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CEREDIST Tablets 5mg(他替瑞林片 セレジスト錠)
药店国别  
产地国家 日本 
处 方 药: 是 
所属类别 5毫克/片 140片/盒 
包装规格 5毫克/片 140片/盒 
计价单位: 盒 
生产厂家中文参考译名:
田边制药公司
生产厂家英文名:
Tanabe Mitubishi
该药品相关信息网址1:
http://www.info.pmda.go.jp/go/pack/1190014F1033_1_04
该药品相关信息网址2:
该药品相关信息网址3:
原产地英文商品名:
CEREDIST(セレジスト錠)5mg/tablet 140tablets/box
原产地英文药品名:
Taltirelin
中文参考商品译名:
CEREDIST(セレジスト錠) 5毫克/片 140片/盒
中文参考药品译名:
他替瑞林
曾用名:
简介:

 

 部份中文他替瑞林处方资料(仅供参考)
英文名:Taltirelin Tablets
商标名:CEREDIST,セレジスト錠
中文名:他替瑞林片
剂型:片
原研厂家:日本田边制药公司
药物分类名称
治疗口服脊髓小脑变性
适应症:
用于改善脊髓小脑变性病人的共济失调。
用法用量:
成人1日2次,1次1片,早晚饭后口服,可根据年龄、症状进行适当增减。
包装规格
片剂
5毫克:
28片(14片x 2),
140片(14粒×10)
制造商
三菱田边制药公司
注:以上中文资料不够完整,使用者以原资料为准。
完整说明书附件:http://www.info.pmda.go.jp/go/pack/1190014F1033_1_04/
产品介绍
他替瑞林(Taltirelin)是世界上第一个批准的口服促甲状腺素释放激素(TRH),除具有内分泌作用外,还可发挥一定的中枢神经系统(CNS)作用,包括提高运动活性,拮抗利舍平诱导的体温降低,以及拮抗戊巴比妥诱导的睡眠。该品种由日本田边制药公司开发,2000年7月在日本上市,用于改善脊髓小脑变性病人的共济失调。药理学研究显示本品经由脑TRH受体对CNS产生强而持久的多重作用。本品对CNS的兴奋作用比TRH强10~100倍,作用持续时间比TRH长约8倍。本品对TRH受体的亲和力约为TRH的1/11,因而本品的内分泌作用比TRH弱,但本品在体内比TRH稳定。另外,本品对促甲状腺素( TSH)释放的作用为TRH的1/6-1/11。
本品对中枢神经系统具有较强的作用,但同时其激素样作用较小,因此副作用较少。不良反应主要是消化系统反应,包括呕吐、恶心和胃不适。所有的不良反应均为轻中度,在治疗期间及(或)停药后消失 
CEREDIST Tablets(taltirelin hydrate)
Information on Taltirelin
Drug name: Taltirelin, TA-0910, Ceredist.
Chemical name: (S)-1-Methyl-4,5-dihydroorotyl-L-histidyl-L-prolinamide; (S)-N-[(1-Methyl-2,6-dioxohexahydropyrimidin-4-yl)carbonyl]-L-histidyl-L-prolinamide.
CAS Number: 103300-74-9.
Manufacturer:Tanabe Seiyaku (Orphan Drug), Tanabe Seiyaku (Originator).
Launched-2000.
Effects: Neurodegenerative Diseases, Treatment of, NEUROLOGIC DRUGS, TRH Analogs
side effects: 
The main side effects is the digestive system adverse reactions, including vomiting, nausea, and stomach discomfort. All the side effects were mild to moderate, during treatment and (or) stop.
Taltirelin (TA-0910), a synthetic thyrotropin-releasing hormone (TRH) analog, has been developed by Tanabe Seiyaku for the treatment of neurodegenerative diseases. An NDA was filed in Japan in April 1999 for the treatment of spinocerebellar degeneration (SCD) and was approved in July 2000; the drug was launched in Japan in September 2000 .
It is the first orally administered drug for this indication. In order to determine whether acute tolerance develops by taltirelin hydrate ((-)-N-[(S)-hexahydro-1-methyl-2,6-dioxo-4-pyrimidinylcarbonyl]-l-histidyl -l-prolinamide tetrahydrate; taltirelin), a thyrotropin-releasing hormone(TRH) analog, we examined the motor behavior, TRH receptors and dopamine D(2) receptors following 2 weeks treatment in rats.
Taltirelin selectively bound to TRH receptors and increased the spontaneous motor activity by a single administration, suggesting that the motor effect of taltirelin is mediated by TRH receptors. Following repeated treatment with TRH, there was a significant reduction in the increment of spontaneous motor activity.
In contrast, after repeated treatment with taltirelin at a dose that increased the motor activity to a similar extent to TRH by a single administration, there was no apparent change in its motor effect. In accord with the motor activity, we found a significant reduction in the H]methyl-TRH binding to TRH receptors in the brain following repeated treatment with TRH but not taltirelin.
However, the [H]spiperone binding to dopamine D receptors in the corpus striatum did not change by repeated taltirelin and TRH treatments.
Thus, the down-regulation of TRH receptors would be a main cause of the behavioral tolerance. These results suggest that taltirelin hardly develops the behavioral tolerance due to the lack of down-regulation of TRH receptors. 
 

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