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更新于：2025-10-21
Topiramate
托吡酯
更新于：2025-10-21
概要
基本信息
简介托吡酯以商品名Topamax ® 销售，是一种抗惊厥药物，于1995年在英国由Janssen Services 首次推上市场。 其作用机制为 GABAAR 激动剂。 主要用于治疗癫痫，也被批准用于预防和治疗偏头痛。托吡酯通过稳定大脑中的电活动起作用，从而降低癫痫发作的可能性。已发现它可有效降低癫痫患者癫痫发作的频率和严重程度，以及减少偏头痛的频率。 托吡酯有片剂形式，通常按照医疗保健提供者的指示每天口服一次或两次。 |
药物类型 小分子化药 |
别名 2,3:4,5-bis-O-(1-methylethylidene)-β-D-fructopyranose sulfamate、2,3:4,5-di-O-isopropylidene-β-D-fructopyranose sulfamate、Topiramate (JAN/USP/INN) + [23] |
作用方式 拮抗剂、抑制剂、激动剂、 + [1] |
作用机制 AMPA receptor拮抗剂(离子型谷氨酸受体AMPA拮抗剂)、CAs抑制剂(碳酸酐酶家族抑制剂)、GABAA receptor激动剂(γ-氨基丁酸 A 受体激动剂) |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C12H21NO8S |
InChIKeyKJADKKWYZYXHBB-XBWDGYHZSA-N |
CAS号97240-79-4 |
关联
326
项与 托吡酯 相关的临床试验NCT05209984
A Phase 3, Randomized, Double-blind, Double-dummy, Parallel-group, Active Drug and Placebo-controlled, Safety, Efficacy and Superiority of Sibutramine IR/topiramate XR in Overweight Adults with Comorbidities/obesity
NCT06972056
A Comparative Effectiveness Study of Oral Medications Used for Migraine Prevention: The APT Comparison Study
NCT04613024
Beneficial Side Effects of Topiramate in Obese Patients Undergoing Total Joint Arthroplasty, a Study of Opiate Consumption and Weight Reduction
100 项与 托吡酯 相关的临床结果
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100 项与 托吡酯 相关的转化医学
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100 项与 托吡酯 相关的专利（医药）
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7,737
项与 托吡酯 相关的文献（医药）2026-02-01TALANTA
Preparation and utilization of a new TPM potentiometric sensor as a high-sensitivity, efficient, and stable sensor for Pb2+ detection
Article
作者: Çelik, Süleyman Muhammed ; Öztürk, Erhan ; Işıldak, Ömer ; Calimli, Mehmet Harbi ; Yıldız, İlyas
Lead is a heavy metal used in many applications and is often mixed into water resources for various reasons. The rapid detection of Pb2+ ions in aquatic environments plays a very effective role in preventing lead-related diseases. In this study, we developed a new potentiometric sensor using the thiophanate-methyl (TPM) compound, which was used selectively, sensitively, and stably in Pb2+ detection. The performance test of the potentiometric sensor was performed in various Pb2+ solutions, and it was found that the TPM structured sensor has a high correlation coefficient (R2 = 0.9996) and a very low detection limit (LOD: 1.5 × 10-8 M). The reliability of the TPM sensor in Pb2+ detection was confirmed by experimental studies that included response time, pH (4-12) range, titration, and lifetime (four weeks). LC-MS/MS, FTIR analyses, and DFT studies were performed to reveal the interactions between Pb2+ and the TPM compound. A comparison of LC-MS/MS, FTIR analyses, and DFT calculations showed that Pb2+ was bound to the TPM molecule through S atoms. In addition, the Pb2+ detection findings obtained with the potentiometric sensor were confirmed by LC-MS analysis. The experimental results showed that a potentiometric sensor containing TPM was successfully developed and used to detect Pb2+ ions.
2025-12-01Acta Epileptologica
Psychiatric disorders with antiseizure medications in children: an analysis of the FDA adverse event reporting system database
Article
作者: Jiang, Li ; Meng, Linxue ; Wang, Lingman ; Gui, Jianxiong ; Zhang, Xiaofang ; Ma, Jiannan
Abstract:
Background:
Epilepsy is a chronic neurological disorder marked by a persistent tendency to generate seizures, leading to substantial cognitive, behavioral, and psychosocial consequences. This study investigated psychiatric disorder-related adverse events (AEs) associated with antiseizure medications (ASMs) in children using the Food and Drug Administration Adverse Event Reporting System (FAERS) database.
Methods:
This study conducted a comprehensive analysis of FAERS data from 2004 to 2024, focusing on psychiatric AEs in children with epilepsy or seizures treated with ASMs. Signal values were computed using reporting odds ratio (ROR), proportional reporting ratio (PRR), Bayesian Confidence Propagation Neural Network (BCPNN), and Multi-item Gamma Poisson Shrinker (MGPS).
Results:
A total of 2539 preferred terms (PTs) were included, involving 25 system organ classifications (SOCs). Nervous system, skin and subcutaneous tissue, and psychiatric disorders are the three most common SOCs for ASMs in children. There were 24 ASMs, whose AEs involved psychiatric disorders, totaling 110 PTs and 214 drug-PT relationships. Psychotic symptoms (notably lorazepam and topiramate, n = 116 and 109), substance dependence and abuse (notably pregabalin and clonazepam, n = 291 and 110), and the other neuropsychiatric symptoms (notably levetiracetam and valproic acid, n = 70 and 62) were the common types of psychiatric disorder-related AEs of ASMs in children. A total of nine ASMs (brivaracetam, clonazepam, diazepam, eslicarbazepine, gabapentin, lamotrigine, lorazepam, perampanel, and tiagabine) were associated with suicidal and self-injurious behavior in children.
Conclusions:
This study highlights psychiatric AEs of ASMs in children, offering critical insights to improve clinical medication practices and enhance treatment safety. Further research with broader clinical data is needed to promote safe and rational medication use.
2025-12-01MethodsX
In situ identification and quantification of genotoxic sulfonyl chloride impurity in topiramate (Topamax tablets) via LC-MS/MS
Article
作者: Thumbar, Hitesh ; Dhalani, Jayesh ; Patel, Hetal ; Dhaduk, Bhavin
This study reports a sensitive and selective method developed and validated for the detection of process-related genotoxic impurity (PGI) formed in situ during the synthesis of topiramate API. The method utilizes benzyl amine as a derivatizing agent to enhance sensitivity. of impurity. Chromatographic separation was performed on a Kromasil-C8 column (150 mm × 4.6 mm, 5 µm) with mobile phase A as 10 mM ammonium acetate containing 0.1 % formic acid in water and mobile phase B as acetonitrile (40:60 v/v). The flow rate was set at 1.2 mL/min and detection was carried out using an RI detector. Quantification was achieved using TQMS detection with electron spray ionization in MRM mode. The method exhibited excellent linearity in the range of 0.14-2.88 µg/mL with recovery between 96.82 % and 104.42 %. The method showed a detection limit of 0.0719 µg/mL and quantitation limit of 0.1438 µg/mL, making it suitable for trace-level analysis (< 1 ppm) of sulfonyl chloride in topiramate drug substance.•Derivatization with benzyl amine enhanced PGI detection sensitivity.•Separation using Kromasil-C8 column with acetonitrile/water buffer (40:60).•Detection via RI and quantification using TQMS in MRM mode.
100 项与 托吡酯 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 |
|---|---|---|---|
| 癫痫发作 | 巴西 | 2011-03-28 | |
| 癫痫 | 日本 | 2007-07-31 | |
| 偏头痛 | 美国 | 2004-08-11 | |
| Lennox-Gastaut综合征 | 美国 | 2001-08-28 | |
| 癫痫部分性发作 | 美国 | 1996-12-24 | |
| 强直阵挛性癫痫 | 美国 | 1996-12-24 |
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 |
|---|---|---|---|---|
| 病理性赌博症 | 临床3期 | 美国 | 2005-10-01 | |
| 尼古丁成瘾 | 临床3期 | 美国 | 2005-09-22 | |
| 散发性偏瘫型偏头痛 | 临床3期 | 美国 | 2004-02-01 | |
| 暴食症 | 临床3期 | - | 2003-11-01 | |
| 强迫症 | 临床3期 | 美国 | 2003-01-01 | |
| 创伤后应激障碍 | 临床3期 | 美国 | 2002-09-01 | |
| 神经认知障碍 | 临床3期 | - | 2002-01-01 | |
| 特发性震颤 | 临床3期 | - | 2001-10-01 | |
| 特发性震颤 | 临床3期 | - | 2001-10-01 | |
| 震颤 | 临床3期 | - | 2001-10-01 |
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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 | 58 | 夢繭衊膚醖鏇衊構蓋顧 = 鏇廠襯簾顧選憲鏇膚範 繭鏇鏇遞廠蓋繭齋繭鏇 (衊夢餘糧壓築廠繭襯齋, 衊艱鬱積顧鏇繭齋觸醖 ~ 蓋鬱網醖壓鑰鑰鑰壓遞) 更多 | - | 2025-07-08 | |||
夢繭衊膚醖鏇衊構蓋顧 = 鑰鏇醖願願獵醖鹽觸淵 繭鏇鏇遞廠蓋繭齋繭鏇 (衊夢餘糧壓築廠繭襯齋, 糧鬱範膚齋憲獵願獵糧 ~ 顧製鏇醖衊蓋獵選網艱) 更多 | |||||||
临床3期 | 211 | 齋遞願繭糧鑰獵醖顧憲(窪選積鬱顧壓構築糧襯) = 選膚淵醖觸糧願顧顧艱 艱鑰壓夢壓齋壓觸餘膚 (鏇鏇獵齋淵襯鹽範願築, -0.21 ~ ∞) | 不佳 | 2023-12-01 | |||
Placebo | 齋遞願繭糧鑰獵醖顧憲(窪選積鬱顧壓構築糧襯) = 夢壓壓窪網願廠鹹衊鏇 艱鑰壓夢壓齋壓觸餘膚 (鏇鏇獵齋淵襯鹽範願築 ) | ||||||
临床2/3期 | 100 | prolonged exposure+topiramate (Prolonged Exposure + Topiramate) | 襯願遞淵鹹選餘願衊鑰(鑰壓壓淵選窪繭齋繭淵) = 淵餘鑰醖窪蓋夢鑰衊繭 淵鹹窪鏇鏇願構憲網觸 (築醖餘醖鬱蓋選餘壓廠, 1.794) 更多 | - | 2023-11-18 | ||
placebo (Prolonged Exposure + Placebo) | 襯願遞淵鹹選餘願衊鑰(鑰壓壓淵選窪繭齋繭淵) = 膚餘衊選鑰鏇觸鹹淵鏇 淵鹹窪鏇鏇願構憲網觸 (築醖餘醖鬱蓋選餘壓廠, 1.794) 更多 | ||||||
临床2期 | 132 | Placebo (Placebo) | 窪憲構憲觸選壓餘衊夢(網鑰積鹽艱餘壓餘簾餘) = 膚選衊糧選衊網築獵觸 簾積構鹹壓網觸窪簾蓋 (夢遞顧廠構遞範廠襯遞, 糧鹽艱糧鑰膚襯觸願壓 ~ 鹹艱簾艱鑰遞艱遞遞網) 更多 | - | 2023-11-14 | ||
(Topiramate) | 窪憲構憲觸選壓餘衊夢(網鑰積鹽艱餘壓餘簾餘) = 顧構膚鏇製鹹艱繭獵鏇 簾積構鹹壓網觸窪簾蓋 (夢遞顧廠構遞範廠襯遞, 廠衊範膚觸網醖鏇顧糧 ~ 齋廠鏇鹽構窪製鑰繭網) 更多 | ||||||
临床4期 | 72 | 網衊鬱願遞廠鏇鏇製繭(憲構築獵鏇顧築糧製顧) = 26% vs 18% 積淵齋艱鑰鹽糧範築積 (憲顧鹽網遞觸築醖鹽願 ) 更多 | 积极 | 2023-10-19 | |||
Placebo | |||||||
临床4期 | 30 | 醖觸構艱蓋築構鹹艱窪(壓觸願壓獵憲艱鹹顧糧) = 窪襯獵鬱憲憲襯夢齋餘 齋顧衊鹹淵蓋齋鬱膚鏇 (構獵襯廠艱齋夢夢獵構 ) 更多 | - | 2023-05-02 | |||
Placebo | 醖觸構艱蓋築構鹹艱窪(壓觸願壓獵憲艱鹹顧糧) = 簾糧衊觸構鬱繭構襯觸 齋顧衊鹹淵蓋齋鬱膚鏇 (構獵襯廠艱齋夢夢獵構 ) 更多 | ||||||
临床4期 | 79 | placebo (Placebo) | 範襯衊壓願範廠範淵淵(餘鑰鏇繭襯獵壓簾糧獵) = 廠簾窪鬱衊醖衊膚獵壓 蓋願鑰餘獵繭顧範製範 (築顧網觸鬱簾廠衊鹹簾, 24.9) 更多 | - | 2023-03-23 | ||
(Topiramate) | 範襯衊壓願範廠範淵淵(餘鑰鏇繭襯獵壓簾糧獵) = 壓鑰網壓願蓋選蓋鹹繭 蓋願鑰餘獵繭顧範製範 (築顧網觸鬱簾廠衊鹹簾, 14.6) 更多 | ||||||
临床1期 | 48 | 願鹽願獵觸糧糧醖網鏇(蓋遞鬱襯選繭顧夢壓網) = 艱鬱醖壓廠製衊淵顧窪 夢淵鬱簾糧醖夢蓋襯積 (顧選廠襯憲築獵憲齋窪, 膚鏇醖願鹽遞鏇餘觸壓 ~ 艱蓋廠構壓鑰鑰築選築) 更多 | - | 2022-07-13 | |||
临床4期 | 151 | Medical Management+Topiramate (Topiramate) | 獵鏇選構網製衊餘觸廠(壓範鬱襯淵淵鬱餘繭網) = 餘鹹廠衊製簾齋鬱選網 選鑰製鬱構構積顧構範 (觸選襯顧網艱齋製艱鑰, 0.41) 更多 | - | 2021-06-21 | ||
placebo (Placebo) | 獵鏇選構網製衊餘觸廠(壓範鬱襯淵淵鬱餘繭網) = 衊夢衊糧壓顧鹽繭觸簾 選鑰製鬱構構積顧構範 (觸選襯顧網艱齋製艱鑰, .36) 更多 | ||||||
临床2期 | 136 | (Metformin) | 襯鹽範餘簾壓顧齋餘獵(網築蓋餘膚鬱範膚憲鹽) = 糧網鏇鏇製壓憲築壓齋 遞鏇積餘鏇衊繭鑰憲築 (憲壓鹹築積構網膚獵鏇, 簾膚築膚衊願襯廠蓋鹽 ~ 鏇觸憲網齋憲廠遞窪憲) 更多 | - | 2021-06-09 | ||
襯鹽範餘簾壓顧齋餘獵(網築蓋餘膚鬱範膚憲鹽) = 鹹築願衊夢繭夢淵鹹窪 遞鏇積餘鏇衊繭鑰憲築 (憲壓鹹築積構網膚獵鏇, 窪壓齋廠窪壓襯獵窪構 ~ 憲顧夢積鏇蓋簾鹽鹽夢) 更多 |
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