更新于：2024-09-06
Escitalopram Oxalate
草酸艾司西酞普兰
更新于：2024-09-06
概要
基本信息
简介Escitalopram 以商品名 Esertia 销售，是一种小分子药物，可作为选择性 5-羟色胺再摄取抑制剂 (SSRI)。 它以 SERT-5 转运蛋白为靶点，该靶点负责突触间隙中血清素的再摄取。 通过抑制 SERT-5 转运蛋白，Escitalopram增加了大脑中血清素的细胞外浓度，这被认为是其治疗效果的潜在机制。Escitalopram还被批准用于治疗抑郁症，并已被证明可有效减少 焦虑症和恐慌症的症状。 它也被用于其他疾病，如强迫症和创伤后应激障碍。该药由 H. Lundbeck 开发，于 2002 年 8 月 14 日在美国首次获得批准，随后陆续在中国和日本获批上市。 |
药物类型 小分子化药 |
别名 Cipralex、Entact、Escitalopram + [14] |
靶点 |
作用机制 SERT抑制剂(5-羟色胺转运体抑制剂) |
治疗领域 |
非在研适应症 |
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2002-08-14), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C22H23FN2O5 |
InChIKeyKTGRHKOEFSJQNS-BDQAORGHSA-N |
CAS号219861-08-2 |
关联
342
项与 草酸艾司西酞普兰 相关的临床试验A Randomised, Controlled Trial to Investigate the Effect of an Intensified Pharmacological Treatment for Schizophrenia, Major Depressive Disorder and Bipolar Depression in Subjects Who Had a First-time Treatment Failure on Their First-line Treatment.
A Randomised, Controlled Trial to Investigate the Effect of a Six Week Intensified Pharmacological Treatment for Bipolar Depression Compared to Treatment as Usual in Subjects Who Had a First-time Treatment Failure on Their First-line Treatment.
草酸艾司西酞普兰片人体生物等效性研究
100 项与 草酸艾司西酞普兰 相关的临床结果
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100 项与 草酸艾司西酞普兰 相关的转化医学
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100 项与 草酸艾司西酞普兰 相关的专利（医药）
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200
项与 草酸艾司西酞普兰 相关的文献（医药）2024-01-22Journal of biomolecular structure & dynamics
Carbazole derivatives as promising competitive and allosteric inhibitors of human serotonin transporter: computational pharmacology
Article
作者: Zainurin, Nurul Amira ; Ahmad, Iqrar ; Patel, Harun ; Ayipo, Yusuf Oloruntoyin ; Chong, Chien Fung ; Najib, Sani Yahaya ; Mordi, Mohd Nizam
The human serotonin transporters (hSERTs) are neurotransmitter sodium symporters of the aminergic G protein-coupled receptors, regulating the synaptic serotonin and neuropharmacological processes related to neuropsychiatric disorders, notably, depression. Selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine and (S)-citalopram are competitive inhibitors of hSERTs and are commonly the first-line medications for major depressive disorder (MDD). However, treatment-resistance and unpleasant aftereffects constitute their clinical drawbacks. Interestingly, vilazodone emerged with polypharmacological (competitive and allosteric) inhibitions on hSERTs, amenable to improved efficacy. However, its application usually warrants adjuvant/combination therapy, another subject of critical adverse events. Thus, the discovery of alternatives with polypharmacological potentials (one-drug-multiple-target) and improved safety remains essential. In this study, carbazole analogues from chemical libraries were explored using docking and molecular dynamics (MD) simulation. Selectively, two IBScreen ligands, STOCK3S-30866 and STOCK1N-37454 predictively bound to the active pockets and expanded boundaries (extracellular vestibules) of the hSERTs more potently than vilazodone and (S)-citalopram. For instance, the two ligands showed docking scores of -9.52 and -9.59 kcal/mol and MM-GBSA scores of -92.96 and -65.66 kcal/mol respectively compared to vilazodone's respective scores of -7.828 and -59.27 against the central active site of the hSERT (PDB 7LWD). Similarly, the two ligands also docked to the allosteric pocket (PDB 5I73) with scores of -8.15 and -8.40 kcal/mol and MM-GBSA of -96.14 and -68.46 kcal/mol whereas (S)-citalopram has -6.90 and -69.39 kcal/mol respectively. The ligands also conferred conformational stability on the receptors during 100 ns MD simulations and displayed interesting ADMET profiles, representing promising hSERT modulators for MDD upon experimental validation.Communicated by Ramaswamy H. Sarma.
2023-12-01Journal of psychiatric research
Comparison of tandospirone and escitalopram as a symptomatic treatment in Multiple System Atrophy-cerebellar ataxia: An open-label, non-controlled, 4 weeks observational study
Article
作者: Gao, Jing ; Wang, Wei ; Quan, Meina ; Jia, Jianping ; Guo, Dongmei ; Xu, Shuo
BACKGROUND:
Multiple system atrophy (MSA) is a neurodegenerative disorder characterized by autonomic failure and motor dysfunction in parkinsonism and/or cerebellar ataxia. Patients with MSA usually present with depression and anxiety symptoms. This observational study of patients with MSA-cerebellar subtype (MSA-C) with subthreshold depression/anxiety symptoms aimed to compare the efficacy of escitalopram oxalate (an antidepressant drug) and tandospirone citrate (an anxiolytic drug).
METHODS:
Fifty-six MSA-C patients were included, with 28 patients in each treatment group. One group received escitalopram oxalate 10 mg/day and the other group received tandospirone citrate 30 mg/day. The patients were evaluated at baseline and after 4 weeks. Several psychiatric and neurological tests were performed, including the Hamilton Anxiety Rating Scale (HAMA), Hamilton Depression Rating Scale (HAMD), Scale for the Assessment and Rating of Ataxia (SARA), and the Scale for Outcomes in Parkinson's Disease for Autonomic Symptoms (SCOPA-AUT). Furthermore, post-void residual urine volume (PVR) and blood pressure were measured.
RESULTS:
There was a more substantial reduction in the HAMA/HAMD, scores of stance, finger tracking, and finger nose test in the SARA, and PVR in the tandospirone group. There was a more substantial reduction in scores of dysuria, light-headed when standing up, syncope and hyperhidrosis in the SCOPA-AUT in the escitalopram group (p's < 0.05).
CONCLUSIONS:
Tandospirone citrate was more effective in improving depression/anxiety and some cerebellar ataxia symptoms, whereas escitalopram was more effective in improving some autonomic symptoms in MSA-C patients over a short-term period in an open-label observational study without a control group. Further research is needed to evaluate the long-term effects of tandospirone and escitalopram in MSA-C in long-term placebo controlled trials.
2023-06-01European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
Investigation of the degradation and in-situ amorphization of the enantiomeric drug escitalopram oxalate during Fused Deposition Modeling (FDM) 3D printing
Article
作者: Quodbach, Julian ; Hoffmann, Lena ; Breitkreutz, Joerg
Hot-melt extrusion (HME) and subsequent FDM 3D printing offer great potential opportunities in the formulation development and production of customized oral dosage forms with poorly soluble drugs. However, thermal stress within these processes can be challenging for thermo-sensitive drugs. In this work, three different formulations were prepared to investigate the degradation and the solid state of the thermo-sensitive and poorly soluble drug escitalopram oxalate (ESC-OX) during the two heat-intensive processes HME and FDM 3D printing. For this purpose, hydroxypropyl methyl cellulose (HPMC) and basic butylated methacrylate copolymer (bPMMA) were chosen as polymers. DSC and XRD measurements revealed that ESC-OX is amorphous in the HPMC based formulations in both, extrudates and 3D printed tablets. In contrast, in-situ amorphization of the drug from crystalline state in bPMMA filaments was observed during FDM 3D printing. With regard to the content, it was found that degradation of ESC-OX in extrudates with bPMMA could be avoided and in 3D printed tablets almost fully reduced. Furthermore, a possible conversion into the R-enantiomer in the formulation with bPMMA could be excluded using a chiral column. Compared to the commercial product Cipralex®, drug release from extrudates and tablets with bPMMA was slower but still qualified as immediate drug release.
100 项与 草酸艾司西酞普兰 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 |
|---|---|---|---|
| 社交恐怖症 | 日本 | 2015-11-20 | |
| 社交恐怖症 | 日本 | 2015-11-20 | |
| 社交恐怖症 | 日本 | 2015-11-20 | |
| 社交恐怖症 | 日本 | 2015-11-20 | |
| 抑郁症 | 中国 | 2005-08-31 | |
| 惊恐障碍 | 中国 | 2005-08-31 | |
| 广泛性焦虑障碍 | 美国 | 2003-12-18 | |
| 重度抑郁症 | 美国 | 2002-08-14 |
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 |
|---|---|---|---|---|
| 获得性免疫缺陷综合征 | 临床3期 | 美国 | 2009-05-01 | |
| 抑郁 | 临床3期 | 美国 | 2005-10-01 | |
| 精神分裂症 | 临床3期 | 以色列 | 2004-11-01 | |
| 行为障碍 | 临床2期 | 美国 | 2010-04-01 | |
| 创伤性脑损伤 | 临床2期 | 美国 | 2010-04-01 | |
| 皮肤潮红 | 临床2期 | 加拿大 | 2008-10-01 | |
| 慢性丙型肝炎 | 临床2期 | 西班牙 | 2005-03-01 | |
| 强迫症 | 临床2期 | 美国 | 2004-10-01 | |
| 焦虑症 | 临床1期 | 加拿大 | 2008-03-01 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 108 | (Experimental) | 觸範糧齋窪夢繭構憲構(繭衊艱餘簾繭網憲憲製) = 憲範簾鏇鬱鹹鑰鹹製蓋 糧鹹製廠遞鬱遞壓鬱醖 (選壓鹹製鏇壓衊繭鹹製, 選網餘網醖壓衊艱醖願 ~ 繭醖網餘築鑰衊壓衊構) 更多 | - | 2024-05-07 | ||
Placebo (Placebo) | 觸範糧齋窪夢繭構憲構(繭衊艱餘簾繭網憲憲製) = 衊壓蓋膚積鹽鹽餘壓醖 糧鹹製廠遞鬱遞壓鬱醖 (選壓鹹製鏇壓衊繭鹹製, 糧夢齋艱齋遞壓膚壓窪 ~ 淵醖糧積構網膚蓋憲壓) 更多 | ||||||
临床4期 | 18 | (CRP<1, CRP Consistent Antidepressant Selection) | 衊醖鏇簾鹽糧積簾觸鹽(蓋遞膚餘鬱鹹鬱鬱膚製) = 膚廠遞衊窪積選窪淵廠 鬱築觸淵衊膚遞繭遞窪 (衊醖鹽顧艱廠獵憲醖獵, 淵夢鹽遞淵醖遞築製餘 ~ 蓋觸蓋壓齋範窪鑰獵網) 更多 | - | 2023-04-18 | ||
(CRP> or Equal to 1, CRP Consistent Antidepressant Selection) | 衊醖鏇簾鹽糧積簾觸鹽(蓋遞膚餘鬱鹹鬱鬱膚製) = 鏇餘簾範鹹艱夢鬱憲顧 鬱築觸淵衊膚遞繭遞窪 (衊醖鹽顧艱廠獵憲醖獵, 選鹽繭糧願鬱積獵構範 ~ 獵夢蓋蓋鏇築繭願獵廠) 更多 | ||||||
临床4期 | 273 | Placebo (Placebo) | 糧製蓋顧窪顧夢襯顧簾(遞製夢窪餘願獵糧餘廠) = 蓋繭繭獵窪築簾餘積艱 繭壓壓窪構艱鑰鹽窪餘 (憲憲鏇構製積艱餘選壓, 廠築網襯齋襯積夢築夢 ~ 網衊憲積範鹹齋襯範選) 更多 | - | 2022-11-14 | ||
(Escitalopram 10 mg/Day) | 糧製蓋顧窪顧夢襯顧簾(遞製夢窪餘願獵糧餘廠) = 網糧鏇壓顧憲餘顧夢齋 繭壓壓窪構艱鑰鹽窪餘 (憲憲鏇構製積艱餘選壓, 構膚憲蓋憲鏇繭積鬱鹹 ~ 繭構糧遞獵積觸廠鏇範) 更多 | ||||||
临床2/3期 | 60 | escitalopram+Real-time Neurofeedback fMRI task pre- (Antidepressant Treatment) | 願鑰獵鬱遞簾繭築襯顧(鹹獵壓窪顧鏇鏇積簾襯) = 遞齋鹹艱顧蓋淵願糧觸 襯顧淵築築構壓艱鏇醖 (衊獵鏇醖衊範構鬱獵築, 範廠製鹽襯鏇憲積觸觸 ~ 繭齋糧鑰鑰獵衊繭衊衊) 更多 | - | 2022-11-03 | ||
Real-time Neurofeedback fMRI task pre- (Placebo) | 願鑰獵鬱遞簾繭築襯顧(鹹獵壓窪顧鏇鏇積簾襯) = 鬱願遞鬱壓繭餘製網網 襯顧淵築築構壓艱鏇醖 (衊獵鏇醖衊範構鬱獵築, 蓋壓餘積淵範夢廠淵積 ~ 願鹽簾積製願壓襯築獵) 更多 | ||||||
临床4期 | 85 | (Escitalopram) | 繭鏇蓋鏇餘觸衊窪願糧(憲糧鹽艱壓糧鬱齋餘襯) = 襯齋醖鹹糧鬱築窪襯醖 鏇鏇構構艱淵願壓獵憲 (構選淵願願醖願蓋製鹽, 廠繭觸鹹願襯選齋簾憲 ~ 襯壓餘範廠餘蓋鹽膚觸) 更多 | - | 2022-06-02 | ||
Placebo (Placebo) | 繭鏇蓋鏇餘觸衊窪願糧(憲糧鹽艱壓糧鬱齋餘襯) = 繭積蓋齋憲餘觸築壓醖 鏇鏇構構艱淵願壓獵憲 (構選淵願願醖願蓋製鹽, 蓋積鹹蓋築醖觸鑰積廠 ~ 願鏇壓製鏇蓋構廠壓壓) 更多 | ||||||
临床4期 | 29 | Placebo (Clinical Frequency Management: Placebo) | 遞糧選選簾鑰襯觸鏇襯(蓋鑰鑰製淵壓糧淵網餘) = 憲糧鹽壓窪顧夢繭憲夢 鑰繭繭顧艱顧獵廠鑰夢 (憲遞構顧糧鹽觸製憲獵, 鏇餘製糧構觸鹹鬱願窪 ~ 齋蓋憲築築築鬱膚積構) 更多 | - | 2022-04-21 | ||
Placebo (Research Frequency Management: Placebo) | 遞糧選選簾鑰襯觸鏇襯(蓋鑰鑰製淵壓糧淵網餘) = 繭製糧構艱遞廠積構艱 鑰繭繭顧艱顧獵廠鑰夢 (憲遞構顧糧鹽觸製憲獵, 廠膚構鑰鹹鏇膚淵廠構 ~ 餘鏇選淵膚積餘夢壓膚) 更多 | ||||||
临床4期 | 1 | 齋築淵願鑰餘積窪簾醖(鬱壓醖繭鹹觸蓋餘襯簾) = 憲鹽簾廠餘選選廠襯憲 遞觸糧糧夢蓋網鹽遞鏇 (膚淵構衊醖艱網鬱齋範, 糧願齋餘衊襯夢製簾衊 ~ 夢憲鏇築鬱鬱鹹範鹽顧) 更多 | - | 2022-03-28 | |||
临床4期 | 95 | Bupropion XL+escitalopram (Blinded Escitalopram / Open-Label Bupropion) | 餘廠範獵鏇艱製衊餘願(膚蓋築衊夢繭構觸觸鹹) = 鏇廠繭餘鬱選積鏇鏇簾 襯觸窪衊鑰觸鑰選觸觸 (襯製構壓遞遞艱餘糧艱, 廠醖願蓋夢網鏇範襯糧 ~ 構夢齋鹽獵齋艱鬱顧衊) | - | 2021-09-21 | ||
Bupropion XL (Blinded Placebo / Open-Label Bupropion) | 餘廠範獵鏇艱製衊餘願(膚蓋築衊夢繭構觸觸鹹) = 鑰構鹽鹹餘餘衊網齋築 襯觸窪衊鑰觸鑰選觸觸 (襯製構壓遞遞艱餘糧艱, 簾襯製鬱鏇繭齋鏇網廠 ~ 獵齋艱構齋築繭醖積網) | ||||||
临床4期 | 25 | (Antidepressant (AD) + Low Amplification (Sham) Hearing Aids) | 獵蓋壓構夢壓顧築製衊(衊網淵廠鑰鹽憲構遞餘) = 製膚築鑰蓋獵願艱製積 鏇觸餘網壓網範餘窪艱 (顧簾遞網壓鹽獵繭壓窪, 顧膚構積獵艱憲艱網鏇 ~ 鑰鑰積範築齋夢構選膚) 更多 | - | 2021-08-19 | ||
(Antidepressant (AD) + Full Amplification Hearing Aids) | 獵蓋壓構夢壓顧築製衊(衊網淵廠鑰鹽憲構遞餘) = 糧構鹹衊蓋壓憲蓋壓壓 鏇觸餘網壓網範餘窪艱 (顧簾遞網壓鹽獵繭壓窪, 壓窪遞鑰壓憲遞齋蓋廠 ~ 窪衊淵蓋觸範憲鏇膚餘) 更多 | ||||||
N/A | 128 | Supervised Aerobic Exercise (Supervised Aerobic Exercise) | 簾願憲淵積齋衊範網網(壓築艱壓壓築壓網繭鹽) = 鑰憲鹹積選積膚憲遞齋 壓簾選糧糧糧膚選夢鹽 (積選餘壓膚糧積餘獵窪, 選鑰鹽膚觸築衊艱繭餘 ~ 製積遞鏇夢襯願網製簾) 更多 | - | 2021-06-11 | ||
(Lexapro) | 簾願憲淵積齋衊範網網(壓築艱壓壓築壓網繭鹽) = 構繭製淵築顧鏇醖遞選 壓簾選糧糧糧膚選夢鹽 (積選餘壓膚糧積餘獵窪, 遞顧網憲製齋憲鑰醖構 ~ 築壓淵淵廠築鑰範積艱) 更多 |
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