Levocetirizine
(Synonyms: LCZ, (R)-Cetirizine) 目录号 : GC25571Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor.
Cas No.:130018-77-8
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
Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor.
[1] Philippe Devillier, et al. Clin Pharmacokinet. 2008;47(4):217-30.
| Cas No. | 130018-77-8 | SDF | Download SDF |
| 别名 | LCZ, (R)-Cetirizine | ||
| 分子式 | C21H25ClN2O3 | 分子量 | 388.89 |
| 溶解度 | DMSO: 78 mg/mL (200.57 mM);Water: 78 mg/mL (200.57 mM);Ethanol: 78 mg/mL (200.57 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 | 2.5714 mL | 12.8571 mL | 25.7142 mL |
| 5 mM | 0.5143 mL | 2.5714 mL | 5.1428 mL |
| 10 mM | 0.2571 mL | 1.2857 mL | 2.5714 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。
Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and Levocetirizine : a comparative review
Clin Pharmacokinet 2008;47(4):217-30.PMID:18336052DOI:10.2165/00003088-200847040-00001.
Second-generation histamine H(1) receptor antagonists were developed to provide efficacious treatment of allergic rhinitis (AR) and chronic idiopathic urticaria (CIU) while decreasing adverse effects associated with first-generation agents. When comparing the efficacy and safety profiles of the newest second-generation antihistamines - desloratadine, fexofenadine and Levocetirizine - many pharmacological and clinical criteria must be considered. Most importantly, these elements should not be evaluated separately but, rather, as parts of a puzzle that create a whole picture. As a class, second-generation antihistamines are highly selective for the H(1) receptor. Some bind to it with high affinity, although there is marked heterogeneity among the various compounds. They have a limited effect on the CNS, and clinical studies have noted almost no significant drug-drug interactions in the agents studied. No major cytochrome P450 inhibition has been reported with desloratadine, fexofenadine and Levocetirizine, and the bioavailability of desloratadine is minimally affected by drugs interfering with transporter molecules. Of the second-generation antihistamines, desloratadine has the greatest binding affinity for the H(1) receptor. The use of desloratadine, fexofenadine and Levocetirizine is not associated with clinically relevant antimuscarinic effects. Desloratadine and fexofenadine do not impair cognitive or psychomotor functioning and are comparable with placebo in terms of somnolence. Based on these pharmacological characteristics, as well as clinical endpoints such as symptom scores, quality-of-life surveys, inflammatory cell counts and investigators' global evaluations, we conclude that desloratadine, fexofenadine and Levocetirizine are all efficacious treatments for AR and CIU. However, differences among the antihistamines in relation to a lack of significant interaction with drug transporter molecules and somnolence in excess of placebo may provide some advantages for the overall profile of desloratadine compared with fexofenadine and Levocetirizine.
Levocetirizine and montelukast in the COVID-19 treatment paradigm
Int Immunopharmacol 2022 Feb;103:108412.PMID:34942461DOI:10.1016/j.intimp.2021.108412.
Levocetirizine, a third-generation antihistamine, and montelukast, a leukotriene receptor antagonist, exhibit remarkable synergistic anti-inflammatory activity across a spectrum of signaling proteins, cell adhesion molecules, and leukocytes. By targeting cellular protein activity, they are uniquely positioned to treat the symptoms of COVID-19. Clinical data to date with an associated six-month follow-up, suggests the combination therapy may prevent the progression of the disease from mild to moderate to severe, as well as prevent/treat many of the aspects of 'Long COVID,' thereby cost effectively reducing both morbidity and mortality. To investigate patient outcomes, 53 consecutive COVID-19 test (+) cases (ages 3-90) from a well-established, single-center practice in Boston, Massachusetts, between March - November 2020, were treated with Levocetirizine and montelukast in addition to then existing protocols [2]. The data set was retrospectively reviewed. Thirty-four cases were considered mild (64%), 17 moderate (32%), and 2 (4%) severe. Several patients presented with significant comorbidities (obesity: n = 22, 41%; diabetes: n = 10, 19%; hypertension: n = 24, 45%). Among the cohort there were no exclusions, no intubations, and no deaths. The pilot study in Massachusetts encompassed the first COVID-19 wave which peaked on April 23, 2020 as well as the ascending portion of the second wave in the fall. During this period the average weekly COVID-19 case mortality rate (confirmed deaths/confirmed cases) varied considerably between 1 and 7.5% [37]. FDA has approved a multicenter, randomized, placebo-controlled, Phase 2 clinical trial design, replete with electronic diaries and laboratory metrics to explore scientific questions not addressed herein.
Levocetirizine: an update
Curr Med Chem 2006;13(22):2711-5.PMID:17017922DOI:10.2174/092986706778201594.
Histamine plays a prominent and diverse role in the pathophysiology of allergic disease and therapeutic intervention is therefore typically focused on blocking the effects of this biogenic amine. A new antihistamine, Levocetirizine, is the R-enantiomer of cetirizine dihydrochloride and like its parent compound undergoes minimal hepatic metabolism. Levocetirizine has pharmacodynamically and pharmacokinetically favourable characteristics, including high bioavailability, rapid onset of action, limited distribution and a low degree of metabolism. Clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis and chronic urticaria with a minimal number of untoward effects. Furthermore, several recent studies have demonstrated that, in addition to its being a potent antihistamine, Levocetirizine has several anti-inflammatory effects that are observed at clinically relevant concentrations that may enhance its therapeutic benefit.
Levocetirizine in the treatment of allergic diseases
Expert Opin Pharmacother 2009 Oct;10(14):2367-77.PMID:19663743DOI:10.1517/14656560903193086.
Background: Levocetirizine, the R-enantiomer of cetirizine dihydrochloride, is a new molecule with a potent and selective antihistamine activity. Objective: To investigate the evidence that Levocetirizine is an effective therapy for allergic disease. Methods: Evaluation of published articles in English, or having an English abstract. Results: Clinical trials indicate that Levocetirizine is safe and effective for the treatment of allergic rhinitis and chronic idiopathic urticaria. The compound shows a rapid onset of action, high bioavailability and affinity for the H1 receptor. Moreover, this molecule demonstrates many anti-inflammatory effects that enhance the clinical therapeutic benefit not only in short-term but also in long-term treatments, as reported in recent trials utilizing Levocetirizine for several months. Conclusion: Levocetirizine confirms its safe effective activity for treatment of allergic disease in both adults and children.
Pharmacokinetic evaluation of Levocetirizine
Expert Opin Drug Metab Toxicol 2011 Aug;7(8):1035-47.PMID:21639816DOI:10.1517/17425255.2011.590131.
Introduction: There have recently been guidelines developed for the diagnosis and treatment of rhinitis and urticaria. For both conditions, second-generation antihistamines remain as the first-line therapy. Areas covered: The article presents the current pharmacology, chemical properties, pharmacokinetics and metabolism of Levocetirizine. The article also reviews the clinical efficacy of Levocetirizine for seasonal allergic and perennial rhinitis, as well as chronic urticaria. The article is formed through the review of all the published literature in English retrieved from the PubMed/MEDLINE database between 1966 and March 2011 using the search terms: Levocetirizine, allergic rhinitis, chronic urticaria and antihistamine. Furthermore, the article also reviews data provided by the manufacturer in addition to reports from governmental agencies. Expert opinion: Levocetirizine has several pharmacokinetic properties that are desirable for an antihistamine providing a combination of both potency and safety. Its clinical advantages are derived from its rapid and extensive absorption, limited distribution and its very low degree of metabolism. Furthermore, Levocetirizine scores very highly in terms of clinical efficacy as well as in patient/physician satisfaction studies. Given the lack of large multi-center studies that compare the treatment options for urticaria, clinicians must rely on potency studies when choosing treatment and Levocetirizine does score very highly. However, other potent skin antihistamines, such as desloratadine or fexofenadine, should be preferred for patients who have a strict contraindication to the sedative effects of the drug.