英文药名:Adempas(Riociguat Tablets)
中文药名:利奥西呱片
生产厂家:拜耳药品
アデムパス錠0.5mg/アデムパス錠1.0mg/アデムパス錠2.5mg
治疗类别名称 可溶性鸟苷酸环化酶(SGC)刺激剤 批准日期:2014年4月 商標名 Adempas tablets 0.5mg Adempas tablets 1mg Adempas tablets 2mg 構造式
一般名 リオシグアト(Riociguat)JAN (riociguat)INN 化学名 Methyl N-(4,6-diamino-2-{1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl}pyrimidin-5-yl)-N-methylcarbamate 分子式 C20H19FN8O2 分子量 422.42 性状 该产品是白色至淡黄色粉末。 产物N,N-二甲基甲酰胺或易溶于二甲亚砜,乙腈或乙醇(99.5)非常微溶,并且实际上不溶于水。 条件批准 *对药品风险管理计划的发展,要正确实施。 <手术治疗失调或手术残留或复发治疗慢性血栓栓塞性肺动脉高血压后> 由于在日本审判的情况下是非常有限的,上市后,直到一定数量的情况下的数据集成,通过实现对一切案件的使用效果调查,药物掌握使用患者数据采集初期这种药物的安全性和有效性的背景信息,采取措施以获得正确使用药物。 <肺动脉高压> 由于在日本审判的情况下是非常有限的,上市后,直到一定数量的情况下的数据集成,通过实现对一切案件的使用效果调查,药物掌握使用患者数据采集初期这种药物的安全性和有效性的背景信息,采取措施以获得正确使用药物。 药效药理 1. 作用机序 通过作用的两种机制的内源性刺激作用和NO无关的方式直接的sGC致敏可溶性鸟苷酸环化酶(sGC的)为一氧化氮(NO),环磷酸鸟苷(cGMP)的促进生产。 2. 肺动脉高压模型的作用 在缺氧诱发的肺动脉高压的小鼠模型和野百合碱诱发的肺动脉高压的大鼠模型中,在升高的口服给药右心室收缩压,抑制右心室肥大和肺血管重构。 适应症 ●手术治疗失调或手术残留或复发的慢性血栓栓塞性肺动脉高血压的治疗后 ●肺动脉高压 用法与用量 ●剂量调整周期 成人:开始一次1.0Mg1_nichi口服三倍Riociguat。当连续收缩压2周不表现出上述95mmHg低血压的症状,虽然在2周的时间间隔的单一剂量,以0.5毫克增加,最高剂量为至多一个2.5Mg1_nichi3次。如果收缩压显示低于95mmHg没有低血压的症状是保持当前的剂量,以指示低血压的症状,由0.5毫克的重量损失1个剂量。 ●剂量维持阶段 维持剂量是确定的滴定期间。即使在剂量维持阶段,最高剂量为0.5毫克做一次2.5Mg1_nichi3次,如所示低血压的症状,在没有耐受性,重量损失一个剂量。 包装规格 片剂 0.5mg:PTP包装100片(10片×10) 1.0mg:PTP包装100片(10片×10) 2.5mg:PTP包装100片(10片×10)
制造厂商 拜耳药品有限公司 国外批准日期(最新) 0.5mg 22015年5月 1.0mg 22015年5月 2.5mg 22015年5月 国际最初批准日期 0.5mg 2013年5月9日 1.0mg 2013年5月9日 2.5mg 2013年5月9日
完整处方资料附件:http://www.info.pmda.go.jp/go/pack/2190034F1027_1_04/ Bayer Yakuhin, CTEPH therapeutic agent "Adempas tablet" Riosocuato: sGC stimulant effective for chronic thromboembolic pulmonary hypertension On January 17, 2014, Rio Siguato (trade name: Adempas tablet 0.5 mg, same tablet 1.0 mg, same tablet 2.5 mg) for chronic thromboembolic pulmonary hypertension treatment approval was obtained. Adaptation is "chronic thromboembolic pulmonary hypertension which remained/relapsed after surgical treatment disorder or surgical treatment", and 1 to 2.5 mg once a day is administered orally three times a day. Chronic thromboembolic pulmonary hypertension (CTEPH) is a type of pulmonary hypertension (PH), a progressive and lethal disease. It is believed that pulmonary artery pressure rises gradually due to thrombus generated in the pulmonary blood vessel, resulting in right heart failure. In some cases, acute pulmonary thromboembolism changes to CTEPH, but the pathogenesis mechanism has not been fully elucidated. In PH, stimulation of soluble guanylate cyclase (sGC) is insufficient due to endothelial dysfunction and synthesis disorder of nitric oxide (NO). SGC is an enzyme found in the cardiopulmonary system and is a receptor for nitric oxide (NO). It is known that sGC binds to NO, thereby promoting the synthesis of cyclic guanosine monophosphate (cGMP) by sGC (NO-sGC-cGMP pathway). CGMP plays an important role in regulating vasodilatation, proliferation, fibrosis, and inflammation. So far, in the treatment of CTEPH, "Pulmonary Arterial Thrombus Endomyectomy" (PEA) which surgically removes thrombus and scar tissue from pulmonary blood vessels has been standardized. However, 20 to 40% of patients with CTEPH are said to be unoperable, and in some patients (up to 35%) the PH persists or recurs after PEA. From these facts, development and approval of effective therapeutic agents for CTEPH were required. Riosocuart is the world's first drug with a novel mechanism of action called sGC stimulant. It stimulates sGC and restores the NO-sGC-GMP pathway to cope with NO deficiency, resulting in improved cGMP production. Rio Siguato has been confirmed to be effective against CTEPH in which surgical maladaptation or persistence/recurrence was observed in clinical trials such as international joint examinations. Overseas, it is approved in the United States (adaptive: CTEPH and pulmonary arterial hypertension of pulmonary artery) in October 2013, Canada (adaptive: CTEPH) in September of the same year and Switzerland (adaptive: CTEPH) in the same year, In the EU, we are applying for production approval. When using Rio Siguato, it is necessary to consider necessity of administration with reference to treatment guidelines in advance. Also, it is necessary to pay close attention to 62.0% of adverse reactions (including clinical laboratory test abnormalities) are recognized in clinical trial until approval. The main side effects are headache (19.0%), indigestion (14.7%), floating dizziness (13.3%), hypotension (8.8%) etc .; serious side effects include hemoptysis (0.2%), pulmonary hemorrhage Notice the frequency unknown). ------------------------------------------------------- 产地国家: 日本 原产地英文商品名: Adempas 0.5mg 100Tablets 原产地英文药品名: Riociquat 中文参考商品译名: Adempas 0.5毫克 100片/盒 中文参考药品译名: 利奥西呱 生产厂家中文参考译名: 拜尔 生产厂家英文名: Bayer ------------------------------------------------------- 产地国家: 日本 原产地英文商品名: Adempas 1mg 100Tablets 原产地英文药品名: Riociquat 中文参考商品译名: Adempas 1毫克 100片/盒 中文参考药品译名: 利奥西呱 生产厂家中文参考译名: 拜尔 生产厂家英文名: Bayer ------------------------------------------------------- 产地国家: 日本 原产地英文商品名: Adempas 2.5mg 100Tablets 原产地英文药品名: Riociquat 中文参考商品译名: Adempas 2.5毫克 100片/盒 中文参考药品译名: 利奥西呱 生产厂家中文参考译名: 拜尔 生产厂家英文名: Bayer
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