部份中文利那洛肽处方资料（仅供参考）
商标名：Linzess Tablets
英文名：Linaclotide
中文名：利那洛肽片
生产商：安斯泰来制药
药品简介
近日，Linzess（linaclotide，利那洛肽）0.25mg片剂已获日本监管机构批准。用于慢性便秘（chronic constipation，CC）的治疗。成为治疗便秘型肠易激综合征(IBS-C)的首个处方药，并于2017年3月在日本上市。
リンゼス錠0.25mg
药物分类名称
鸟苷酸环化酶C受体激动剂
批准日期：2017年3月
商標名
Linzess Tablets 0.25mg
一般名
リナクロチド（Linaclotide）
本質
利那洛肽是一种鸟苷酸环化酶 C 受体激动剂，是一种由 14 个氨基酸残基组成的合成肽。 化学名称如下。
L-Cysteinyl-L-cysteinyl-L-α-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-L-tyrosine cyclic (1→6),(2→10),(5→13)-tris(disulfide)
構造式
分子式
C59H79N15O21S6
分子量
1526.74
性状
利那洛肽是一种白色粉末。易溶于二甲基亚砜，难溶于水和乙醇（99.5）。
操作注意事项
注意：
通过具有防潮和干燥功能的铝包装使片剂保持质量。取出平板电脑之前取出平板电脑，不要将其存储在未打包的状态或转移到另一个容器。
审批条件
制定药品风险管理计划并适当执行。
药效药理
作用机制
认为该药物的肠分泌和肠转运能力促进作用和大肠痛觉过敏改善作用有助于排便异常和腹痛/腹部不适的改善。
药理作用
鸟苷酸环化酶C(GC-C) 受体亲和力
该药物在受体结合实验（体外研究）中显示出对人GC-C受体的高亲和力。
GC-C受体刺激作用
该药物增加了人结肠上皮细胞中的细胞内环GMP浓度（体外研究）。
对肠道分泌和肠道运输能力的影响
这种药物促进大鼠和小鼠的肠道分泌和小肠转运能力。
对结直肠痛觉过敏的影响
这种药物可抑制大鼠和小鼠因压力和结肠炎引起的结直肠痛觉过敏。
适应症
○便秘型肠易激综合征
○慢性便秘（不包括器质性便秘）
用法与用量
利那洛肽的常用成人剂量为0.5mg，每日一次，饭前口服。根据症状，剂量可减至0.25mg。
包装
100錠（10錠×10）
制造业销售
安斯泰来制药公司
提携
Ironwood
注：以上中文资料不够完整，使用者以原处方资料为准。
完整说明书附件：
https://www.info.pmda.go.jp/go/pack/2399017F1020_1_06/
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The difference between "rinses tablets 0.25mg (linacclotide)" and Amiti-za, a sensitive bowel syndrome (IBS-C) Therapeutic Agent
On Friday, November 25, 2016, the pharmaceutical and Food Hygiene Council of the Ministry of Health, Labour and welfare will deliberate on the production approval of medicines for constipation-type irritable bowel syndrome(IBS-C)Therapeutics "linses tablets 0.25 mg".Report on Astellas ' rinses tablets [linasclotide]
Pharmacological action of linses tablets 0.25 mg The main function of the "linses tablets 0.25 mg" applied to constipation-type irritable bowel syndrome is to promote intestinal secretion and intestinal transport ability by binding to gc-c receptors expressed in intestinal mucosa epithelial cells.
In addition, the effect of improving visceral hyperalgesia has also been reported.
According to the results of phase III studies in Japan,the results of clinical trials of adult patients 500 cases of irritable bowel syndrome symptoms were administered orally for 12 weeks, while the improvement rate of the placebo administered group is 18%,
In the group taking 0.5 mg of linses tablets, there is data that the improvement of 34% has been confirmed.
The linses tablets 0.25 mg is a drug that is used in more than 30 countries around the world due to indications of constipation-type irritable bowel syndrome and chronic idiopathic constipation.
○ CG-C Receptor Expressing on intestinal epithelial cells which is the site of action of the linses tablets 0.25 mg The CG-C receptor acts as a receptor for transmitting information from the intestinal cavity to the intestinal tract (intracellular).
In vivo, hormones such as the endogenous hormone, ganiline-uloganiline, etc., as the signaling substance of the intestinal cavity side, work as ligands for cg-c receptors. When a ligand such as ganiline is bonded to the cg-c receptor, the intracellular cGMP concentration rises and the CFTR chloride channel and the unknown CA channel operate.
This causes the secretion of chloride ions and the influx of calcium ions, and the water molecules can be moved to the intestinal cavity with the ions. In addition to biological hormone substances, intestinal infections that induce diarrhea (such as toxin prokaryotic Escherichia coli and plague bacteria) release toxins (heat-resistant enterotoxin) is strong binding to cg-c receptor, It promotes chloride ion secretion in intestinal epithelial cells, which causes prolonged diarrhea.