Lofexidine
(Synonyms: 洛非西定) 目录号 : GC36477
An α2-
Cas No.:31036-80-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lofexidine is an α2-
1.Jarrott, B., Louis, W.J., and Summers, R.J.Characterization of central α-adrenoceptors using 3H-clonidine and its derivativesChest83(2 Suppl)339-340(1983) 2.Bennett, D.A., and Lal, H.Discriminative stimuli produced by clonidine: An investigation of the possible relationship to adrenoceptor stimulation and hypotensionJ. Pharmacol. Exp. Ther.223(3)642-648(1982) 3.Ling, W., Mooney, L., Zhao, M., et al.Selective review and commentary on emerging pharmacotherapies for opioid addictionSubst. Abuse Rehabil.2181-188(2011) 4.Gerra, G., Zaimovic, A., Giusti, F., et al.Lofexidine versus clonidine in rapid opiate detoxificationJ. Subst. Abuse Treat.21(1)11-17(2001)
| Cas No. | 31036-80-3 | SDF | |
| 别名 | 洛非西定 | ||
| Canonical SMILES | CC(C1=NCCN1)OC2=C(Cl)C=CC=C2Cl | ||
| 分子式 | C11H12Cl2N2O | 分子量 | 259.13 |
| 溶解度 | DMSO: 62.5 mg/mL (241.19 mM) | 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 | 3.8591 mL | 19.2953 mL | 38.5907 mL |
| 5 mM | 0.7718 mL | 3.8591 mL | 7.7181 mL |
| 10 mM | 0.3859 mL | 1.9295 mL | 3.8591 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。
Lofexidine: A Newly FDA-Approved, Nonopioid Treatment for Opioid Withdrawal
Ann Pharmacother 2019 Jul;53(7):746-753.PMID:30724094DOI:10.1177/1060028019828954.
Objective: To review the pharmacology, efficacy, and safety of Lofexidine for the treatment of opioid withdrawal secondary to the recent Food and Drug Administration (FDA) approval. Data sources: A literature search using PubMed was conducted (inception to December 2018) using the terms Lofexidine, opioid, opiate, and withdrawal. References from retrieved articles and the prescribing information were reviewed for any additional material. Study selection/data extraction: The literature search was limited to human studies published in English that pertained to human pharmacology, pharmacokinetics, pharmacodynamics, dosing, efficacy, and safety regarding opioid withdrawal. Phase I, II, and III studies of Lofexidine for opioid withdrawal were reviewed for inclusion. Data synthesis: Lofexidine is newly FDA approved in the United States for the treatment of opioid withdrawal symptoms in adults. Several randomized controlled trials and a Cochrane review noted the effectiveness of Lofexidine versus placebo for this indication. The efficacy of Lofexidine has also been shown to be comparable to that of other indicated first- and second-line pharmacological agents. Relevance to Patient Care and Clinical Practice: This article examines the trials that led to Lofexidine's new FDA-approved indication as well as other recent literature published since its last major review, seeking to guide providers in the appropriate use of Lofexidine for its new indication. Conclusions: Lofexidine is an effective and safe agent in treating symptoms related to opioid withdrawal in adults when compared with placebo; although it is more widely accessible than other first-line therapies, its use in practice may be limited by cost.
Lofexidine versus clonidine for mitigation of opioid withdrawal symptoms: A systematic review
J Am Pharm Assoc (2003) 2020 Jan-Feb;60(1):145-152.PMID:31791720DOI:10.1016/j.japh.2019.10.004.
Objectives: The U.S. Food and Drug Administration recently approved Lofexidine, an α-2-adrenergic agonist, as the first non-opioid medication for mitigation of opioid withdrawal symptoms. Clonidine, an α-2-adrenergic agonist, historically was used off-label for this indication. This review aimed to evaluate the effectiveness of Lofexidine versus clonidine for mitigation of opioid withdrawal symptoms and to discuss the current role of Lofexidine in the management of patients at risk of experiencing opioid withdrawal. Data sources: MEDLINE/PubMed, EBSCO, and CENTRAL were searched using the terms "Lofexidine," "clonidine," and "opioid withdrawal." Study selection: The literature search included English-language studies involving administration and prescription of Lofexidine and clonidine for the management of opioid withdrawal symptoms in adults. Data sources were searched to include articles published between October 1993 and May 2019. Data extraction: Three independent reviewers analyzed the title and abstract of studies to identify studies involving comparisons of Lofexidine with clonidine for mitigation of opioid withdrawal symptoms. Reviewers were initially blinded to the individual determinations. Results were then unblinded and discussed among reviewers. Results: Of the 110 citations screened, 5 articles were included. One study demonstrated a statistically significant reduction in opioid withdrawal symptom severity with Lofexidine compared with clonidine, whereas the other 4 studies showed no significant difference. Three studies reported the completion of opioid detoxification treatment, with no significant differences seen. In 1 study that compared Lofexidine with placebo, Lofexidine caused significant hypotension, bradycardia, and pupillary constriction. Three studies showed significant adverse effects of hypotension and symptoms of feeling unwell with clonidine compared with Lofexidine. Conclusion: Lofexidine appears equivalent in efficacy to clonidine, with fewer adverse effects, and it may have a limited role in the management of opioid withdrawal symptoms. However, cost, detoxification venue, and value of other preferred treatment modalities may affect the comparative efficacy of Lofexidine to other agents.
Lofexidine: A Novel Treatment Option for Opioid Withdrawal Symptoms
Sr Care Pharm 2020 Oct 1;35(10):413-418.PMID:32972491DOI:10.4140/TCP.n.2020.413.
Substance misuse in adults 60 years of age and older is one of the fastest-growing health issues in the United States. Alcohol and prescription drugs are among the most commonly misused agents. With growing concern for opioid-overdose deaths and the use of opioids in the treatment of persistent pain in older adults, it is imperative that practitioners are aware of emerging therapies used to manage the symptoms that may result after discontinuation of opioid medications. This review highlights the first nonopioid treatment plan for the management of opioid withdrawal symptoms with a novel pharmacologic mechanism.
The Role of Lofexidine in Management of Opioid Withdrawal
Pain Ther 2019 Jun;8(1):67-78.PMID:30565033DOI:10.1007/s40122-018-0108-7.
Fear of withdrawal symptoms has been cited by survey respondents as the main reason that they continued to use opioids. Lofexidine is an α2-adrenergic agonist that decreases the sympathetic outflow that results in the characteristic symptoms of opioid withdrawal. A structural analog of clonidine, Lofexidine has a higher affinity and specificity for the α2a receptors and does not reinforce opioid dependence. Withdrawal symptoms correlate approximately to the half-life of the opioid; patient factors such as age, duration of opioid exposure, physical status, and other considerations may influence the nature and duration of withdrawal symptoms. For patients with opioid use disorder and psychiatric comorbidities, withdrawal may be destabilizing and may exacerbate mental health status. Lofexidine has been shown in clinical trials to be safe and effective in helping to manage the symptoms of withdrawal and has been recommended in guidelines for this purpose. Adverse events associated with Lofexidine include QT prolongation, hypotension, orthostasis, and bradycardia. The maximum course of treatment is 14 days, and doses should be titrated, with the recommended maximum dose to coincide with the most severe withdrawal symptoms (about 5-7 days after opioid discontinuation).
Lofexidine, an {alpha}2-receptor agonist for opioid detoxification
Ann Pharmacother 2010 Feb;44(2):343-51.PMID:20040696DOI:10.1345/aph.1M347.
Objective: To review the pharmacology, toxicology, pharmacokinetics, efficacy, adverse effects, drug interactions, and dosage guidelines for Lofexidine, an alpha(2)-agonist, for opioid detoxification. Data sources: Primary literature was identified through a MEDLINE search (1950-September 2009), EMBASE (1988-July 2009), International Pharmaceutical Abstracts (1970-September 2009), and the Cochrane Library (1996-September 2009) using the key words Lofexidine and opioid withdrawal. Abstracts were included in the absence of published results of studies. Study selection and data extraction: Studies published in English-language literature reporting on animal and human pharmacology, toxicology, and pharmacokinetics were included in addition to clinical trials using Lofexidine for opioid detoxification in comparison to placebo or active controls. Data synthesis: Lofexidine is an alpha(2)-agonist structurally related to clonidine. It is not an effective antihypertensive agent; however, it decreases the sympathetic outflow responsible for many opioid withdrawal symptoms. Nine clinical studies were reviewed representing 354 patients receiving Lofexidine including a recent Phase 3 clinical trial. Eight studies involved comparisons of Lofexidine to an opioid receptor agonist or clonidine for opioid detoxification. In these trials, Lofexidine dosing was titrated to a maximum of 1.6-3.2 mg/day in divided doses for a total of 5-18 days. The data suggest that Lofexidine has positive efficacy in reducing opioid withdrawal symptoms and is at least as effective as the opioid receptor agonists utilized for detoxification. Not all withdrawal symptoms are alleviated by alpha(2)-agonists, with many patients complaining of insomnia and aching. The most common adverse event with Lofexidine in the Phase 3 trial was insomnia. Hypotension was also reported; however, the studies comparing clonidine with Lofexidine suggest decreased incidence and severity of adverse events with Lofexidine. Conclusions: Lofexidine appears to be a promising agent for opioid detoxification. If approved, it would be the first nonopioid agent approved for this indication. Further large-scale controlled studies are needed to identify the safest, most effective dosage regimen required to achieve opioid detoxification.