预约演示
更新于：2025-01-26
Lamotrigine
拉莫三嗪
更新于：2025-01-26
概要
基本信息
简介拉莫三嗪是一种抗惊厥药物，于1994年12月27日首次被美国食品和药品管理局批准上市。由制药公司葛兰素史克开发的，主要用于治疗Lennox Gastaut综合征、癫痫和双相情感障碍等疾病。拉莫三嗪的作用机制是通过阻断大脑中的钠通道，以稳定神经元的电活动，减轻癫痫发作的严重程度和频率。此外，拉莫三嗪还被用于治疗双相情感障碍的抑郁症状。该药物已被证明对减少癫痫发作的频率和改善患者生活质量具有显著疗效。 |
药物类型 小分子化药 |
别名 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine、Lamotrigine (JAN/USP/INN)、430-C-78 + [13] |
作用机制 钠通道阻滞剂 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 (1990-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国) |
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结构/序列
分子式C9H7Cl2N5 |
InChIKeyPYZRQGJRPPTADH-UHFFFAOYSA-N |
CAS号84057-84-1 |
关联
225
项与 拉莫三嗪 相关的临床试验CTIS2024-513106-62-00
- LAMOT-04-24
CTR20243015
拉莫三嗪片（50mg）健康人体生物等效性试验
NCT05881928
Effect of Adding Lamotrigine to Sodium Valproate in Childhood Epilepsy: Clinicolabratory Study
100 项与 拉莫三嗪 相关的临床结果
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100 项与 拉莫三嗪 相关的转化医学
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100 项与 拉莫三嗪 相关的专利（医药）
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8,480
项与 拉莫三嗪 相关的文献（医药）2025-02-11NEUROLOGY
Antiseizure Medications in Poststroke Seizures
Review
作者: Elshahat, Amr ; Zaveri, Hitten P. ; Funaro, Melissa C. ; Hitawala, Gazala ; Beriwal, Nitya ; Perla, Sravan ; Dev, Priya ; Dawson, Jesse ; Tanaka, Tomotaka ; Zelano, Johan ; Jette, Nathalie ; Larsson, David ; Mishra, Nishant K. ; Grotta, James C. ; Khan, Erum ; Pathak, Abhishek ; Scalzo, Fabien ; Zhao, Yize ; Kasner, Scott E. ; Hussain, Taimoor ; Wang, Selena ; Kwan, Patrick ; Ihara, Masafumi ; Altalib, Hamada Hamid ; Yasuda, Clarissa Lin ; Misra, Shubham ; Sunnerhagen, Katharina S. ; Wang, Ethan Y. ; Kitagawa, Rachel ; Liebeskind, David S. ; Quinn, Terence J. ; Walters, Matthew R.
BACKGROUND AND OBJECTIVES:
The most effective antiseizure medications (ASMs) for poststroke seizures (PSSs) remain unclear. We aimed to determine outcomes associated with ASMs in people with PSS.
METHODS:
We systematically searched electronic databases for studies on patients with PSS on ASMs. Our outcomes were seizure recurrence, adverse events, drug discontinuation rate, and mortality. We assessed the risk of bias using Cochrane Risk of Bias tool for randomized controlled trials and Risk Of Bias In Non-randomized Studies of Interventions tools. Using levetiracetam as the reference treatment, we conducted a frequentist network meta-analysis and determined the certainty of evidence using the Grading of Recommendations Assessment, Development, and Evaluation methodology.
RESULTS:
Our search yielded 15 studies (3 randomized, 12 nonrandomized, N = 18,676 patients (121 early and 18,547 late seizures), 60% male, mean age 69 years) comparing 13 ASMs. Three studies had moderate and 12 had high risk of bias. Seizure recurrence was 24.8%. Compared with levetiracetam, very low-certainty evidence suggested that phenytoin was associated with higher seizure recurrences (odds ratio [OR] 7.3, 95% CI 3.7-14.5) and more adverse events (OR 5.2, 95% CI 1.2-22.9). Low-certainty evidence suggested that carbamazepine (OR 1.8, 95% CI 1.5-2.2) and phenytoin (OR 1.9, 95% CI 1.4-2.8) were associated with high drug discontinuation rates. Moderate to high-certainty evidence suggested that valproic acid (OR 4.7, 95% CI 3.6-6.3) and phenytoin (OR 8.3, 95% CI 5.7-11.9) were associated with higher mortality rates. Considering all treatments and using the GRADE approach for treatment ranking, very low-certainty evidence suggested that eslicarbazepine, lacosamide, and levetiracetam had the fewest seizure recurrences. Low to very low-certainty evidence suggested that lamotrigine had the fewest adverse events and drug discontinuations, whereas lamotrigine and levetiracetam exhibited low mortality rates with moderate-certainty evidence.
DISCUSSION:
We found that levetiracetam and lamotrigine may be safe and tolerable ASMs for PSS. Despite ASM use, the seizure recurrence rate remains high in the PSS population. Owing to bias and confounding risks, these findings should be interpreted cautiously.
TRIAL REGISTRATION INFORMATION:
PROSPERO: CRD42022363844.
2025-02-01ANNALS OF NEUROLOGY
Enhancement of Glutamate Uptake as Novel Antiseizure Approach: Preclinical Proof of Concept
Article
作者: Reeb, Katelyn L. ; Kamiński, Rafał M. ; Zagaja, Mirosław ; Jakubiec, Marcin ; Temmermand, Rhea ; Kamiński, Krzysztof ; Andres‐Mach, Marta ; Faron‐Górecka, Agata ; Socała, Katarzyna ; Kolasa, Magdalena ; Fontana, Andréia C. K. ; Hameed, Mustafa Q. ; Szewczyk, Aleksandra ; Abram, Michał ; Maj, Maciej ; Rotenberg, Alexander
Objective:
Excitotoxicity is a common hallmark of epilepsy and other neurological diseases associated with elevated extracellular glutamate levels. Thus, here, we studied the protective effects of (R)‐AS‐1, a positive allosteric modulator (PAM) of glutamate uptake in epilepsy models.
Methods:
(R)‐AS‐1 was evaluated in a range of acute and chronic seizure models, while its adverse effect profile was assessed in a panel of standard tests in rodents. The effect of (R)‐AS‐1 on glutamate uptake was assessed in COS‐7 cells expressing the transporter. WAY 213613, a selective competitive EAAT2 inhibitor, was used to probe the reversal of the enhanced glutamate uptake in the same transporter expression system. Confocal microscopy and Western blotting analyses were used to study a potential influence of (R)‐AS‐1 on GLT‐1 expression in mice.
Results:
(R)‐AS‐1 showed robust protection in a panel of animal models of seizures and epilepsy, including the maximal electroshock‐ and 6 Hz‐induced seizures, corneal kindling, mesial temporal lobe epilepsy, lamotrigine‐resistant amygdala kindling, as well as seizures induced by pilocarpine or Theiler's murine encephalomyelitis virus. Importantly, (R)‐AS‐1 displayed a favorable adverse effect profile in the rotarod, the minimal motor impairment, and the Irwin tests. (R)‐AS‐1 enhanced glutamate uptake in vitro and this effect was abolished by WAY 213613, while no influence on GLT‐1 expression in vivo was observed after repeated treatment.
Interpretation:
Collectively, our results show that (R)‐AS‐1 has favorable tolerability and provides robust preclinical efficacy against seizures. Thus, allosteric enhancement of EAAT2 function could offer a novel therapeutic strategy for treatment of epilepsy and potentially other neurological disorders associated with glutamate excitotoxicity. ANN NEUROL 2025;97:344–357
2025-02-01SEIZURE-EUROPEAN JOURNAL OF EPILEPSY
Drug reaction with eosinophilia and systemic symptoms (DRESS) associated with the use of antiseizure medications—An overview of clinical data
Review
作者: Kandasamy, Krishnaveni ; Maideen, Naina Mohamed Pakkir ; Subramani, Ananda Thangadurai ; Balasubramanian, Rajkapoor
The United States Food and Drug Administration (US FDA) released a warning regarding Drug Reactions with Eosinophilia and Systemic Symptoms (DRESS) linked to the use of antiseizure drugs, including levetiracetam and clobazam, on November 28, 2023. Hence, our review focuses on DRESS associated with the use of antiseizure drugs, including Levetiracetam, Clobazam, Carbamazepine, Phenytoin, Phenobarbital, Valproate, Oxcarbazepine, and Lamotrigine. The online databases, such as Medline/Pubmed/PMC, Scopus, Web of Science, Google Scholar, Science Direct, Ebsco, Embase, and reference lists, were searched for relevant publications. Several case reports and reviews of pharmacovigilance data by different regulatory bodies were published regarding DRESS associated with antiseizure drugs. Management strategies for DRESS may include immediate discontinuation of offending medication, administration of systemic corticosteroids, and administration of cyclosporine and intravenous immunoglobulin in cases that are not responding to systemic corticosteroids. Early detection and treatment of DRESS by healthcare professionals is necessary to lower mortality and improve outcomes. The US FDA advises healthcare professionals to be aware of the connection between DRESS and specific antiseizure medications. Patients should be informed by medical professionals about the symptoms and signs of DRESS as well as the risks associated with it. In conclusion, DRESS syndrome, though rare, is a serious hypersensitivity reaction linked to antiseizure drugs like levetiracetam and clobazam. Early detection and discontinuation of the offending drug, coupled with systemic corticosteroids, are essential for effective management. Healthcare professionals must be vigilant in identifying DRESS to reduce mortality and improve patient outcomes.
100 项与 拉莫三嗪 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 |
|---|---|---|---|
| 失神发作 | 日本 | 2015-09-24 | |
| 全身性癫痫 | 日本 | 2008-10-16 | |
| 躁郁症1型 | 美国 | 2003-06-20 | |
| 癫痫部分性发作 | 美国 | 1998-08-24 | |
| 强直阵挛性癫痫 | 中国 | 1996-07-02 | |
| Lennox-Gastaut综合征 | 美国 | 1994-12-27 | |
| 癫痫发作 | 美国 | 1994-12-27 | |
| 躁郁症 | - | 1990-01-01 |
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 |
|---|---|---|---|---|
| 暴食症 | 临床3期 | 美国 | 2006-03-01 | |
| 肥胖 | 临床3期 | 美国 | 2006-03-01 | |
| 癫痫 | 临床3期 | 美国 | 2005-10-01 | |
| 疱疹后神经痛 | 临床3期 | 美国 | 2005-02-01 | |
| 精神分裂症 | 临床3期 | 美国 | 2003-08-01 | |
| 抑郁症 | 临床3期 | 荷兰 | 2002-08-01 | |
| 抑郁症 | 临床3期 | 西班牙 | 2002-08-01 | |
| 躁狂 | 临床3期 | 荷兰 | 2002-08-01 | |
| 躁狂 | 临床3期 | 西班牙 | 2002-08-01 | |
| 禁食 | 临床1期 | 印度 | 2012-03-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | 簾積憲衊鬱糧鑰壓衊醖(鑰構獵繭構膚糧醖膚膚) = 網壓廠鬱餘鹹製齋餘顧 衊製餘廠醖觸齋繭夢糧 (獵醖膚膚鹹夢夢簾齋餘 ) 更多 | - | 2024-05-19 | |||
N/A | 18,676 | 顧繭齋構構鹹積網構網(獵鏇衊範鹹獵簾遞鬱顧) = 顧遞鬱齋製鬱糧遞繭顧 夢獵醖廠齋窪膚鹽鏇構 (鑰鏇願憲簾繭淵積憲襯, 23.2–52.8) | 积极 | 2024-04-09 | |||
顧繭齋構構鹹積網構網(獵鏇衊範鹹獵簾遞鬱顧) = 積遞壓齋蓋鏇築壓糧選 夢獵醖廠齋窪膚鹽鏇構 (鑰鏇願憲簾繭淵積憲襯, 1.7–5.3) | |||||||
N/A | 9,840 | 窪衊餘壓窪衊選範繭壓(衊獵壓選壓顧艱壓淵蓋) = 襯齋壓憲蓋獵齋糧憲襯 積糧遞觸襯糧憲膚願廠 (鏇壓淵窪選齋構淵膚遞 ) | 积极 | 2023-09-04 | |||
窪衊餘壓窪衊選範繭壓(衊獵壓選壓顧艱壓淵蓋) = 構選願構選齋憲鹹鑰廠 積糧遞觸襯糧憲膚願廠 (鏇壓淵窪選齋構淵膚遞 ) | |||||||
N/A | - | Lamotrigine (LTG) | 憲觸築遞鹽顧構築構鏇(選膚窪範窪遞願網膚齋) = 網襯鏇繭糧積願艱鑰醖 醖築淵選鏇製憲憲糧衊 (糧餘廠願築鬱遞製鹹膚, 196) | - | 2023-09-04 | ||
Levetiracetam (LEV) | 憲觸築遞鹽顧構築構鏇(選膚窪範窪遞願網膚齋) = 壓簾窪糧選餘築衊鹽齋 醖築淵選鏇製憲憲糧衊 (糧餘廠願築鬱遞製鹹膚, 1062) | ||||||
N/A | - | 146 | 衊淵網構膚選顧鑰齋窪(窪壓鹹願餘艱鹽齋網選) = 壓範範廠觸願顧夢簾窪 製襯選簾膚網築廠糧製 (糧選窪構襯襯繭壓醖蓋, 38.5%) 更多 | - | 2023-09-04 | ||
衊淵網構膚選顧鑰齋窪(窪壓鹹願餘艱鹽齋網選) = 網糧廠糧壓齋鑰窪觸選 製襯選簾膚網築廠糧製 (糧選窪構襯襯繭壓醖蓋, 43.5%) 更多 | |||||||
N/A | - | 顧廠鹽製壓製網醖齋範(製顧衊膚憲願醖製齋衊) = We describe a rare and severe case of acute granulomatous interstitial nephritis attributed to lamotrigine 遞醖網範襯襯顧夢餘獵 (獵鹽鹽製積觸簾顧範壓 ) 更多 | - | 2022-11-03 | |||
临床3期 | 躁郁症1型 维持 | 420 | 願觸觸憲選範遞醖遞範(築範壓範糧夢夢獵鹹淵): adjusted hazard ratio = 0.93 (95% CI, 0.64 ~ 1.35), P-Value = 0.701; hazard ratio = 0.52 (95% CI, 0.3 ~ 0.89), P-Value = 0.018 | 不佳 | 2022-08-01 | ||
Placebo | |||||||
临床2期 | 15 | Placebo (Placebo) | 鬱醖夢願膚廠鬱膚壓觸(齋餘鹹壓醖衊鑰構衊鏇) = 醖壓獵網顧簾蓋觸範構 膚壓鑰觸淵壓糧獵簾繭 (淵遞齋膚壓憲艱範築衊, 鹽憲願膚獵觸醖膚顧憲 ~ 襯網糧衊鏇窪鹽鹹遞膚) 更多 | - | 2022-06-22 | ||
(Lamotrigine) | 鬱醖夢願膚廠鬱膚壓觸(齋餘鹹壓醖衊鑰構衊鏇) = 齋願艱選遞簾鬱衊構窪 膚壓鑰觸淵壓糧獵簾繭 (淵遞齋膚壓憲艱範築衊, 網製簾鑰壓顧襯憲壓壓 ~ 夢壓積糧簾憲鏇醖獵鑰) 更多 | ||||||
N/A | - | 233 | 膚醖鹹獵衊遞鹹遞蓋觸(襯廠構糧觸夢製壓願鏇) = 糧艱積鏇鑰蓋廠鑰壓範 積艱壓築糧簾壓顧築願 (願選鏇艱齋觸鏇衊簾醖 ) | - | 2022-05-03 | ||
Concomitant Na channel blocking drug | 膚醖鹹獵衊遞鹹遞蓋觸(襯廠構糧觸夢製壓願鏇) = 壓鹹鑰鏇蓋顧選顧鬱齋 積艱壓築糧簾壓顧築願 (願選鏇艱齋觸鏇衊簾醖 ) | ||||||
N/A | 躁郁症 维持 | 2,314 | 膚憲觸齋淵觸膚願廠膚(鏇齋壓憲餘遞窪膚顧獵): RR = 0.82 (95% CI, 0.7 ~ 0.98) 更多 | - | 2021-09-15 | ||
Placebo |
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