Permethrin (NRDC-143)
(Synonyms: 氯菊酯; NRDC-143) 目录号 : GC33928
A modulator of voltage-gated sodium channels
Cas No.:52645-53-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Permethrin is a modulator of voltage-gated sodium channels (NaV) that is used as an insecticide.1 It delays channel deactivation of the NaV1.8 channel expressed in X. laevis oocytes. It is at least 100-fold more potent at insect than mammalian sodium channels, leading to slow deactivation of D. para/TipE, but not rat brain IIA or β1, sodium channels expressed in X. laevis oocytes when used at a concentration of 500 nM.2 Permethrin (5 ?M) increases sodium influx in BV-2 and primary microglial cells by approximately 28 and 29%, respectively, and activates microglia.3 Long-term application of permethrin leads to dose- and time-dependent intracellular sodium accumulation and TNF-α release in microglia in vitro. Formulations containing permethrin have been used for the treatment of head lice and scabies infestations.
1.Choi, J.S., and Soderlund, D.M.Structure-activity relationships for the action of 11 pyrethroid insecticides on rat Nav1.8 sodium channels expressed in Xenopus oocytesToxicol. Appl. Pharmacol.211(3)233-244(2006) 2.Warmke, J.W., Reenan, R.A., Wang, P., et al.Functional expression of Drosophila para sodium channels. Modulation by the membrane protein TipE and toxin pharmacologyJ. Gen. Physiol.110(2)119-133(1997) 3.Hossain, M.M., Liu, J., and Richardson, J.R.Pyrethroid insecticides directly activate microglia through interaction with voltage-gated sodium channelsToxicol. Sci.155(1)112-123(2017)
| Cas No. | 52645-53-1 | SDF | |
| 别名 | 氯菊酯; NRDC-143 | ||
| Canonical SMILES | O=C(C1C(C)(C)C1/C=C(Cl)\Cl)OCC2=CC=CC(OC3=CC=CC=C3)=C2 | ||
| 分子式 | C21H20Cl2O3 | 分子量 | 391.29 |
| 溶解度 | DMSO : 50 mg/mL (127.78 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5556 mL | 12.7782 mL | 25.5565 mL |
| 5 mM | 0.5111 mL | 2.5556 mL | 5.1113 mL |
| 10 mM | 0.2556 mL | 1.2778 mL | 2.5556 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
[Treatment of scabies]
Aten Primaria 2022 Mar;54(3):102231.PMID:35051892DOI:10.1016/j.aprim.2021.102231.
Scabies affects more than 200 million people around the world, and causes a significant socioeconomic impact. Prolonged skin-to-skin contact is the primary mode of transmission. Fomite-mediated transmission is uncommon, although it can be significant in crusted scabies. Topical therapy with Permethrin 5% is recommended as first-line treatment. It can be indicated during pregnancy and lactation, and appears to be safe in children <2 months. However, a decrease in the effectiveness of this drug has recently been reported. Another first-line therapeutic alternative is oral ivermectin. It can be administered during lactation, and new evidence suggests that it is safe in children >15kg. Diverse systematic reviews and meta-analysis have concluded that oral ivermectin is as effective and safe as topical Permethrin. Mass drug administration of oral ivermectin is an excellent option for the management of scabies in communities with high prevalence, or for scabies outbreaks in institutions.
Management of scabies
Singapore Med J 2019 Jun;60(6):281-285.PMID:31243462DOI:10.11622/smedj.2019058.
Scabies is a common infestation worldwide, affecting persons of any age and socioeconomic status. In Singapore, it is more common in institutions rather than in homes. The two variants are classic scabies and crusted scabies, with the latter having a significantly higher mite burden. Early identification, isolation of index patients and prophylactic treatment of contacts are essential in dealing with the outbreak. Locally, most primary care practitioners make the diagnosis based on visual inspection and clinical examination. A skin scrape is done to confirm the diagnosis, especially in atypical presentations. Scabietic mites, eggs or faeces can be seen on microscopy. The usual treatment for adult scabies in Singapore is the use of topical malathion or Permethrin. A combination of topical Permethrin and oral ivermectin is used for crusted scabies.
Ivermectin and Permethrin for treating scabies
Cochrane Database Syst Rev 2018 Apr 2;4(4):CD012994.PMID:29608022DOI:10.1002/14651858.CD012994.
Background: Scabies is an intensely itchy parasitic infection of the skin. It occurs worldwide, but is particularly problematic in areas of poor sanitation, overcrowding, and social disruption. In recent years, Permethrin and ivermectin have become the most relevant treatment options for scabies. Objectives: To assess the efficacy and safety of topical Permethrin and topical or systemic ivermectin for scabies in people of all ages. Search methods: We searched the following databases up to 25 April 2017: the Cochrane Infectious Diseases Group Specialized Register, CENTRAL, MEDLINE, Embase, LILACS, and IndMED. We searched the World Health Organization International Clinical Trials Registry Platform, the ISRCTN registry, CenterWatch Clinical Trials Listing, ClinicalTrials.gov, TrialsCentral, and the UK Department of Health National Research Register for ongoing trials. We also searched multiple sources for grey literature and checked reference lists of included studies for additional trials. Selection criteria: We included randomized controlled trials that compared Permethrin or ivermectin against each other for people with scabies of all ages and either sex. Data collection and analysis: Two review authors independently screened the identified records, extracted data, and assessed the risk of bias for the included trials.The primary outcome was complete clearance of scabies. Secondary outcomes were number of participants re-treated, number of participants with at least one adverse event, and number of participants withdrawn from study due to an adverse event.We summarized dichotomous outcomes using risk ratios (RR) with 95% confidence intervals (CI). If it was not possible to calculate the point estimate, we described the data qualitatively. Where appropriate, we calculated combined effect estimates using a random-effects model and assessed heterogeneity. We calculated numbers needed to treat for an additional beneficial outcome when we found a difference.We assessed the certainty of the evidence using the GRADE approach. We used the control rate average to provide illustrative clearance rates in the comparison groups. Main results: Fifteen studies (1896 participants) comparing topical Permethrin, systemic ivermectin, or topical ivermectin met the inclusion criteria. Overall, the risk of bias in the included trials was moderate: reporting in many studies was poor. Nearly all studies were conducted in South Asia or North Africa, where the disease is more common, and is associated with poverty.EfficacyOral ivermectin (at a standard dose of 200 μg/kg) may lead to slightly lower rates of complete clearance after one week compared to Permethrin 5% cream. Using the average clearance rate of 65% in the trials with Permethrin, the illustrative clearance with ivermectin is 43% (RR 0.65, 95% CI 0.54 to 0.78; 613 participants, 6 studies; low-certainty evidence). However, by week two there may be little or no difference (illustrative clearance of Permethrin 74% compared to ivermectin 68%; RR 0.91, 95% CI 0.76 to 1.08; 459 participants, 5 studies; low-certainty evidence). Treatments with one to three doses of ivermectin or one to three applications of Permethrin may lead to little or no difference in rates of complete clearance after four weeks' follow-up (illustrative cures with 1 to 3 applications of Permethrin 93% and with 1 to 3 doses of ivermectin 86%; RR 0.92, 95% CI 0.82 to 1.03; 581 participants, 5 studies; low-certainty evidence).After one week of treatment with oral ivermectin at a standard dose of 200 μg/kg or one application of Permethrin 5% lotion, there is probably little or no difference in complete clearance rates (illustrative cure rates: Permethrin 73%, ivermectin 68%; RR 0.93, 95% CI 0.74 to 1.17; 120 participants, 1 study; moderate-certainty evidence). After two weeks of treatment, one dose of systemic ivermectin compared to one application of Permethrin lotion may lead to similar complete clearance rates (extrapolated cure rates: 67% in both groups; RR 1.00, 95% CI 0.78 to 1.29; 120 participants, 1 study; low-certainty evidence).There is probably little or no difference in rates of complete clearance between systemic ivermectin at standard dose and topical ivermectin 1% lotion four weeks after initiation of treatment (illustrative cure rates: oral ivermectin 97%, ivermectin lotion 96%; RR 0.99, 95% CI 0.95 to 1.03; 272 participants, 2 studies; moderate-certainty evidence). Likewise, after four weeks, ivermectin lotion probably leads to little or no difference in rates of complete clearance when compared to Permethrin cream (extrapolated cure rates: Permethrin cream 94%, ivermectin lotion 96%; RR 1.02, 95% CI 0.96 to 1.08; 210 participants, 1 study; moderate-certainty evidence), and there is little or no difference among systemic ivermectin in different doses (extrapolated cure rates: 2 doses 90%, 1 dose 87%; RR 0.97, 95% CI 0.83 to 1.14; 80 participants, 1 study; high-certainty evidence).SafetyReporting of adverse events in the included studies was suboptimal. No withdrawals due to adverse events occurred in either the systemic ivermectin or the Permethrin group (moderate-certainty evidence). Two weeks after treatment initiation, there is probably little or no difference in the proportion of participants treated with systemic ivermectin or Permethrin cream who experienced at least one adverse event (55 participants, 1 study; moderate-certainty evidence). After four weeks, ivermectin may lead to a slightly larger proportion of participants with at least one adverse event (extrapolated rates: Permethrin 4%, ivermectin 5%; RR 1.30, 95% CI 0.35 to 4.83; 502 participants, 4 studies; low-certainty evidence).Adverse events in participants treated with topical ivermectin were rare and of mild intensity and comparable to those with systemic ivermectin. For this comparison, it is uncertain whether there is any difference in the number of participants with at least one adverse event (very low-certainty evidence). No withdrawals due to adverse events occurred (62 participants, 1 study; moderate-certainty evidence).It is uncertain whether topical ivermectin or Permethrin differ in the number of participants with at least one adverse event (very low-certainty evidence). We found no studies comparing systemic ivermectin in different doses that assessed safety outcomes. Authors' conclusions: We found that for the most part, there was no difference detected in the efficacy of Permethrin compared to systemic or topical ivermectin. Overall, few and mild adverse events were reported. Our confidence in the effect estimates was mostly low to moderate. Poor reporting is a major limitation.
The Treatment of Scabies
Dtsch Arztebl Int 2016 Nov 14;113(45):757-762.PMID:27974144DOI:10.3238/arztebl.2016.0757.
Background: Scabies is a contagious infestation transmitted by skin-to-skin contact and sometimes by contact with contaminated material. The scabies mite burrows into the skin, producing a papular rash and severe itch at typical sites of predilection. Methods: We systematically reviewed the literature to compare the efficacy of various anti-scabies agents, including a calculation of relative risks and confidence intervals. Results: A literature search yielded 596 initial hits; after screening in accor-dance with the defined inclusion and exclusion criteria, 16 studies were selected for this review. Among topical treatments for scabies, Permethrin was equally effective or more effective than crotamiton or benzyl benzoate. In a comparison of topical versus systemic treatment, topical Permethrin and systemic ivermectin did not differ substantially in efficacy (7 comparative studies revealed no difference; one revealed a difference in favor of Permethrin). Comparative trials of topical benzyl benzoate versus systemic ivermectin yielded inconsistent findings. Single and double administrations of ivermectin were similarly effective. In trials involving entire populations with a high prevalence of scabies, systemic ivermectin was found to be superior to topical Permethrin. Conclusion: There are hardly any differences in efficacy between the available treatments for scabies. Single administrations of Permethrin 5%, crotamiton 10%, and systemic ivermectin are all comparably effective. There are differences in the frequeny and ease of application as well as when eradicating scabies in populations with a high prevalence.
Scabies
Tidsskr Nor Laegeforen 2020 Oct 26;140(15).PMID:33118775DOI:10.4045/tidsskr.20.0095.
Background: This article describes a scabies outbreak at a boarding school where failure of the first-line therapy was suspected. Case presentation: A group of five students, two of whom were room-mates, presented with a varying degree of pruritic papular rash. Repeated treatments with Permethrin monitored by the school nurse, in conjunction with a rigorous hygiene regimen, proved to be ineffective. Eventually all five students were prescribed a combination therapy consisting of Permethrin and ivermectin. This treatment proved effective in all five students. Despite closely monitored treatment, monotherapy with Permethrin failed in all five patients. We discuss whether the lack of response was due to failed application, inability to rid the home environment of mites, reinfection by unidentified infected individuals or increased tolerance to Permethrin. Interpretation: Repeated therapeutic failure when Permethrin was used under controlled conditions and documented mechanisms for increased tolerance may indicate the last possibility. We therefore call for additional research on this topic.