部份中文艾曲波帕处方资料（仅供参考） 英文药名：PROMACTA(eltrombopag) 中文药名: 艾曲波帕片剂/口服悬浮液 生产厂家: Glaxo Smith Kline 药品介绍 批准日期：2008年11月20日；公司：GlaxoSmithKline PROMACTA (艾曲波帕[eltrombopag]) 片剂, 用于口腔使用 PROMACTA (艾曲波帕[eltrombopag]) 口服悬浮液 美国初步批准: 2008 警告: 慢性丙型肝炎患者肝失代偿危险见完整的盒装警告的完整处方信息。 在慢性丙型肝炎患者中, PROMACTA 联合干扰素和利巴韦林可增加肝失代偿的风险。 最近的重大变化 慢性 itp:08/2015 患者血小板减少症的适应症及用法及治疗 重度再生障碍 anemia:08/2014 的适应症及使用及治疗 剂量和管理, 慢性免疫 (特发性) thrombocytopenia:08/2015 重度再生障碍 anemia的剂量与管理:08/2014 剂量和管理, administration:08/2015 作用机制 Eltrombopag 是一种口服生物可利用, 小分子 TPO 受体激动剂, 与人类 TPO 受体的跨膜领域相互作用, 并启动信号级联, 诱导骨髓祖细胞的增殖和细胞分化。 适应症和用法 PROMACTA 是一种血小板生成素受体激动剂表示为治疗: •thrombocytopenia 的成人和儿科患者1岁以上的慢性免疫 (特发性) 血小板减少 (ITP) 谁对皮质类固醇, 免疫球蛋白, 或脾切除反应不足。 •thrombocytopenia 慢性丙型肝炎患者, 允许启动和维持干扰素为主的治疗。 •patients 严重的再生障碍性贫血患者对免疫抑制治疗反应不足。 使用限制: •PROMACTA 应仅用于 ITP 患者, 其血小板减少程度和临床状况增加了出血的风险。 •PROMACTA 只应用于慢性丙型肝炎的患者, 其血小板减少程度阻止了干扰素治疗的启动, 或限制了维持干扰素治疗的能力。 •Safety 和疗效并没有与直接作用的抗病毒药物联合使用, 没有干扰素治疗慢性丙型肝炎感染。 剂量和管理 •Take 空腹 (饭后1小时或2小时后)。 •Chronic ITP: 每天为6岁以上的成人和儿科患者每日50毫克启动 PROMACTA, 每天25毫克为1岁至5岁的儿科患者。肝损害患者和东亚血统患者需要剂量减少。调整以保持血小板计数大于或等于50x 10 9/升。不要超过75毫克每天。 •Chronic 丙型肝炎相关血小板减少: 为所有患者每天启动 PROMACTA 25毫克。调整以达到启动抗病毒治疗所需的血小板计数指标。不要超过每日剂量的100毫克。 •Severe 再生障碍性贫血: 为大多数患者每天启动 PROMACTA 50毫克。减少肝脏损害患者或东亚血统患者的初始剂量。调整以保持血小板计数大于 50x109/升。不要超过150毫克每天。 剂型和强度 •Tablets: 12.5mg、25mg、50mg、75mg 和100mg •For 口服悬浮液: 25mg 禁忌 没有. 警告和预防措施 •Hepatotoxicity: 在治疗前后监测肝功能。 •Thrombotic/血栓栓塞并发症: 在接受 PROMACTA 的慢性肝病患者中, 门静脉血栓形成。定期监测血小板计数。 不良反应 •In 成人患者的 ITP, 最常见的不良反应 (大于或等于5% 和大于安慰剂) 是: 恶心, 腹泻, 上呼吸道感染, 呕吐, 增加 ALT, 肌痛, 和泌尿道感染。 •In 儿科患者年龄1岁, 与 ITP, 最常见的不良反应 (大于或等于10% 和大于安慰剂) 是上呼吸道感染, 和鼻咽炎。 •In 患者慢性丙型肝炎相关血小板减少, 最常见的不良反应 (大于或等于10% 和大于安慰剂) 是: 贫血, 发热, 疲劳, 头痛, 恶心, 腹泻, 食欲减退, 流感样疾病, 乏力, 失眠, 咳嗽, 瘙痒, 寒战, 肌痛, 脱发, 周围水肿。 •In 严重再生障碍性贫血患者, 最常见的不良反应 (大于或等于 20%) 是: 恶心, 疲劳, 咳嗽, 腹泻和头痛。 药物相互作用 服用 PROMACTA 至少2小时前或4小时后, 任何药物或产品含有多功能阳离子, 如抗酸剂, 富含钙的食品, 和矿物质补充剂。 在特定人群中使用 •Pregnancy: 根据动物资料, PROMACTA 可能会造成胎儿伤害。 •Nursing 母亲: 应作出决定停止 PROMACTA 或护理, 考虑到 PROMACTA 对母亲的重要性。 包装提供/存储和处理 片 ·12.5 毫克片剂是圆的, 凸透镜, 白色, 涂膜片 debossed 与 GS MZ1 和12.5 在一边和是可利用的在瓶 30: NDC 0007-4643-13。 ·25毫克片剂是圆的, 凸透镜, 橙色, 涂膜片 debossed 与 GS NX3 和25在一边和是可利用的在瓶 30: NDC 0007-4640-13。 ·50毫克片剂是圆的, 凸透镜, 蓝色, 涂膜片 debossed 与 GS UFU 和50在一边和是可利用的在瓶 30: NDC 0007-4641-13。 ·75毫克片剂是圆的, 凸透镜, 粉红色, 涂膜片 debossed 与 GS FFS 和75在一边, 是可利用的瓶 30: NDC 0007-4642-13。 ·100毫克片剂是圆的, 凸透镜, 绿色, 涂膜片 debossed 与 GS 1L5, 并可在瓶 30: NDC 0007-4646-13。本产品含有干燥剂。 室温贮存在20°c 和25°c 之间 (68°F 到 77°F);允许到30°c 的游览 (59°F 到 86°F) [参见 USP 控制室温]。如果存在, 请勿去除干燥剂。免除原来的瓶子。 口服悬浮液 25毫克口服悬浮液是一种红棕色到黄色粉末的单位剂量包, 共同包装在一个套件与 40 cc 重组容器, 口服剂量注射器, 和螺纹关闭与注射器端口能力。 每个套件 (NDC 0007-4515-27) 包含30个数据包: NDC 0007-4515-01。 室温贮存在20°c 和25°c 之间 (68°F 到 77°F);允许到30°c 的游览 (59°F 到 86°F) [参见 USP 控制室温]。重组后, 该产品应立即管理, 但可能被储存在20°c 和25°c 之间的最长时间30分钟 (68°F 到 77°F);允许到30°c 的游览 (59°F 到 86°F) [参见 USP 控制室温]。如果30分钟内不使用, 扔掉 (丢弃) 混合物。 患者咨询信息和药物见指南。 PROMACTA(eltrombopag) PROMACTA is indicated for the treatment of thrombocytopenia in patients with chronic immune (idiopathic) thrombocytopenia (ITP) who have had an insufficient response to corticosteroids, immunoglobulins, or splenectomy. Limitations of use: PROMACTA should not be used to normalize platelet counts. PROMACTA should be used only in patients with ITP whose degree of thrombocytopenia and clinical condition increase the risk for bleeding. Important Safety Information WARNING: RISK FOR HEPATIC DECOMPENSATION IN PATIENTS WITH CHRONIC HEPATITIS C In patients with chronic hepatitis C, PROMACTA in combination with interferon and ribavirin may increase the risk of hepatic decompensation. (See Section 5.1 of the full Prescribing Information for additional information). Hepatotoxicity: PROMACTA can cause liver enzyme elevations. Measure serum ALT, AST, and bilirubin prior to initiation of PROMACTA, every 2 weeks during the dose adjustment phase, and monthly following establishment of a stable dose. PROMACTA inhibits UGT1A1 and OATP1B1, which may lead to indirect hyperbilirubinemia. If bilirubin is elevated, perform fractionation. Evaluate abnormal serum liver tests with repeat testing within 3 to 5 days. If the abnormalities are confirmed, monitor serum liver tests weekly until resolved or stabilized. Discontinue PROMACTA if ALT levels increase to ≥3X upper limit of normal (ULN) in patients with normal liver function or ≥3X baseline in patients with pre-treatment elevations in transaminases and are: progressively increasing; or persistent for ≥4 weeks; or accompanied by increased direct bilirubin; or accompanied by clinical symptoms of liver injury or evidence for hepatic decompensation. If the potential benefit for reinitiating treatment with PROMACTA is considered to outweigh the risk for hepatotoxicity, then consider cautiously reintroducing PROMACTA and measure serum liver tests weekly during the dose adjustment phase. Hepatotoxicity may reoccur if PROMACTA is reinitiated. If liver tests abnormalities persist, worsen or recur, then permanently discontinue PROMACTA. Thrombotic/Thromboembolic Complications: Thrombotic/thromboembolic complications may result from increases in platelet counts with PROMACTA. Reported thrombotic/thromboembolic complications included both venous and arterial events and were observed at low and at normal platelet counts. Consider the potential for an increased risk of thromboembolism when administering PROMACTA to patients with known risk factors for thromboembolism. To minimize the risk for thrombotic/thromboembolic complications, do not use PROMACTA in an attempt to normalize platelet counts. Follow the dose adjustment guidelines to achieve and maintain target platelet counts. In 2 controlled clinical trials in patients with chronic hepatitis C and thrombocytopenia, 3% (31/955) treated with PROMACTA experienced a thrombotic event compared to 1% (5/484) on placebo. The majority of events were of the portal venous system (1% in patients treated with PROMACTA versus <1% for placebo). In a controlled trial in non-ITP thrombocytopenic patients with chronic liver disease undergoing elective invasive procedures (N=292), seven thrombotic complications (six patients) were reported within the group that received PROMACTA and three thrombotic complications (two patients) within the placebo group. All of the thrombotic complications reported in the group that received PROMACTA were portal vein thrombosis, with thrombotic complications occurring in five of the six patients at a platelet count above 200 x 109/L. PROMACTA is not indicated for the treatment of thrombocytopenia in patients with CLD in preparation for invasive procedures. Cataracts: In the 3 controlled clinical trials in chronic ITP, cataracts developed or worsened in 15 (7%) patients who received 50 mg PROMACTA daily and 8 (7%) placebo-group patients. In the extension trial, cataracts developed or worsened in 4% of patients who underwent ocular examination prior to therapy with PROMACTA. Cataracts were observed in toxicology studies of eltrombopag in rodents. Perform a baseline ocular examination prior to administration of PROMACTA and, during therapy with PROMACTA, regularly monitor patients for signs and symptoms of cataracts. Laboratory Monitoring: Monitor serum liver tests (see Hepatotoxicity section). During therapy with PROMACTA, assess complete blood counts (CBCs) with differentials, including platelet counts, weekly until a stable platelet count has been achieved. Monitor platelet counts monthly thereafter. Obtain CBCs with differentials, including platelet counts, weekly for at least 4 weeks following discontinuation of PROMACTA. Drug Interactions: PROMACTA must not be taken within 4 hours of any medications or products containing polyvalent cations such as antacids, dairy products, and mineral supplements. Adverse Reactions: The most common adverse reactions in 3 placebo-controlled clinical trials in chronic ITP patients (≥3% and greater than placebo) for PROMACTA versus placebo were: nausea (9% vs. 3%), diarrhea (9% vs. 7%), upper respiratory tract infection (7% vs. 6%), vomiting (6% vs. <1%), increased ALT (5% vs. 3%), myalgia (5% vs. 2%), urinary tract infection (5% vs. 3%), oropharyngeal pain (4% vs. 3%), increased AST (4% vs. 2%), pharyngitis (4% vs. 2%), back pain (3% vs. 2%), influenza (3% vs. 2%), paresthesia (3% vs. 2%), and rash (3% vs. 2%). FDA批准艾曲波帕(Promacta)用于治疗严重的再生障碍性贫血 美国食品和药物管理局（FDA）近日批准了一项补充新药艾曲波帕（葛兰素史克公司），用于治疗严重的再生障碍性贫血病人，该病人一般对免疫抑制剂疗法没有明显的反应。 艾曲波帕，是一种口服的促血小板生成素受体激动剂，可以诱导骨髓干细胞的增殖和分化，增加新生的血细胞。FDA之所以能批准该药，是基于国家心脏、肺和血液研究所进行的2期试验研究，包含43名患有严重再生障碍性贫血的病人，他们都至少对1次以上的免疫抑制剂疗法没有充足的治疗反应。 艾曲波帕最开始接受的剂量为50mg/天，为期2周，两周之后增加的最大剂量为150mg/天。首次结点是根据12周以后的血液缓解就行评估，如果在16周时还未发现血液缓解，则中止该治疗。然而，研究发现，在使用艾曲波帕药物以后，有40%的病人可在12周后检测到血小板、血细胞以及白细胞的血液缓解状态。 完整说明书附件： https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=616224ff-a925-4b38-9ca2-00fbf669380f