英文药名：Linzess（Linaclotide Tablets） 中文药名：利那洛肽片 生产厂家：安斯泰来制药 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 リナクロチドは、グアニル酸シクラーゼC受容体アゴニストであり、14個のアミノ酸残基からなる合成ペプチドである。化学名は以下のとおりである。 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 1. 薬理作用 (1) 鸟苷酸环化酶C（GC-C）受体亲和力 该产物在受体结合实验中显示出对人GC-C受体的高亲和力。 (2) GC-C受体刺激作用 该产物增加人结肠上皮细胞中的细胞内环GMP浓度。 (3) 对肠道分泌和肠道运输能力的作用 本品除促进大鼠和小鼠肠道分泌外，还能促进小肠输血能力。 (4) 对结肠痛觉过敏的作用 该药抑制由大鼠和小鼠的应激和结肠炎引起的结肠痛觉过敏。 2. 作用机序 这种药物的肠分泌和肠分泌促进作用和结肠痛觉过敏作用改善作用被认为有助于改善便秘型肠易激综合征中的排便异常和腹痛/腹部不适。 适应症 便秘型肠易激综合征 用法与用量 成年人，每日一餐前服用0.5毫克。此外，根据症状减至0.25毫克。 临床结果 在强制便秘型肠易激综合征相双盲，平行组比较测试和长期治疗研究之间III安慰剂对照为国内如下。 1.第三阶段安慰剂对照双盲平行组比较研究。 此药为0.5mg或安慰剂治疗12周，每天一次，结果在早餐前口服给药，在12周肠易激综合症的症状普遍改善反应率是两个主要终点，12周对于该药0.5mg组完全自然排便反应率，在安慰剂组之上观察到显着差异。（见“临床结果表”表1和表2） 2.长期学习 在完成III期安慰剂对照双盲平行组比较测试的受试者中，在早餐前一天给予0.5mg该药物，用于安慰剂对照的双重包括盲法平行组比较试验，口服52周。 该试剂的每周应答率是在施用164箱子中的肠易激综合征症状一般改善52周每周应答率和启动这种药物的给药后完全自然排便，随着时间的推移增加。 包装规格 100錠（10錠×10） 制造业销售 安斯泰来制药公司 提示：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：http://www.info.pmda.go.jp/go/pack/2399017F1020_1_02 Release of Lenzeth tablets 0.25 mg for treatment of constipation type irritable bowel syndrome - Astellas Constipation-type irritable bowel syndrome treatment for novel mechanism of action On March 22, 2017, linaclotide (a trade name Rinzess tablet 0.25 mg) for the treatment of constipation type irritable bowel syndrome was released. This product is approved for manufacture and sales on December 19, 2016 and is listed on the drug price on February 15. Administer 0.5 mg before meals once a day and reduce to 0.25 mg according to symptoms. Irritable bowel syndrome (IBS) is a functional gastrointestinal disease with no organic disease, abdominal pain or abdominal discomfort and bowel movement associated therewith persisting chronically or recurrently. According to the Rome IV criteria based on the shape of the feces, IBS is divided into four groups of constipation type IBS (IBS - C), diarrhea type IBS (IBS - D), mixed type IBS (IBS - M), and unclassifiable type IBS It is classified as subtype. Although IBS is not a fatal disease, the prevalence rate of IBS is as very high as 10 to 20%, and the quality of life is markedly reduced by the restriction of daily life due to symptoms. For this reason, early diagnosis and treatment of IBS is required. Treatment of IBS is to consider drug treatment in patients who do not have symptomatic improvement in parallel with improvement of lifestyle habits including eating habits. Examples of therapeutic agents include gastrointestinal function regulators such as trimebutine maleate (Selequinone et al.), Lactobacillus preparations (Miya BM et al.) As probiotics, polycarbophil calcium (Coronel, Polyflu, etc.) , Lubiprostone (Amitiza), a mucosal epithelial function-altering agent, and further clinically used salt laxatives such as magnesium oxide (Magmit et al.) Unless improvement is made in IBS-C. Linaclotide is a guanylate cyclase C (GC-C) receptor agonist consisting of 14 amino acids showing a novel mechanism of action different from existing drugs. By activating the GC - C receptor on the luminal surface of the intestinal tract, it increases the intracellular cGMP concentration and shows intestinal secretion promoting action, small intestine transporting ability promoting action, colonic hyperalgesia improving action. Efficacy and safety of linaclotide have been confirmed in a phase III placebo-controlled double-blind, parallel-group comparison study for domestic IBS-C patients and a long-term administration study thereafter (total 52 weeks) There. Overseas, until August 2016, it has been approved in six countries and regions around the world including the United States, the EU and others. When drugs are used, pay attention to the fact that 21.5% of adverse reactions including clinical laboratory test abnormalities are accepted from domestic clinical trials. The main side effect is diarrhea (13.0%), etc. Severe diarrhea is reported as a serious side effect.