| 简介：
部份中文他替瑞林处方资料（仅供参考）
英文名：taltirelin hydrate
商品名：Ceredist Tablets
中文名：他替瑞林片
生产商：田边三菱制药
药品简介
Ceredist（Taltirelin，セレジスト錠，中文译名：他替瑞林）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。
セレジスト錠5mg
药效分类名称
脊髓小脑变性的口服治疗
批准日期：2012年6月
商標名
CEREDIST Tablets 5mg
一般名
タルチレリン水和物（taltirelin hydrate）
*化学名
N-［(4S)-1-Methyl-2,6-dioxohexahydropyrimidine-4-carbonyl］-L-histidyl-L-prolinamide tetrahydrate
分子式
C17H23N7O5・4H2O
分子量
477.47
構造式
性状
它是白色晶体或结晶性粉末。
溶于水，乙醇（99.5）或乙酸（100），微溶于甲醇。
溶于1mol/L盐酸测试溶液。
观察到晶体多态性。
药效药理
共济失调改善效果
（1）水飞石瑞林（1mg/kg，po）改善了遗传性共济失调小鼠Rolling Mouse Nagoya的跌倒指数（跌倒次数/自愿运动能力），同时也改善了脑干腹侧被盖区的跌倒指数。降低的脑葡萄糖代谢率增加到正常水平（3mg/kg，ip）。
（2）水合泰特列林（3mg/kg，p.o.）改善了3-乙酰吡啶共济失调大鼠的共济失调（行走速度，步长和行走角度）。兴奋性氨基酸拮抗剂消除了这种作用。
（3）在使用大鼠进行的毒性试验中，暂时性活动过度，震颤等（以药物功效为基础）以1.5mg/kg，p.o发生。
神经营养因子样作用。
Tartirelin的水合物为10-12M，以浓度依赖的方式刺激大鼠胚胎腹侧脊髓培养细胞中的神经突生长，并以2mg/kg/day的天数新生大鼠新生坐骨神经横断后诱导运动神经元变性，持续2周。通过反复腹膜内给药抑制了它。
垂体-甲状腺激素的刺激作用
口服给予2.75μmol/粒的酒石酸水合物可使雄性大鼠的血液TSH升高至对照组的5倍，直至给药后3小时。通过口服给予TRH 0.275μmol/体，观察到相似的TSH升高作用。
作用机理。
（1）在检查水合他替瑞林对各种受体和离子通道的亲和力时，显示仅对TRH受体具有亲和力。
（2）在研究水合他替瑞林对各种神经递质的释放和更新的作用时，分别通过腹膜内给药0.1mg/kg或更高和1mg/kg或更高的剂量来维持大鼠脑内乙酰胆碱和多巴胺的释放。发现它还促进神经递质的更新或合成。
临床药理学。
研究了健康成年人单次口服0.5-40mg的他替瑞林水合物的促甲状腺激素（TSH）分泌作用，并且每剂量5 mg或更高剂量的血液中促甲状腺激素（TSH）浓度呈剂量依赖性增加。此外，一次10 mg或以上时，观察到T3的显着增加。
适应症
改善脊髓小脑变性的共济失调
用法与用量
成人通常的剂量是5毫克他替瑞林水合物，每天饭后（早上和晚上）口服两次。
剂量可以根据年龄和症状进行调整。
临床结果
1.临床疗效
一项对427名脊髓小脑变性患者进行安慰剂对照长达一年的双盲比较研究显示，给药后28周，各种共济失调测试均无明显差异。 主要终点，总体改善和共济失调测试总体改善表明，该药物明显优于安慰剂。 另外，天青片给药组在28周后通过Kaplan-Meier法的累积恶化率是27.7％，安慰剂给药组是41.7％，差异是显着的。 服用后直至1年的总体改善（恶化率）的对数检验显示与安慰剂无差异。
2.老年人（65岁以上）的管理
使用超过65年的经验的96例患者中，有14例（14.6％），18例是副作用，主要的副作用是胃部不适，食欲不振，头晕，头晕和头痛。
包装
片
5毫克：
28片（14片x 2），
140片（14片x10）
制造商
田边三菱制药公司
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整说明资料附件：
https://www.info.pmda.go.jp/go/pack/1190014F1033_1_04/
CEREDIST Tablets 5mg（Taltirelin hydrate）
Brand name:CEREDIST Tablets 5mg
Active ingredient:Taltirelin hydrate
Dosage form:white tablet, diameter 7.0mm, thickness 3.0mm
Print on wrapping:セレジスト5, Ceredist5mg, TA137, セレジスト5mg
Effects of this medicine
This medicine activates neuronal cells through promoting the release and turnover of neurotransmitters(acetylcholine, dopamine)and its nerve growth factor-like action.
It is usually used to improve ataxia (daily activities such as gait, eating, and conversation) in spinocerebellar degeneration.
Before using this medicine, be sure to tell your doctor and pharmacist
・If you have previously experienced any allergic reactions(itch, rash, etc.)to any medicines.
・If you are pregnant or breastfeeding.
・If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines)
Dosing schedule(How to take this medicine)
・Your dosing schedule prescribed by your doctor is((to be written by a healthcare professional))
・In general, for adults, take 1 tablet(5mg of the active ingredient)at a time, twice a day after breakfast and dinner. The dosage may be adjusted according to age and the symptoms. Strictly follow the instructions.
・If you miss a dose, take a dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time.
・If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
・Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include nausea, vomiting, diarrhea, stomach discomfort, headache, dizziness, lightheadedness, and rash. If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
・spasms occur in local or whole body muscles [convulsion]
・fever (over 37.5 degrees Celsius), muscle stiffness, tremor of limbs [malignant syndrome]
・general malaise, loss of appetite, yellowing of the skin and whites of the eyes [hepatic dysfunction, jaundice]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
・Keep out of the reach of children. Store away from direct sunlight, heat and moisture.
・Discard the remainder. Do not store them.
Internal
Revised: 12/2016
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.
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