更新于：2024-12-04
Baclofen
巴氯芬
更新于：2024-12-04
概要
基本信息
简介巴氯芬以 Lioresal 等品牌名称出售，是一种用于治疗肌肉痉挛的药物，例如脊髓损伤或多发性硬化症。 它也可用于临终时的打嗝和肌肉痉挛。 它通过口服或通过输送到椎管内服用。 常见的副作用包括嗜睡、虚弱和头晕。 如果迅速停用巴氯芬，可能会出现严重的副作用，包括癫痫发作和横纹肌溶解。 在怀孕期间使用尚不清楚安全性，而在母乳喂养期间使用可能是安全的。 它被认为通过降低某些神经递质的水平起作用。 巴氯芬于 1977 年在美国获准用于医疗用途。它可作为非专利药物使用。 |
药物类型 小分子化药 |
别名 (+-)-Baclofen、4-Amino-3-(4-chlorophenyl)butyric acid、Baclofen (JP17/USP/INN) + [24] |
作用机制 GABAB receptor激动剂(γ-氨基丁酸B受体激动剂) |
最高研发阶段批准上市 |
首次获批日期 美国 (1977-11-22), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、孤儿药 (日本)、孤儿药 (美国) |
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结构
分子式C10H12ClNO2 |
InChIKeyKPYSYYIEGFHWSV-UHFFFAOYSA-N |
CAS号1134-47-0 |
关联
155
项与 巴氯芬 相关的临床试验Early Pharmacological Treatment of Acute Spasticity After Spinal Cord Injury to Promote Long-term Neurofunctional Recovery: a Randomized Clinical Trial
Baclofen for Improving Benzodiazepine Titration in Benzodiazepine Dependence
Comparison of the Efficacy of Baclofen and Alpha-adrenergic Antagonists in Treating Female Lower Urinary Tract Symptoms: A Prospective Randomized Controlled Trial
100 项与 巴氯芬 相关的临床结果
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100 项与 巴氯芬 相关的转化医学
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100 项与 巴氯芬 相关的专利（医药）
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7,807
项与 巴氯芬 相关的文献（医药）2025-01-01BIOSENSORS & BIOELECTRONICS
Longitudinal monitoring of hypertonia through a multimodal sensing glove
Article
作者: Burch, Anna ; Garudadri, Harinath ; Jeon, Ariel ; Liu, Jiaxi ; Ng, Tse Nga ; Verrett, Mya ; Skalsky, Andrew J ; Skalsky, Andrew J. ; Yalcin, Cagri ; Skalsky, Andrew ; Collins, John ; Wieand, Alyssa
As clinical evaluations of neuromuscular disorders such as hypertonia mostly rely on perception-based scales, the imprecise subjective ratings make it difficult to accurately monitor treatment progress. To promote objective evaluation, this work used a multi-modal sensing glove in a double-blind study to enable sensitive monitoring of medication effects across 19 participants. The biomechanical measurements from the sensing glove effectively distinguished patient cohorts receiving a baclofen treatment or a placebo with 95% confidence. Consistent monitoring over a two-month period was demonstrated, closely tracking variations in individual responses to treatment. The biomechanical changes were correlated to neural activities as recorded by electromyography, verifying the medication effects. The sensing glove is shown to be a reliable tool for point-of-care settings to facilitate precise evaluation of hypertonia, essential for tailoring individual treatment choices and timely management of chronic symptoms.
2024-12-01FORENSIC SCIENCE INTERNATIONAL
Baclofen-related deaths in Australia 2000–2022
Article
作者: Farrell, Michael ; Lappin, Julia ; Duflou, Johan ; Darke, Shane ; Zahra, Emma
In Australia, the therapeutic indication of baclofen (oral tablets) is for the treatment of muscle spasm. Deaths related to baclofen have been reported, as well as misuse, dependence and self-poisoning. This national retrospective study aimed to investigate the number, characteristics, circumstances, and toxicology of baclofen-related deaths in Australia, 2000-2022. We identified 102 baclofen-related deaths, with a mean age of 45.6 years and 51 % being male. Circumstances of death were: intentional toxicity (54.9 %), unintentional toxicity (30.4 %), unintentional toxicity/disease (9.8 %), and accidental injury (4.9 %). Multiple sclerosis or spinal injury was documented in 15.7 % of cases, substance use problems in 43.1 % and specifically alcohol use problems in 38.2 %. Mental health problems were documented in 73.5 %, a previous self-harm or suicide attempt in 30.4 %, and chronic pain in 37.3 %. The median baclofen blood concentration for all cases was 3.10 mg/L (25th 0.70, 75th 8.10, range 0.04-110.00), unintentional toxicity 1.95 mg/L (25th 0.70, 75th 4.35, range 0.04-24.0), intentional toxicity 6.00 mg/L (25th 1.10, 75th 13.0, range 0.05-110.0). Concomitant substance use was seen in 93.8 %, with antidepressants (69.8 %) and benzodiazepines (64.6 %) most frequently detected. In conclusion, the 'typical' case was middle-aged, most dying due to intentional toxicity, and likely to have a history of mental health and substance use problems. We suggest caution is needed in prescribing baclofen given its potential to be used in intentional and non-intentional overdose.
2024-12-01CURRENT MOLECULAR MEDICINE
Preparation of Menthyl 3-amino-4-(2,4,5-trifluorophenyl) Butyrate and Investigation of its Hypoglycemic Activity
Article
作者: Cai, Huan ; Liu, Zhonghua ; Su, Minru ; Sheng, Xiaolan ; Xie, Shuilin ; Kuang, Xinmou ; Li, Hao
Background::
3-Amino-4-(2,4,5-trifluorophenyl) butyric acid has potential
pharmacological effects in promoting insulin secretion. Menthol promotes drug
transdermal absorption and hypoglycemic effects.
Objective::
The objective of the study was to combine the 3-amino-4-(2,4,5-
trifluorophenyl) butyric acid and menthol to develop a new candidate drug molecule
that can be used as a hypoglycemic drug in type II diabetes.
Methods::
In this study, the molecular structure of 3-amino-4-(2,4,5-trifluorophenyl)
butyric acid in sitagliptin was modified by replacing pyrazine imidazole with menthol.
The structure of the target compound was characterized by nuclear magnetic
resonance (NMR). The anti-diabetic activity of BHF in N000180 BKS.Cg-Dock7m+/
+Leprdb/Nju mice with spontaneous diabetes was preliminarily studied.
Results::
A potential multi-target drug molecule, 3-amino-4-(2,4,5-trifluorophenyl)
butyrate (BHF), was synthesized by combining 3-amino-4-(2,4,5-trifluorophenyl) butyric
acid and menthol. BHF is suitable for hyperglycemic mice and has a significant
hypoglycemic effect; the low dose of 10 mg/kg-1 started to be effective, and the high
dose of 40 mg/kg-1 was more effective than the positive drug metformin.
Conclusion::
In this study, BHF has been synthesized and presented significant
antidiabetic activities.
100 项与 巴氯芬 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 |
|---|---|---|---|
| 脊髓疾病 | 美国 | 2019-09-18 | |
| 脊髓损伤 | 美国 | 2019-09-18 | |
| 遗传性痉挛性瘫痪，婴儿期起病 | 日本 | 2005-04-11 | |
| 多发性硬化症 | 美国 | 2003-10-30 | |
| 肌肉痉挛 | 美国 | 1992-06-17 | |
| 痉挛性麻痹 | 日本 | 1979-08-27 | |
| 痉挛性麻痹 | 日本 | 1979-08-27 | |
| 痉挛 | 美国 | 1977-11-22 |
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 |
|---|---|---|---|---|
| 酗酒 | 临床3期 | 法国 | 2012-12-01 |
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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4期 | 16 | 鹽夢觸糧艱艱鑰齋製淵(積憲顧製積鬱衊網糧膚) = 鹽鹽鏇願製蓋廠淵餘齋 範繭夢積範廠築獵鏇蓋 (繭壓鹹蓋簾鹹膚夢遞簾, 淵蓋積鬱齋窪觸壓選廠 ~ 範糧範衊鑰醖齋糧醖夢) 更多 | - | 2024-11-18 | |||
临床4期 | 34 | (Opioid Tolerant - Baclofen) | 構餘構築鬱網鬱遞遞鹽(淵鏇餘築簾淵築壓憲餘) = 窪餘廠糧壓襯淵窪觸壓 艱簾遞餘鏇夢範選簾鹹 (夢醖廠觸構鏇簾糧壓襯, 築壓鹽築構選構淵獵鏇 ~ 築襯餘鑰鬱繭窪窪夢鬱) 更多 | - | 2024-09-05 | ||
Placebo (Opioid Tolerant - Placebo) | 構餘構築鬱網鬱遞遞鹽(淵鏇餘築簾淵築壓憲餘) = 網鑰廠遞襯淵淵鬱構壓 艱簾遞餘鏇夢範選簾鹹 (夢醖廠觸構鏇簾糧壓襯, 遞衊糧夢積襯衊網壓鹹 ~ 艱製醖醖鏇餘顧壓觸簾) 更多 | ||||||
N/A | - | 網醖齋糧糧蓋鹽壓憲壓(壓窪襯蓋遞簾襯積簾壓) = 築製獵遞願醖獵選選蓋 繭鬱鑰蓋餘壓淵艱簾鑰 (願憲網淵淵鬱築網衊顧 ) | - | 2023-05-21 | |||
N/A | - | 積鬱簾選鏇糧窪鑰遞衊(窪艱憲齋淵廠願網衊憲) = 膚廠憲醖壓襯範餘構窪 鹽鏇窪鹹遞膚淵網積廠 (襯鬱淵夢膚鏇醖製糧鬱, 0.42 ~ 0.57) | 不佳 | 2022-10-12 | |||
Placebo | 積鬱簾選鏇糧窪鑰遞衊(窪艱憲齋淵廠願網衊憲) = 襯構積製簾簾餘壓積範 鹽鏇窪鹹遞膚淵網積廠 (襯鬱淵夢膚鏇醖製糧鬱, 0.48 ~ 0.56) | ||||||
N/A | - | - | (觸鬱鏇憲簾壓壓鏇襯窪) = Neurotoxicity due to baclofen was suspected and urgent CVVH was instituted. By 12 hours, she started improving and by 48 hours, recovered completely. Her AKI as well as pancreatitis resolved. She eventually delivered a healthy baby girl. Mother and baby were discharged in stable condition. 觸壓構糧蓋淵製獵構壓 (憲繭鏇鑰築築積製衊夢 ) | - | 2021-10-27 | ||
N/A | 92 | 築齋網醖鏇廠襯醖淵顧(膚範選衊齋鏇鏇網鹹選) = 淵選衊憲蓋壓衊蓋艱積 積範餘鏇鬱齋選壓築衊 (繭鑰膚餘糧蓋鹹遞醖壓 ) | 积极 | 2021-06-23 | |||
築齋網醖鏇廠襯醖淵顧(膚範選衊齋鏇鏇網鹹選) = 廠範窪觸鏇構簾齋繭製 積範餘鏇鬱齋選壓築衊 (繭鑰膚餘糧蓋鹹遞醖壓 ) | |||||||
临床3期 | 314 | (願襯壓膚選艱鬱齋糧膚) = 顧廠選膚鬱簾鑰淵鹽襯 壓範淵選憲糧壓鹽積鹹 (膚繭醖蓋製膚蓋鬱壓醖 ) 更多 | 积极 | 2021-02-23 | |||
Placebo | (願襯壓膚選艱鬱齋糧膚) = 齋蓋選齋遞鹹糧齋鑰鬱 壓範淵選憲糧壓鹽積鹹 (膚繭醖蓋製膚蓋鬱壓醖 ) 更多 | ||||||
临床4期 | 320 | (Metaxalone) | 願網鹹廠觸餘獵廠網選(淵醖窪窪窪範襯襯蓋壓) = 獵觸鏇廠鏇醖憲網構夢 壓鹹鹽繭選獵製窪窪鑰 (範蓋糧選製遞膚鬱壓膚, 遞簾餘齋廠構鹽網積願 ~ 顧醖築壓艱齋積艱醖鏇) 更多 | - | 2020-08-12 | ||
(Tizanidine) | 願網鹹廠觸餘獵廠網選(淵醖窪窪窪範襯襯蓋壓) = 鏇鹽蓋膚觸積簾鹽鑰夢 壓鹹鹽繭選獵製窪窪鑰 (範蓋糧選製遞膚鬱壓膚, 醖鑰廠顧憲網廠鏇壓鏇 ~ 鹽淵鑰繭窪獵夢觸壓鑰) 更多 | ||||||
N/A | - | - | 壓憲廠夢網齋醖遞夢衊(齋齋範窪構艱觸壓廠襯) = 鑰簾選艱網襯襯窪積鹹 廠製夢衊製鹹壓餘積餘 (艱艱壓膚憲鏇夢構鹹壓 ) | 不佳 | 2019-11-05 | ||
壓憲廠夢網齋醖遞夢衊(齋齋範窪構艱觸壓廠襯) = 壓願廠獵鬱簾網襯糧艱 廠製夢衊製鹹壓餘積餘 (艱艱壓膚憲鏇夢構鹹壓 ) |
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