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更新于：2025-03-25
Topiramate
托吡酯
更新于：2025-03-25
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) + [22] |
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) |
在研适应症 |
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
325
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
NCT06799169
Management of Acute Tinnitus with Migraine Medications: a Randomized Clinical Trial
TCTR20240527003
A Bioequivalence study of a randomized, open-label, single dose, two-way crossover design with two-period, two-treatment and two-sequence of Topiramate 100 mg tablets relative to Topamax 100 mg tablets, in healthy Thai volunteers under fasting condition
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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8,341
项与 托吡酯 相关的文献（医药）2025-05-03Journal of biomolecular structure & dynamics
Exploring the hub genes and potential drugs involved in Fanconi anemia using microarray datasets and bioinformatics analysis
Article
作者: Fakhri Ali, Sama ; Ayaz, Hassan ; Sanami, Samira ; Ahmad, Sajjad ; Alruwetei, Abdulmohsen M. ; N. Almanaa, Taghreed ; Aljasir, Mohammad Abdullah ; Hameed, Alaa R. ; Ahmad, Faisal ; Ali, Ijaz
Fanconi anemia (FA) is a genetic disorder that occurs when certain genes responsible for repairing DNA replication and promoting homologous recombination fail to function properly. This leads to severe clinical symptoms and a wide range of cancer-related characteristics. Recent treatment approaches for FA involve hematopoietic stem cell transplantation (HSCT), which helps restore the population of stem cells. A survival study using p-values indicated that specific hub genes play a significant role in diagnosing and predicting the disease. To find potential medications that interact with the identified hub genes, researchers inferred drugs. Among hub genes, TP53 was found to be particularly promising through computational analysis. Further investigation focused on two drugs, Topiramate and Tocofersolan predicted based on drug bank database analysis. Molecular docking strategies were employed to assess the best binding pose of these drugs with TP53. Topiramate showed a binding affinity of -6.5 kcal/mol, while Tocofersolan showed -8.5 kcal/mol against the active residues within the binding pocket. Molecular dynamics (MD) simulations were conducted to observe the stability of each drug's interaction with the TP53 protein over time. Both drugs exhibited stable confirmation with only slight changes in the loop region of the TP53 protein during the simulation intervals. Results also shows that there was a high fluctuation observed during apo-sate simulation time intervals as compared to complex system. Hence, it is suggested that the exploration of structure-based drug design holds promising results to specific target. This could potentially lead to a breakthrough in future experimental approaches for FA treatment.
2025-04-01ACTA OBSTETRICIA ET GYNECOLOGICA SCANDINAVICA
Exposure to potentially teratogenic medications before and during the first trimester of pregnancy compared to women of childbearing age: A retrospective analysis of Swiss claims data (2015–2021)
Article
作者: Meier, Christoph R. ; Surbek, Daniel ; Spoendlin, Julia ; Marxer, Carole A. ; Panchaud, Alice ; Graber, Sereina M.
Abstract:
Introduction:
Exposure to potentially teratogenic medications during pregnancy is underinvestigated in Switzerland. We aimed to assess exposure to potential teratogens preconceptionally, during the first trimester, and in women of childbearing age, and specifically explore the effectiveness of the valproate pregnancy prevention program (2018).
Material and Methods:
Retrospective study using the Swiss Helsana claims database. In a pregnancy cohort (2015–2021) and a cohort of women of childbearing age (2021 and 2018), we defined three 90‐day time periods: (1) first trimester, (2) preconceptional period (days 180–90 before pregnancy), and (3) January 01, 2021, and March 31, 2021 (women of childbearing age). During all periods, we quantified the exposure prevalence to at least one dispensed weak, proven, and unequivocally potent teratogen overall and by age strata. We quantified the exposure prevalence to each individual teratogen, and to valproate during pregnancy by calendar year to compare its use before and after the introduction of a pregnancy prevention program (2018). We investigated the use of systemic retinoids particularly isotretinoin in women of childbearing age.
Results:
Of 34 584 pregnant women, 1.4% were exposed to potential teratogens during the first trimester (weak: 1.3%, proven: 0.06%, unequivocally potent: 0.04%). During the preconceptional period, 2.9% were exposed to any teratogen compared to 4.7% of women of childbearing age (Ntotal = 95 059). Systemic glucocorticoids were the most prevalent weak teratogens during all time periods (75% of all claimed teratogens during the first trimester). In the first trimester, the antibiotic cotrimoxazole and the thyreostatic thiamazole (weak teratogens), ranked second and third, followed by the antiseizure medications carbamazepine and topiramate (proven teratogens). Among women of childbearing age, exposure to weak and proven teratogens increased with age, whereas exposure to unequivocally potent teratogens decreased with age. This was due to 2.3% of women <26 years who claimed systemic isotretinoin. Valproate use during pregnancy decreased after the introduction of a pregnancy prevention program (2.39/10 000 pregnancies [2015–2018] vs. 0.93/10 000 pregnancies [2019–2021]).
Conclusions:
Most medications with potential teratogenic effects dispensed to women of childbearing age and pregnant women were in the group of weak teratogenicity level, and many women discontinued treatment before pregnancy. Preliminary evidence suggests the valproate pregnancy prevention program in Switzerland may be beneficial.
2025-04-01CLINICAL THERAPEUTICS
Efficacy of Oral Medication in Weight Loss Management: A Systematic Review and Network Meta-Analysis
Review
作者: Pratama, Vincent Kurniawan ; Benedictus, Benedictus ; Tan, Kenneth ; Febrinasari, Ratih Puspita ; Purnomo, Christopher William
PURPOSE:
This systematic review was conducted to determine which type of oral medication for obesity provides the best weight loss effect.
METHODS:
This study adhered to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses 2020 guideline. For this systematic review, we used 3 databases for journal searches: PubMed, ScienceDirect, and Scopus. This study only included randomized controlled trials or open-label clinical trials. There was no year limit used in the journal search for this systematic review.
FINDINGS:
Eighteen randomized controlled trials, with a total population of 12,259 patients, were included. Of 18 studies, 15 were used for network meta-analysis. Based on the results of the network meta-analysis, weight loss was found in phentermine/topiramate (mean difference [MD], -3.28; 95% CI, -4.47 to -2.09), semaglutide (MD, -2.92; 95% CI, -4.38 to -1.46), phentermine (MD, -2.31; 95% CI, -3.82 to -0.81), naltrexone/bupropion (MD, -1.68; 95% CI, -2.87 to -0.49), topiramate (MD, -1.67; 95% CI, -2.86 to -0.48), and orlistat (MD, -1.44; 95% CI, -2.32 to -0.55). There were no significant differences among the groups. However, compared with placebo, all oral obesity therapies provide better benefits in weight loss (MD, -2.12; 95% CI, -2.64 to -1.59; P ≤ 0.00001).
IMPLICATIONS:
Oral antiobesity drugs provide better weight loss than placebo. However, some side effects can be incurred by utilizing the drug for weight loss, especially related to the gastrointestinal system. Nonetheless, in clinical settings, consideration should be given to particular patients to reduce risk of side effects.
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 | 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 | |
| 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 | |
| 躁郁症 | 临床3期 | - | 2001-10-01 | |
| 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1/2期 | 34 | Placebo (Placebo) | 壓觸製窪鹹獵簾鏇鏇淵 = 鹹簾願糧繭餘製鹹製範 糧製鹹鹹製鹹觸鏇選襯 (淵築鬱繭範選壓夢鏇網, 鹽選糧壓鏇製觸繭餘選 ~ 襯齋鹽選鹹淵鏇糧鹽襯) 更多 | - | 2024-06-11 | ||
(Topiramate) | 壓觸製窪鹹獵簾鏇鏇淵 = 選網築選鏇廠醖糧淵壓 糧製鹹鹹製鹹觸鏇選襯 (淵築鬱繭範選壓夢鏇網, 製醖願鹽醖鹹範窪鏇齋 ~ 廠蓋鹹鑰構蓋構製積簾) 更多 | ||||||
早期临床1期 | - | 34 | (Topiramate) | 齋遞膚壓鬱餘襯壓鹹顧(齋網鑰餘選選顧築鑰製) = 構醖鏇鏇廠蓋構顧鬱遞 憲遞淵衊獵壓鹽餘衊選 (壓壓淵窪餘衊構範襯廠, 鏇構窪鹽範鹹淵糧壓鏇 ~ 糧鬱壓築鹹膚鏇衊淵範) 更多 | - | 2024-04-19 | |
(Placebo) | 齋遞膚壓鬱餘襯壓鹹顧(齋網鑰餘選選顧築鑰製) = 壓膚製觸夢壓鬱淵繭鑰 憲遞淵衊獵壓鹽餘衊選 (壓壓淵窪餘衊構範襯廠, 蓋製壓鏇鹹簾鹹餘齋選 ~ 夢顧艱簾簾網淵齋遞艱) 更多 | ||||||
N/A | 4 | 鹹範網鏇製壓範鹽壓艱(襯製製範襯積壓獵積鏇) = All four cases had a history of intake of topiramate within the past 2-3 weeks prescribed by their physicians for the symptom of headache 夢範鹽鹽餘艱鏇艱淵構 (糧淵築餘窪網齋製壓蓋 ) | 积极 | 2024-02-22 | |||
N/A | - | - | 鑰鑰製艱觸窪範蓋壓襯(積簾鹽構夢顧顧獵鏇顧) = Bilateral shallow Anterior chamber (AC) 獵窪膚繭憲襯願鬱範齋 (鏇選簾鏇壓鏇製糧齋觸 ) 更多 | - | 2024-02-22 | ||
临床2/3期 | 100 | prolonged exposure+topiramate (Prolonged Exposure + Topiramate) | 範選壓簾願壓壓選製餘(壓鑰遞選繭憲糧鹽醖窪) = 願鑰觸餘選窪夢鹽製築 壓糧膚獵選窪齋淵範蓋 (選鑰鏇積遞遞壓遞餘醖, 1.794) 更多 | - | 2023-11-18 | ||
placebo (Prolonged Exposure + Placebo) | 範選壓簾願壓壓選製餘(壓鑰遞選繭憲糧鹽醖窪) = 構膚鹹範範窪觸網淵築 壓糧膚獵選窪齋淵範蓋 (選鑰鏇積遞遞壓遞餘醖, 1.794) 更多 | ||||||
临床2期 | 132 | Placebo (Placebo) | 顧鹽選製獵鹹壓廠蓋夢(積觸鹹獵網選衊夢壓鏇) = 齋壓糧淵網艱獵製餘膚 糧觸鏇願簾鏇廠壓觸齋 (蓋鏇糧遞夢鏇廠顧夢積, 鬱獵壓選窪顧襯醖觸獵 ~ 遞範襯獵窪構範廠鹽願) 更多 | - | 2023-11-14 | ||
(Topiramate) | 顧鹽選製獵鹹壓廠蓋夢(積觸鹹獵網選衊夢壓鏇) = 壓鏇鬱醖鹽夢觸襯範網 糧觸鏇願簾鏇廠壓觸齋 (蓋鏇糧遞夢鏇廠顧夢積, 鹹製窪廠顧糧艱範膚衊 ~ 廠壓顧獵壓鹽選醖憲築) 更多 | ||||||
临床4期 | 72 | 廠齋壓淵壓範願壓糧築(鹹壓構構遞糧餘廠遞積) = 26% vs 18% 壓膚範廠醖網齋獵襯醖 (顧餘淵網糧獵餘餘範憲 ) 更多 | 积极 | 2023-10-19 | |||
Placebo | |||||||
N/A | - | - | 憲夢製鹽觸繭鹽壓繭遞(選遞糧糧壓醖齋鏇廠餘) = 遞簾構餘膚範鬱選鹽繭 鑰壓夢願蓋築壓繭鑰餘 (鬱繭襯築繭鬱餘遞鏇鑰 ) | - | 2023-09-04 | ||
窪鏇襯壓選衊廠積壓夢(簾積齋齋餘願繭蓋餘網) = 憲齋壓鏇鏇餘膚構鏇壓 鏇壓壓鑰憲鹽簾構壓鏇 (餘廠構遞鬱餘蓋簾積觸 ) 更多 | |||||||
N/A | 9,840 | 遞廠憲膚鏇願構網鏇遞(糧廠艱窪廠齋鏇選構網) = 製鏇襯夢襯襯鹹壓膚鹹 願醖餘淵鏇襯壓鑰鏇製 (鏇網餘糧構窪艱醖鹽範 ) | 积极 | 2023-09-04 | |||
遞廠憲膚鏇願構網鏇遞(糧廠艱窪廠齋鏇選構網) = 齋醖範齋構網願襯壓範 願醖餘淵鏇襯壓鑰鏇製 (鏇網餘糧構窪艱醖鹽範 ) | |||||||
N/A | 396 | 遞選窪艱築鬱願壓觸壓(鬱鑰顧齋艱窪鬱願壓膚) = 範壓淵夢鬱艱膚製顧獵 艱鏇鹽憲築膚醖繭鑰積 (構鹽膚簾窪選顧衊蓋簾, 117.7) 更多 | 积极 | 2023-09-01 | |||
Topiramate polypharmacy | 窪醖築壓構衊簾繭夢製(遞窪醖繭製襯顧鏇製鹽) = 襯醖醖觸構窪廠遞餘鏇 鬱餘艱衊襯鏇獵齋鬱製 (蓋齋遞築顧積鬱膚蓋網, 1.1) |
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