更新于：2024-12-20
Lacosamide
拉考沙胺
更新于：2024-12-20
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2008-08-29), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构
分子式C13H18N2O3 |
InChIKeyVPPJLAIAVCUEMN-GFCCVEGCSA-N |
CAS号175481-36-4 |
关联
176
项与 拉考沙胺 相关的临床试验A Bioequivalence study of a randomized, single dose, two-way crossover design with two-period, two-treatment, and two-sequence of Lacosamide Film Coated Tablet 100 mg (Test) relative to Vimpat Film Coated Tablet 100 mg (Reference) in healthy Thai adult volunteers under fasting condition.
- LACOS-06-23
Lacosamide Versus Topiramate in Migraine, a Ranodmized Trial
100 项与 拉考沙胺 相关的临床结果
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100 项与 拉考沙胺 相关的转化医学
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100 项与 拉考沙胺 相关的专利（医药）
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1,296
项与 拉考沙胺 相关的文献（医药）2025-03-01BRAIN RESEARCH
CRMP2 regulates mossy fiber sprouting and modulates microtubule dynamics in a pilocarpine induced rat model of epilepsy
Article
作者: Li, Yuxiang ; Li, Yuanfang ; Wang, Xin ; Wang, Qiang ; Cai, Yiying ; Su, Zhongqian ; Tong, Fangchao ; Ding, Jing
OBJECTIVE:
Our study aimed to investigate the role of CRMP2 in mossy fiber sprouting (MFS) using a pilocarpine-induced rat model of epilepsy.
METHODS:
First, the rats were sacrificed on the 1, 7, 14 and 28 day after pilocarpine injection. Quantitative Real-time PCR (qPCR) and Western blot (WB) were performed to assess mRNA and protein levels in the hippocampus and cortex. Next, shCRMP2 AAV was injected into the dentate gyrus of hippocampus to knock down CRMP2 expression. Two weeks later, the epileptic rat model was induced by pilocarpine injection. On the day of status epilepticus (SE) induction, animals in the shCtrl + EP + LCM and shCRMP2 + EP + LCM group received twice-daily intragastric administration of Lacosamide (LCM). The rats were video monitored from day 7 to 28, and were sacrificed on day 28 after pilocarpine injection for subsequent experiment.
RESULTS:
In the present study, we observed downregulation of phosphorylated CRMP2 in the hippocampus of epileptic rats. Additionally, LCM treatment reduces the expression level of CRMP2 protein in the hippocampus of these rats. Both CRMP2 knockdown and LCM treatment were found to decrease mossy fiber sprouting (MFS) in the dentate gyrus and shorten the duration of seizures in epileptic rats. Furthermore, we discovered that microtubule dynamics are reduced in the hippocampus of epileptic rats. Both CRMP2 Knockdown and LCM treatment were shown to increase the microtubule dynamics in the hippocampus of rats with epilepsy.
CONCLUSION:
In conclusion, we demonstrated convincingly that CRMP2 regulates mossy fiber sprouting and modulates microtubule dynamics in a pilocarpine induced rat model of epilepsy.
2025-02-01EPILEPSY & BEHAVIOR
Assessment of temporal changes in cognitive effects induced by antiseizure medications in epilepsy patients
Article
作者: Shafiyev, Javid ; Karadaş, Akçay Övünç ; Özmenek, Özlem Aksoy ; Karadaş, Ömer ; Şimşek, Uğur Burak ; Özenç, Betül
OBJECTIVE:
Numerous studies have been conducted investigating the effects of antiseizure medications (ASMs) on cognitive functions, and the cognitive side effects of some ASMs have been demonstrated. However, data on whether tolerance to these side effects develops over time is insufficient. The aim of this study is to evaluate the reversibility of cognitive impairments caused by ASMs in patients, utilizing event-related potentials (ERPs) and the Montreal Cognitive Assessment (MoCA) test.
MATERIALS AND METHODS:
The single-center prospective study was conducted from July 2022 to August 2023. This study enrolled participants aged 18 to 50 who had been diagnosed with epilepsy and were planning to commence treatment with an antiseizure medication (ASM). The inclusion criteria comprised individuals aged between 18 and 50 years, with a diagnosis of epilepsy, and who were intending to initiate a new ASM as monotherapy. Exclusion criteria encompassed individuals younger than 18 or older than 50 years, those diagnosed with psychogenic non-epileptic seizures, those currently on antiepileptic drugs, and those with cognitive dysfunction or dementia. Before starting treatment, patients were subjected to the MoCA test and ERP measurements by a neurologist. These tests and measurements were repeated at the second and sixth months of treatment.
RESULT:
The study included a cohort of 254 participants with a mean age of 32.6 (±14) years. At the second month after starting treatment with carbamazepine (CBZ), zonisamide (ZNS), valproic acid (VPA), and topiramate (TPM), both MoCA and ERP values showed significantly worse cognitive impairment compared to before treatment (p < 0.05). This impairment showed a significant improvement by the sixth month for CBZ, ZNS, and VPA (p < 0.05). Although there was improvement in MoCA and ERP values in patients using TPM, the changes remained statistically significant compared to baseline values (p < 0.05). In patients using levetiracetam, lamotrigine, oxcarbazepine, and lacosamide, cognitive impairment was not statistically significant at either the second or sixth month.
CONCLUSION:
This study demonstrated that the detrimental cognitive effects associated with CBZ, VPA, and ZNS could be reversible. Although some improvement was observed over time with TPM, the absence of significant recovery suggests that additional time may be required for a substantial reversal of these effects.
2024-12-01Neuropsychopharmacology reports
Effects of frequently prescribed antiseizure medications on motor vehicle driving performance: Narrative review based on a tiered approach for the assessment of clinically meaningful driving impairment in the Ministry of Health, Labour, and Welfare guideline
Review
作者: Yoshimura, Reiji ; Aoki, Hirofumi ; Iwamoto, Kunihiro ; Kanemoto, Kousuke ; Nakabayashi, Tetsuo ; Ozaki, Norio ; Yamaguchi, Akiko ; Konishi, Yuki ; Saji, Momoe ; Ando, Masahiko
Abstract:
Patients with epilepsy often require long‐term treatment with antiseizure medications, and their impact on daily activities, particularly driving, is of significant concern. The recently published “Guideline for Evaluating Effects of Psychotropic Drugs on the Performance to Drive a Motor Vehicle” in Japan provides a framework that can be referred to for not only the evaluation of new drugs but also the reevaluation of approved drugs. This study conducted a literature review regarding the effects of carbamazepine, valproate, lamotrigine, lacosamide, and levetiracetam, which are frequently prescribed for epilepsy, on driving performance following the guideline's tiered evaluation approach. Analyses of pharmacological, pharmacodynamic, and adverse events suggested that these drugs primarily affect arousal function. Driving studies showed that acute administration of carbamazepine, but not chronic monotherapy with carbamazepine, valproate, lamotrigine, and levetiracetam, significantly impairs driving performance. Epidemiological studies have not identified a definitive association between these drugs and traffic accidents. Initial administration of these five antiseizure medications may affect driving performance, warranting special attention, but the influence appears to diminish with continued use. Nevertheless, while long‐term administration of these five drugs may not have a clinically meaningful effect on driving performance, safe driving is not guaranteed for each individual patient, and appropriate individualized guidance is important in clinical practice.
100 项与 拉考沙胺 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 |
|---|---|---|---|
| 癫痫 | 欧盟 | 2017-09-18 | |
| 癫痫 | 冰岛 | 2017-09-18 | |
| 癫痫 | 列支敦士登 | 2017-09-18 | |
| 癫痫 | 挪威 | 2017-09-18 | |
| 强直阵挛性癫痫 | 日本 | 2016-07-04 | |
| 特发全身性癫痫 | 澳大利亚 | 2009-07-20 | |
| 癫痫发作 | 澳大利亚 | 2009-07-20 | |
| 癫痫部分性发作 | 欧盟 | 2008-08-29 | |
| 癫痫部分性发作 | 冰岛 | 2008-08-29 | |
| 癫痫部分性发作 | 列支敦士登 | 2008-08-29 | |
| 癫痫部分性发作 | 挪威 | 2008-08-29 |
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 |
|---|---|---|---|---|
| 糖尿病性神经病变 | 临床3期 | 德国 | 2003-12-01 | |
| 新生儿癫痫 | 临床2期 | 美国 | 2021-03-31 | |
| 新生儿癫痫 | 临床2期 | 澳大利亚 | 2021-03-31 | |
| 新生儿癫痫 | 临床2期 | 加拿大 | 2021-03-31 | |
| 癫痫综合征 | 临床2期 | 美国 | 2014-02-13 | |
| 癫痫综合征 | 临床2期 | 法国 | 2014-02-13 | |
| 癫痫综合征 | 临床2期 | 匈牙利 | 2014-02-13 | |
| 癫痫综合征 | 临床2期 | 墨西哥 | 2014-02-13 | |
| 癫痫综合征 | 临床2期 | 波兰 | 2014-02-13 | |
| 膝关节炎 | 临床2期 | 捷克 | 2007-03-01 |
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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3期 | 239 | 獵齋醖顧網壓餘遞憲製(窪獵鬱築鑰膚顧壓醖艱) = 窪網觸顧願餘醖膚網簾 繭製餘膚遞遞觸構醖繭 (餘繭願艱遞選淵餘醖鹽 ) 更多 | 积极 | 2024-10-26 | |||
N/A | - | 衊簾衊鹽艱鑰夢壓鹽衊(遞廠網夢網鏇齋範窪鹹) = 鹽憲鏇繭齋網壓鬱鏇廠 觸醖願築鏇衊鑰壓築醖 (壓積築鏇選鹽衊鑰鏇觸 ) 更多 | - | 2024-04-09 | |||
Lacosamide polytherapy | 衊簾衊鹽艱鑰夢壓鹽衊(遞廠網夢網鏇齋範窪鹹) = 糧觸鹽願糧襯壓糧鹹觸 觸醖願築鏇衊鑰壓築醖 (壓積築鏇選鹽衊鑰鏇觸 ) 更多 | ||||||
临床3期 | 239 | 醖鹽鬱窪獵醖構膚襯顧(鏇襯餘衊膚艱鹽鏇簾醖) = 遞選鹽顧遞餘夢壓繭衊 製淵獵淵鏇繭簾鑰蓋醖 (鏇淵遞鹽蓋憲憲顧糧淵, 觸齋願願憲膚獵鹽構觸 ~ 願餘顧鏇廠衊鹹餘鹽廠) 更多 | - | 2023-12-14 | |||
临床2期 | - | Lacosamide up to 12 mg/kg/day or 600 mg/day | 觸鬱鏇鑰鏇淵繭鏇簾窪(壓範築蓋襯壓構鹹憲簾) = 壓範鏇築積鬱範鑰鹹醖 淵膚築衊窪餘衊鹹襯製 (鏇鑰獵壓鬱鬱窪鑰築遞 ) | 积极 | 2023-11-01 | ||
N/A | 62 | 製積獵艱獵壓襯壓糧繭(選憲鹽遞鑰範糧窪壓鹹) = Adverse events (AEs) were reported in 53%, none of which were attributed to lacosamide 窪窪範鏇憲蓋構蓋窪壓 (鏇製鹹蓋鑰蓋夢範選壓 ) 更多 | - | 2023-10-01 | |||
N/A | 二线 | 67 | 壓製遞廠獵範獵顧顧願(積鹽鏇衊鹽壓鬱範憲醖) = 18 (26.9%) patient experienced bradycardia 顧積窪夢餘網淵遞獵艱 (觸窪鏇獵衊觸鑰夢製艱 ) 更多 | 积极 | 2023-09-04 | ||
N/A | - | 夢選壓築獵壓艱遞顧築(鑰觸簾簾遞願襯鬱醖夢) = No side effects 鹹遞製選網膚壓網獵網 (願獵簾蓋夢獵鬱願襯鬱 ) 更多 | - | 2023-09-04 | |||
临床3期 | 371 | 積夢憲衊淵蓋夢網鑰壓(衊選鹽簾構夢齋顧窪構) = 築窪範鬱繭構構憲鏇廠 觸選襯簾網膚顧範壓憲 (積積鹽獵廠築願鹽醖齋, 遞繭構觸築壓構夢膚醖 ~ 壓積廠網構範網鏇製鹽) 更多 | - | 2023-07-24 | |||
N/A | 676 | 積繭選鹽鹽鹽鹽積積膚(襯獵膚範製網餘築觸顧) = 鏇齋窪糧醖窪淵範顧廠 齋願淵醖鑰襯艱鏇獵遞 (鏇鏇壓憲築獵獵鬱齋廠, 1 ~ 480) | 积极 | 2023-04-25 | |||
临床3期 | 540 | 壓選觸醖窪糧鏇簾襯鹽(衊鹽觸艱蓋簾齋壓觸蓋) = 網蓋壓鹹醖蓋廠餘製鏇 鏇獵鬱廠鏇築糧繭選齋 (廠糧顧繭獵膚襯鹹遞糧, 繭壓艱齋積糧艱鹽鑰構 ~ 鏇窪蓋簾鹽齋廠壓願製) 更多 | - | 2022-10-25 |
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