作用机制

艾曲波帕是一种口服生物可利用的，小分子的TPO受体激动剂，其与人TPO受体的跨膜结构域相互作用，并启动信号级联诱导细胞增殖和分化的骨髓祖细胞。

适应症和用法

PROMACTA是用于治疗所表示的血小板生成素受体激动剂：

血小板减少症在成人和儿童患者6年以上有慢性免疫（特发性）血小板减少症（ITP）谁曾不充分响应糖皮质激素，免疫球蛋白，或脾切除术。 

血小板减少症患者的慢性丙型肝炎，以允许干扰素为基础的治疗的起始和维持。 

例重症再生障碍性贫血谁曾不充分反应免疫抑制治疗。

使用限制：

PROMACTA应仅用于ITP患者的血小板减少症的程度和临床病症增加出血风险。

PROMACTA应仅用于治疗慢性丙型肝炎的血小板减少症的程度防止干扰素为基础的治疗开始或限制，以保持干扰素为基础的治疗的能力。

安全性和有效性尚未确定结合使用而不干扰素治疗的慢性丙型肝炎感染的直接作用的抗病毒剂。 

重型再生障碍性贫血：每天对大多数患者一旦启动PROMACTA在50毫克。减少患者的肝功能损害或东亚血统的患者初始剂量。调整以维持血小板计数大于50×10 9 /L。不要超过每天150毫克。

肝损伤：减少患者withchronic ITP和肝功能损害的初始剂量。 

剂型和规格

禁忌

无。 

警告和注意事项

肝毒性：之前和治疗期间监测肝功能。 

血栓/血栓栓塞性并发症：门静脉血栓形成有报道在慢性肝病患者接受PROMACTA。定期监测血小板计数。 

不良反应

在成年ITP患者中，最常见的不良反应（大于或等于5％和大于安慰剂）分别为：恶心，腹泻，上呼吸道感染，呕吐，ALT升高，肌肉痛，和泌尿道感染。 

在儿科患者年龄6岁及以上的ITP，最常见的不良反应（大于或等于10％和高于安慰剂）是上呼吸道感染，鼻咽炎，和鼻炎。 

在慢性丙型肝炎相关的血小板减少症中，最常见的不良反应（比安慰剂大于或等于10％和更高）分别为：贫血，发热，疲劳，头痛，恶心，腹泻，食欲降低，流感样疾病，乏力，失眠，咳嗽，皮肤瘙痒，寒战，肌肉痛，脱发和外周水肿。 （

重症患者再生障碍性贫血，最常见的不良反应（大于或等于20％）为：恶心，疲劳，咳嗽，腹泻，和头痛。 

药物相互作用

PROMACTA不能在4个小时的任何药物或含有多价阳离子如抗酸剂，钙丰富的食物，和矿物质补充剂产品内拍摄。

特殊人群中使用

?妊娠：根据动物实验数据，PROMACTA可能对胎儿造成伤害。

?哺乳母亲：应做出决定停止PROMACTA或哺乳，考虑到PROMACTA的重视母亲。

储存

在储存在20°C至25°C（68°F至77°F）的室温;允许15°C至30°C（59°F至86°F），游览[见USP控制室温。如果存在的话，不要取出干燥剂。

トロンボポエチン受容体に作用し、骨髄前駆細胞から巨核球系への細胞増殖ならびに分化誘導を促進させることで、血小板数を増加させます。
通常、待機的な観血的手技を予定している慢性肝疾患患者における血小板減少症の改善に用いられます。

以前に薬を使用して、かゆみ、発疹などのアレルギー症状が出たことがある。肝機能障害がある。

妊娠または授乳中

他に薬などを使っている（お互いに作用を強めたり、弱めたりする可能性もありますので、他に使用中の一般用医薬品や食品も含めて注意してください）。

通常、成人は1回1錠（主成分として3mg）を1日1回、7日間服用します。この薬は手術予定日の8～13日前から服用を開始します。必ず指示された服用方法に従ってください。

服用期間中から服用後にかけて血小板数の測定が行われますので、指示された通りに受診してください。

飲み忘れた場合は、気がついたときすぐに飲んでください。ただし、次に飲む時間が近いときは、1回とばしてください。絶対に2回分を一度に飲んではいけません。

誤って多く飲んだ場合は医師または薬剤師に相談してください。

医師の指示なしに、自分の判断で飲むのを止めないでください。

主な副作用として、発熱、発疹などが報告されています。このような症状に気づいたら、担当の医師または薬剤師に相談してください。

まれに下記のような症状があらわれ、[　]内に示した副作用の初期症状である可能性があります。
このような場合には、使用をやめて、すぐに医師の診療を受けてください。

・激しい腹痛、吐き気、嘔吐 [血栓症]

以上の副作用はすべてを記載したものではありません。上記以外でも気になる症状が出た場合は、医師または薬剤師に相談してください。

乳幼児、小児の手の届かないところで、直射日光、湿気を避けて室温（1～30℃）で保管してください。

薬が残った場合、保管しないで廃棄してください。

更新日付：2015年12月01日

机器翻译

它作用于血小板生成素受体，通过促进细胞增殖，诱导来自骨髓祖细胞分化成巨核细胞和血小板增加的数量。

它通常被用来改善择期有创操作慢性肝病患者的血小板减少症。

请务必在人们面前，告诉你的医生和药剂师，如使用以下。

使用药物，止痒之前，有时不得不任何不寻常或过敏反应症状，如皮疹。有肝功能障碍。

如果你是孕妇或哺乳。

正在使用，如其他药物（或加强相互的作用，所以也有可能弱化，请注意，包括非处方药品和食品中使用的除外）。

剂量和给药方法

通常情况下，成人每天一次1片（3毫克作为主要成分），将需要7天。这种药将开始从以前的8至13天的手术预定日期服用。请按照医生的指示。

由于血小板计数测量从同时服用期间拍完后，请访问遵医嘱。

如果你忘了喝，请注意的时候立即饮用。但是，如果它几乎是下一个剂量，请跳过一次。不要采取两种剂量一次绝对的。

请咨询你的医生或药剂师，如果你花了太多的错误。

如果没有医生的指导，请不要停止服用中药在自己的判断。

关于副作用

常见的副作用包括发热，皮疹等相继报道。如果您发现这样的症状，请咨询你的医生或主管药师。

在罕见的情况下出现的症状，如下文中，它可以是在方括号[]中指示的不利影响的初期症状。

在这种情况下，应停止使用，请立即就医。

- 剧烈腹痛，恶心，呕吐[血栓]

其他副作用没有说明所有。如果您发现上述以外关心的任何症状，请咨询你的医生或药剂师。

存储等

婴幼儿，儿童，阳光直射，接触不到的地方，以免水分请保持在室温（1〜30℃）。

如果您有任何遗留的药，请抛弃它。

Revolade

Active Substance: eltrombopag olamine 
Common Name: eltrombopag 
ATC Code: B02BX05
Marketing Authorisation Holder: Novartis Europharm Limited
Active Substance: eltrombopag olamine 
Status: Authorised
Authorisation Date: 2010-03-11
Therapeutic Area: Purpura, Thrombocytopenic, Idiopathic
Pharmacotherapeutic Group: Antihaemorrhagics

Therapeutic Indication

Revolade is indicated for chronic immune (idiopathic) thrombocytopenic purpura (ITP) patients aged 1 year and above who are refractory to other treatments (e.g. corticosteroids, immunoglobulins) (see sections 4.2 and 5.1).

Revolade is indicated in adult patients with chronic hepatitis C virus (HCV) infection for the treatment of thrombocytopenia, where the degree of thrombocytopenia is the main factor preventing the initiation or limiting the ability to maintain optimal interferon-based therapy (see sections 4.4 and 5.1).

Revolade is indicated in adult patients with acquired severe aplastic anaemia (SAA) who were either refractory to prior immunosuppressive therapy or heavily pretreated and are unsuitable for haematopoietic stem cell transplantation (see section 5.1).

What is Revolade and what is it used for?

Revolade is a medicine that is used for the treatment of:

long-term immune (idiopathic) thrombocytopenic purpura (ITP), a disease in which the patient’s immune system destroys the platelets (components in the blood that help it to clot). Patients with ITP have low platelet counts in the blood (thrombocytopenia) and are at risk of bleeding. Revolade is used in patients aged 1 year and above who do not respond to treatment with medicines such as corticosteroids or immunoglobulins;thrombocytopenia in adult patients with chronic (long-term) hepatitis C, a disease of the liver caused by infection with the hepatitis C virus, when the severity of thrombocytopenia is preventing antiviral therapy;acquired severe aplastic anaemia (a disease in which the bone marrow does not make enough blood cells or platelets) in adult patients. Revolade is used in patients who did not respond to or had received multiple courses of immunosuppressive therapy (medicines that lower the body’s immune defences) and cannot receive haematopoietic (blood) stem cell transplantation.

Revolade contains the active substance eltrombopag.

How is Revolade used?

Revolade is available as tablets (12.5, 25, 50 and 75 mg) and as a powder (25 mg) to prepare a suspension (a liquid to be taken by mouth). The medicine can only be obtained with a prescription and treatment should be started and supervised by a doctor who has experience in treating blood diseases or chronic hepatitis C and its complications.

The dose depends on the patient’s age and the disease Revolade is being used to treat; it is adjusted as needed to maintain the appropriate platelet level. For ITP and aplastic anaemia, a lower starting dose may be needed in patients of East Asian descent (such as Chinese, Japanese, Korean or Taiwanese).

Patients should not take any antacids, dairy products or mineral supplements in the four hours before and in the two hours after taking Revolade. For more information, see the package leaflet.

How does Revolade work?

In the body, a hormone called ‘thrombopoietin’ stimulates the production of platelets by attaching to certain targets in the bone marrow. The active substance in Revolade, eltrombopag, attaches to and stimulates the same receptors as thrombopoietin. This leads to an increased production of platelets, improving platelet counts.

What benefits of Revolade have been shown in studies?

For the treatment of chronic ITP in adults, Revolade was compared with placebo (a dummy treatment) in two main studies involving a total of 311 patients who had previously been treated, but the treatments had not worked or the disease had come back.

Revolade was shown to be more effective than placebo: in the first study, 59% of the patients who took Revolade (43 out of 73) achieved a platelet count of at least 50,000 per microlitre (a platelet level considered adequate to prevent the risk of bleeding complications) after six weeks (the main measure of effectiveness), compared with 16% of those who took placebo (6 out of 37). In the second study, patients taking Revolade were around eight times more likely than those taking placebo to reach the target platelet count of between 50,000 and 400,000 per microlitre during the six months of treatment.

In children with chronic ITP, Revolade was shown to be more effective than placebo in one main study involving a total of 92 children between 1 and 17 years of age who had previously received treatment for ITP. This study lasted 13 weeks and looked at the proportion of patients whose platelet count had increased to at least 50,000 per microlitre for at least 6 out of 8 weeks, between week 5 to 12 of the study in the absence of rescue medication. This occurred in around 40% of those taking Revolade (25 out of 63) compared with around 3% (1 out of 29) of those who took placebo. The study had also an extension phase, in which all patients received Revolade. This showed that Revolade was also effective at maintaining adequate levels of platelets in the long term.

For the treatment of thrombocytopenia associated with hepatitis C, two main studies involving a total of 1,441 adults were carried out. These compared Revolade with placebo for allowing the starting and maintenance of antiviral treatment in patients with hepatitis C whose platelet count was initially too low to allow starting such treatment (less than 75,000 per microlitre). In both studies, the main measure of effectiveness was the number of patients whose blood tests did not show any sign of hepatitis C virus 6 months after the end of treatment.

In these two studies, a higher proportion of patients who took Revolade tested negative for hepatitis C, compared with those who took placebo (23% versus 14% in the first study, and 19% versus 13% in the second study).

For the treatment of severe aplastic anaemia, Revolade was studied in 43 patients and it was not compared with any other medicine. The main measure of effectiveness was the number of patients who responded to Revolade (whose platelet, red or white blood cell count remained above pre-set levels) after 12 or 16 weeks of treatment.

In this study, 40% of patients (17 out of 43) responded to treatment after 12 weeks, and 65% of responders (11 out of 17) either had a platelet count increase of at least 20,000 per microliter or had a platelet count that was stable without need for blood transfusions. Preliminary data from a supportive study are consistent with the result of the main study, with 46% of patients responding to treatment after 12 weeks.

What are the risks associated with Revolade?

The most common side effects with Revolade in adults with chronic ITP and hepatitis C (seen in more than 1 patient in 10) are headache, anaemia (low red blood cell counts), decreased appetite, insomnia (difficulty sleeping), cough, nausea (feeling sick), diarrhoea, pruritus (itching), alopecia (hair loss), myalgia (muscle pain), pyrexia (fever), fatigue (tiredness), influenza (flu)-like illness, asthenia (weakness), chills and peripheral oedema (swelling, especially of the ankles and feet). In addition, in children with ITP the most common side effects also included colds, nasopharyngitis (inflammation of the nose and throat), rhinitis (inflammation of the lining of the nose), pain in the belly or in the mouth and throat, toothache, rash, runny nose and abnormal blood levels of certain liver enzymes (AST).

In adults with severe aplastic anaemia the most common side effects included headache, dizziness, insomnia, cough, dyspnoea (difficulty breathing), pain in the belly or in the mouth and throat, nausea, diarrhoea, joint pain, muscle spasms, pain in limbs, fatigue, fever, ecchymosis (discoloration of the skin resulting from bleeding underneath), abnormal blood levels of certain liver enzymes and runny nose.

In patients with thrombocytopenia and advanced chronic hepatitis C who are treated with a medicine called interferon and Revolade liver problems and thromboembolic complications (problems with clots in blood vessels) are the most important serious side effects. In these patients Revolade should only be used if clinically indicated and patients should then be closely monitored. Bleeding can also come back after the medicine is stopped.

For the full list of restrictions and side effects with Revolade, see the package leaflet.

Why has Revolade been approved?

The European Medicines Agency decided that Revolade’s benefits are greater than its risks and recommended that it be given marketing authorisation.

What measures are being taken to ensure the safe and effective use of Revolade?

Recommendations and precautions to be followed by healthcare professionals and patients for the safe and effective use of Revolade have been included in the summary of product characteristics and the package leaflet.

Other information about Revolade

The European Commission granted a marketing authorisation valid throughout the European Union for Revolade on 11 March 2010.

For more information about treatment with Revolade, read the package leaflet (also part of the EPAR) or contact your doctor or pharmacist.

Source: European Medicines Agency