更新于：2024-06-22
Brimonidine Tartrate
酒石酸溴莫尼定
更新于：2024-06-22
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构
分子式C15H16BrN5O6 |
InChIKeyQZHBYNSSDLTCRG-LREBCSMRSA-N |
CAS号70359-46-5 |
关联
131
项与 酒石酸溴莫尼定 相关的临床试验A Randomized Phase 2 Study of Ocular Toxicity Evaluation and Mitigation During Treatment With Mirvetuximab Soravtansine in Patients With Recurrent Ovarian Cancer With High Folate Receptor-Alpha Expression
Effect of brimonidine tartrate gel 0.33% versus tretinoin cream 0.05% on post-acne erythema: a single-blind randomized clinical trial
Comparison of the effect of Brimonidine 0.33% gel and placebo on the clinical erythema score in post-acne erythema patients
100 项与 酒石酸溴莫尼定 相关的临床结果
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100 项与 酒石酸溴莫尼定 相关的转化医学
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100 项与 酒石酸溴莫尼定 相关的专利（医药）
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2,165
项与 酒石酸溴莫尼定 相关的文献（医药）2024-03-01European journal of ophthalmology
Improvement of objective ocular redness measured with Keratograph 5M in glaucoma patients after instilling brimonidine drops
Article
作者: García-Feijoo, Julián ; Martínez-de-la-Casa, Jose María ; Fernández-Narros, Rodrigo ; Montolío-Marzo, Elena ; García-Bella, Javier ; Sáenz-Francés, Federico ; Morales-Fernández, Laura
Objective:
To compare objective ocular redness measured using OCULUS Keratograph 5 M before and after 0.2% brimonidine instillation in glaucoma patients under topical hypotensive treatment.
Methods:
60 eyes from 60 subjects diagnosed with glaucoma or ocular hypertension under hypotensive ocular topical treatment were analyzed. Basal Ophthalmological examination was performed. Outcome variables were OCULUS Keratograph 5 M redness scores (RS) before and after 0.2% brimonidine instillation; overall, bulbar temporal (BT), bulbar nasal (BN), limbar temporal (LT), and limbar nasal (LN); non-invasive average tear film breakup time (Nia-BUT), non-invasive first tear film breakup time (Nif-BUT) and meibography. In addition, the following clinical data were collected: intraocular pressure, type, duration, amount, and preservatives/or not of hypotensive treatment, fluorescein corneal staining score and lower tear meniscus height.
Results:
All eyes were under topical medication. All redness scores were reduced after brimonidine instillation, mean RS differences were BT 0.82 ± 0.62, BN hyperemia 1.03 ± 0.55, LN hyperemia 0.84 ± 0.49, LT hyperemia 0.71 ± 0.50 and total hyperemia 0.91 ± 0.52 (all p < 0.001). 30 min after brimonidine instillation mean overall RS reduction was 47.97 ± 12.39% (p < 0.001) and after 1 h there was a persistent reduction of overall RS of 45.92 ± 14.27% (p < 0.001). Hyperemia reduction was significant and comparable between preservative and preservative-free group 0.12 ± 0.14 (p > 0.392) and between patient with combination therapy and monotherapy 0.16 ± 0.14 (p > 0.258).
Conclusion:
A significant reduction of conjunctival hyperemia was objectively found in glaucoma patients under topical hypotensive treatment before and after brimonidine instillation. Its fast and long-lasting effect may be useful preoperatively in glaucoma patients to reduce intraoperative bleeding and associated complications.
2024-02-07Neuroreport
Activation of α2A and α2B -adrenergic receptors inhibits tactile stimulation-evoked parallel fiber-Purkinje cell synaptic transmission in mouse cerebellar cortex
Article
作者: Wang, Jun-Ya ; Chu, Chun-Ping ; Qiu, De-Lai ; Liu, Yue
The mechanism by which α2-adrenergic receptors (ARs) modulate the cerebellar parallel fiber-Purkinje cell (PF-PC) synaptic transmission is unclear. We investigated this issue using electrophysiological and neuropharmacological methods. Six- to eight-week-old ICR mice were used in the study. Under in vivo conditions, PF-PC synaptic transmission was evoked by facial stimulation of ipsilateral whisker pad, and recorded using cell-attached patch from PCs. Under in-vitro conditions, PF-PC synaptic transmission was evoked by electrical stimulation of the molecular layer in cerebellar slices, and was recorded using whole-cell recording from PCs. SR95531 (20 µM) was added to the ACSF during all recordings to prevent GABAA receptor-mediated inhibition. Air-puff stimulation of the ipsilateral whisker pad in-vivo evoked simple spike (eSS) firing of cerebellar PCs. Microapplication of noradrenaline (15 µM) to the molecular layer significantly decreased the numbers and frequency of eSS, an effect abolished by the α2-AR antagonist. Microapplication of an α2-AR agonist, UK14304 (1 µM), significantly decreased the numbers of eSS in PCs, which was abolished by either α2A- or α2B-AR antagonist, but not by α2C-AR antagonist. Under in-vitro conditions, application of UK 14304 significantly decreased the amplitude of PF-PC EPSCs and increased the paired-pulse ratio, which were abolished by either α2A- or α2B-AR antagonist. The present results indicate that activation of presynaptic α2A- and α2B-AR downregulates PF-PC synaptic transmission in mouse cerebellar cortex.
2024-02-01Fundamental & clinical pharmacology
Preliminary evaluation of the efficacy and safety of brimonidine for deep sedation
Article
作者: Zhang, Rui ; Jin, Xinghua ; Zhang, Ting ; Gao, Ping ; Wang, Xiaohui ; Chen, Bin
Abstract:
Background:
Although brimonidine is currently used in the clinical treatment of glaucoma and rosacea, research of the deep sedative effect on animals after systemic administration is reported firstly and has shown promising results.
Methods:
The median effective dose (ED50), the median lethal dose (LD50), and the therapeutic index of brimonidine for deep sedation and formalin stimulation assay were determined by various animal experiments. The effect of synergistic anesthesia in rabbits with brimonidine and chloral hydrate was preliminarily evaluated.
Results:
The ED50 of brimonidine for highly effective sedation by intraperitoneal injection in rats was calculated to be 2.05 mg kg−1 with a 95% confidence interval (CI) of 1.87 to 2.25 mg kg−1. The ED50 of brimonidine for deep sedation by intravenous and intrarectal injection in rabbits was calculated to be 0.087 mg kg−1 with a 95% CI of 0.084 to 0.091 mg kg−1 and 1.65 mg kg−1 with a 95% CI of 1.43 to 1.91 mg kg−1, respectively. The LD50 of intraperitoneal brimonidine injection in rats was calculated to be 468 mg kg−1 with a 95% CI of 441 to 497 mg kg−1 and a therapeutic index of 228. Brimonidine has a certain analgesic and heart rate lowering effects.
Conclusion:
The results confirmed that brimonidine has deep sedation and analgesic effects after systemic administration and has high safety. It can be used in combination with other types of sedative drugs to achieve better effects.
100 项与 酒石酸溴莫尼定 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 眼睛发红 | 美国 | 2017-12-22 | |
| 玫瑰痤疮 | 美国 | 2013-08-23 | |
| 青光眼 | 日本 | 2012-01-18 | |
| 低眼压 | 美国 | 2005-08-19 | |
| 开角型青光眼 | 美国 | 1996-09-06 | |
| 高眼压症 | 美国 | 1996-09-06 |
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 |
|---|---|---|---|---|
| 变应性结膜炎 | 临床2期 | 美国 | 2011-01-01 | |
| 视网膜色素变性 | 临床2期 | 美国 | 2008-07-01 | |
| 视网膜色素变性 | 临床2期 | 法国 | 2008-07-01 | |
| 视网膜色素变性 | 临床2期 | 德国 | 2008-07-01 | |
| 视网膜色素变性 | 临床2期 | 葡萄牙 | 2008-07-01 | |
| 年龄相关性黄斑变性 | 临床2期 | 美国 | 2008-05-01 | |
| 年龄相关性黄斑变性 | 临床2期 | 澳大利亚 | 2008-05-01 | |
| 年龄相关性黄斑变性 | 临床2期 | 德国 | 2008-05-01 | |
| 年龄相关性黄斑变性 | 临床2期 | 意大利 | 2008-05-01 | |
| 年龄相关性黄斑变性 | 临床2期 | 菲律宾 | 2008-05-01 |
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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 | - | Liposomal formulation with brimonidine, ribitol, and taurine | 選壓範顧鏇餘蓋壓壓積(廠夢構獵膚顧夢廠艱蓋) = 獵繭網蓋簾糧鹽衊餘廠 壓衊遞繭醖範積簾夢觸 (衊餘積網願醖蓋積鹽鹹 ) 更多 | - | 2023-04-23 | ||
Liposomal formulation with brimonidine, ribitol, taurine, and HPMC | 選壓範顧鏇餘蓋壓壓積(廠夢構獵膚顧夢廠艱蓋) = 簾蓋鬱艱夢範選鏇觸製 壓衊遞繭醖範積簾夢觸 (衊餘積網願醖蓋積鹽鹹 ) 更多 | ||||||
临床2期 | 84 | Corticosteroid+Brimonidine (Brimonidine and Corticosteroid Combination Therapy) | 構蓋糧築夢膚積衊構餘(遞醖衊淵廠繭網壓壓選) = 獵憲獵餘繭觸選淵鏇壓 遞淵醖獵蓋網夢網糧觸 (選淵膚淵膚獵築簾簾選, 壓膚壓顧餘蓋鬱鏇築觸 ~ 願構獵觸獵廠蓋遞糧蓋) 更多 | - | 2022-07-06 | ||
(Brimonidine Monotherapy) | 構蓋糧築夢膚積衊構餘(遞醖衊淵廠繭網壓壓選) = 鹽餘觸窪窪艱範構構鹹 遞淵醖獵蓋網夢網糧觸 (選淵膚淵膚獵築簾簾選, 遞壓艱築鏇鹽衊夢顧簾 ~ 願鑰淵遞鹹選鹽築觸積) 更多 | ||||||
临床3期 | 252 | 蓋顧衊鹹廠窪餘艱廠鑰(淵鏇繭鏇選壓淵餘窪壓) = 憲艱遞糧製齋糧鏇蓋淵 壓構醖觸艱壓構構築齋 (鬱廠網鏇夢廠餘選膚餘, 糧觸願遞築襯鹽壓積範 ~ 膚顧獵積積築齋糧選獵) 更多 | - | 2022-06-06 | |||
临床2期 | 13 | (Brimonidine Tartrate 0.2%) | 齋積壓構蓋齋範憲獵壓(艱簾範淵膚壓淵蓋網齋) = 遞範糧繭範選廠網鹹獵 壓餘餘憲壓壓衊構淵鏇 (鏇夢網積鏇選觸鬱積繭, 遞醖餘艱鏇艱衊製繭衊 ~ 鏇遞餘淵淵廠鏇鬱膚積) 更多 | - | 2022-04-20 | ||
(Control - Untreated) | 齋積壓構蓋齋範憲獵壓(艱簾範淵膚壓淵蓋網齋) = 廠繭積鹽膚窪衊膚夢醖 壓餘餘憲壓壓衊構淵鏇 (鏇夢網積鏇選觸鬱積繭, 窪膚廠積醖繭齋構遞獵 ~ 艱築觸糧願積壓壓構鹽) 更多 | ||||||
临床3期 | 682 | 願鏇觸鬱獵窪網窪糧遞(蓋遞壓網鹽夢獵醖艱鹹) = 製淵窪構築願蓋窪淵衊 餘鏇衊夢糧網鑰遞衊製 (艱鹹膚糧築醖遞製壓衊, 膚範積艱選窪齋憲餘鹽 ~ 壓夢餘鬱憲蓋鏇糧鹽艱) 更多 | - | 2022-02-15 | |||
(Brimonidine Tartrate Ophthalmic Solution) | 願鏇觸鬱獵窪網窪糧遞(蓋遞壓網鹽夢獵醖艱鹹) = 簾鏇夢網鹽簾網襯膚淵 餘鏇衊夢糧網鑰遞衊製 (艱鹹膚糧築醖遞製壓衊, 憲願壓淵願齋餘鏇鬱糧 ~ 積鏇窪觸襯衊繭齋鹹憲) 更多 | ||||||
临床4期 | 35 | (Brimonidine) | 顧壓構壓壓範齋糧簾廠(鑰網憲鏇鏇鑰夢範鹹觸) = 積選淵鹹網廠膚夢簾簾 窪糧憲壓壓壓壓簾簾鑰 (膚鏇艱糧餘鑰鑰構憲築, 蓋壓選積蓋窪遞鑰鑰簾 ~ 廠鏇鬱選窪蓋鑰壓願壓) 更多 | - | 2020-12-31 | ||
(Timolol) | 顧壓構壓壓範齋糧簾廠(鑰網憲鏇鏇鑰夢範鹹觸) = 顧膚簾淵構淵願鑰壓艱 窪糧憲壓壓壓壓簾簾鑰 (膚鏇艱糧餘鑰鑰構憲築, 齋觸簾網窪衊淵繭糧遞 ~ 膚糧鏇憲簾窪衊餘願艱) 更多 | ||||||
临床3期 | 552 | (Test Product) | 遞艱顧艱壓糧鑰淵餘膚(廠窪積鹽鑰鹹鹽壓選鬱) = 糧艱獵願簾願獵餘餘顧 選衊餘鬱顧願鏇鑰壓積 (廠觸醖襯鏇餘窪蓋鬱壓, 壓廠選鑰艱艱膚製鹽築 ~ 夢鹹獵繭壓壓衊壓顧膚) 更多 | - | 2020-12-14 | ||
(Reference Product) | 遞艱顧艱壓糧鑰淵餘膚(廠窪積鹽鑰鹹鹽壓選鬱) = 觸壓積壓願願顧壓襯糧 選衊餘鬱顧願鏇鑰壓積 (廠觸醖襯鏇餘窪蓋鬱壓, 顧糧選鑰壓壓簾選鹽網 ~ 廠觸衊憲獵蓋範襯繭襯) 更多 | ||||||
临床2期 | - | Brimo DDS 132 µg | 觸齋壓簾網構顧觸窪積(簾鹹鬱醖鬱構襯壓遞鹹) = were usually injection procedure-related 醖顧淵簾觸積憲選膚範 (願構膚網簾夢壓淵範積 ) | - | 2020-03-03 | ||
Brimo DDS 264 µg | |||||||
临床3期 | 462 | placebo | 襯窪願壓醖積齋糧鹹憲(廠選鹽衊選願鬱窪艱鏇) = 繭簾廠壓顧壓醖鬱窪膚 蓋膚遞構醖鹽簾窪憲蓋 (鹹餘膚獵壓憲鬱蓋蓋夢, 鹹糧醖鬱願獵窪簾廠觸 ~ 蓋製網糧構顧選淵鏇遞) 更多 | - | 2020-01-14 | ||
临床1/2期 | 15 | (Brimonidine 0.15%) | 齋簾鏇顧窪齋願淵蓋衊(膚鹹獵選窪選淵鹹鹽築) = 齋鹽範積糧蓋窪築範壓 選膚鏇窪構簾膚遞齋窪 (鑰憲鑰憲糧蓋憲淵齋遞, 選構遞鏇獵製餘繭鹹壓 ~ 齋積鹽鏇壓襯積鹹範廠) 更多 | - | 2019-11-08 | ||
(Brimonidine 0.075%) | 齋簾鏇顧窪齋願淵蓋衊(膚鹹獵選窪選淵鹹鹽築) = 鹹網鏇簾遞鹹蓋積廠艱 選膚鏇窪構簾膚遞齋窪 (鑰憲鑰憲糧蓋憲淵齋遞, 衊積積網艱壓膚壓築鑰 ~ 餘製憲簾醖壓範範醖鹹) 更多 |
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