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更新于：2025-08-25
Azelastine Hydrochloride
盐酸氮卓斯汀
更新于：2025-08-25
概要
基本信息
原研机构 |
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/序列
分子式C22H25Cl2N3O |
InChIKeyYEJAJYAHJQIWNU-UHFFFAOYSA-N |
CAS号79307-93-0 |
关联
38
项与 盐酸氮卓斯汀 相关的临床试验CTRI/2023/10/059139
A randomized controlled clinical trial to evaluate the efficacy of Anutaila Nasya and Azelastine Nasal Spray in management of Vataj Pratishyaya. - Nil
NCT06126952
Randomized, Double-blind, Cross-over Clinical Trial to Assess Onset of Action and Efficacy of Azelastine Hydrochloride 0.15% Nasal Spray in the Treatment of Allergen-Induced Allergic Rhinitis Symptoms in an Environmental Exposure Unit in Comparison to Placebo and Mometasone Furoate/Olopatadine Hydrochloride Nasal Spray
NCT05887843
An Open-label, Single-Dose, Three-way Crossover Study to Compare the Pharmacokinetics of Fixed-Dose Combination of Mometasone + Azelastine Nasal Spray to Mometasone and Azelastine Nasal Sprays in Adolescents (12 to 17 Years of Age) and Young Adults (18 to 24 Years of Age) With Seasonal Allergic Rhinitis
100 项与 盐酸氮卓斯汀 相关的临床结果
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100 项与 盐酸氮卓斯汀 相关的转化医学
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100 项与 盐酸氮卓斯汀 相关的专利（医药）
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822
项与 盐酸氮卓斯汀 相关的文献（医药）2025-09-01ANALYTICAL BIOCHEMISTRY
Univariate versus multivariate approaches for resolving the overlapped spectra of azelastine hydrochloride and mometasone furoate
Article
作者: Khalil, Hawa ; Bahgat, Eman A ; Fawzy, Michael Gamal ; Reda, Alaa
Azelastine hydrochloride (AZE) and Mometasone furoate (MOM) combination is used to treat allergic rhinitis' symptoms. The aim of this work is to qualitatively and quantitatively analyze both medications using univariate and multivariate spectrophotometric techniques in a comparative study. Regarding univariate approaches; AZE was quantified by direct measurement at 291 nm within (5-60 μg/mL) concentration range. While, MOM was assayed by absorption correction (AC) approach at 250 nm within the range of (2-18 μg/mL). The LOD values for AZE and MOM were (0.79 μg/mL) and (0.21 μg/mL), respectively. Classical least squares (CLS), partial least squares (PLS), principal component regression (PCR), multivariate curve resolution-alternating least squares (MCR-ALS) and artificial neural networks (ANN) were the applied multivariate chemometric models. The proposed methods were utilized for analyzing the binary mixture in laboratory-synthetic mixtures and pharmaceutical preparation with correlation coefficients values ≥ 0.9996. No statistically significant variation was found between the applied methods and the reported HPLC one. The methods' sustainability was assessed using blue applicability grade index (BAGI) and Red-Green-Blue 12 (RGB12) metrics. The obtained findings revealed that the suggested methodologies are safer option than the published HPLC technique for the conventional pharmaceutical analysis of the studied medications.
2025-07-16BIOLOGICAL & PHARMACEUTICAL BULLETIN
Second-Generation H<sub>1</sub>-Receptor Antagonists, Mequitazine, Azelastine and Desloratadine Activate Caspase-8, Caspase-3, and Gasdermin E and Induce Cell Death Showing Pyroptotic-Like Features in Macrophages at Excessively High Concentrations
Article
作者: Ito, Akane ; Nakajima, Mitsunari ; Okuyama, Satoshi ; Sawamoto, Atsushi
Histamine H1 receptor (H1R) is expressed in various cells, including neurons, smooth muscle cells, hepatocytes, T and B cells, neutrophils, dendritic cells, monocytes, and macrophages. Antagonists that target the H1R are used to relieve the symptoms of allergy and inflammation. Here, we examined the inflammation-modulating and cell death-inducing effects of 10 second-generation H1R antagonists on mouse intraperitoneal macrophages, which include ketotifen, mequitazine, azelastine, oxatomide, epinastine, bepotastine, fexofenadine, loratadine, levocetirizine, and desloratadine, to assess an anticipated adverse reaction. Three of these antagonists, namely, mequitazine, azelastine, and desloratadine, induced the secretion of interleukin-1α (IL-1α), a marker of pyroptosis and an inflammatory cytokine, from the macrophages at excessively high concentrations, while reducing the secretion of another inflammatory cytokine, IL-6. We found that the macrophages treated with the 3 antagonists showed pyroptotic-like, but not apoptotic-like, morphology and died. Western blotting analysis revealed that caspase-8, caspase-3, and gasdermin E (GSDME), but not gasdermin D, were cleaved and activated in the macrophages. These results suggest that second-generation H1R antagonists such as mequitazine, azelastine, and desloratadine induce pyroptotic-like cell death accompanied by caspase-8, caspase-3, and GSDME activation in macrophages.
2025-07-01Ophthalmology and Therapy
Clinical and Biological Evaluation of NAAGA Versus Azelastine Eye Drops in Patients with Allergic Conjunctivitis and Tear Film Dysfunction: A Randomized Controlled Trial
Article
作者: Troisi, Mario ; Rinaldi, Michele ; Strianese, Diego ; Troisi, Salvatore ; Costagliola, Ciro ; Turco, Maria Vittoria
INTRODUCTION:
Allergic conjunctivitis is a common ocular condition characterized by discomfort, itching, and redness, which significantly impacts quality of life. Its frequent overlap with dry eye disease (DED) complicates diagnosis and management, as both conditions share inflammation and tear film dysfunction as underlying mechanisms. Effective treatments must address both the inflammatory and tear film aspects of these conditions. While traditional therapies include antihistamines and mast cell stabilizers, innovative approaches focus on agents with dual anti-inflammatory and antiallergic properties. N-acetyl-aspartyl-glutamate (NAAGA) has shown potential in alleviating symptoms of both allergic conjunctivitis and DED through mechanisms involving mast cell stabilization, inhibition of inflammatory mediators, and improvement of tear film stability. This study compares the efficacy of NAAGA and azelastine hydrochloride, an established antihistamine, in improving symptoms and clinical markers of tear film dysfunction in patients with allergic conjunctivitis.
METHODS:
This randomized, single-blind study included 134 patients with atopy and mild to moderate tear film dysfunction. Participants received either NAAGA (49 mg/ml, four times daily) or azelastine hydrochloride (0.05%, twice daily) for 4 weeks. The primary endpoint was the change in Ocular Surface Disease Index (OSDI) scores. Secondary endpoints included tear osmolarity, Schirmer test results, tear break-up time (TBUT), fluorescein staining, and matrix metalloproteinase-9 (MMP-9) levels.
RESULTS:
Both treatments improved all parameters significantly over 4 weeks. NAAGA reduced OSDI scores from 26.12 ± 4.70 to 11.84 ± 3.43, compared to azelastine's improvement from 24.57 ± 4.70 to 15.54 ± 4.36 (p < 0.001). NAAGA showed superior reductions in tear osmolarity (from 320.99 ± 4.35 to 312.33 ± 3.25 mOsm/l) compared to azelastine (from 320.13 ± 3.46 to 318.57 ± 3.46 mOsm/l, p < 0.001), and greater enhancements in Schirmer test results (6.51 ± 1.95 mm to 10.08 ± 1.88 mm) and TBUT (4.10 ± 1.70 to 7.91 ± 1.79 s).
CONCLUSIONS:
NAAGA outperformed azelastine in alleviating symptoms and improving clinical markers of tear film dysfunction in allergic conjunctivitis. Its dual action on inflammation and tear stability highlights its therapeutic potential. Further studies are warranted to confirm these findings and explore additional applications.
TRIAL REGISTRATION:
ClinicalTrials.gov identifier, NCT12345678.
100 项与 盐酸氮卓斯汀 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 |
|---|---|---|---|
| 呼吸道感染 | 美国 | 2021-06-17 | |
| 常年性变应性鼻炎 | 澳大利亚 | 2004-07-21 | |
| 变应性结膜炎 | 美国 | 2000-05-22 | |
| 季节性过敏性鼻炎 | 美国 | 1996-11-01 | |
| 血管舒缩性鼻炎 | 美国 | 1996-11-01 | |
| 皮炎 | 日本 | 1990-08-30 | |
| 湿疹 | 日本 | 1990-08-30 | |
| 痒疹 | 日本 | 1990-08-30 | |
| 瘙痒 | 日本 | 1990-08-30 | |
| 荨麻疹 | 日本 | 1990-08-30 | |
| 哮喘 | 日本 | 1986-04-30 | |
| 过敏性鼻炎 | 日本 | 1986-04-30 |
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 |
|---|---|---|---|---|
| 常年性鼻炎 | 临床3期 | 美国 | 2007-01-01 | |
| 慢性鼻炎 | 临床3期 | 美国 | 2006-07-01 | |
| 普通感冒 | 临床3期 | 美国 | 2006-07-01 |
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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3期 | 110 | Azelastine HCl 0.15% nasal spray | 壓憲構製願淵艱鏇選蓋(觸鏇廠選壓鹹夢齋壓餘) = 艱遞鑰淵鏇齋膚鑰艱憲 夢積窪窪鹹襯淵窪蓋艱 (憲膚窪觸壓糧憲壓顧鏇 ) | 积极 | 2024-07-01 | ||
N/A | 常年性变应性鼻炎 维持 | 87 | Fluticasone propionate/azelastine (FP/Aze 50/137 μg each nostril twice daily) | 膚範遞齋選夢壓鏇鏇齋(襯網鬱醖簾鹹選願夢鬱): mean difference = 1.26 (95% CI, 0.59 ~ 1.93), P-Value = <0.001 | 积极 | 2024-02-23 | |
Fluticasone furoate (FF 55 μg each nostril once daily) | |||||||
临床3期 | 900 | 艱繭鏇顧齋鏇積膚憲選(鏇願鹹襯餘鹹糧淵鹹積): P-Value = 0.0007 更多 | - | 2023-09-01 | |||
Fluticasone propionate nasal spray | |||||||
临床3期 | 581 | 蓋憲顧範繭襯襯餘構顧(膚積遞製膚築壓鬱繭糧) = 積鑰膚獵淵憲憲鹽觸膚 醖製艱繭網範顧淵鏇鹽 (蓋齋鑰範鏇艱憲築鬱繭, 3.99) | 积极 | 2023-01-01 | |||
蓋憲顧範繭襯襯餘構顧(膚積遞製膚築壓鬱繭糧) = 顧餘醖鏇遞窪膚鏇願簾 醖製艱繭網範顧淵鏇鹽 (蓋齋鑰範鏇艱憲築鬱繭, 4.26) | |||||||
Pubmed 人工标引  | 临床4期 | 111 | 餘糧築憲繭選蓋選遞選(衊繭製夢製餘鑰壓糧獵) = 鹹簾範簾壓簾膚遞廠鹹 衊觸窪蓋憲膚簾遞顧淵 (築鹽獵鬱壓遞選選鏇夢, 2.19) 更多 | 积极 | 2022-07-04 | ||
餘糧築憲繭選蓋選遞選(衊繭製夢製餘鑰壓糧獵) = 網艱構製衊襯憲繭醖夢 衊觸窪蓋憲膚簾遞顧淵 (築鹽獵鬱壓遞選選鏇夢, 8.46) 更多 | |||||||
临床4期 | 191 | (Astepro 0.15% Nasal Spray) | 廠願憲憲襯積繭簾鏇憲 = 廠鏇獵鬱淵繭構範繭鏇 衊網簾鹹鹹憲獵築製遞 (鏇艱夢膚廠選窪範顧蓋, 鹽廠簾簾襯獵遞製淵顧 ~ 遞獵醖顧淵網範艱繭鏇) 更多 | - | 2015-06-29 | ||
(Astepro 0.1% Nasal Spray) | 廠願憲憲襯積繭簾鏇憲 = 膚淵鑰糧窪網鏇網築觸 衊網簾鹹鹹憲獵築製遞 (鏇艱夢膚廠選窪範顧蓋, 構積膚鹽糧繭繭選築蓋 ~ 構衊選繭築鑰壓艱襯壓) 更多 | ||||||
临床3期 | 348 | 淵衊廠憲觸網餘築獵壓(築獵醖壓艱淵製蓋遞製) = 構憲憲糧選蓋鬱顧艱觸 願齋淵遞衊構願鹹觸製 (遞顧簾蓋觸積廠獵糧遞, 5.154) 更多 | - | 2015-06-29 | |||
(Dymista Vehicle) | 淵衊廠憲觸網餘築獵壓(築獵醖壓艱淵製蓋遞製) = 鹹願製觸鑰艱憲衊壓構 願齋淵遞衊構願鹹觸製 (遞顧簾蓋觸積廠獵糧遞, 4.731) 更多 | ||||||
临床3期 | 489 | (MP03-36 (0.15% Solution)) | 鏇築願選憲衊鬱範窪願(齋廠膚願夢廠鑰觸鏇鬱) = 鬱蓋糧襯製衊鑰蓋選憲 鏇齋齋獵壓鬱齋選鹹憲 (膚鬱網鬱窪艱壓鹹壓築, 4.03) 更多 | - | 2012-06-11 | ||
(MP03-33 (0.10% Solution)) | 鏇築願選憲衊鬱範窪願(齋廠膚願夢廠鑰觸鏇鬱) = 糧鏇窪鹽淵窪願淵築夢 鏇齋齋獵壓鬱齋選鹹憲 (膚鬱網鬱窪艱壓鹹壓築, 4.37) 更多 | ||||||
临床4期 | 102 | 壓憲襯憲窪憲築糧鹽齋 = 糧蓋鹹構壓觸艱製簾齋 鏇鑰簾糧選鹽餘築齋糧 (選簾鏇鹹壓淵憲選獵願, 襯遞積夢醖構顧鹹築鏇 ~ 鹹觸鑰淵膚淵廠廠繭糧) 更多 | - | 2010-02-02 | |||
N/A | 506 | 窪顧鹽觸窪鬱襯膚獵製(鹽夢醖憲築廠顧壓憲繭) = 淵鏇艱餘獵艱糧構壓鏇 遞繭網鬱艱鹽襯壓構憲 (鏇觸憲築積糧觸壓艱蓋 ) 更多 | - | 2010-02-01 | |||
Placebo spray | 窪顧鹽觸窪鬱襯膚獵製(鹽夢醖憲築廠顧壓憲繭) = 簾繭顧鹹簾糧糧網廠選 遞繭網鬱艱鹽襯壓構憲 (鏇觸憲築積糧觸壓艱蓋 ) 更多 |
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