英文药名：REMITCH OD TABLETS（Nalfurafine Hydrochloride）

中文药名：盐酸纳呋拉啡口腔崩解片

生产厂家：鸟居药业

レミッチOD錠2.5μg

REMITCH口腔崩解片2.5μg（Nalfurafine Hydrochloride）由日本鸟居药业开发的新药。它是一种专为进行透析患者，慢性肝病患者提供的口服抗搔痒症高效药物
药物分类名称
口服瘙痒改善剂
批准日期：2017年6月
商標名
REMITCH OD TABLETS 2.5μg
一般名
ナルフラフィン塩酸塩　Nalfurafine Hydrochloride
化学名
（2E）-N-［（5R,6R）-17-（Cyclopropylmethyl）-4,5-epoxy-3,14-dihydroxymorphinan-6-yl］-3-（furan-3-yl）-N-methylprop-2-enamide monohydrochloride
3分子式
C28H32N2O5・HCl
分子量
513.03
構造式

性状
白色至淡黄色粉末。 吸湿性高，对光线稍微不稳定。 溶解度易溶于水和甲醇，难溶于乙醇（95），难溶于乙酸乙酯和乙醚。
分配系数
0.95 [1-辛醇/pH6.8缓冲溶液（Log D）中的分配系数]
操作注意事项
使用自动点胶机时，部分胶片可能会剥落，因此请注意盒子的位置。
审批条件
制定药品风险管理计划并适当执行。
药效药理
1.对瘙痒症采取作用
抗组胺药，现有的止痒剂，抑制有效的组胺皮内给药诱导的小鼠搔抓行为和P物质皮内给药诱导的物质搔抓行为，其中抗组胺药效果较差。
抗组胺药还能抑制小鼠脑池内诱导的小鼠搔抓行为，这是一种无效的中枢瘙痒模型。
2. 作用机序
从体外受体结合试验和使用人类阿片受体表达细胞的受体激动试验的结果来看，已经显示它是一种选择性阿片样物质κ受体激动剂。
见表14“人类阿片受体结合试验和可操作性试验结果”。
此外，体外试验不结合除含有组胺受体的阿片受体以外的各种受体，转运蛋白和离子通道，也显示对来自肥大细胞的脱粒反应没有抑制作用。 另外，P物质皮内给药诱导的P物质抑制作用，通过侧脑室给药阿片κ受体拮抗剂norbinaltorphine（nor-BNI）完全拮抗。
3. 依存性
由于在大鼠戒断症状观察中在吗啡中观察到不存在戒断症状的情况下贝伐珠单抗的物理依赖性较弱，所以在猴自我接受测试中没有观察到强化作用，因此精神依赖性 它被认为不是。
药理药理学表
表14人类阿片受体结合试验和功效试验结果

試験項目	κ	μ	δ	κ:μ:δ比
結合試験 Ki値（nmol/L）	0.244±0.0256	2.21±0.214	484±59.6	1：9：1980
作動性試験 EC50（nmol/L）	0.00816±0.00138	1.66±0.09	21.3±1.0	1：203：2610

（平均值±标准误差）
适应病症
下一个病人瘙痒的改善（只有在现有治疗效果不足的情况下）
透析患者，慢性肝病患者
用法与用量
成人，晚餐后或睡前口服盐酸萘拉芬盐酸盐每日2.5微克。 虽然可以根据症状增加，但每天一次限制在5μg。
包装规格
OD片
2.5μg：14PTP（14片×1），PTP 140片（14片×10）

制造商
鳥居薬品株式
提示：以上中文资料不够完整，使用者请以原处方为准。
完整说明书附件：http://www.info.pmda.go.jp/go/pack/1190015M1029_1_13/
Remediation ® OD tablet 2.5 μg "(orally disintegrating tablet) of pruritus amelioration agent
Announcement of drug price listing and new release in Japan
Toray Industries, Inc. (Headquarters: Chuo-ku, Tokyo; President: Akihiro Nisi, Toray "hereinafter) acquired Toray market approval for production and manufacture, Torii Pharmaceutical Co., Ltd. (Head office: Chuo-ku, Tokyo, President: Takagi Shoichiro, hereinafter "Torii drug") sells it as a pruritus ameliorating agent (limited to cases where efficacy is insufficient in existing treatments) in hemodialysis patients and patients with chronic liver disease in Japan (partnership: Japan Tobacco Inc. Promotion alliance of pruritus in patients with chronic liver disease with Dainippon Sumitomo Pharmaceutical Co., Ltd. (Headquarters: Osaka City, President: Masayo Tada, hereinafter "Dainippon Sumitomo Pharma"), head office: Tokyo, President: Today announced that "Remic ® ® OX tablets 2.5 μg" of orally disintegrating tablets ("OD tablets") acquired approval for manufacture and marketing on March 30, 2017 as a new dosage form of "Remitch ® capsule 2.5μg" In accordance with the fact that it was included in the drug price standard, in 2017 6 13 days since you started selling from (Tuesday), it will be announced.
Since "Remic о Ol tablets 2.5μg" listed in the drug price standards can be taken either with or without water, patients with swallowing functions such as the elderly who are declining or patients taking water intake It is expected that the convenience of patients needing restrictions will be improved and lead to improved compliance with medications.
Four companies are hoping that this drug can greatly contribute to treatment as a new option for the treatment of pruritus in hemodialysis patients and patients with chronic liver disease due to the addition of this dosage form.
The outline of "Remitch ® OD tablets 2.5μg" is as follows.
Sales name: Remitch ® OOD tablets 2.5μg
Common name: nalfurafine hydrochloride
Efficacy or effect: Improvement of pruritus in the following patients (only when the effect is insufficient in existing treatment)
Hemodialysis patients, chronic liver disease patients
Dosage and Dosage: Usually for adults, 2.5μg once daily as nalfurafine hydrochloride is administered orally after dinner or before going to bed. Although it can be increased according to symptoms, it is limited to 5μg once a day.
Manufacture and marketing approval date concerning additional dosage form: March 30, 2017
Drug price criteria Listed date: May 31, 2017
Release date: June 13, 2017
Manufacture and seller: Toray Industries, Inc.
About Remicro® Ol tablets 2.5 μg
Remich ® is the world's first selective opioid κ(kappa) receptor agonist created by Toray and Torii Pharmaceuticals has been selling in Japan in March 2009 as a pruritus ameliorating agent in hemodialysis patients I will. Because this drug suppresses itching by a mechanism different from antihistamine drugs and antiallergic drugs, it is expected to demonstrate effectiveness against itchy effectiveness with existing drugs, and it was developed. In addition, in May 2015, we approved partial change approval for manufacturing and marketing approval as pruritus ameliorating agent in patients with chronic liver disease, and we are promoting partnership with Dainippon Sumitomo Pharma for pruritus in patients with chronic liver disease.
Up to now, the dosage form was a soft capsule formulation, but by launching OD tablets that can be taken without water, patients with decreased swallowing function such as the elderly and patients requiring restriction of water intake amount We are working on the development of OD tablets because it can be expected to improve convenience.