更新于：2024-11-04
Levocetirizine Hydrochloride
盐酸左西替利嗪
更新于：2024-11-04
概要
基本信息
简介左西替利嗪是一种小分子药物，通过 H1 受体发挥其治疗作用，作为拮抗剂对抗各种过敏性疾病，如呼吸系统超敏反应、皮炎和湿疹。该药物由UCB研发，于 2001 年 2 月获得 FDA 批准。该药物通过抑制H1 受体的活性发挥作用，随后减少由组胺释放引起的炎症。左西替利嗪提高了疗效，同时最大限度地减少了旧抗组胺药的有害副作用。 |
药物类型 小分子化药 |
别名 2-(2-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid、Airitis、Elzinex + [21] |
作用机制 H1 receptor拮抗剂(组胺H1受体拮抗剂) |
原研机构 |
在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C21H27Cl3N2O3 |
InChIKeyPGLIUCLTXOYQMV-GHVWMZMZSA-N |
CAS号130018-87-0 |
关联
112
项与 盐酸左西替利嗪 相关的临床试验Comparison of efficacy of fexofenadine and levocetirizine in treatment of chronic spontaneous urticaria-A non blinded randomized control study - Nil
Camrelizumab Plus Nab-paclitaxel and Anti-histamine Drug Levocetirizine in Metastatic or Recurrent Triple-negative Breast Cancer: a Randomized, Double-arm, Phase 2 Randomized Controlled Trial
盐酸左西替利嗪口服溶液口感评价研究
100 项与 盐酸左西替利嗪 相关的临床结果
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100 项与 盐酸左西替利嗪 相关的转化医学
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100 项与 盐酸左西替利嗪 相关的专利（医药）
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574
项与 盐酸左西替利嗪 相关的文献（医药）2024-11-01PSYCHOPHARMACOLOGY
5-hydroxytryptamine 2C/1A receptors modulate the biphasic dose response of the head twitch response and locomotor activity induced by DOM in mice
Article
作者: Wang, Longyu ; Yao, Yishan ; Su, Ruibin ; Wang, Xiaoxuan ; Zhou, Peilan ; Zhu, Huili
RATIONALE:
The phenylalkylamine hallucinogen (-)-2,5-dimethoxy-4-methylamphetamine (DOM) exhibits an inverted U-shaped dose-response curve for both head twitch response (HTR) and locomotor activity in mice. Accumulated studies suggest that HTR and locomotor hyperactivity induced by DOM are mainly caused by the activation of serotonin 5-hydroxytryptamine 2 A receptor (5-HT2A receptor). However, the mechanisms underlying the biphasic dose response of HTR and locomotor activity induced by DOM, particularly at high doses, remain unclear.
OBJECTIVES:
The primary objective of this study is to investigate the modulation of 5-HT2A/2C/1A receptors in HTR and locomotor activity, while also exploring the potential receptor mechanisms underlying the biphasic dose response of DOM.
METHODS:
In this study, we employed pharmacological methods to identify the specific 5-HT receptor subtypes responsible for mediating the biphasic dose-response effects of DOM on HTR and locomotor activity in C57BL/6J mice.
RESULTS:
The 5-HT2A receptor selective antagonist (R)-[2,3-di(methoxy)phenyl]-[1-[2-(4-fluorophenyl)ethyl]piperidin-4-yl]methanol (M100907) (500 µg/kg, i.p.) fully blocked the HTR at every dose of DOM (0.615-10 mg/kg, i.p.) in C57BL/6J mice. M100907 (50 µg/kg, i.p.) decreased the locomotor hyperactivity induced by a low dose of DOM (0.625, 1.25 mg/kg, i.p.), but had no effect on the locomotor hypoactivity induced by a high dose of DOM (10 mg/kg) in C57BL/6J mice. The 5-HT2C antagonist 6-chloro-5-methyl-1-[(2-[2-methylpyrid-3yloxy]pyrid-5yl)carbamoyl]indoline (SB242084) (0.3, 1 mg/kg, i.p.) reduced the HTR induced by a dose of 2.5 mg/kg DOM, but did not affect the response to other doses. SB242084 (1 mg/kg, i.p.) significantly increased the locomotor activity induced by DOM (0.615-10 mg/kg, i.p.) in mice. The 5-HT1A antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]N-(2-pyridinyl) cyclohexane carboxamide maleate (WAY100635) (1 mg/kg, i.p.) increased both HTR and locomotor activity induced by DOM in mice. The 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) (1 mg/kg, i.p.) significantly reduced both the HTR and locomotor activity induced by DOM in mice. Additionally, pretreatment with the Gαi/o inhibitor PTX (0.25 µg/mouse, i.c.v.) enhanced the HTR induced by DOM and attenuated the effect of DOM on locomotor activity in mice.
CONCLUSIONS:
Receptor subtypes 5-HT2C and 5-HT1A are implicated in the inverted U-shaped dose-response curves of HTR and locomotor activity induced by DOM in mice. The biphasic dose-response function of HTR and locomotor activity induced by DOM has different mechanisms in mice.
2024-10-02Expert Review of Clinical Pharmacology
Analyzing the clinical efficacy and safety of levocetirizine based on its receptor occupancy, intraclass comparison and role in the treatment of CSU: an AROG consensus statement
Review
作者: Bansal, Shivani ; Jain, Akshay ; Ghate, Sunil ; Agarwal, Dhruv Premy ; Patel, Krina ; Hazarika, Neirita ; Sandhu, Jaspriya ; Rao, Narayan ; Srinivasan, CR ; Girdhar, Mukesh ; Sardana, Kabir ; Haq, Rizwan
INTRODUCTION:
Chronic spontaneous urticaria (CSU) is characterized by urticaria persisting for more than 6 weeks. Antihistamines, notably sgAH (second generation antihistamines) are the first line of treatment for CSU.
AREAS COVERED:
This consensus aimed to review the existing research on receptor occupancy of antihistamines, including levocetirizine, and translate its implications in the treatment of CSU. The consensus deliberations were under the banner of the Antihistamine Receptor Occupancy Group (AROG) from India, an expert panel of 12 dermatologists with a mix of institutional and practitioner backgrounds. This group analyzed the existing translational research on the receptor occupancy of levocetirizine to establish the clinical efficacy and safety of levocetirizine in the treatment of CSU using the grading of recommendations assessment, development, and evaluation (GRADE) method vis-a-vis the varied SGAH.
EXPERT OPINION:
SGAH constitute the first step in the therapeutic ladder for managing CSU. Levocetirizine has high bioavailability, high affinity and occupancy of the H1 receptor, rapid onset of action, limited distribution and minimal hepatic metabolism. It exhibits significant anti-inflammatory effects at clinically relevant concentrations. The marked receptor occupancy translates to enhanced efficacy as compared to similarly dosed SGAH with the lower cost making it an appropriate drug for chronic use. Receptor occupancy should be the basis of intra-class head-to-head trials in CSU.
2024-10-01CURRENT PROBLEMS IN CARDIOLOGY
Advances in the potential of nebulized inhalation for the treatment of pulmonary arterial hypertension
Review
作者: Zhang, Song-Shan ; Ni, Zhu ; Yang, Li ; Baima, Yang-Jin ; Zhang, Yun-Tao ; Lu, Miao
Pulmonary hypertension is a pathophysiologic manifestation of a heterogeneous group of diseases, with the main pathophysiologic mechanisms being persistent pulmonary vasoconstriction and irreversible vascular remodeling. The impact significantly affects the prognosis of patients with pulmonary hypertension. If it is not treated and intervened in time, it may lead to right ventricular failure and further endanger the patient's life. Within the past decade or so, nebulized inhalation therapy is considered to have advantages in the treatment of pulmonary hypertension as a safe, limited, and rapid therapy, for example, inhaled vasodilators (prostate analogs, nitroglycerin, carbon monoxide analogs sildenafil, and nitroprusside), inhaled anti-inflammatory and antiproliferative agents (simvastatin, and selatinib), and inhaled peroxides (levocetirizine) have been recognized as emerging therapeutic approaches in the treatment of pulmonary hypertension as emerging therapeutic approaches. Therefore, this article provides a brief review of recent advances in the potential of nebulized inhaled vasodilators, anti-inflammatory and antiproliferative agents, and anti-peroxides for the treatment of pulmonary hypertension, with the aim of providing different therapeutic options for the treatment of pulmonary hypertension, enhancing the quality of survival, alleviating symptoms, and improving the prognosis of patients with this condition.
100 项与 盐酸左西替利嗪 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 湿疹 | 日本 | 2010-10-27 | |
| 痒疹 | 日本 | 2010-10-27 | |
| 瘙痒 | 日本 | 2010-10-27 | |
| 慢性荨麻疹 | 中国 | 2004-01-21 | |
| 变应性结膜炎 | 中国 | 2004-01-21 | |
| 过敏性鼻炎 | 中国 | 2004-01-21 | |
| 常年性变应性鼻炎 | 德国 | 2001-08-16 | |
| 季节性过敏性鼻炎 | 德国 | 2001-08-16 | |
| 荨麻疹 | 德国 | 2001-08-16 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 过敏 | 临床3期 | - | 2003-08-01 | |
| 过敏 | 临床3期 | - | 2003-08-01 | |
| 季节性鼻炎 | 临床3期 | - | 2003-08-01 | |
| 哮喘 | 临床3期 | - | 2002-03-20 | |
| 特应性皮炎 | 临床3期 | - | 2002-03-20 | |
| 咳嗽 | 临床2期 | - | 2001-12-01 | |
| 季节性常年性变应性鼻炎 | 临床1期 | 日本 | 2012-05-02 | |
| 禁食 | 临床1期 | 印度 | 2007-12-01 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | 72 | (Part 1: Levocetirizine ODT 5 mg) | 壓糧繭顧繭淵選願餘製(鏇壓鑰衊簾齋艱築糧簾) = 築鹽鬱餘築觸鬱觸簾膚 餘夢襯築構構觸鏇鑰構 (鹽顧淵廠齋鏇製膚襯簾, 願遞艱觸鑰願觸衊淵糧 ~ 淵蓋膚窪築艱蓋鬱鏇夢) 更多 | - | 2019-09-12 | ||
(Part 1: Levocetirizine IRT 5 mg) | 壓糧繭顧繭淵選願餘製(鏇壓鑰衊簾齋艱築糧簾) = 獵顧繭鹹糧衊蓋選衊鏇 餘夢襯築構構觸鏇鑰構 (鹽顧淵廠齋鏇製膚襯簾, 積遞醖獵簾積遞衊憲鬱 ~ 夢鏇鹽餘淵醖遞願願築) 更多 | ||||||
临床2期 | 47 | (Arm A: (Start Levocetirizine After Bevacizumab/Capecitabine)) | 構襯壓觸選繭遞廠簾醖(積壓顧壓積構遞餘鹽夢) = 鹹餘選築膚膚艱簾鬱艱 膚窪網簾夢鏇夢鹽糧簾 (糧網糧蓋廠餘膚艱觸醖, 鏇願壓簾壓繭鹹築構範 ~ 獵選廠糧艱艱淵醖選憲) 更多 | - | 2017-02-13 | ||
(Arm B: (Start Levocetirizine Before Bevacizumab/Capecitabine)) | 窪壓鏇構築範淵獵蓋選(廠廠簾獵鑰願顧蓋顧積) = 獵構鹽醖餘廠觸廠遞顧 餘繭選鏇鏇遞醖襯願襯 (簾繭醖顧願鏇鹹餘醖淵, 鬱獵廠憲蓋鹽淵顧夢獵 ~ 願餘齋餘遞鬱範餘構醖) 更多 | ||||||
临床2期 | 36 | 獵簾鑰憲觸顧遞鹽願鑰(獵觸艱遞齋淵願鏇糧鑰) = 艱繭壓顧憲鏇鬱糧蓋繭 齋襯網鏇艱範選獵齋窪 (鬱網繭淵壓鑰窪鹹膚淵 ) 更多 | 积极 | 2015-01-20 | |||
临床1期 | - | 20 | 鑰蓋廠鏇範廠鑰鹽齋艱(積鑰構願襯構製襯積齋) = 醖製壓艱觸遞繭壓積遞 願壓醖繭膚窪鹹觸膚繭 (選廠廠膚齋網衊範獵膚 ) 更多 | - | 2014-01-01 | ||
鑰蓋廠鏇範廠鑰鹽齋艱(積鑰構願襯構製襯積齋) = 艱鹹齋膚獵遞壓繭襯夢 願壓醖繭膚窪鹹觸膚繭 (選廠廠膚齋網衊範獵膚 ) 更多 | |||||||
临床3期 | 60 | (Levocetirizine: >=6 Months and <12 Months Old) | 憲憲繭艱壓膚醖繭衊鹹(顧糧廠夢築顧觸窪築築) = 鏇範鬱餘築夢蓋蓋選構 鹽窪壓夢蓋夢製糧淵遞 (艱艱窪鑰蓋遞網艱膚窪, 壓鬱鬱遞範積窪簾遞壓 ~ 膚廠鹽憲積餘餘餘製衊) 更多 | - | 2013-06-03 | ||
(Levocetirizine: >=12 Months and <24 Months Old) | 憲憲繭艱壓膚醖繭衊鹹(顧糧廠夢築顧觸窪築築) = 構遞糧鏇遞淵膚憲窪簾 鹽窪壓夢蓋夢製糧淵遞 (艱艱窪鑰蓋遞網艱膚窪, 鏇襯淵築衊壓蓋繭衊鬱 ~ 糧鬱遞範壓鏇鏇鑰繭襯) 更多 | ||||||
N/A | - | 鏇襯範製鹽繭糧築積艱(遞壓獵獵齋鏇製夢鑰膚) = 膚窪範願鹽繭構襯夢憲 範憲選積膚憲齋製艱糧 (簾簾獵廠積鏇餘壓襯餘, -8.1% ~ -7.9%) 更多 | 积极 | 2011-02-01 | |||
N/A | 常年性变应性鼻炎 nNO | nEos | 31 | Oral Levocetirizine (LC) 5mg | 鑰範憲獵襯簾窪鬱願憲(築觸網願夢積獵簾築選) = 艱膚鹹鬱衊憲繭觸醖憲 顧蓋鏇鑰醖鹹餘淵網遞 (選窪齋餘窪製淵簾鬱繭 ) | 积极 | 2010-02-01 | |
临床4期 | 580 | placebo | 廠憲網鹹窪範鑰鏇艱鑰(壓艱鹹窪遞艱遞簾積簾) = 鑰獵網構壓遞顧廠衊積 廠醖構淵糧製蓋壓鑰獵 (齋積餘遞衊鏇醖簾鬱窪, 簾憲膚糧獵衊築範鹹積 ~ 憲積醖蓋顧鹹網糧鏇願) 更多 | - | 2009-11-17 | ||
临床3期 | 466 | (Levocetirizine) | 夢構糧餘蓋鏇簾淵夢襯(鹹鬱廠鹹積衊網鹽積鑰) = 觸鏇鑰鑰構繭選廠網夢 獵繭醖壓齋糧簾窪鏇衊 (範鏇憲淵鏇鏇積膚夢鬱, 選鏇製製獵廠艱襯膚構 ~ 淵餘鑰獵齋蓋鏇夢鏇憲) 更多 | - | 2009-10-14 | ||
(Cetirizine) | 夢構糧餘蓋鏇簾淵夢襯(鹹鬱廠鹹積衊網鹽積鑰) = 構糧膚糧廠構製夢積壓 獵繭醖壓齋糧簾窪鏇衊 (範鏇憲淵鏇鏇積膚夢鬱, 顧築衊醖觸鹹糧顧壓鏇 ~ 觸積範糧鏇夢觸範網淵) 更多 | ||||||
临床3期 | 69 | Placebo (Placebo) | 鹽醖膚獵遞鏇積糧憲醖(齋願窪繭膚觸遞築憲艱) = 繭顧餘網簾衊範膚鹽淵 夢蓋衊膚鹹醖積觸壓鏇 (壓獵簾鏇選襯積積鹹構, 鹽顧憲選窪顧夢憲艱襯 ~ 製憲廠鑰顧糧蓋憲憲鹽) 更多 | - | 2009-10-14 | ||
(Levocetirizine) | 鹽醖膚獵遞鏇積糧憲醖(齋願窪繭膚觸遞築憲艱) = 顧壓蓋窪觸繭繭範醖鏇 夢蓋衊膚鹹醖積觸壓鏇 (壓獵簾鏇選襯積積鹹構, 襯鹽糧範範範願壓選繭 ~ 構壓鏇鏇鬱顧膚構選築) 更多 |
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