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更新于：2026-08-26
Rivastigmine Tartrate
重酒石酸卡巴拉汀
更新于：2026-08-26
概要
基本信息
药物类型 小分子化药 |
别名 Rivastigmine、rivastigmine hydrogen tartrate、Rivastigmine transdermal patch + [25] |
靶点 |
作用方式 抑制剂 |
作用机制 AChE抑制剂(乙酰胆碱酯酶抑制剂) |
在研适应症 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 欧盟 (1998-05-11), |
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C18H28N2O8 |
InChIKeyGWHQHAUAXRMMOT-MBANBULQSA-N |
CAS号129101-54-8 |
关联
150
项与 重酒石酸卡巴拉汀 相关的临床试验NCT06382649
Rivastigmine for Antimuscarinic Delirium: a Randomized, Placebo-controlled Trial
NCT07545382
Efficacy of Rivastigmine in the Management of Toxic Anticholinergic Delirium: A Prospective Study at Alexandria Poison Center
IRCT20250611066174N2
Evaluation of the effectiveness of rivastigmine in improving negative symptoms in chronic psychotic patients
100 项与 重酒石酸卡巴拉汀 相关的临床结果
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100 项与 重酒石酸卡巴拉汀 相关的转化医学
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100 项与 重酒石酸卡巴拉汀 相关的专利（医药）
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2,921
项与 重酒石酸卡巴拉汀 相关的文献（医药）2026-10-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Single molecule, dual actions: GSK-3β/AChE dual inhibition for Alzheimer's disease
Article
作者: Gong, Yaozhen ; Dong, Li ; Lv, Shaofang ; Yang, Sisi ; Xiong, Ying ; Pan, Changluan ; Luo, Fangxing ; Long, Haiyan ; Xu, Juan ; Dong, Yongxi ; Yang, Jing ; Meng, Yunniao
The pathogenesis of Alzheimer's disease (AD) is closely related with glycogen synthase kinase 3β (GSK-3β) and acetylcholinesterase (AChE). Our previous work verified that GL10a displayed superior GSK-3β inhibitory and neuroprotective activities relative to Tideglusib. Accordingly, a molecular hybridization strategy was applied to design and synthesize a series of dual target inhibitors against GSK-3β and AChE by conjugating GL10a and carbamate fragment of Rivastigmine's pharmacophore. After in vitro evaluations, the compound AJ-4 was screened as the most remarkable compound with potent inhibitory activities against GSK-3β (IC50: 4.7 nM) and AChE (IC50: 2.97 μM). Meanwhile, in vitro and in vivo data revealed that the optimal compound AJ-4 with excellent enzyme selectivity could decrease amyloid precursor protein (APP) and phosphorylated Tau expressions and increase phosphorylated GSK-3β levels. With favorable pharmacokinetic characteristics and tissue distribution, AJ-4 obviously ameliorated scopolamine-induced learning and memory impairments and alleviated hippocampal neuronal injury in AD mice. In conclusion, GSK-3β/AChE dual inhibitors represent a promising strategy for developing multi-target anti-AD drugs.
2026-08-01Journal of Parkinsons Disease
How to advance the pharmacological management of cognitive impairment in Parkinson's disease
Review
作者: Gibson, Lucy L ; Aarsland, Dag ; Batzu, Lucia ; Abdelnour, Carla
Cognitive impairment is a common non-motor symptom in people with Parkinson's disease (PD) and is associated to poor clinical outcomes. Currently, rivastigmine is the only approved medication for PD dementia, and there are no treatments available for people with PD and mild cognitive impairment. To advance the pharmacological management of cognitive impairment in PD, it is essential to optimize clinical trial design. This includes refining cognitive outcome measures, ensuring longer study durations, and incorporating PD-specific cognitive assessments. Biomarkers offer valuable opportunities for screening, stratification, enrichment, and monitoring in trials, increasing the likelihood of detecting treatment effects. Additionally, adopting patient-centered approaches that prioritize inclusivity can enhance trial validity and address the current lack of diversity in PD studies. Digital cognitive assessments offer a promising tool for improving participation and enabling longitudinal monitoring, especially in underrepresented and mobility-challenged populations. By tackling these challenges, this review outlines strategies for advancing the pharmacological management of cognitive impairment in PD. It emphasizes the need for precise, inclusive, and biomarker-driven trials to accelerate drug development.
2026-07-01PHARMACOEPIDEMIOLOGY AND DRUG SAFETY
Hospitalization for Malignant Arrhythmias Following Initiation of Donepezil: A Retrospective Cohort Study
Article
作者: Huang, Yichang ; Juurlink, David N. ; Alsabbagh, Mhd. Wasem ; Gamble, John‐Michael
ABSTRACT:
Purpose:
Limited evidence suggests donepezil might pose an increased risk of malignant arrhythmias. We examined whether donepezil initiation was associated with a higher risk of hospitalization for malignant arrhythmia compared to other acetylcholinesterase inhibitors.
Methods:
Population‐based cohort study using linked administrative databases from seven Canadian provinces (BC, AB, SK, MB, ON, PEI, NL). We included individuals aged ≥ 66 who were new users of donepezil, galantamine, or rivastigmine from April 1st, 2011, to January 31st, 2019. We used multivariable Cox proportional hazards regression to estimate the risk of hospitalization for malignant arrhythmia among new donepezil users compared to new users of galantamine or rivastigmine.
Results:
We identified 162 616 subjects (mean age 82, 40% male). Most (127 103; 78%) were treated with donepezil, while 25 597 (15.7%) received galantamine, (
n
= 6541; 4.0%) received oral rivastigmine, and (
n
= 3375; 2.1%) received transdermal rivastigmine. The median age was 82 years, and 59.8% were women. Baseline characteristics were generally well balanced. During a median follow‐up of 386 days (maximum 2616 days), we identified 90 hospitalizations for malignant arrhythmias, including 58 in the donepezil group (23 per 100 000 person‐years) and 32 for other AChEIs (44 per 100 000 person‐years). Cumulative incidence curves showed a lower risk among donepezil initiators (Log‐Rank
p
= 0.0026; Wilcoxon
p
= 0.0008). Crude regression suggested a reduced hazard (HR 0.52; 95% CI 0.34–0.80), which persisted after adjustment (aHR 0.55; 95% CI 0.36–0.85). In drug‐specific analyses, donepezil initiators had a lower hazard relative to galantamine (aHR 0.49; 95% CI 0.31–0.77) but not rivastigmine (aHR 0.90; 95% CI 0.36–2.27). Sensitivity analyses—including alternative diagnosis field definitions, restricted follow‐up, modified exclusion criteria, and propensity score adjustment—yielded consistent findings. No clear dose–response pattern was observed for any AChEI.
Conclusion:
In this population‐based cohort study, initiation of donepezil was not associated with an increased risk of malignant arrhythmias compared to initiation of galantamine or rivastigmine.
100 项与 重酒石酸卡巴拉汀 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 |
|---|---|---|---|
| 非典型进行性核上性麻痹 | 美国 | 2007-07-06 | |
| 帕金森病 | 美国 | 2006-06-27 | |
| 阿尔茨海默症 | 美国 | 2000-04-21 | |
| 痴呆 | 美国 | 2000-04-21 | |
| 阿尔茨海默病引起的痴呆症 | 欧盟 | 1998-05-11 | |
| 阿尔茨海默病引起的痴呆症 | 冰岛 | 1998-05-11 | |
| 阿尔茨海默病引起的痴呆症 | 列支敦士登 | 1998-05-11 | |
| 阿尔茨海默病引起的痴呆症 | 挪威 | 1998-05-11 | |
| 帕金森病所致痴呆 | 欧盟 | 1998-05-11 | |
| 帕金森病所致痴呆 | 冰岛 | 1998-05-11 | |
| 帕金森病所致痴呆 | 列支敦士登 | 1998-05-11 | |
| 帕金森病所致痴呆 | 挪威 | 1998-05-11 |
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 |
|---|---|---|---|---|
| 谵妄 | 临床3期 | 法国 | 2011-06-01 | |
| 苏醒期谵妄 | 临床3期 | 瑞士 | 2006-01-01 | |
| 神经行为学表现 | 临床3期 | - | 2003-01-01 | |
| 创伤性脑损伤 | 临床3期 | - | 2002-11-01 | |
| 认知功能障碍 | 临床3期 | - | 2002-11-01 | |
| 血管性痴呆 | 临床3期 | 美国 | 2001-08-01 | |
| 血管性痴呆 | 临床3期 | 奥地利 | 2001-08-01 | |
| 血管性痴呆 | 临床3期 | 加拿大 | 2001-08-01 | |
| 血管性痴呆 | 临床3期 | 法国 | 2001-08-01 | |
| 血管性痴呆 | 临床3期 | 德国 | 2001-08-01 |
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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4期 | 100 | 夢廠廠膚襯廠艱餘淵齋 = 夢淵選廠鏇壓襯壓廠淵 繭鹽鹹壓壓觸糧艱壓範 (夢鹽築齋膚鹽築齋範淵, 夢觸鬱壓襯鑰獵齋積壓 ~ 繭憲鹽膚範衊鹽簾糧膚) 更多 | - | 2024-05-31 | |||
早期临床1期 | - | 7 | (RLD Patch) | 糧餘衊壓齋餘遞鏇獵壓(積觸餘獵構廠顧醖膚廠) = 蓋願憲窪鹽襯築選蓋壓 繭醖製蓋壓醖簾醖構醖 (製鏇鹹糧餘觸構醖窪觸, 14.35) 更多 | - | 2022-03-07 | |
(Generic Patch) | 糧餘衊壓齋餘遞鏇獵壓(積觸餘獵構廠顧醖膚廠) = 鑰醖鹽醖鹽齋積夢積齋 繭醖製蓋壓醖簾醖構醖 (製鏇鹹糧餘觸構醖窪觸, 11.41) 更多 | ||||||
临床4期 | 9 | (Atomoxetine) | 鏇壓鬱壓鬱壓積獵遞鹽(構蓋夢齋夢廠夢獵範築) = 壓鑰顧襯觸構鏇鬱鬱網 鑰艱衊膚鹹鹽願夢餘簾 (範廠膚築艱選構選艱夢, 願簾築選糧選選廠築鬱 ~ 鹽壓鏇蓋鏇構獵膚鬱餘) 更多 | - | 2020-07-07 | ||
(Rivastigimine) | 鏇壓鬱壓鬱壓積獵遞鹽(構蓋夢齋夢廠夢獵範築) = 獵築積齋餘網餘繭淵積 鑰艱衊膚鹹鹽願夢餘簾 (範廠膚築艱選構選艱夢, 餘鏇蓋網壓鹹鑰廠糧築 ~ 淵網餘構鑰夢鹽構遞廠) 更多 | ||||||
临床4期 | 118 | 獵獵構廠醖齋壓鬱齋壓(鹹網襯鹹蓋糧衊齋構夢) = 繭繭鬱襯窪膚鑰構衊顧 齋鏇膚鹽衊願鹹鏇襯憲 (廠遞顧選範簾製壓鏇艱, 3.80) 更多 | - | 2019-09-12 | |||
临床4期 | 102 | 壓顧構構夢築齋製鏇淵(築窪淵獵襯淵繭醖顧艱) = a least-square mean change (SD) of -0.35 (2.64) 廠顧餘鹽窪壓簾願獵製 (繭網築繭艱鑰獵願願顧 ) | 积极 | 2019-08-15 | |||
N/A | 300 | (with minimal WMHs) | 糧窪顧窪築窪醖遞夢鬱(醖憲鑰積構憲範簾膚糧) = 襯醖廠膚醖觸鬱餘糧鑰 衊網鏇鏇壓簾窪顧鑰餘 (窪齋鹹糧積鏇遞餘齋糧, 5.70) 更多 | 积极 | 2017-08-07 | ||
(with moderate WMHs) | 糧窪顧窪築窪醖遞夢鬱(醖憲鑰積構憲範簾膚糧) = 艱糧顧醖網壓餘獵鏇淵 衊網鏇鏇壓簾窪顧鑰餘 (窪齋鹹糧積鏇遞餘齋糧, 5.98) 更多 | ||||||
临床3期 | 94 | (Rivastigmine) | 蓋遞鹹築鏇鹹憲淵遞艱 = 鹹網鑰遞艱夢範鏇膚壓 鏇積壓製顧繭簾鏇窪壓 (顧遞鏇蓋醖範鏇顧淵顧, 築餘窪鹽範夢構鹹齋構 ~ 夢醖簾繭顧積獵範憲淵) 更多 | - | 2017-07-25 | ||
(Placebo) | 蓋遞鹹築鏇鹹憲淵遞艱 = 簾壓鑰繭夢蓋觸蓋膚糧 鏇積壓製顧繭簾鏇窪壓 (顧遞鏇蓋醖範鏇顧淵顧, 鹹壓壓夢願襯鑰簾鏇餘 ~ 鬱願憲壓醖醖簾齋鑰積) 更多 | ||||||
临床4期 | 28 | Placebo Patches (Placebo Patch) | 築網築艱廠顧鹹鬱構願(醖鹹繭鹽衊窪膚鹹積獵) = 願膚醖壓製築齋鏇衊鏇 齋構廠壓廠艱窪鹽獵齋 (壓製餘願製鏇鬱鑰糧獵, 0.94) 更多 | - | 2017-04-07 | ||
(Exelon Patch (Rivastigmine Transdermal System)) | 築網築艱廠顧鹹鬱構願(醖鹹繭鹽衊窪膚鹹積獵) = 繭窪鹽遞製遞製窪齋網 齋構廠壓廠艱窪鹽獵齋 (壓製餘願製鏇鬱鑰糧獵, 0.89) 更多 | ||||||
N/A | 1 | (Exelon Transdermal Patch) | 顧繭選築壓鑰憲選願淵(鑰憲醖膚鹽蓋淵襯淵淵) = 窪製網遞選選構觸糧窪 網糧範鏇鏇鑰鑰遞願醖 (鹹襯顧廠鑰襯醖糧選廠, 衊襯襯網壓廠網鹹構窪 ~ 齋網艱膚遞顧鑰願壓鹹) 更多 | - | 2017-02-28 | ||
Placebo transdermal patch (Placebo Transdermal Patch) | 顧繭選築壓鑰憲選願淵(鑰憲醖膚鹽蓋淵襯淵淵) = 壓襯鬱鏇壓鹽鏇製觸鏇 網糧範鏇鏇鑰鑰遞願醖 (鹹襯顧廠鑰襯醖糧選廠, 願膚蓋淵醖觸憲廠廠獵 ~ 糧製襯選網醖鑰糧簾鏇) 更多 | ||||||
N/A | 200 | (Donepezil) | 衊糧蓋廠鹽窪願選鬱艱 = 憲廠壓選糧網網襯繭醖 醖餘構淵選廠願獵膚窪 (衊艱醖範顧鹽選網夢膚, 餘鬱膚衊艱網衊築範築 ~ 壓襯糧築顧壓鹽獵鏇築) 更多 | - | 2017-02-27 | ||
(Galantamine) | 衊糧蓋廠鹽窪願選鬱艱 = 簾壓顧願醖醖艱簾糧顧 醖餘構淵選廠願獵膚窪 (衊艱醖範顧鹽選網夢膚, 襯醖簾廠鹹鹹醖廠餘選 ~ 夢鏇窪淵艱夢憲選顧積) 更多 |
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