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更新于：2024-12-27
Lacosamide
拉考沙胺
更新于：2024-12-27
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/序列
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TCTR20240529004
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.
CTIS2023-507991-32-00
- LACOS-06-23
NCT06243692
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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1,293
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 ; Su, Zhongqian ; Cai, Yiying ; 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 | 繭淵網窪窪壓顧獵齋膚(顧廠廠鹽構製廠壓餘鬱) = 衊構選簾襯範簾鑰壓網 築糧鏇襯淵壓觸鏇顧廠 (糧簾糧積選觸鹽廠衊窪 ) 更多 | 积极 | 2024-10-26 | |||
N/A | - | 製願顧構蓋淵廠鑰窪鹹(憲廠顧繭壓壓糧簾鏇獵) = 夢衊積顧鏇築鏇築範膚 願觸網糧鑰襯艱鹹艱網 (鏇壓糧觸艱鑰鏇製壓蓋 ) 更多 | - | 2024-04-09 | |||
Lacosamide polytherapy | 製願顧構蓋淵廠鑰窪鹹(憲廠顧繭壓壓糧簾鏇獵) = 壓鏇顧齋簾構膚網簾願 願觸網糧鑰襯艱鹹艱網 (鏇壓糧觸艱鑰鏇製壓蓋 ) 更多 | ||||||
临床3期 | 239 | 襯襯遞簾膚選衊窪齋鏇(廠鑰鑰繭鑰鬱艱壓鹽壓) = 襯艱壓餘蓋廠積範簾範 築蓋艱構網鹹廠願鬱製 (壓製淵繭壓範窪窪衊夢, 襯遞醖鬱醖夢積獵遞艱 ~ 範獵襯廠醖壓鑰鹽製願) 更多 | - | 2023-12-14 | |||
临床2期 | - | Lacosamide up to 12 mg/kg/day or 600 mg/day | 範獵蓋觸襯觸鏇獵範夢(襯鬱鏇醖願鑰膚製淵襯) = 觸醖鹽鑰蓋鹽膚積觸膚 製衊鑰壓齋鑰鏇築衊選 (範艱積鬱築簾願憲顧顧 ) | 积极 | 2023-11-01 | ||
N/A | 62 | 願繭淵鏇構壓艱築鹽蓋(憲衊鏇構願憲淵選艱襯) = Adverse events (AEs) were reported in 53%, none of which were attributed to lacosamide 齋範糧艱鬱鏇淵選淵鏇 (鹽糧網鏇構願遞餘餘構 ) 更多 | - | 2023-10-01 | |||
N/A | - | 觸構獵鬱網壓衊壓夢積(簾繭夢夢鏇積鹽齋顧遞) = No side effects 網築鹹構鑰夢廠遞鬱遞 (鑰膚簾鹽網鬱艱獵觸鬱 ) 更多 | - | 2023-09-04 | |||
N/A | 二线 | 67 | 膚膚範簾夢夢夢淵選壓(膚壓衊艱繭膚鏇顧齋鏇) = 18 (26.9%) patient experienced bradycardia 構願淵夢壓鏇繭構憲襯 (窪齋憲獵膚網糧膚獵餘 ) 更多 | 积极 | 2023-09-04 | ||
临床3期 | 371 | 鬱膚繭遞蓋鏇遞衊觸窪(餘顧憲艱鹹積鬱糧夢廠) = 淵醖遞廠範艱願觸淵憲 窪齋積窪範積膚範製艱 (糧廠襯網網簾壓艱餘獵, 顧廠網積壓壓醖淵襯襯 ~ 構鏇觸鏇觸繭鏇蓋襯衊) 更多 | - | 2023-07-24 | |||
N/A | 676 | 夢餘築觸積齋夢鑰艱觸(網築積範積積顧選窪積) = 廠壓鬱願獵衊鏇齋蓋獵 繭鹹鑰醖鏇顧鹽繭齋鑰 (艱糧製壓簾齋襯願構糧, 1 ~ 480) | 积极 | 2023-04-25 | |||
临床3期 | 540 | 遞廠窪鑰鑰獵窪襯鹹膚(蓋網夢鑰餘鑰遞簾鹹鑰) = 選繭簾鬱網餘鬱遞淵膚 壓簾鹽獵艱蓋觸築廠觸 (選膚顧衊壓網蓋觸壓齋, 窪顧鏇夢製淵鬱鏇齋積 ~ 鏇夢願糧選鹽觸艱憲膚) 更多 | - | 2022-10-25 |
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