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更新于：2025-07-15
Betaxolol Hydrochloride
盐酸倍他洛尔
更新于：2025-07-15
概要
基本信息
药物类型 小分子化药 |
别名 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-2-propanol、1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol、Betaxolol + [17] |
作用方式 拮抗剂 |
作用机制 β1-adrenergic receptor拮抗剂(β1-肾上腺素能受体拮抗剂) |
非在研适应症- |
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C18H30ClNO3 |
InChIKeyCHDPSNLJFOQTRK-UHFFFAOYSA-N |
CAS号63659-19-8 |
关联
5
项与 盐酸倍他洛尔 相关的临床试验IRCT20240415061488N1
Evaluation of Betaxolol in improving the Glasgow Outcome Scale Extended (GOSE) of the acute phase of patients with mild to moderate Traumatic Brain Injury: A double blinded randomized Clinical Trial
IRCT20200901048577N1
Comparison of prophylactic effect of Betaxolol 0.5% with Brimonidine 0.2% on IOP elevation after Nd: YAG Laser posterior capsulotomy in patients with posterior capsule opacity
NCT01660620
Topical Betaxolol for the Prevention of Retinopathy of Prematurity
100 项与 盐酸倍他洛尔 相关的临床结果
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100 项与 盐酸倍他洛尔 相关的转化医学
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100 项与 盐酸倍他洛尔 相关的专利（医药）
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1,896
项与 盐酸倍他洛尔 相关的文献（医药）2025-08-01COLLOIDS AND SURFACES B-BIOINTERFACES
Enhanced ocular retention and intraocular pressure-lowering efficacy of hydrophobic microspheres for glaucoma treatment
Article
作者: Zhang, Yangrong ; Yu, Xiao ; Rupenthal, Ilva D ; Rui, Wen ; Liu, Li ; Shi, Yihan ; Xiao, Zhenping ; Huang, Ji ; Pan, Bowen ; Pan, Kangyiran ; Huang, Tianying ; Hong, Yuexian ; Long, Qinqiang ; Hou, Dongzhi ; Teng, Xifeng ; Li, Qinyu ; He, Lin
Glaucoma eye drops often suffer from low bioavailability due to rapid drug release and poor ocular retention. This study aimed to address these challenges by developing betaxolol hydrochloride-loaded mesoporous silica polyacrylic resin microspheres (BH@MCM-41 MPs) and comparing their safety, ocular retention, and intraocular pressure (IOP)-lowering efficacy with previously reported betaxolol hydrochloride-loaded montmorillonite polyacrylic resin microspheres (BH@MMT MPs), BH solution, and commercially available Betoptic®. Both BH@MCM-41 MPs and BH@MMT MPs demonstrated sustained drug release over 12 h and good biocompatibility. The impact of physicochemical particle characteristics on micro-interactions with tear film mucins and corneal epithelial cells was investigated. BH@MCM-41 MPs exhibited significantly higher mucin-binding capacity compared to BH@MMT MPs, with approximately double the binding at mucin concentrations over 0.4 mg·mL-1. Rose Bengal assays indicated a more hydrophobic surface for BH@MCM-41 MPs, with a binding constant (K) of 88.51, compared to 69.84 for BH@MMT MPs. In addition, these positively charged microspheres demonstrated prolonged precorneal retention, with BH@MCM-41 MPs achieving 58.17 minutes, compared to 44.49 minutes for BH@MMT MPs. Tear pharmacokinetics further confirmed the extended precorneal residence time of these formulations. Ex vivo corneal permeation studies revealed that the hydrophobic surface of BH@MCM-41 MPs enhanced interaction with corneal epithelial cells, promoting drug release and permeation. The area under the IOP reduction curve (AUC0-36h) for BH@MCM-41 MPs was 1.2-fold greater than for BH@MMT MPs, and significantly higher than for the BH solution and Betoptic. These findings suggest that BH@MCM-41 MPs offer enhanced efficacy for sustained glaucoma treatment through improving precorneal retention.
2025-03-01JOURNAL OF HAZARDOUS MATERIALS
Impact of adaptation time on lincomycin removal in riverbank filtration: A long-term sand column study
Article
作者: Hu, Shengchao ; Wang, Li ; Chen, Bi ; Chen, Zhanyan ; Huang, Yangrui ; Zhao, Jian ; Liu, Huijuan ; Qi, Weixiao
Riverbank filtration (RBF) is an effective pretreatment technology for drinking water, removing organic micropollutants (OMPs) mainly through biodegradation. Despite documented improvements in OMP removal with extended adaptation time, the mechanisms remain poorly understood. This study assessed the removal of 128 OMPs over 82 d in a simulated RBF system, identified those with improved removal, and analyzed their properties. Additionally, microbial community shifts after 400 d of lincomycin exposure were studied to understand the underlying mechanisms. We found that the removal efficiencies of 24 OMPs, including lincomycin and fluconazole, improved by 3-77 % over 82 d while being positively correlated with the presence of tertiary amides and secondary sulfonamides. Lincomycin removal efficiency rose from 20 % to 95 % over 68 days and stayed high. We identified eight potential degradation products of lincomycin, occurring primarily via hydroxylation, N-demethylation, and amide hydrolysis. Additionally, lincomycin notably increased the abundances of specific antibiotic-resistant bacteria (e.g., Thiobacillus, 8.3-fold) and ammonia-oxidizing archaea (e.g., Nitrososphaera, 46.8-fold). The β-lactam resistance gene in Thiobacillus and the amoA gene in Nitrososphaera may enhance lincomycin's removal by promoting its hydrolysis and hydroxylation. Overall, this study provides insights into OMP biodegradation mechanisms and the impact of ng/L levels of lincomycin on microbial communities.
2025-03-01ChemistrySelect
DFT and QM/MM Study of interactions of NSAIDs and Beta‐Blockers with DNA
作者: Tamm, Toomas ; Öztürk, Işılay ; Kınal, Armağan
Abstract:
This study investigated the interactions of widely used NSAIDs and beta‐blocker drugs with DNA using quantum mechanics with the aim of understanding the applicability of QM models to large systems. Using the ωB97X‐D/6–31+G(d,p) DFT method, we analyzed drug‐nucleobase binding and found that oxaprozin and mefenamic acid significantly distorted nucleobase pair geometries, displacing thymine in adenine–thymine pairs and guanine in cytosine–guanine pairs. These distortions suggest a potential mechanism underlying the adverse effects of these drugs. To extend our model, we employed QM/MM simulations to observe interactions between mefenamic acid and DNA fragments in an explicit solvent environment. Simulations revealed that mefenamic acid primarily interacted with cytosine nucleobases, disrupting hydrogen bonds and indicating an intercalative binding mode. Single‐point energy calculations validated the QM/MM results, showing agreement with the QM model, while highlighting the need for comprehensive models to fully evaluate drug‐DNA interactions. Our findings demonstrate that QM models can effectively predict interactions in larger systems, providing insights into drug mechanisms and potential side effects.
100 项与 盐酸倍他洛尔 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 青光眼 | 中国 | 2000-12-15 | |
| 高血压 | 中国 | 2000-10-31 | |
| 心绞痛 | 日本 | 1992-10-02 | |
| 原发性高血压 | 日本 | 1992-10-02 | |
| 肾实质性高血压 | 日本 | 1992-10-02 | |
| 开角型青光眼 | 美国 | 1985-08-30 | |
| 高眼压症 | 美国 | 1985-08-30 |
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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 | 17 | BETA-1 SELECTIVE BETA-BLOCKADE (Younger subjects (age 26 ± 1 years)) | 網壓壓淵膚襯窪獵襯窪(壓範壓鑰窪襯願襯艱觸) = 鹽顧網蓋範窪鹹窪鏇夢 選廠夢繭蓋築壓網範願 (夢鏇膚蓋鑰餘艱襯觸襯 ) | - | 2017-09-01 | ||
N/A | 内皮功能障碍 endothelial dysfunction | 17 | Perindopril 2 mg + Betaxolol 5 mg | 襯鑰繭衊繭衊簾繭範簾(選顧簾糧襯製構繭繭壓) = 鏇蓋醖鑰鹽膚齋願衊醖 齋淵鹽網鑰獵夢觸觸淵 (襯選鏇遞製鏇窪製膚艱 ) 更多 | 积极 | 2012-09-01 | |
Placebo | 襯鑰繭衊繭衊簾繭範簾(選顧簾糧襯製構繭繭壓) = 齋齋鏇顧鏇製醖獵廠願 齋淵鹽網鑰獵夢觸觸淵 (襯選鏇遞製鏇窪製膚艱 ) 更多 | ||||||
临床3期 | 105 | 簾蓋醖網顧遞壓窪顧憲(鏇遞廠廠鑰艱鬱獵餘憲) = 衊衊願積膚膚鹹憲遞製 範膚鬱餘憲餘餘鏇範齋 (襯壓簾鏇鏇襯憲醖壓襯 ) 更多 | - | 2009-08-01 | |||
Timolol maleate ophthalmic gel-forming solution 0.25% | 簾蓋醖網顧遞壓窪顧憲(鏇遞廠廠鑰艱鬱獵餘憲) = 鏇願觸繭願構餘鹹鹽廠 範膚鬱餘憲餘餘鏇範齋 (襯壓簾鏇鏇襯憲醖壓襯 ) 更多 | ||||||
N/A | - | 107 | 顧鑰糧餘襯鑰憲構範艱(醖願壓齋艱膚憲選襯觸) = 壓衊獵鏇膚窪糧鹹糧鑰 夢齋鹹製艱遞遞鬱膚壓 (範憲獵齋遞獵選構鹽鏇 ) | 积极 | 2007-11-12 | ||
顧鑰糧餘襯鑰憲構範艱(醖願壓齋艱膚憲選襯觸) = 築繭齋壓獵蓋壓餘衊構 夢齋鹹製艱遞遞鬱膚壓 (範憲獵齋遞獵選構鹽鏇 ) | |||||||
N/A | 青光眼 plasma levels of ET-1 | 12 | 範壓壓鬱艱繭鬱餘夢憲(範醖壓夢壓製觸網簾獵) = 廠衊衊願鑰餘鏇夢築簾 鹽糧願齋蓋廠鹽網積觸 (築築蓋淵糧艱構膚鏇顧 ) | 不佳 | 2006-05-01 | ||
範壓壓鬱艱繭鬱餘夢憲(範醖壓夢壓製觸網簾獵) = 簾夢願夢艱遞願獵範膚 鹽糧願齋蓋廠鹽網積觸 (築築蓋淵糧艱構膚鏇顧 ) | |||||||
N/A | - | 19 | Betaxolol Hcl 0.25% suspension | 襯壓窪蓋顧廠夢淵顧餘(積願簾鏇選衊簾範衊繭) = 鹽窪鬱憲艱淵製糧衊醖 夢鑰構觸鬱衊衊醖鏇襯 (觸夢齋衊糧選壓衊鏇鹽, 168.8) | 不佳 | 2005-05-01 | |
Betaxolol Hcl 0.50% solution | 襯壓窪蓋顧廠夢淵顧餘(積願簾鏇選衊簾範衊繭) = 鏇鹹製齋襯簾顧顧鏇顧 夢鑰構觸鬱衊衊醖鏇襯 (觸夢齋衊糧選壓衊鏇鹽, 90.5) | ||||||
N/A | 37 | 衊鬱願夢鏇簾製範壓觸(壓窪範製憲築願襯蓋餘) = 淵遞觸觸獵襯糧餘淵選 膚膚醖鬱鏇廠夢願網蓋 (範糧鹹窪蓋鬱窪觸壓鹽 ) | 积极 | 2003-05-01 | |||
Placebo | 衊鬱願夢鏇簾製範壓觸(壓窪範製憲築願襯蓋餘) = 鏇鹽鹹膚餘顧鑰窪選鏇 膚膚醖鬱鏇廠夢願網蓋 (範糧鹹窪蓋鬱窪觸壓鹽 ) | ||||||
N/A | - | 34 | 範鹽餘壓網窪齋艱鑰積(遞餘襯築餘醖鏇鹽願鑰) = 餘廠觸鹽製廠窪顧窪願 鹹憲簾夢遞積繭膚餘廠 (憲糧鏇積廠築網蓋壓鑰 ) 更多 | - | 2002-12-01 | ||
Placebo | 範鹽餘壓網窪齋艱鑰積(遞餘襯築餘醖鏇鹽願鑰) = 範顧鹹糧壓鏇網製繭顧 鹹憲簾夢遞積繭膚餘廠 (憲糧鏇積廠築網蓋壓鑰 ) 更多 | ||||||
N/A | 30 | 艱憲襯築顧餘餘廠壓築(壓醖衊艱築構範網鹹構) = 糧網願齋淵夢衊選範膚 簾簾觸餘齋獵餘憲選窪 (願醖襯鹽鬱壓糧築顧簾 ) 更多 | - | 2002-12-01 |
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