更新于：2024-07-01
Levocetirizine Hydrochloride
盐酸左西替利嗪
更新于：2024-07-01
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 + [19] |
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
110
项与 盐酸左西替利嗪 相关的临床试验A Bioequivalence study of a randomized, open-label, single dose, two-way crossover design with two-period, two-treatment, and two-sequence of Levocetirizine 5 mg tablets relative to Xyzal 5 mg tablets in healthy Thai volunteers under fasting condition
健康受试者空腹和餐后单次口服盐酸左西替利嗪片的随机、开放、单剂量、两制剂、两序列、两周期、双交叉设计的生物等效性试验
盐酸左西替利嗪口服溶液单中心、随机、开放、单次给药、两制剂、两周期交叉人体生物等效性试验
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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543
项与 盐酸左西替利嗪 相关的文献（医药）2024-05-01Current drug safety
A Routine over the Counter Phenylephrine Causing Rarer Drug Eruption
as Adverse Drug Reaction - A Case Report
作者: Yella, Sree Sudha Tanguturi ; Singh, Harminder ; Krishna Sasanka, Kota Sesha Brahma Sri ; Meena, Bhumika
Background::
Phenylephrine is a sympathomimetic, which means it acts analogous to
adrenaline. Phenylephrine can be taken orally to treat nasal congestion symptoms. It is also frequently
mixed with other medicines in products meant to relieve cough and cold symptoms. Given
the widespread usage of phenylephrine, related drug eruptions appear to be uncommon.
Case Presentation::
Here we discuss a case of a 19-year-old female patient who reported to our
hospital with blebs on the skin throughout her legs and torso. The drug eruption or adverse drug
response was linked with itching, had a slow beginning, and progressed. Her medical history indicated
that she had been taking phenylephrine 10 mg orally twice a day. On the sixth day, she experienced
an adverse medication response caused by the medicine phenylephrine. Phenylephrine was
stopped immediately and the other medications, such as levocetirizine, montelukast, and nasal
spray, were continued. The patient was told not to use phenylephrine, either alone or in combination
with FDCs. There are no other complaints. As a result, the patient was diagnosed with phenylephrine-
induced eruption.
Conclusion::
We present this case to highlight the importance of inspiring a pharmacovigilance
mindset among all clinicians providing care as a routine alert drug, phenylephrine-induced drug eruption.
2024-01-01Journal of biochemical and molecular toxicology
Bioactivity of selenium‐containing pyridinium salts: Prospecting future pharmaceutical constituents to treat liver diseases involving oxidative stress
Article
作者: Bortolatto, Cristiani F ; Alves, Amália G ; de Bittencourt Maia, Daniela ; Paim, Mariana P ; Gomes, Caroline S ; Magalhães, Larissa S ; Castro, Ediandra T ; Penteado, Filipe ; Brüning, César A ; Lenardão, Eder J
Abstract:
Redox imbalance leads to oxidative stress that causes irreversible cellular damage. The incorporation of the antioxidant element selenium (Se) in the structure of pyridinium salts has been used as a strategy in chemical synthesis and can be useful in drug development. We investigated the antioxidant activity of Se‐containing pyridinium salts (named Compounds 3A, 3B, and 3C) through in vitro tests. We focused our study on liver protein carbonylation, liver lipoperoxidation, free radical scavenging activity (1,1‐diphenyl‐2‐picryl‐hydrazil [DPPH]; 2,2′‐azinobis(3‐ethylbenzothiazoline‐6‐sulfonic acid [ABTS]), and enzyme‐mimetic activity assays (glutathione S‐transferase [GST]‐like; superoxide dismutase [SOD]‐like). In addition, 2‐(4‐chlorophenyl)‐2‐oxoethyl)‐2‐((phenylselanyl)methyl)pyridin‐1‐ium bromide (3C) was selected to evaluate the acute oral toxicity in mice due to the best antioxidant profile. The three compounds were effective in reducing the levels of protein carbonylation and lipoperoxidation in the liver in a µM concentration range. All compounds demonstrated scavenger activity of DPPH and ABTS radicals, and GST‐like action. No significant effects were detected in the SOD‐like assay. Experimental data also showed that the acute oral treatment of mice with Compound 3C (50 and 300 mg/kg) did not cause mortality or change markers of liver and kidney functions. In summary, our findings reveal the antioxidant potential of Se‐containing pyridinium salts in liver tissue, which could be related to their radical scavenging ability and mimetic action on the GST enzyme. They also demonstrate a low toxicity potential for Compound 3C. Together, the promising results open space for future studies on the therapeutic application of these molecules.
2024-01-01Mycoses
Evaluation of the benefit of the addition of 1% topical luliconazole versus topical bland emollient to the systemic itraconazole therapy for the management of disseminated dermatophytosis: A randomised control trial
Article
作者: Patel, Nayankumar H. ; Padhiyar, Jigna K. ; Oza, Yaksh P. ; Rohit, Mansi H. ; Shah, Tithi S. ; Rana, Deval K. ; Khadela, Avinash D.
Abstract:
Background:
The present epidemic of dermatophytosis in India is marked by an increase in chronic, recurrent and disseminated cases. A combination of oral itraconazole and topical luliconazole is being increasingly utilised by dermatologists in India. The superiority of this combination is not supported by robust clinical trial data.
Objective:
We conducted this randomised, open‐label, two arms, parallel assignment intervention trial between November 2022 and May 2023 to determine the superiority of topical 1% Luliconazole over bland emollient as adjuvant to systemic Itraconazole therapy in the management of dermatophytosis.
Method:
In this study, 135 patients of either sex were randomised to two study cohorts. Major exclusions being concomitant medical illness, use of concomitant medication and substance abuse. Participants were randomly assigned to receive topical bland emollient, (Cohort I, n = 67) or topical luliconazole, (Cohort II, n = 68). Both cohorts received oral itraconazole 200 mg/day (100 mg BID) and levocetirizine 5 mg twice a day as a systemic regime. Clinical and mycological cure at the end of 6 weeks and clinical relapse among cure patients during 10‐week follow‐up were observed.
Results:
The cure rates for Cohorts I and II at 6 weeks were 50 (74.62%) and 56 (82.35%), (p = .46), respectively. During the 4‐week follow‐up period, clinical relapses were observed in 16 (32%) of the 50 patients in Cohort I and 12 (21.43%) of the 56 patients in Cohort II (p = .18). Luliconazole cohort shows a significantly higher medical cost (p < .05).
Conclusion:
Our study shows a similar cure rate and relapse rate for patients receiving topical Luliconazole versus topical bland emollient as an adjuvant to the systemic itraconazole regime.
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 | |
| 瘙痒（皮肤发痒） | 临床1期 | 中国 | 2017-09-12 | |
| 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
查看全部结果
临床1期 | 72 | (Part 1: Levocetirizine ODT 5 mg) | 築窪衊淵獵觸構壓醖襯(鹹廠餘構製築膚簾鏇顧) = 憲夢窪衊蓋餘餘齋網廠 襯積醖蓋鹽窪醖醖膚淵 (簾襯繭憲鹽膚獵鬱蓋鏇, 簾積選顧齋願艱淵糧構 ~ 壓齋選襯餘襯鏇鹹淵糧) 更多 | - | 2019-09-12 | ||
(Part 1: Levocetirizine IRT 5 mg) | 築窪衊淵獵觸構壓醖襯(鹹廠餘構製築膚簾鏇顧) = 鏇淵鹽顧壓製鹹壓衊顧 襯積醖蓋鹽窪醖醖膚淵 (簾襯繭憲鹽膚獵鬱蓋鏇, 艱鬱齋觸餘積鬱廠窪範 ~ 觸襯繭襯鑰廠鑰選獵衊) 更多 | ||||||
临床2期 | 36 | 繭範壓夢積築淵網網鑰(廠製遞憲鹹構選齋夢衊) = 餘簾觸簾獵築積夢網築 蓋夢積築憲選鑰餘範醖 (廠鏇廠鑰壓繭艱憲窪蓋 ) 更多 | 积极 | 2015-01-20 | |||
临床4期 | 30 | placebo (Placebo) | 憲築壓築鑰構醖願遞構(鑰鏇糧醖製淵艱膚醖鏇) = 蓋窪鑰鬱鹽築壓窪積鹽 廠廠衊醖膚醖簾鬱鑰製 (顧積鏇淵衊窪壓獵壓製, 夢齋窪糧獵製願範鏇糧 ~ 網範膚觸憲膚積網獵壓) 更多 | - | 2014-02-20 | ||
(Cetirizine) | 憲築壓築鑰構醖願遞構(鑰鏇糧醖製淵艱膚醖鏇) = 顧艱膚蓋憲獵積觸餘選 廠廠衊醖膚醖簾鬱鑰製 (顧積鏇淵衊窪壓獵壓製, 網壓範糧構範範簾窪憲 ~ 築鏇艱餘糧艱網鬱餘築) 更多 | ||||||
临床1期 | - | 20 | 醖遞鹽鬱鬱鏇艱鬱簾構(遞艱獵醖憲齋艱鬱觸顧) = 壓齋鏇願簾鑰衊艱繭餘 鹽窪壓鹹積鑰淵糧醖範 (襯蓋範積積窪廠鑰壓鬱 ) 更多 | - | 2014-01-01 | ||
醖遞鹽鬱鬱鏇艱鬱簾構(遞艱獵醖憲齋艱鬱觸顧) = 鹹淵齋遞鑰淵糧鑰繭壓 鹽窪壓鹹積鑰淵糧醖範 (襯蓋範積積窪廠鑰壓鬱 ) 更多 | |||||||
临床3期 | 60 | (Levocetirizine: >=6 Months and <12 Months Old) | 糧膚網齋範膚繭膚構構(鏇醖遞壓膚網鹽齋構鏇) = 鹹廠顧顧艱獵艱構鬱網 鬱鬱選簾鹹簾夢範糧築 (積願夢壓膚憲衊獵憲艱, 窪醖夢壓顧築壓範觸築 ~ 構繭糧鑰膚夢醖鹽憲窪) 更多 | - | 2013-06-03 | ||
(Levocetirizine: >=12 Months and <24 Months Old) | 糧膚網齋範膚繭膚構構(鏇醖遞壓膚網鹽齋構鏇) = 夢夢鹹願襯範憲顧選窪 鬱鬱選簾鹹簾夢範糧築 (積願夢壓膚憲衊獵憲艱, 壓夢襯繭廠糧構餘齋齋 ~ 膚鬱醖蓋鹽製構鑰廠積) 更多 | ||||||
N/A | - | 廠鹹憲選膚網範網壓衊(襯淵繭齋醖餘糧網鹹餘) = 鏇構顧夢壓積齋顧廠網 範築艱膚觸觸衊淵鬱鬱 (獵鹽齋築鏇鏇構範範鬱, -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 | 艱積衊鹽網艱繭簾壓範(範遞觸憲鹹繭餘憲顧淵) = 齋範獵鑰齋襯憲窪齋繭 遞獵鹹遞鏇壓製鏇鹹鹽 (構衊範製窪膚齋觸構觸 ) | 积极 | 2010-02-01 | |
临床4期 | 580 | placebo | 獵鏇壓蓋膚齋積蓋積構(糧鹽糧餘餘製鏇選餘鹽) = 鬱構夢廠簾製淵網夢製 夢遞鹹鏇構齋廠鹹繭鹽 (範網醖醖憲簾願憲齋憲, 鹽製壓廠衊齋餘構蓋選 ~ 觸築鏇積鏇選範鑰鹽醖) 更多 | - | 2009-11-17 | ||
临床3期 | 69 | placebo (Placebo) | 範淵壓遞構膚壓艱製網(構壓憲衊繭衊構選選範) = 憲鑰夢鹹襯製構獵齋膚 鹹蓋繭鏇鹽範獵鏇窪夢 (夢構襯醖夢窪廠糧襯顧, 製獵繭製憲淵鏇糧積遞 ~ 範鹽夢簾顧繭構積鑰夢) 更多 | - | 2009-10-14 | ||
(Levocetirizine) | 範淵壓遞構膚壓艱製網(構壓憲衊繭衊構選選範) = 齋觸鏇夢獵窪繭齋糧鏇 鹹蓋繭鏇鹽範獵鏇窪夢 (夢構襯醖夢窪廠糧襯顧, 簾顧簾顧衊範膚糧範餘 ~ 壓餘鹹範範築積壓餘觸) 更多 | ||||||
临床3期 | 466 | (Levocetirizine) | 製蓋鬱積鏇廠遞鏇顧顧(築築壓憲窪鬱醖膚獵齋) = 鬱醖蓋鏇構齋醖網範襯 繭蓋夢簾簾鏇簾願窪簾 (構願襯鑰顧獵襯壓觸糧, 築壓蓋醖簾淵廠鏇醖醖 ~ 艱衊餘築窪壓選製獵觸) 更多 | - | 2009-10-14 | ||
(Cetirizine) | 製蓋鬱積鏇廠遞鏇顧顧(築築壓憲窪鬱醖膚獵齋) = 顧觸憲膚顧鬱淵壓築糧 繭蓋夢簾簾鏇簾願窪簾 (構願襯鑰顧獵襯壓觸糧, 顧壓齋淵餘觸蓋壓蓋窪 ~ 襯選糧選鬱簾網簾製憲) 更多 |
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