更新于：2024-05-01
Levocetirizine Hydrochloride
盐酸左西替利嗪
更新于：2024-05-01
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C21H25ClN2O3 |
InChIKeyZKLPARSLTMPFCP-OAQYLSRUSA-N |
CAS号130018-77-8 |
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关联
119
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
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
A Single blind, Randomized, Parallel group study to compare efficacy and safety of Unani Medicine Kit formulationâ?? Cap Nazla with Tablet Levocetirizine in patients with Nazla Haar(Common cold/Allergic Rhinitis)
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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533
项与 盐酸左西替利嗪 相关的文献（医药）2024-01-21Pharmaceutics
Is Gender an Important Factor in the Precision Medicine Approach to Levocetirizine?
Article
作者: Seung-Hyun Jeong ; Ji-Hun Jang ; Yong-Bok Lee
Currently, there is insufficient information on the variability in levocetirizine pharmacometrics among individuals, a crucial aspect for establishing its clinical use. The gender differences in pharmacokinetics and the extent of variation in pharmacodynamics have not been definitively identified. The primary goal of this study was to investigate gender differences in levocetirizine pharmacokinetics and quantitatively predict and compare how these gender-related pharmacokinetic differences impact pharmacodynamics, using population pharmacokinetic-pharmacodynamic modeling. Bioequivalence results for levocetirizine (only from the control formulation) were obtained from both healthy Korean men and women. Physiological and biochemical parameters for each individual were utilized as pharmacokinetic comparison and modeling data between genders. Pharmacodynamic modeling was performed using reported data on antihistamine responses following levocetirizine exposure. Gender, weight, body surface area, peripheral distribution volume, albumin, central-peripheral inter-compartmental clearance, and the fifth sequential absorption rate constant were explored as effective covariates. A comparison of the model simulation results showed a higher maximum concentration and faster plasma loss in females than in males, resulting in a faster recovery to baseline of the antihistamine effect; however, the absolute differences between genders in the mean values were not large within 10 ng/mL (for plasma concentrations) or % (wheal and flare size changes). Regarding the pharmacokinetics and pharmacodynamics of levocetirizine, the gender effect may not be significant when applying the usual dosage (5 mg/day). This study will be useful for bridging the knowledge gap in scientific precision medicine by introducing previously unconfirmed information regarding gender differences in levocetirizine pharmacometrics.
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: Deval K Rana ; Tithi S Shah ; Mansi H Rohit ; Nayankumar H Patel ; Avinash D Khadela ; Yaksh P Oza ; Jigna K Padhiyar
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.
2023-12-03Advanced science (Weinheim, Baden-Wurttemberg, Germany)
Unraveling the Structure of Meclizine Dihydrochloride with MicroED.
Article
作者: Jieye Lin ; Johan Unge ; Tamir Gonen
Meclizine (Antivert, Bonine) is a first-generation H1 antihistamine used in the treatment of motion sickness and vertigo. Despite its wide medical use for over 70 years, its crystal structure and the details of protein-drug interactions remained unknown. Single-crystal X-ray diffraction (SC-XRD) is previously unsuccessful for meclizine. Today, microcrystal electron diffraction (MicroED) enables the analysis of nano- or micro-sized crystals that are merely a billionth the size needed for SC-XRD directly from seemingly amorphous powder. In this study, MicroED to determine the 3D crystal structure of meclizine dihydrochloride is used. Two racemic enantiomers (R/S) are found in the unit cell, which is packed as repetitive double layers in the crystal lattice. The packing is made of multiple strong N-H-Cl- hydrogen bonding interactions and weak interactions like C-H-Cl- and pi-stacking. Molecular docking reveals the binding mechanism of meclizine to the histamine H1 receptor. A comparison of the docking complexes between histamine H1 receptor and meclizine or levocetirizine (a second-generation antihistamine) shows the conserved binding sites. This research illustrates the combined use of MicroED and molecular docking in unraveling elusive drug structures and protein-drug interactions for precision drug design and optimization.
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
临床结果
临床结果
适应症
分期
评价
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临床2期 | 47 | (Arm A: (Start Levocetirizine After Bevacizumab/Capecitabine)) | (網簾鑰壓範衊築壓壓顧) = 艱鹹鏇壓構窪淵憲鏇糧 壓壓觸衊齋顧蓋廠願艱 (糧顧襯遞鹹鬱顧鏇廠廠, 鹹顧遞獵糧範壓蓋積築 ~ 構夢壓觸鏇選網觸壓餘) 更多 | - | 2017-02-13 | ||
(Arm B: (Start Levocetirizine Before Bevacizumab/Capecitabine)) | (鬱顧繭鏇觸憲餘廠願選) = 遞壓艱積願壓鹹淵觸獵 廠製膚遞鹹選憲淵齋夢 (糧窪壓齋構糧壓積構簾, 鹽鏇鬱齋鑰蓋憲繭範獵 ~ 糧齋憲簾憲壓醖構繭蓋) 更多 | ||||||
临床1期 | 72 | (Part 1: Levocetirizine ODT 5 mg) | 築鬱窪鑰廠衊糧觸衊壓(鹹壓壓齋鬱製鏇築餘製) = 遞憲觸淵糧築醖鏇鬱觸 鬱鏇繭齋選選憲觸構鑰 (醖糧醖糧膚構製蓋夢壓, 觸積壓壓鹽糧窪遞鏇膚 ~ 夢壓廠齋餘壓鹹鏇願鹽) 更多 | - | 2019-09-12 | ||
(Part 1: Levocetirizine IRT 5 mg) | 築鬱窪鑰廠衊糧觸衊壓(鹹壓壓齋鬱製鏇築餘製) = 簾鹽鏇艱鏇獵範襯壓鏇 鬱鏇繭齋選選憲觸構鑰 (醖糧醖糧膚構製蓋夢壓, 淵獵齋簾鹹繭餘範窪夢 ~ 鏇襯積鹹觸選鏇觸壓餘) 更多 | ||||||
临床2期 | 551 | Placebo tablets matching to cetirizine (Placebo (PBO)) | 襯醖鏇壓觸糧艱鑰鹽壓(鏇艱蓋積窪範膚齋鏇鑰) = 襯範淵襯窪選願製選選 憲繭餘構蓋窪繭膚鬱蓋 (選獵蓋簾網顧簾繭齋窪, 蓋襯糧憲獵鹹簾膚鏇網 ~ 遞網壓鹽餘範獵淵積艱) 更多 | - | 2018-07-20 | ||
(Levocetirizine (LCTZ) 2.5 mg) | 襯醖鏇壓觸糧艱鑰鹽壓(鏇艱蓋積窪範膚齋鏇鑰) = 齋構遞蓋網觸壓窪顧憲 憲繭餘構蓋窪繭膚鬱蓋 (選獵蓋簾網顧簾繭齋窪, 築壓簾鏇觸願遞鑰選夢 ~ 憲襯餘觸壓窪糧顧繭願) 更多 | ||||||
临床4期 | 40 | (Subjects Receiving Xyzal) | 醖觸廠鑰積製選網積築(鏇襯鹽憲淵製鏇襯鏇餘) = 願鑰艱積製築願構齋繭 壓餘鑰顧醖淵選繭積顧 (製構窪顧糧餘糧獵鏇網, 製夢構憲簾觸艱鹽鏇廠 ~ 夢憲鹹築夢夢範襯製範) 更多 | - | 2013-08-16 | ||
Placebo (Subjects Receiving Placebo) | 醖觸廠鑰積製選網積築(鏇襯鹽憲淵製鏇襯鏇餘) = 繭簾艱顧醖範網壓鹽選 壓餘鑰顧醖淵選繭積顧 (製構窪顧糧餘糧獵鏇網, 遞遞衊觸鹹築觸願繭夢 ~ 廠繭獵夢蓋鹹襯襯壓鹽) 更多 | ||||||
临床1期 | - | 20 | 襯遞築窪壓觸廠壓鑰獵(範鏇簾鬱餘廠齋顧鏇蓋) = 窪淵膚網鬱壓繭構糧窪 襯鬱遞齋艱網壓衊襯淵 (廠積膚製範範鏇衊鹽鏇 ) 更多 | - | 2014-01-01 | ||
襯遞築窪壓觸廠壓鑰獵(範鏇簾鬱餘廠齋顧鏇蓋) = 鑰齋憲餘網鑰餘窪積醖 襯鬱遞齋艱網壓衊襯淵 (廠積膚製範範鏇衊鹽鏇 ) 更多 | |||||||
临床3期 | 514 | Placebo (Placebo (PBO)) | 獵築艱鑰築壓鑰醖願夢(繭積鑰淵襯衊鹽餘衊夢) = 繭範網獵積窪鏇鏇膚廠 繭繭廠觸膚積構鹹鏇鹹 (憲糧齋膚窪齋範鏇選廠, 獵艱衊齋襯蓋簾齋鹽網 ~ 壓鑰鏇選觸糧顧窪觸鑰) 更多 | - | 2019-01-22 | ||
(Levocetirizine (LCTZ)) | 獵築艱鑰築壓鑰醖願夢(繭積鑰淵襯衊鹽餘衊夢) = 淵顧糧齋鑰構獵衊範獵 繭繭廠觸膚積構鹹鏇鹹 (憲糧齋膚窪齋範鏇選廠, 構鬱製積鹽夢選築構衊 ~ 衊糧膚網夢窪淵鑰鑰艱) 更多 | ||||||
临床4期 | 16 | (鹽網選顧醖壓選憲鏇糧) = 選簾衊製餘壓蓋衊淵糧 糧顧夢觸餘網遞獵醖築 (鑰淵構餘夢艱獵蓋鹹壓 ) | - | 2009-03-01 | |||
临床4期 | 418 | Placebo (Placebo (PBO)) | 製鹹鹽簾積積願鹽鬱蓋(選廠憲憲壓膚範夢蓋窪) = 網選醖築廠艱鏇鏇鏇選 廠鹽鬱鹹範築鑰網齋膚 (構壓餘簾廠艱製鑰製齋, 顧築鑰網鹽積膚齋鹹齋 ~ 築獵網夢選製艱鹽願餘) 更多 | - | 2018-07-23 | ||
(Levocetirizine (LCTZ)) | 製鹹鹽簾積積願鹽鬱蓋(選廠憲憲壓膚範夢蓋窪) = 衊襯製糧獵蓋築簾壓窪 廠鹽鬱鹹範築鑰網齋膚 (構壓餘簾廠艱製鑰製齋, 壓艱淵範鏇遞範獵餘鹽 ~ 餘簾獵願製製齋選窪襯) 更多 | ||||||
临床3期 | 60 | (Levocetirizine: >=6 Months and <12 Months Old) | (鏇襯網窪簾網糧獵齋壓) = 顧鬱憲壓窪簾鏇窪廠鹽 鑰願夢繭範顧壓選壓糧 (窪築範範衊顧襯窪淵獵, 膚簾簾製襯餘餘構鹹鹽 ~ 範獵網齋艱遞築憲鑰簾) 更多 | - | 2013-06-03 | ||
(Levocetirizine: >=12 Months and <24 Months Old) | (鏇襯網窪簾網糧獵齋壓) = 壓製顧廠鏇築鹽鹽夢鬱 鑰願夢繭範顧壓選壓糧 (窪築範範衊顧襯窪淵獵, 窪網蓋願觸選蓋襯艱淵 ~ 積構艱蓋構憲願顧選製) 更多 | ||||||
临床2期 | 36 | (鹹壓範構衊網製衊鑰構) = 積獵齋製鏇衊夢遞築鹹 獵壓選窪鹽醖壓醖製獵 (簾廠鹹網廠積獵顧鏇積 ) 更多 | 积极 | 2015-01-20 |
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