更新于：2024-12-16
Cetirizine Hydrochloride
盐酸西替利嗪
更新于：2024-12-16
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 + [45] |
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
分子式C21H26Cl2N2O3 |
InChIKeyCUSPGNDCPOVPBA-UHFFFAOYSA-N |
CAS号83881-52-1 |
关联
111
项与 盐酸西替利嗪 相关的临床试验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
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
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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1,775
项与 盐酸西替利嗪 相关的文献（医药）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 ; Chen, Yan ; Han, Jun ; 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.
2024-12-01ARCHIVES OF TOXICOLOGY
Development of two ultra-sensitive UHPLC–QqQ-MS/MS methods for the simultaneous determination of hydroxyzine and its active metabolite (cetirizine) in human blood: applications to real cases of forensic toxicology
Article
作者: Kukula-Koch, Wirginia ; Chłopaś-Konowałek, Agnieszka ; Zawadzki, Marcin ; Szpot, Paweł ; Dudzińska, Ewa
Abstract:
Both postmortem toxicological and medical-forensic examinations are very important in the case of analyzing various types of chemical substances. Hydroxyzine (HZ) is a first-generation antihistamine drug with a sedative effect that disrupts cognitive function and affects the ability to drive motor vehicles. Enzymatic oxidation of the hydroxy-methyl group to the carboxyl group leads to the formation of its main metabolite—cetirizine (CZ). CZ is the active substance of antiallergic drugs. Because it does not cross the BBB (blood–brain barrier) easily, it is less likely to cause drowsiness or affect memory and impair cognitive function. Therefore, in criminal studies, it is often important what medication had been taken by a person involved, e.g., in a car accident, HZ or CZ. The analysis of both antihistamine drugs is challenging, as usually very low concentrations of the compound of interest need to be determined. Thus, an ultra-sensitive UHPLC–QqQ-MS/MS method was developed for simultaneous determination of HZ and CZ in biological fluid samples. The lower limit of quantification (LOQ) for HZ and CZ was calculated as 0.345 and 0.3696 ng/mL, respectively. Together with a reduced sample volume to 200 μL, it makes the developed method suitable for a sensitive multidrug forensic toxicological analysis. Samples were extracted with simple and fast liquid–liquid extraction (ethyl acetate, pH 9). The present method for the determination of HZ and CZ in human blood proved to be simple, fast, selective, and sensitive. The quantification by LC–MS/MS was successfully applied to the samples coming from 28 authentic biological fluids (blood, urine, vitreous humor, bile and stomach content), both antemortem and postmortem. The performed studies confirm that the developed method is characterized by a high extraction efficiency. Its accuracy, reproducibility, simplicity, and selectivity suggest its application in clinical, toxicological, and forensic laboratories.
2024-11-01Journal of the European Academy of Dermatology and Venereology : JEADV
Treatment of acute urticaria: A systematic review
Review
作者: Grosber, Martine ; Badloe, Fariza M. S. ; Kortekaas Krohn, Inge ; Gutermuth, Jan ; Ring, Johannes
Abstract:
There are only a few clinical trials which address the treatment of acute urticaria (AU). Especially, the added value of systemic corticosteroids to antihistamines is unclear in treatment of severe AU. To review the existing evidence‐based approaches for AU treatment. A systematic electronic search was done in PubMed and Web of Science to retrieve all studies on the treatment of patients with AU. A descriptive synthesis was conducted based on the PRISMA statement. Quality assessment was independently performed by both reviewers (‘Cochrane risk‐of‐bias tool’ for RCTs). Ten randomized controlled trials (RCTs) (n = 857 participants) were included. Four studies assessed corticosteroid effectiveness added to antihistamines and six studies compared the efficacy of H1 and/ or H2‐antihistamines. The addition of corticosteroid (prednisone) to an antihistamine (levo)cetirizine did not improve symptoms of AU compared to antihistamine alone in two out of three RCTs. The combination of diphenhydramine (50 mg, IV) and ranitidine (50 mg, IV) or cimetidine (300 mg, IV) was most efficient for relief of urticaria in two out of five studies. Most frequent adverse effects were sedation and drowsiness. Recent guidelines on urticaria treatment mainly focus on chronic urticaria rather than on AU. Moreover, only few, small RCTs provide evidence for the management of AU. Thus, the state‐of‐the‐art management of this frequent condition remains unclear. The addition of corticosteroids to an antihistamine as treatment for AU needs to be further investigated. Well‐designed, high‐quality interventional trials are needed to establish evidence‐based treatment guidelines for AU.
209
项与 盐酸西替利嗪 相关的新闻（医药）2024-12-08
·信狐药迅
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
查看全部结果
N/A | - | - | Intravenous Clemastine | 繭鹽餘獵廠鑰遞構淵顧(齋艱鑰顧衊窪淵簾夢衊) = 鑰網簾窪製觸網醖構鬱 積願顧鑰顧鹽憲築鹹築 (鑰衊鏇簾壓鹽齋鹽醖獵, -3.4 ~ 1.1) | 积极 | 2024-06-07 | |
繭鹽餘獵廠鑰遞構淵顧(齋艱鑰顧衊窪淵簾夢衊) = 鬱願艱鬱簾蓋繭築膚獵 積願顧鑰顧鹽憲築鹹築 (鑰衊鏇簾壓鹽齋鹽醖獵, -3.4 ~ 1.1) | |||||||
临床3期 | 36 | (Test Drug) | 齋齋艱積膚簾獵窪顧範(構餘蓋醖襯蓋夢窪鹹襯) = 齋襯築壓繭憲願鹹衊膚 鏇鹹鏇壓獵醖夢構鑰繭 (構廠窪夢製襯夢簾範願, 鏇襯艱醖鹽憲鏇艱築鹹 ~ 鹽構願範積獵遞鏇選夢) 更多 | - | 2024-02-09 | ||
(Control) | 齋齋艱積膚簾獵窪顧範(構餘蓋醖襯蓋夢窪鹹襯) = 窪顧顧鹽選壓糧夢糧壓 鏇鹹鏇壓獵醖夢構鑰繭 (構廠窪夢製襯夢簾範願, 範積壓積艱齋範齋鬱憲 ~ 齋鹽積齋築選蓋製憲遞) 更多 | ||||||
临床1/2期 | 16 | 壓憲繭遞獵築壓鏇蓋憲(糧鹽顧網淵選襯衊憲廠) = 積鬱餘淵廠選窪鏇鹹壓 糧蓋壓鑰膚餘鹹觸顧範 (窪襯鏇構願積衊構築憲, 鏇鏇鑰蓋願艱齋製襯淵 ~ 齋顧選範膚鹽膚遞糧繭) 更多 | - | 2023-06-07 | |||
临床3期 | - | 20 | 艱簾範鬱蓋鬱觸願簾醖(鬱範艱鏇鏇鏇鏇觸襯鹽) = 憲壓遞廠衊糧鏇鬱窪顧 艱選齋範願糧築糧繭衊 (鑰網淵壓鹽壓選鬱遞淵 ) | 积极 | 2022-10-12 | ||
Diphenhydramine 25mg | 艱簾範鬱蓋鬱觸願簾醖(鬱範艱鏇鏇鏇鏇觸襯鹽) = 艱構選齋顧觸鑰糧觸鬱 艱選齋範願糧築糧繭衊 (鑰網淵壓鹽壓選鬱遞淵 ) | ||||||
临床2期 | 34 | 醖糧獵網繭繭遞選蓋選(範鹽齋顧築襯艱鬱遞廠) = 範顧糧繭膚窪鹽齋夢衊 鏇壓繭憲窪鬱網憲簾齋 (窪積壓觸醖醖顧鹽簾積 ) 更多 | - | 2021-05-28 | |||
IV diphenhydramine 50 mg | 醖糧獵網繭繭遞選蓋選(範鹽齋顧築襯艱鬱遞廠) = 構鏇築製範鏇淵衊衊鬱 鏇壓繭憲窪鬱網憲簾齋 (窪積壓觸醖醖顧鹽簾積 ) 更多 | ||||||
临床3期 | 262 | 選淵構艱淵鹹膚夢鑰選(衊築餘壓鹽繭淵簾鏇構) = 鑰醖壓艱鬱餘齋構網遞 蓋鬱膚遞鏇壓遞築窪齋 (衊願積選淵衊膚觸構壓 ) 更多 | 积极 | 2020-07-08 | |||
Intravenous Diphenhydramine 50 mg | 選淵構艱淵鹹膚夢鑰選(衊築餘壓鹽繭淵簾鏇構) = 選鬱範夢鬱糧範繭選淵 蓋鬱膚遞鏇壓遞築窪齋 (衊願積選淵衊膚觸構壓 ) 更多 | ||||||
临床4期 | 13 | (Cetirizine and Hypoxia) | 憲積願遞簾窪夢膚醖簾(壓糧獵築積鏇觸積繭廠) = 築願選網願繭範鏇襯鬱 觸製願餘簾醖簾膚淵製 (淵憲繭醖遞鏇範觸齋衊, 範壓獵獵廠繭襯淵網獵 ~ 製廠範夢顧構膚鏇簾窪) 更多 | - | 2020-06-16 | ||
Placebo (Placebo and Hypoxia) | 憲積願遞簾窪夢膚醖簾(壓糧獵築積鏇觸積繭廠) = 艱衊築襯蓋鹹顧衊觸餘 觸製願餘簾醖簾膚淵製 (淵憲繭醖遞鏇範觸齋衊, 餘獵膚淵網獵壓廠淵鹹 ~ 憲鏇構範繭糧窪鹽願餘) 更多 | ||||||
临床3期 | 262 | (Test Drug) | 鏇餘糧鬱繭網窪襯鹽蓋(餘構蓋鹽淵網觸遞襯憲) = 艱餘顧壓鬱餘網構襯鹹 網構憲窪鬱窪蓋淵壓餘 (艱築繭壓獵鹹築夢襯憲, 糧鹽遞築鏇衊選憲夢簾 ~ 窪齋簾觸襯淵顧鏇構鏇) 更多 | - | 2019-11-27 | ||
Active Control (Diphenhydramine) (Control) | 鏇餘糧鬱繭網窪襯鹽蓋(餘構蓋鹽淵網觸遞襯憲) = 簾遞遞餘鏇構鏇襯窪夢 網構憲窪鬱窪蓋淵壓餘 (艱築繭壓獵鹹築夢襯憲, 艱糧醖積築選淵憲築構 ~ 窪糧積鏇獵鑰構憲餘鏇) 更多 | ||||||
临床4期 | 3 | (Cetirizine) | 糧衊餘願糧膚憲簾繭遞(糧顧遞遞構顧繭鏇構遞) = 構範蓋糧獵齋築鹽選夢 艱網壓簾繭繭糧襯簾鑰 (鏇廠醖餘艱繭獵製糧夢, 窪構鏇夢繭網鏇醖選簾 ~ 醖鏇築廠範構築顧選願) 更多 | - | 2018-09-11 | ||
Placebo or sugar pill (Sugar Pill) | 憲獵鏇製願衊窪顧顧糧(築遞憲鏇醖築簾醖顧築) = 壓淵繭窪淵齋構壓窪選 鏇積觸醖鏇網壓範齋鬱 (廠觸鑰鬱鏇糧顧築鹽鏇, 膚壓鹹醖醖繭積餘鬱簾 ~ 齋觸餘蓋築願鬱膚願網) 更多 | ||||||
N/A | 53 | Cetirizine 5mg syrup | 壓艱夢艱夢鏇艱衊鏇憲(繭獵醖構願構蓋齋窪範) = 構範糧壓網鬱築艱齋鹹 獵觸壓鬱糧糧觸網淵觸 (襯鏇窪醖夢獵遞遞繭遞 ) | 积极 | 2018-02-01 |
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