative study to evaluate Efficacy and Safety of Topical Permethrin versus Oral Ivermectin in patients with scabies at a tertiary care centre: A Randomised controlled study. - NIL

开始日期2024-11-30

申办/合作机构-

CTRI/2024/10/075991

/ Not yet recruitingN/A

A Randomized, Double-Blind, Multi-Center, Parallel Study to Evaluate the Bioequivalenceusing Clinical Endpoint of Permethrin Cream, 5 percentage of KLM Laboratories Pvt. Ltd., India toPermethrin Cream, 5 percentage of Padagis Israel Pharmaceuticals Ltd in Subjects with scabies. - nil

开始日期2024-11-18

申办/合作机构-

IRCT20110420006243N5

/ Recruiting临床3期IIT

Comparison effect of permethrin shampoo to permethrin shampoo with vinegar in the treatment of head lice in children aged 6-13 years

开始日期2024-09-22

申办/合作机构

Shahed University

100 项与扑灭司林相关的临床结果

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100 项与扑灭司林相关的转化医学

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100 项与扑灭司林相关的专利（医药）

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11,393

项与扑灭司林相关的文献（医药）

2025-04-01·Pest Management Science

Alanine to glycine substitution in the PyR2 confers sodium channel resistance to Type I pyrethroids

Article

作者: Wang, Likui ; Yan, Ru ; Qian, Jiali ; Wu, Huiming ; Xu, Zhanyi ; Zhou, Xiangyi ; Chen, Mengli ; Chen, Guoxing ; Wu, Shaoying ; Zhu, Guonian

AbstractBACKGROUNDAedes aegypti is a primary urban vector of dengue, yellow fever, Zika and chikungunya worldwide. Pyrethroid insecticides are the most effective insecticides for controlling Ae. aegypti. However, pyrethroid resistance has developed due to the long‐term overuse of the insecticides, and many knockdown resistance (kdr) mutations have been identified in the resistant populations. A1007G, an alanine to glycine substitution, was found in resistant Ae. aegypti from Vietnam and Malaysia, which has always co‐existed with F1534C and V1016G. However, the role of A1007G in pyrethroid resistance and the linkage of A1007G and F1534C or V1016G remain unknown.RESULTSIn this study, we examined the effects of mutations on the sodium channel gating properties and pyrethroid sensitivity in Xenopus oocytes. We found mutations A1007G, A1007G + F1534C and A1007G + V1016G + F1534C shifted the voltage dependence of activation in the depolarizing direction. Mutations A1007G + F1534C and A1007G + V1016G + F1534C shifted the voltage dependence of inactivation in the depolarizing direction. Both mutations A1007G and F1534C reduced the channel sensitivity to two Type I pyrethroids, permethrin and bifenthrin, and synergistic effects were observed between mutations A1007G and F1534C. However, none of the mutations, A1007G, F1534C and A1007G + F1534C affected the channel sensitivity to two Type II pyrethroids, deltamethrin and cypermethrin. Furthermore, triple mutations A1007G + V1016G + F1534C significantly reduced the channel sensitivity to both Type I and Type II pyrethroids.CONCLUSIONWe identified A1007G had a distinct effect on sodium channel sensitivity to Type I, but not to Type II pyrethroids, also A1007G exhibited synergistic effects with F1534C to Type I pyrethroids, which will provide a fundamental insight into the distinct molecular interactions between insect sodium channel and Type I or Type II pyrethroids. © 2024 Society of Chemical Industry.

2025-04-01·Journal of Hazardous Materials

Pesticide dynamics and risk assessment in a plateau lake: Multiphase partitioning, drivers, and distribution in Southwestern China

Article

作者: Feng, Jimeng ; Wang, Tiantian ; Shen, Jian ; Wang, Ronghui ; Wang, Xinze ; Cai, Feixuan

Erhai Lake, a vital drinking water source for Dali, a highland agricultural city, faces potential contamination from pesticide residues, yet limited studies have assessed their distribution and impacts. This study investigates the occurrence, transport, partitioning, and ecological risks of pesticides in the lake's dissolved phase (DP), suspended particulate matter (SPM), and sediment (SD) samples collected from 22 sites across different seasons. The results showed significant temporal variations across different media, with spatial variations driven by crop-related patterns. Atrazine, etridiazole, and cis-permethrin were identified as the most abundant pesticides in DP, SPM, and SD, respectively. Notably, the source-sink dynamics were not only driven by deposition and resuspension but influenced by multiple sources and hydrodynamic processes such as precipitation, phytoplankton biomass, organic carbon, and winds. Ecotoxicological assessments indicated that permethrin, endrin, and endosulfan sulfate posed significant ecological risks to aquatic organisms. Although human health risks from pesticides were low, ongoing monitoring of atrazine is recommended due to its extensive use around Dali City.

2025-04-01·Talanta

Dispersive liquid-liquid microextraction based on temperature-responsive supramolecular solvent followed by HPLC-DAD for the determination of pyrethroid pesticides in tobacco samples

Article

作者: Zhu, Min ; Xie, Jiahan ; Ding, Jinru ; Chen, Shurong ; Wang, Zhibing ; Tan, Mingji ; Wang, Ying ; Zhao, Jindou

A novel temperature-responsive supramolecular solvent was prepared with cetyltributylphosphonium tetrafluoroborate and sodium citrate. It served as the extraction solvent of dispersive liquid-liquid microextraction for the extraction and enrichment of pyrethroids in tobacco samples. In this study, the preparation of the temperature-responsive supramolecular solvent and the extraction of the target analytes were integrated into one step, which simplified the experimental process. Due to the low melting point of the prepared supramolecular solvent, the traditional liquid-liquid separation can be converted to solid-liquid separation at low temperatures. This conversion facilitates precise collection of the supramolecular solvent and reduces the loss of target analytes. The composition, structure, physicochemical properties, and micromorphology of the supramolecular solvent were characterized. The formation and extraction mechanism of supramolecular solvent were explored, and the extraction conditions were optimized. The results indicated that good linearity of target analytes (R² > 0.9998) was obtained within the linear range. The limits of detection and quantification for the five pyrethroids were in the range of 0.25-0.50 μg L^-1 and 0.85-1.65 μg L^-1, respectively. The present method can be used for the analysis of pyrethroid pesticide residues in tobacco samples.

项与扑灭司林相关的新闻（医药）

2024-12-14

·drugs

Wintertime Is Prime Time for Head Lice: What Parents Need to Know

SATURDAY, Dec. 14, 2024 -- Head lice can be a wintertime headache for families and schools, but simple precautions can stop the spread of these pesky parasites. Every year, 6 million to 12 million children in the United States, ages 3 to 11, experience head lice infestations, according to the U.S. Centers for Disease Control and Prevention. Contrary to popular belief, these tiny insects don’t jump or fly, said Ali Wurster , a nurse practitioner with the Texas A&M Health Mobile Health Clinic. “They actually crawl,” Wurster explained in a university release. “A kid can be sitting in a classroom even a foot away from another child, and if their heads don't touch, the lice are not going to jump onto someone else.” While many believe individuals with dirty or unclean hair are more likely to attract lice, the reverse is true, Wurster said. The small, sesame seed-sized parasites prefer a clean scalp. They spread most commonly among school-aged children through shared items like hats, coats, brushes or dress-up clothes, which present prime modes of transfer for the parasites. To prevent head lice, avoid sharing hats, brushes or clothing. School staff should regularly sanitize common items. Wurster also recommended keeping heads apart during nap time to further deter spread. While not harmful, head lice can cause significant discomfort and should be mitigated as soon as possible both to ease symptoms and stymie further spread. If lice are found, treatment is straightforward. Over-the-counter and prescription topical creams such as Nix and Permethrin work effectively, Wurster said. After applying the treatment, remove lice eggs (nits) with a fine-toothed comb, seal them in a plastic bag and repeat treatment in seven days if needed. Wash clothing, bedding and other fabric items in hot water and dry on high heat. Non-washable items, like stuffed animals, should be sealed in a plastic bag for two weeks. The CDC no longer requires children with lice to be sent home immediately; they can finish the school day, begin treatment after school, and return the next day. Despite misconceptions, families and schools can quickly address and oftentimes prevent head lice with an accurate understanding of how the parasites spread and best practices for treatment. SOURCE: Texas A&M Health, news release, Dec. 9, 2024 Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

2024-08-13

·drugs

Pesticide Exposure Tied to Increased Risk for Stillbirth

TUESDAY, Aug. 13, 2024 -- Pesticide exposures during preconception and the first trimester may be associated with stillbirth, according to a study published online July 16 in the American Journal of Epidemiology . Melissa A. Furlong, Ph.D., from the University of Arizona College of Public Health in Tucson, and colleagues linked Arizona pesticide use records (27 types) with birth certificates (2006 to 2020) to estimate associations between living within 500 m of any application site and stillbirth. The researchers found that during 90 days preconception, any exposures to pesticides were associated with stillbirth, including cyfluthrin (relative risk [RR], 1.97), zeta-cypermethrin (RR, 1.81), organophosphates as a class (RR, 1.60), malathion (RR, 2.02), carbaryl (RR, 6.39), and propamocarb hydrochloride (RR, 7.72). During the first trimester, fenpropathrin (RR, 4.36), permethrin (RR, 1.57), organophosphates as a class (RR, 1.50), acephate (RR, 2.31), and formetanate hydrochloride (RR, 7.22) were associated with stillbirth. "These findings underscore the importance of considering individual pesticides rather than just the overall pesticide class, as specific chemical compounds may pose unique risks," Furlong said in a statement. "It also highlights the potential for prepregnancy exposures to affect reproductive outcomes." One author disclosed ties to pesticide registrants unrelated to the research.

2023-12-27

·生物谷

Molecular Cell | 蒋辉实验室揭示线粒体自噬的感知和抑制因子PPTC7及其对线粒体数量的调控作用

线粒体自噬(mitophagy)是重要的线粒体质量及数量调控机制, 与发育、癌症、衰老和神经退行性病变等生理病理状况高度相关。现已知两类哺乳动物mitophagy通路：由PINK1-Parkin介导的泛素依赖途径，以及由BNIP3, NIX和FUNDC1等介导的受体依赖途径。然而，人们对mitophagy调控机制及其生理病理意义仍有待探索。突出的表现是，缺失已知mitophagy通路的小鼠(如Pink1-/-、Parkin-/-、Bnip3-/-等)表型微弱，与普遍认知的mitophagy重要性有明显差距。2023年12月26日，北京生命科学研究所/清华大学生物医学交叉研究院蒋辉实验室在Molecular Cell在线发表了题为"A mitophagy sensor PPTC7 controls BNIP3 and NIX degradation to regulate mitochondrial mass"的论文。该论文发现了一个感知并抑制mitophagy的因子PPTC7，阐明了PPTC7调控mitophagy的分子机制并揭示其对线粒体数量和代谢稳态的调控作用。作为监控mitophagy水平的关键因子，PPTC7感知mitophagy受体BNIP3和NIX的蛋白水平，进而起始BNIP3/NIX-PPTC7-SCFFBXL4完整复合物的组装，促进SCFFBXL4泛素化和降解BNIP3和NIX，从而抑制mitophagy。该通路对维持细胞线粒体数量、代谢平衡、和个体存活至关重要。01FBXL4介导的mitophagy调控与退行性疾病MTDPS13蒋辉实验室长期从事线粒体蛋白稳态调控机制研究，之前报道了一个线粒体外膜复合物UBXD8-VCP介导BNIP3降解，从而抑制mitophagy(链接：EMBO Reports | 蒋辉实验室揭示UBXD8调控凋亡和线粒体自噬的分子机制)。为进一步发掘mitophagy调控机制，研究生曹钰通过靶向线粒体的遗传筛选发现多个mitophagy抑制因子，其中包括FBXL4和PPTC7(链接：EMBO Journal | 蒋辉实验室揭示线粒体自噬调控及线粒体疾病新机制)。已知FBXL4突变导致致死性退行性疾病线粒体DNA耗竭综合征13(MTDPS13)1,2，但其机理未明。作者发现FBXL4定位于线粒体外膜，与Skp1和Cullin1组成SCFFBXL4 E3泛素连接酶。SCFFBXL4通过泛素化降解BNIP3和NIX来抑制mitophagy。而病人来源的FBXL4突变抑制SCFFBXL4组装，导致BNIP3和NIX蛋白积累和mitophagy过度激活。FBXL4突变患者表现出mtDNA耗竭、线粒体数量减少、酸中毒、神经和肌肉退行性病变等严重症状。与FBXL4突变病人类似，Fbxl4-/-小鼠表现出BNIP3和NIX蛋白积累、mitophagy失控、线粒体数量减少、代谢紊乱和围产期死亡等严重表型。更重要的是，在Fbxl4-/-小鼠中敲除Bnip3或Nix可以挽救线粒体数量、恢复代谢平衡并挽救小鼠寿命。这些结果表明过度mitophagy导致的线粒体数量减少是MTDPS13的致病原因并为治疗提供了思路。02PPTC7调控FBXL4介导的BNIP3和NIX降解鉴于BNIP3和NIX强大且危险的线粒体清除能力，细胞必须牢牢控制其水平，但细胞监控并调节BNIP3和NIX降解的分子机制仍不清楚。研究生孙雨秋研究另一个筛选发现的mitophagy抑制因子PPTC7。前人研究表明PPTC7是定位于线粒体基质的磷酸酶。但令人诧异的是，与敲除FBXL4类似，敲除PPTC7同样导致BNIP3和NIX的积累和过度mitophagy；Pptc7-/-小鼠表现出mitophagy失控、线粒体数量减少和围产期死亡的表型，且该表型可以被Nix敲除所挽救(图1)。此外，PPTC7过表达可促进内源BNIP3和NIX被FBXL4降解，而FBXL4过表达则没有效果，提示PPTC7作为上游限速因子调控FBXL4介导的BNIP3和NIX降解。但是，线粒体基质蛋白PPTC7如何调控线粒体外膜上的蛋白降解？图1PPTC7缺失过度激活BNIP3和NIX依赖的mitophagy，造成线粒体数量减少和小鼠死亡。A,Pptc7 -KO升高小鼠肝脏中mitophagy受体BNIP3和NIX的蛋白水平(红框)并导致其他线粒体蛋白减少(蓝框)。B,小鼠生存曲线。03PPTC7前体通过与BNIP3/NIX直接互作，滞留在线粒体外膜通常情况下，线粒体基质蛋白的前体形式(precursor)在N端定位序列(targeting sequence)的引导下进入线粒体，并在线粒体基质切除定位序列，完成成熟过程。作者发现在野生型细胞里，PPTC7以成熟形式(mature form,切除了定位序列)存在于线粒体基质，而在FBXL4-KO细胞里，PPTC7同时具有定位于线粒体基质的成熟形式和定位于线粒体外膜的前体形式。进一步分析表明，FBXL4-KO细胞中积累的BNIP3和NIX导致PPTC7前体出现在线粒体外膜;在野生型细胞中直接过表达BNIP3或NIX也可诱导PPTC7前体出现在线粒体外膜定位。通过体外重组蛋白实验，作者发现BNIP3和NIX与PPTC7直接互作，并使用交联质谱分析了NIX-PPTC7的互作区域。在截去NIX与PPTC7的直接互作区域后，NIX无法诱导PPTC7前体的外膜定位，表明BNIP3和NIX通过与PPTC7的直接互作，将PPTC7前体定位于线粒体外膜。04弱化的PPTC7定位序列帮助PPTC7在线粒体外膜滞留有意思的是，作者发现与经典线粒体基质定位序列相比，PPTC7的定位序列长度短且引导能力差，推测该特征削弱了PPTC7前体进入线粒体基质的能力，有利于PPTC7前体被外膜BNIP3/NIX滞留。因此，研究者将PPTC7的定位序列替换成经典序列，发现它使PPTC7全部进入线粒体基质，无法被滞留在外膜，失去调节BNIP3和NIX降解的能力。05外膜PPTC7起始组装BNIP3/NIX-PPTC7-SCFFBXL4复合物那么外膜PPTC7如何促进SCFFBXL4介导的BNIP3和NIX降解呢？作者发现除与BNIP3/NIX直接互作之外，PPTC7还与SCFFBXL4复合物中的Cullin1直接互作。作者表达纯化了NIX，PPTC7，FBXL4,Cullin1-Rbx1和Skp1的重组蛋白，发现只有在所有蛋白都存在的情况下，这些蛋白才能组装成完整的NIX-PPTC7-SCFFBXL4复合物，缺少NIX，PPTC7，FBXL4任何一个组分都导致复合物散架。以上结果提供了一个mitophagy的负反馈调控模型:积累在线粒体外膜的mitophagy受体BNIP3和NIX与PPTC7前体直接互作，将其滞留在外膜，起始BNIP3/NIX-PPTC7-SCFFBXL4复合物的组装，从而泛素化和降解BNIP3和NIX，防止mitophagy过度激活(图2)。06禁食情况下，肝脏诱导PPTC7来抑制mitophagy和维持代谢稳态一个重要的问题是在负反馈调控mitophagy之外，PPTC7是否还会响应生理信号？鉴于PPTC7过表达能促进BNIP3和NIX降解，作者重点研究了生理信号对PPTC7表达的调节，发现禁食不改变骨骼肌PPTC7的表达，但在肝脏强烈诱导PPTC7。与之相对应，禁食强烈诱导骨骼肌mitophagy，但不改变肝脏mitophagy水平，作者推测肝脏mitophagy受到PPTC7上调的压制。因此，作者在小鼠肝脏敲除PPTC7，发现禁食导致缺失PPTC7的肝脏丢失大量线粒体。禁食情况下，肝脏负有重要使命-通过糖异生(gluconeogenesis)维持血糖水平。而糖异生需要线粒体提供两个重要支持：ATP和丙酮酸羧化酶(pyruvate carboxylase)。作者发现，敲除肝脏PPTC7导致禁食状态下肝脏ATP缺乏，糖异生受阻，造成严重的低血糖。因此，禁食情况下，肝脏特异上调PPTC7以压制mitophagy，从而维持线粒体数量和代谢稳态(图2)。图2 PPTC7调控mitophagy的工作模型。1. mitophagy的负反馈稳态调控。正常情况下，PPTC7表达后进入线粒体基质行使正常功能。当mitophagy受体BNIP3和NIX积累时，BNIP3/NIX将PPTC7前体滞留于外膜，起始BNIP3/NIX-PPTC7-SCFFBXL4复合物组装，从而降解BNIP3和NIX，防止mitophagy过度激活和线粒体丢失。2. 在禁食情况下，肝脏上调PPTC7以压制mitophagy，从而维持肝脏能量供应和糖异生通路活力，维持血糖水平。综上，该工作报道了一个感知和抑制mitophagy的PPTC7-SCFFBXL4通路。PPTC7作为关键调控因子，能够整合稳态维持和生理信号来调控mitophagy水平，以此维持线粒体数量和细胞代谢稳态。该通路的发现显著增进了我们对mitophagy与线粒体数量控制(mitochondrial mass control)的理解。禁食情况下，肝脏和骨骼肌对mitophagy的差异化调节及其功能研究也丰富了我们对生理情况下组织特异性mitophagy调控的认知。清华大学生物医学交叉研究院博士生孙雨秋为论文第一作者，蒋辉博士为通讯作者。该论文其他作者包括蒋辉课题组的曹钰和万华云，董梦秋实验室的阿达莱提买买提明和董梦秋博士，代谢组学中心的马燕博士和曹杨，蛋白质组中心的陈涉博士和李琳，遗传筛选中心的李祺博士和吴重阳，刘清华实验室的王濛。该研究由科技部、北京市政府和清华大学共同资助，在北京生命科学研究所完成。论文链接：https://www-cell-com.libproxy1.nus.edu.sg/molecular-cell/fulltext/S1097-2765(23)01014-6本文仅用于学术分享，转载请注明出处。若有侵权，请联系微信：bioonSir 删除或修改！

临床1期蛋白降解靶向嵌合体引进/卖出

100 项与扑灭司林相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D05443	扑灭司林	P03AC04	DB04930

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
虱病	美国	Aurobindo Pharma USA, Inc.	1989-08-25
疥疮	美国	Aurobindo Pharma USA, Inc.	1989-08-25

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


WCD2023	N/A	疥疮	-	5% permethrin cream	觸範壓襯鬱鑰鹹膚憲醖(蓋壓獵衊壓醖顧糧築襯) = 壓膚鹽顧構廠餘蓋齋淵齋鏇獵襯鏇積齋憲醖遞 (淵壓餘構積鏇願膚願廠 )	积极	2023-07-03
NCT02978508 (CTgov)	临床3期	疥疮	140	Permethrin Cream, 5% (Permethrin Cream, 5%)	壓淵齋鹽鬱簾獵顧顧遞(齋築餘簾餘積繭鹽選餘) = 鑰夢構遞築壓積鹹醖膚醖鏇製鹹糧蓋網獵願憲 (製餘憲齋淵遞積淵淵願, 製醖鹹襯艱獵淵鏇鹹艱 ~ 鏇窪襯簾蓋蓋蓋艱觸積) 更多	-	2020-09-02
				Elimite (Elimite)	壓淵齋鹽鬱簾獵顧顧遞(齋築餘簾餘積繭鹽選餘) = 淵顧廠鏇襯衊蓋廠窪顧醖鏇製鹹糧蓋網獵願憲 (製餘憲齋淵遞積淵淵願, 窪簾淵醖廠齋築壓壓觸 ~ 壓製壓廠艱鹹遞淵壓網) 更多
NCT03178942 (CTgov)	临床3期	疥疮	254	Elimite™ Cream (permethrin) 5% (Reference: Elimite™ Cream)	廠餘繭襯糧醖淵簾鑰鬱(襯構獵獵簾繭齋網鹹廠) = 鑰網糧襯獵壓網鏇網範糧鬱範糧鏇鏇選製顧齋 (遞憲醖衊憲鬱壓醖鑰鏇, 構醖憲願積範餘製網願 ~ 衊衊齋積積憲選網獵顧) 更多	-	2019-03-14
				Permethrin Cream, 5% (Test: Permethrin Cream, 5%)	廠餘繭襯糧醖淵簾鑰鬱(襯構獵獵簾繭齋網鹹廠) = 鬱範餘鏇顧鏇鹽願鹹獵糧鬱範糧鏇鏇選製顧齋 (遞憲醖衊憲鬱壓醖鑰鏇, 艱網窪蓋壓觸獵遞餘淵 ~ 艱範夢蓋選築廠蓋憲築) 更多
ISRCTN88144046 (Pubmed)	N/A	头虱	90	4% dimeticone liquid gel	糧顧淵繭廠鬱顧觸襯壓(範築顧構鹽窪獵範顧夢) = 膚遞餘蓋糧築齋鹽壓憲範艱齋衊構鹽築鏇製齋 (遞壓鏇襯餘選窪齋積糧 )	积极	2013-04-01
				1% permethrin creme rinse	糧顧淵繭廠鬱顧觸襯壓(範築顧構鹽窪獵範顧夢) = 艱淵繭顧餘膚醖簾淵鏇範艱齋衊構鹽築鏇製齋 (遞壓鏇襯餘選窪齋積糧 )