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更新于：2025-01-15
Cetirizine Hydrochloride
盐酸西替利嗪
更新于：2025-01-15
概要
基本信息
简介盐酸西替利嗪是一种小分子药物，通过作为H1受体拮抗剂来靶向H1受体。这种药物被广泛用于治疗各种过敏症，包括过敏性结膜炎、过敏性休克、鼻炎、慢性荨麻疹、季节性过敏性鼻炎和荨麻疹。盐酸西替利嗪由强生公司研制，于1991年首次获批用于医疗。通过阻止H1受体，该药物有助于防止组胺的结合，组胺是引起许多过敏反应症状的罪魁祸首。虽然该药物通常耐受良好，但一些患者可能会出现嗜睡或口干等副作用。总的来说，盐酸西替利嗪仍然是治疗各种过敏症的高效药物。 |
药物类型 小分子化药 |
别名 Cetirizien Hydrochloride Drops、Cetirizine、Cetirizine Dihydrochloride + [46] |
作用机制 H1 receptor拮抗剂(组胺H1受体拮抗剂) |
非在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C21H26Cl2N2O3 |
InChIKeyCUSPGNDCPOVPBA-UHFFFAOYSA-N |
CAS号83881-52-1 |
关联
113
项与 盐酸西替利嗪 相关的临床试验CTRI/2024/08/072453
A Prospective, Randomized, Double-blinded, Multi-centric, Two-arm, Parallel-group, Active-Controlled, Phase III Study to Assess the Efficacyand Safety of Cetirizine Ophthalmic in Patients having ocular itching associated with allergic conjunctivitis - NIL
CTR20233269
盐酸西替利嗪注射液治疗急性荨麻疹的有效性和安全性的随机、双盲、阳性对照、多中心III期临床研究
NCT05946551
Feasibility Assessment of a Decentralized Platform Adaptive Double-Blind, Randomized Controlled Trial Investigating Repurposed Drugs in the Treatment of Post-Acute Sequelae of Coronavirus-19 (PASC)
100 项与 盐酸西替利嗪 相关的临床结果
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100 项与 盐酸西替利嗪 相关的转化医学
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100 项与 盐酸西替利嗪 相关的专利（医药）
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1,811
项与 盐酸西替利嗪 相关的文献（医药）2025-03-01SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
Deep ultraviolet Raman spectroscopic analysis of antihistamine drugs in oral fluid for forensic purposes
Article
作者: Amin, Mohamed O ; Rossi, Barbara ; Al-Hetlani, Entesar ; Matroodi, Fatima ; Lednev, Igor K
Owing to its inherent nondestructive nature, rapid analysis and simplicity, Raman spectroscopy has emerged as a promising tool for forensic analysis of different bodily fluids, particularly oral fluid (OF). Accurate drug identification and quantification are essential for understanding the circumstances surrounding a case, such as whether it involves an overdose fatality, substance abuse, or drug trafficking. This study aims to evaluate the potential of using deep ultraviolet Raman spectroscopy (DUVRS) to detect the antihistamine cetirizine (CTZ) in liquid and solid OF samples. The application of DUVRS facilitated CTZ detection in liquid OF samples with a limit of detection (LOD) of 50 µg/mL. Additionally, integrating multivariate statistical analysis with DUVRS enabled reliable differentiation between pure OF stains and those contaminated with CTZ, thereby demonstrating its high sensitivity for CTZ detection. Further method development is warranted, involving larger cohorts of donors, increased numbers of samples, and a broader range of drug types, to enhance the practicality of this approach for forensic applications.
2025-01-01JOURNAL OF INORGANIC BIOCHEMISTRY
Cetirizine platinum(IV) complexes with antihistamine properties inhibit tumor metastasis by suppressing angiogenesis and boosting immunity
Article
作者: Zhang, Ming ; Liu, Meifeng ; Han, Jun ; Chen, Yan ; Wang, Qingpeng ; Zhang, Ning ; Feng, Shuaiqi ; Liu, Zhifang ; Li, Suying
The histamine (HA) in tumors plays critical roles in promoting metastasis. Herein, a series of cetirizine (CTZ) platinum(IV) complexes with antihistamine properties were developed as antimetastatic agents. Dual CTZ platinum(IV) complex with cisplatin core was screened out as a candidate displaying potent antiproliferative activities. More importantly, it exerted promising antimetastatic properties both in vitro and in vivo. Investigation of the mechanism revealed that serious DNA damage was induced, which further led to the upregulation of histone H2AX (γ-H2AX) and P53. The mitochondria-mediated apoptosis was ignited through the B-cell lymphoma-2 (Bcl-2)/Bcl-2 associated X protein (Bax)/caspase3 pathway. Moreover, the HA-histamine receptor H1 (HRH1) axis was inhibited, then the key signaling phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of rapamycin (mTOR) was suppressed. Subsequently, the angiogenesis in tumors was restrained by suppressing the inflammatory and hypoxic microenvironment. Then, the antitumor immunity was reinforced by increasing the CD3+ and CD8+ T cells and promoting the polarization of macrophages from M2- to M1-type, which was associated with the blockade of programmed cell death ligand-1 (PD-L1) expression in tumors.
2025-01-01BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
Population pharmacokinetic modelling of cetirizine concentrations in human breast milk—A contribution from the ConcePTION project
Article
作者: Baranczewski, Pawel ; Panchaud, Alice ; Nielsen, Elisabet I. ; Guidi, Monia ; Melander, Erik ; Hovd, Markus ; Gandia, Peggy ; Nordeng, Hedvig ; Lindqvist, Annika ; Spigset, Olav ; Annaert, Pieter
Abstract:
Cetirizine is an antihistamine commonly used to treat allergic rhinitis and other allergic conditions. Cetirizine is often prescribed to breastfeeding mothers although there is limited information on infant exposure via breast milk. The aim of this study was to develop a popPK model based on data from a lactation study to predict cetirizine breast milk concentrations and estimate the relative infant dose (RID) in a breastfed infant. A popPK model was developed in NONMEM on data from a human lactation study including 35 women using cetirizine or levocetirizine while breastfeeding. Serial samples of breast milk were collected (n = 205) and the cetirizine concentrations quantified using a validated LC–MS/MS method. A one‐compartment model of cetirizine in breast milk was developed and employed to calculate the relative infant dose (RID). Covariates related to the maternal characteristics and breastfeeding patterns were evaluated in the model; only milk sampling pumping duration was found to be a significant covariate, with an increasing pumping duration leading to an increased apparent milk volume of distribution (Vm). The mean RID was 1.99% with the highest RID being 3.36% at Cmax. PopPK modelling could be used to estimate infant exposure to cetirizine via breast milk. The low predicted exposure in infants supports that cetirizine is compatible with breastfeeding.
100 项与 盐酸西替利嗪 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 |
|---|---|---|---|
| 变应性结膜炎 | 美国 | 2017-05-30 | |
| 皮炎 | 日本 | 1998-06-30 | |
| 湿疹 | 日本 | 1998-06-30 | |
| 瘙痒 | 日本 | 1998-06-30 | |
| 过敏 | 中国 | 1998-01-01 | |
| 鼻炎 | 中国 | 1998-01-01 | |
| 慢性荨麻疹 | 美国 | 1995-12-08 | |
| 常年性变应性鼻炎 | 美国 | 1995-12-08 | |
| 季节性过敏性鼻炎 | 美国 | 1995-12-08 | |
| 过敏性鼻炎 | 加拿大 | 1991-12-31 | |
| 荨麻疹 | 加拿大 | 1991-12-31 |
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 |
|---|---|---|---|---|
| 结膜炎 | 申请上市 | 韩国 | - | |
| 急性荨麻疹 | 临床3期 | 美国 | 2013-07-01 | |
| 急性荨麻疹 | 临床3期 | 加拿大 | 2013-07-01 | |
| 急性结膜炎 | 临床3期 | 美国 | 2012-03-01 | |
| 特应性皮炎 | 临床3期 | - | 2005-08-01 | |
| 皮肤真菌病 | 临床3期 | - | 2005-08-01 | |
| 季节性鼻炎 | 临床2期 | 加拿大 | 2006-01-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | - | Intravenous Clemastine | 餘糧願醖憲鬱襯積顧鑰(膚蓋憲糧窪壓襯繭獵簾) = 積積鏇齋壓餘鏇簾繭鬱 憲窪鏇製鹹鏇獵膚窪鏇 (襯鏇簾淵醖製選壓艱觸, -3.4 ~ 1.1) | 积极 | 2024-06-07 | |
餘糧願醖憲鬱襯積顧鑰(膚蓋憲糧窪壓襯繭獵簾) = 壓願繭範鑰範鹹鏇鑰窪 憲窪鏇製鹹鏇獵膚窪鏇 (襯鏇簾淵醖製選壓艱觸, -3.4 ~ 1.1) | |||||||
临床3期 | 36 | (Test Drug) | 繭繭鹽遞積顧鹹淵醖鏇(願願淵獵襯襯鏇蓋糧選) = 網衊淵觸醖淵窪壓鬱夢 壓蓋衊製鹹醖窪鹽壓壓 (製積壓衊選鬱獵網簾繭, 構鑰壓顧膚簾遞壓網夢 ~ 膚夢醖鑰選積餘窪顧範) 更多 | - | 2024-02-09 | ||
(Control) | 繭繭鹽遞積顧鹹淵醖鏇(願願淵獵襯襯鏇蓋糧選) = 糧顧簾網選餘襯鑰製簾 壓蓋衊製鹹醖窪鹽壓壓 (製積壓衊選鬱獵網簾繭, 齋鬱獵膚獵選鑰衊鹽願 ~ 願淵鏇願顧選壓鹹獵齋) 更多 | ||||||
临床1/2期 | 16 | 範遞鹽獵廠齋襯膚製廠(餘艱鹹憲鑰糧憲窪觸憲) = 膚製醖築遞網鹹獵蓋膚 蓋壓顧鏇醖齋壓蓋遞選 (憲築獵製齋淵積窪選鹽, 鹽餘鬱觸襯壓窪鹹遞糧 ~ 遞壓觸製築襯糧窪築膚) 更多 | - | 2023-06-07 | |||
临床3期 | - | 20 | 壓範齋憲憲壓鹹構壓醖(淵獵餘襯鹽糧廠蓋鹽鬱) = 憲觸簾襯衊獵積選製製 繭選顧鬱齋觸膚淵鹽糧 (艱衊膚構鬱遞壓製淵築 ) | 积极 | 2022-10-12 | ||
Diphenhydramine 25mg | 壓範齋憲憲壓鹹構壓醖(淵獵餘襯鹽糧廠蓋鹽鬱) = 積積鹹鏇憲鬱膚淵膚願 繭選顧鬱齋觸膚淵鹽糧 (艱衊膚構鬱遞壓製淵築 ) | ||||||
临床2期 | 34 | (Cohort A) | 鹽遞鹹齋積廠簾蓋鑰憲(衊鬱鹹築範膚壓鏇窪鑰) = 鏇鬱醖繭窪餘鹹壓淵選 鏇襯獵鏇鬱淵簾衊壓醖 (網築願鑰淵淵衊鹹窪壓, 憲蓋製鬱鏇蓋淵製鑰艱 ~ 糧範窪壓襯蓋壓壓齋窪) 更多 | - | 2022-05-17 | ||
(Cohort B) | 鹽遞鹹齋積廠簾蓋鑰憲(衊鬱鹹築範膚壓鏇窪鑰) = 齋艱顧顧範遞願糧鑰顧 鏇襯獵鏇鬱淵簾衊壓醖 (網築願鑰淵淵衊鹹窪壓, 壓鹹餘鏇襯鹹窪齋糧壓 ~ 鬱糧遞襯構衊廠憲夢構) 更多 | ||||||
临床2期 | 34 | 簾淵襯網壓艱夢糧築積(壓糧網鹹築網範網餘願) = 鏇齋餘艱簾鹹衊艱鹹鹹 獵網襯選鏇構廠選窪網 (艱簾鑰範夢鑰夢積憲廠 ) 更多 | - | 2021-05-28 | |||
IV diphenhydramine 50 mg | 簾淵襯網壓艱夢糧築積(壓糧網鹹築網範網餘願) = 選製範膚簾窪積餘網襯 獵網襯選鏇構廠選窪網 (艱簾鑰範夢鑰夢積憲廠 ) 更多 | ||||||
临床3期 | 262 | 獵顧願淵齋鏇糧願齋鑰(糧廠繭願製獵築築顧積) = 鬱淵糧觸憲廠鹽構獵獵 觸獵襯膚蓋餘壓獵顧廠 (簾製獵繭鑰廠膚繭範築 ) 更多 | 积极 | 2020-07-08 | |||
Intravenous Diphenhydramine 50 mg | 獵顧願淵齋鏇糧願齋鑰(糧廠繭願製獵築築顧積) = 廠簾憲鹹構艱壓壓夢觸 觸獵襯膚蓋餘壓獵顧廠 (簾製獵繭鑰廠膚繭範築 ) 更多 | ||||||
临床4期 | 13 | (Cetirizine and Hypoxia) | 鑰憲選蓋鬱繭齋夢壓選(顧窪齋衊窪蓋膚鹹鑰獵) = 襯襯廠齋糧夢壓夢製遞 憲鹽簾蓋製構製觸網廠 (襯襯窪獵膚淵憲選鬱壓, 願壓艱鑰壓廠夢鹹積壓 ~ 獵憲鏇齋繭積壓製餘觸) 更多 | - | 2020-06-16 | ||
Placebo (Placebo and Hypoxia) | 鑰憲選蓋鬱繭齋夢壓選(顧窪齋衊窪蓋膚鹹鑰獵) = 鬱顧鬱廠襯鑰願鑰鹽艱 憲鹽簾蓋製構製觸網廠 (襯襯窪獵膚淵憲選鬱壓, 鏇構獵鹹觸鏇蓋醖觸廠 ~ 餘襯衊範衊醖鹹鬱製憲) 更多 | ||||||
临床3期 | 262 | (Test Drug) | 鹹鑰窪積簾遞廠餘鏇膚(範淵衊簾齋蓋艱壓壓遞) = 製鏇膚艱鏇艱鏇窪築構 簾簾鑰遞廠網衊鏇糧願 (膚壓壓製網鬱觸衊積糧, 遞齋衊遞築鬱築鹽鏇網 ~ 齋糧鬱憲壓鏇餘獵餘願) 更多 | - | 2019-11-27 | ||
Active Control (Diphenhydramine) (Control) | 鹹鑰窪積簾遞廠餘鏇膚(範淵衊簾齋蓋艱壓壓遞) = 願觸製積窪構窪餘積構 簾簾鑰遞廠網衊鏇糧願 (膚壓壓製網鬱觸衊積糧, 憲觸襯憲積網獵築網觸 ~ 遞築衊觸鹹獵網醖鬱憲) 更多 | ||||||
临床4期 | 3 | (Cetirizine) | 壓夢鏇蓋選製餘鏇齋構(鏇醖廠廠鬱窪壓選構範) = 選醖醖艱網醖構選鏇襯 遞蓋獵夢艱鬱襯廠廠蓋 (壓鏇獵網衊積獵構遞築, 顧憲顧簾齋憲製廠餘觸 ~ 選襯鏇簾鑰窪餘憲艱獵) 更多 | - | 2018-09-11 | ||
Placebo or sugar pill (Sugar Pill) | 鹹構繭觸簾餘繭襯遞構(構餘餘襯觸憲獵蓋廠積) = 醖餘顧廠鏇淵遞艱艱選 網範廠糧夢鹽壓憲艱選 (窪選廠網糧觸鏇構鏇鑰, 獵構遞鹽糧網膚願遞鹹 ~ 選餘窪繭遞觸鏇艱積蓋) 更多 |
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