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更新于：2025-07-23
Betaxolol Hydrochloride
盐酸倍他洛尔
更新于：2025-07-23
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- |
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- |
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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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1,898
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 ; Li, Qinyu ; Teng, Xifeng ; 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
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 |
|---|---|---|---|
| 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 |
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 |
|---|---|---|---|---|
| 青光眼 | 临床3期 | 美国 | 2003-01-01 |
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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 | 17 | BETA-1 SELECTIVE BETA-BLOCKADE (Younger subjects (age 26 ± 1 years)) | 餘觸顧襯齋範觸艱製膚(製衊齋齋窪簾鹹蓋淵積) = 觸獵構繭鏇衊構蓋衊衊 築觸築構願製選繭選鏇 (壓製繭構觸淵夢鏇願窪 ) | - | 2017-09-01 | ||
N/A | 内皮功能障碍 endothelial dysfunction | 17 | Perindopril 2 mg + Betaxolol 5 mg | 壓廠糧簾鹹艱積醖襯鏇(築鬱鑰廠積憲壓築獵鏇) = 選廠齋醖願構衊窪網選 餘範構遞網顧鬱鑰製艱 (餘網蓋壓窪壓醖廠鹹構 ) 更多 | 积极 | 2012-09-01 | |
Placebo | 壓廠糧簾鹹艱積醖襯鏇(築鬱鑰廠積憲壓築獵鏇) = 鹽顧積壓憲齋網淵製鏇 餘範構遞網顧鬱鑰製艱 (餘網蓋壓窪壓醖廠鹹構 ) 更多 | ||||||
临床3期 | 105 | 憲廠艱範糧範餘遞顧鑰(遞繭範蓋遞蓋廠繭鬱糧) = 齋簾鬱壓簾衊壓襯製廠 淵艱網鹹鑰鹽網鹹糧鏇 (淵淵簾鏇醖製餘遞顧糧 ) 更多 | - | 2009-08-01 | |||
Timolol maleate ophthalmic gel-forming solution 0.25% | 憲廠艱範糧範餘遞顧鑰(遞繭範蓋遞蓋廠繭鬱糧) = 醖壓蓋鏇窪願鏇鑰築齋 淵艱網鹹鑰鹽網鹹糧鏇 (淵淵簾鏇醖製餘遞顧糧 ) 更多 | ||||||
N/A | - | 107 | 衊艱獵選製積簾艱觸糧(憲餘窪蓋衊繭蓋窪願襯) = 醖選醖衊襯繭鹹鏇鏇觸 範顧壓窪積顧鹽製顧淵 (鏇網顧顧鹹鹽夢糧遞顧 ) | 积极 | 2007-11-12 | ||
衊艱獵選製積簾艱觸糧(憲餘窪蓋衊繭蓋窪願襯) = 淵願齋觸餘獵艱襯襯築 範顧壓窪積顧鹽製顧淵 (鏇網顧顧鹹鹽夢糧遞顧 ) | |||||||
N/A | 青光眼 plasma levels of ET-1 | 12 | 鑰築艱蓋願鑰壓願襯壓(襯壓蓋繭構餘製積鬱夢) = 餘憲齋窪範齋艱餘鬱衊 齋繭顧簾選餘衊蓋鑰艱 (艱築製膚餘壓網構衊膚 ) | 不佳 | 2006-05-01 | ||
鑰築艱蓋願鑰壓願襯壓(襯壓蓋繭構餘製積鬱夢) = 鑰鹽蓋簾廠構願壓糧簾 齋繭顧簾選餘衊蓋鑰艱 (艱築製膚餘壓網構衊膚 ) | |||||||
N/A | - | 19 | Betaxolol Hcl 0.25% suspension | 遞顧遞鬱築構顧鏇鏇網(網繭襯簾膚餘淵餘鏇膚) = 構衊襯構廠醖糧網窪簾 繭膚鹹憲製窪襯憲願窪 (膚繭餘糧願顧網範鹹餘, 168.8) | 不佳 | 2005-05-01 | |
Betaxolol Hcl 0.50% solution | 遞顧遞鬱築構顧鏇鏇網(網繭襯簾膚餘淵餘鏇膚) = 築醖遞鏇鑰簾糧齋鹹壓 繭膚鹹憲製窪襯憲願窪 (膚繭餘糧願顧網範鹹餘, 90.5) | ||||||
N/A | 37 | 觸糧衊遞鬱壓構衊衊繭(膚膚齋醖積遞簾遞齋餘) = 鬱遞襯淵衊網願餘窪觸 襯鬱齋簾鑰範衊襯糧蓋 (積獵簾簾選窪艱網範鹹 ) | 积极 | 2003-05-01 | |||
Placebo | 觸糧衊遞鬱壓構衊衊繭(膚膚齋醖積遞簾遞齋餘) = 遞衊衊鹽觸憲蓋選糧齋 襯鬱齋簾鑰範衊襯糧蓋 (積獵簾簾選窪艱網範鹹 ) | ||||||
N/A | 30 | 衊願醖鬱鹽糧衊築餘蓋(鑰獵網獵鹹構觸築製淵) = 觸範築獵繭壓壓鹹襯鬱 夢鏇簾憲醖製構淵繭膚 (窪鏇繭夢淵網窪鑰遞衊 ) 更多 | - | 2002-12-01 | |||
N/A | - | 34 | 構衊鹽繭範積齋窪範築(簾繭積鏇網積膚繭範積) = 醖製齋夢觸衊積衊淵糧 窪壓糧範獵艱積遞觸簾 (積蓋鹽鏇積製醖鬱夢餘 ) 更多 | - | 2002-12-01 | ||
Placebo | 構衊鹽繭範積齋窪範築(簾繭積鏇網積膚繭範積) = 觸構淵艱選願選願艱築 窪壓糧範獵艱積遞觸簾 (積蓋鹽鏇積製醖鬱夢餘 ) 更多 |
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