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  药店国别: 英国药房
产地国家: 英国
所属类别: 神经系统药物->抗癫痫药物
处方药:处方药
包装规格: 50毫克/片 84片/盒
计价单位:
  点击放大  
生产厂家中文参考译名:
葛兰素史克
生产厂家英文名:
GSK
该药品相关信息网址1:
http://www.gsk.com/media/pressreleases/2011/2011-pressrelease-381864.htm
原产地英文商品名:
TROBALT 50mg/tab 84tabs/box
原产地英文药品名:
RETIGABINE
原产地英文化合物名称:
2-AMINO-4-(4-FLUORBENZYLAMINO)-1-ETHOXYCARBONYLAMINOBENZENE
中文参考商品译名:
TROBALT 50毫克/片 84片/盒
中文参考药品译名:
瑞替加滨
中文参考化合物名称:
2-氨基-4-(4-氟苄基氨基)-1-乙氧羰基氨基苯
原产地国家批准上市年份:
0000/00/00
英文适应病症1:
Epilepsy
临床试验期:
完成
中文适应病症参考翻译1:
癫痫
药品信息:

温馨提示:2011年3月29日,Potiga更名为Trobalt。

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 详细处方信息以本药内容附件PDF文件(201161619444017.pdf)的“原文Priscribing Information”为准
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部分中文瑞替加滨处方资料(仅供参考)

中文名称:瑞替加滨
 
中文别名:2-氨基-4-(4-氟苄基氨基)-1-乙氧羰基氨基苯 

英文名称:RETIGABINE

英文别名:2-AMINO-4-(4-FLUORBENZYLAMINO)-1-ETHOXYCARBONYLAMINOBENZENE; D2312; N-(2-Amino-4-(4-fluorobenzylamino)phenyl)carbamic Acid Ethyl Ester; D 23129; Retigabin; Ethyl [2-amino-4-[[(4-fluorophenyl)methyl]amino]phenyl]carbamate; RetigabineDiscontinued See: R189051; ethyl {2-amino-4-[(4-fluorobenzyl)amino]phenyl}carbamate
Retigabine(D-23129)为合成的氨基吡啶类似物,具强效抗惊厥活性。
 
药理作用
    在传统的MES(最大电休克惊厥) 试验中,给小鼠和大鼠腹腔注射retigabine后采用超大电流刺激, 本品表现出有效的抗惊厥作用, 其 ED50分别为9.3和5.1 mg·kg-1,且经口给予本品也可产生同样疗效,表明本品具良好的系统生物利用度。一系列的小鼠试验显示,本品还可有效拮抗化学诱导的癫痫发作,如可剂量依赖性地抑制皮下注射戊四氮和印防己病毒所致阵挛性惊厥, ED50分别为13.5和18.6 mg·kg-1;缓解侧脑室注射N 2甲基2 D-天冬氨酸(NMDA, 3μg/5μL或012 μg/5μL)所致强直性前肢伸展或阵挛性癫痫;但未见其对皮下注射荷包牡丹碱和士的宁达30 mg·kg-1诱导的癫痫发作产生拮抗作用。  
    常用的人类复杂性部分发作型癫痫预防模型——杏仁核电点燃局灶性癫痫大鼠模型试验显示,经口和腹腔注射给药后,本品能极为有效地产生剂量依赖性抗惊厥作用,即在低剂量[0.01(ip)和 0.1(po)mg·kg-1]下可显著增加后放电阈值,且在高剂量[2.5~5(ip)和10~15(po)mg·kg-1]下还会影响模型大鼠的其他癫痫发作参数,如发作的严重度和持续时程以及后放电时程;在015 mg·kg-1(ip) 剂量下可显著抑制杏仁核点燃性癫痫发作, 但 0.1和1 mg·kg-1(ip)剂量下无效。最初有关本品抗惊厥作用机制的研究显示,本品可阻断钠和钙电流,增强神经元细胞中GABA所诱导的电流。另有研究显示,本品可较其他对照化合物更有效地逆转4-氨基吡啶诱导海马脑片区过度兴奋和癫痫样放电的作用,并致海马脑片中新合成的GABA量增加。最新研究表明,本品为一种神经元钾通道开放剂和GABA增强剂,可降低神经元兴奋性。由此可见,本品的抗惊厥作用具有多重机制。而目前大多数抗癫痫药物均是作用于钠和钙通道或不同的GABA受体。  

药动学与毒性 
    在大鼠和犬中进行的药动学试验显示,由于缺乏广泛的首过效应, retigabine单剂量经口给药,即可达到较高的血药浓度和较低的血浆药物清除率,且在犬体内终末半衰期较长;大鼠间的药动学个体差异小;在犬体内,本品的血浆蛋白结合率较低,足以避免其与具高蛋白结合率药物发生相互作用。  
    在大鼠和犬实验中,未观察到本品具有任何急性和亚慢性毒性作用,也未见有遗传毒性作用。临床研究 在一项大规模的Ⅱ期临床试验中,受试患者被分成4组,分别接受retigabine 600、900和 1 200 mg·d-1及安慰剂的治疗。结果, 4组受试患者每月癫痫发作率中值分别减少23%、29%、35%及 13% ,可见本品两高剂量组的疗效明显高于安慰组。在73名部分发作型癫痫患者中进行的一项随机临床试验比较了本品3种给药方案的安全性:所有受试者最初均接受剂量为300 mg·d-1的本品治疗,随后治疗剂量逐渐递增至目标剂量1 200 mg·d-1 ,其中剂量快速递增组、中速递增组和慢速递增组分别于第 13、25和42天后达到目标剂量。结果,各组中因不良反应而退出治疗的受试者分别为43.5%、31.8% 和13.0%。  
    在另一项双盲、随机临床试验中, 399名顽固性部分发作型癫痫患者分别接受安慰剂和本品(200、 300或400 mg, tid)治疗,且均同时合用其他抗癫痫药物,结果总共有220名受试者完成试验,并参加了接下来的延长期开标记试验。在开标记试验中,受试者同时接受本品(300 mg, tid;随后剂量减少或增至最大剂量1 200 mg·d-1)和其他抗癫痫药物的联合治疗。到开标记试验结束时,与治疗前相比,受试者每月总的部分发作频次下降率中值为48.3%;在第3和6个月,主要因中枢神经系统不良反应而退出试验的受试者分别为8%和18%。  
    葛兰素史克/Valeant制药公司最近已在欧美递交了retigabine用于辅助治疗部分发作型癫痫的上市申请,该上市申请是基于两项关键性Ⅲ期临床试验。其中一项名为RESTORE 1 的试验涉及 306名顽固性部分发作型癫痫患者,受试者在使用一种其他抗癫痫药物的同时, 分别接受本品 (1 200 mg, tid)或安慰剂治疗;而另一项RESTORE 2试验中, 1 000多名受试患者在接受正常的抗癫痫药物治疗的同时,也分别服用本品600、900 mg或安慰剂。结果,两项试验均达到了其共同的主要终点考察指标预期,即本品受试患者28天总的部分与作频次减少28%~40%(安慰剂组为16%)以及疗效反应率(28天发作频次减少50%以上的受试者比例)达39%~47%(安慰剂组为19%);常见不良反应包括头晕、疲劳、精神恍惚、眩晕、震颤、协调性异常、复视、注意障碍、虚弱和视力模糊。  
    此外,目前本品用于治疗疱疹后神经痛的Ⅱ期临床试验也在进行中。

欧盟批准癫痫治疗药Trobalt (retigabine)上市
葛兰素史克声称它与Valeant制药公司合作开发的癫痫药物Trobalt已获得欧盟的上市许可。
Trobalt主要治疗成人癫痫的部分发作。此前,在人用医药产品委员会建议将Trobalt应用于已经使用其他疗法的病人后,此药才获得欧盟的批准。委员会向欧洲药品管理局提出了建议。
Trobalt又称瑞替加滨,而在美国它被称为ezogabine。美国食品和药物管理局曾在十二月时拒绝批准该药物,称它需要额外的非临床资料。

Valeant的新药Trobalt获欧盟当局正面评价
GlaxoSmithKline与Valeant PharmaceuticaLS International宣布,欧盟医药管理局(EMA)的人用药品委员会(CHMP)对於Trobalt (retigabine)的行销申请给予正面评价,作为治疗局部发作型癫痫的佐剂。

欧盟批准癫痫新药
英国GlaxoSmithKline和Valeant制药公司于 3月29日宣布,它们联合开发的Trobalt已经获得欧盟上市授权。
Trobalt用于成人癫痫部分发作。欧盟人用药品委员会推荐其用于正在使用其它抗癫痫药的患者。
Trobalt通用名为retigabine(瑞替加滨,INN,国际非专利药品名称)或ezogabine (依佐加滨,USAN,美国通用名)。去年12月美国FDA拒绝批准Trobalt,要求申报者提供补充资料。
本品主要的作用是作为钾离子通道开放剂,也就是说,通过激活大脑中电压门控钾通道。这种作用机制在抗癫痫药物中独树一帜,并有望用于其他神经疾病,包括偏头痛和神经性疼痛。一项评估其治疗带状疱疹后神经痛安全性和疗效II期临床试验正在进行中。

GSK and Valeant receive European authorisation for Trobalt (retigabine)
Issued:
Tuesday 29 March 2011, London UK & Mississauga, Ontario

GlaxoSmithKline (GSK) and Valeant Pharmaceuticals International, Inc. (NYSE & TSX: VRX) announced today that the European Commission has granted marketing authorisation for Trobalt™(retigabine) as an adjunctive (add-on) treatment of partial onset seizures (a form of epilepsy where a seizure begins in a specific area in one side of the brain), with or without secondary generalisation in adults aged 18 years and above with epilepsy.1

“The European authorisation of retigabine is very welcome as it will provide neurologists within Europe with a new therapeutic option for the management of appropriate patients with uncontrolled partial onset seizures,” said Dr Tony Hoos, Senior Vice President, European Medical Affairs, GSK. 

This European licence was supported by the results of the pivotal phase III studies RESTORE 1 and 2, and Study 205, a phase IIb study. The results of these three studies showed that more patients with partial onset seizures saw a reduction of 50% or more in seizure frequency compared to placebo, when a 600mg, 900mg or 1200mg dose of retigabine was added to their current anti-epileptic drug (AED) therapy.1 

In controlled clinical studies with retigabine, urinary retention occurred at a rate of 0.9 percent in patients receiving the drug compared to 0.5 percent on placebo. Across the phase II/III safety population there were four (0.3%) serious adverse events of urinary retention, three of which were known to have resulted in withdrawal. The EU prescribing information therefore recommends that retigabine is used with caution in patients at risk of urinary retention.1

Retigabine also caused a prolongation of the QT interval (electrical activity of the heart) when used at the highest dose in healthy volunteers in a thorough QT study. As a precaution, the EU prescribing information recommends that an ECG is recorded before the initiation of retigabine in patients who are taking any medication that may interfere with QT intervals or who may have congestive heart failure, ventricular hypertrophy, hypokalaemia or hypomagnesaemia and in patients initiating treatment who are 65 years of age and above.1

In the pivotal trials, the most frequently reported adverse events with the use of retigabine in combination with other AEDs (occurring in at least 5 percent of subjects and at least twice the placebo rate) were dizziness (23 percent), fatigue (15 percent), confusion (9 percent), vertigo (8 percent), tremor (8 percent), abnormal coordination (7 percent), double vision (7 percent), disturbance in attention (6 percent), memory impairment (6 percent), and visual blurring (5 percent). In addition, somnolence occurred in 22 percent of patients on retigabine compared to 12 percent on placebo.2-4  

Retigabine, referred to as ezogabine in the US and Canada, is being jointly developed by GSK and Valeant.

“We are very pleased to have reached such an important milestone in the development of retigabine,” said Susan Hall, PhD, Head of Research and Development at Valeant.  “There is a significant need for new AEDs and retigabine could potentially play an important role in the management of partial onset seizures in appropriate patients.”

This European authorisation represents the first licence for retigabine. Preliminary authorisation was granted by the Swiss Agency for Therapeutics Products in December 2010.  Applications for marketing authorisation have been submitted in six countries in addition to the EU.  In December 2010, GSK and Valeant announced receipt of a Complete Response letter from the U.S. Food and Drug Administration (FDA) for the New Drug Application for ezogabine, the US generic name for retigabine, and are working to submit a response to the FDA as soon as possible in 2011.

GlaxoSmithKline – one of the world’s leading research-based pharmaceutical and healthcare companies – is committed to improving the quality of human life by enabling people to do more, feel better and live longer. 

About Valeant Pharmaceuticals
Valeant Pharmaceuticals International, Inc. (NYSE/TSX: VRX) is a multinational specialty pharmaceutical company that develops, manufactures and markets a broad range of pharmaceutical products primarily in the areas of neurology, dermatology and branded generics. 

About Trobalt™(retigabine/ezogabine)
Trobalt™ has been developed by Valeant and GSK as an adjunctive treatment for epilepsy patients aged 18 years and above with partial-onset seizures. Retigabine is the non-proprietary name adopted by the International Non-proprietary Name for Pharmaceuticals Substances Program. In the US and Canada, ezogabine is the non-proprietary name adopted by the United States Adopted Name Council. GlaxoSmithKline and Valeant entered into an exclusive worldwide collaboration agreement for Trobalt™ in 2008.

About partial onset seizures in epilepsy
Epilepsy is a neurological condition that produces brief disturbances in the normal electrical signals of the brain5 Partial seizures, which begin in a specific area in one side of the brain, are the most common type of seizure experienced by adults with epilepsy.6

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 详细处方信息以本药内容附件PDF文件(201161619444017.pdf)的“原文Priscribing Information”为准
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