印度艾曲博帕说明书，怎么吃？|艾曲博帕 Eltrombopag PROMACTA-印度药房网

【印度艾曲博帕说明书，怎么吃？】

【艾曲博帕药品特色】

艾曲波帕是一种促血小板生成素受体激动剂适用于治疗慢性免疫性血小板减少性紫癜患者的血小板减少，对皮质激素、免疫球蛋白或脾切除反应不佳的患者。艾曲波帕只应用于有ITP其血小板减少程度和临床情况增加出血风险的患者。

【艾曲博帕使用限制】

PROMACTA不适用于治疗骨髓增生异常综合征（MDS）患者。

与没有使用干扰素的直接作用抗病毒药物联合治疗慢性丙型肝炎感染的安全性和有效性尚未确定。

【艾曲博帕剂量和给药】

空腹服用（餐前1小时或餐后2小时）。

慢性ITP：对于大多数成人和儿童（6岁以上），每日一次以50mg开始，1至5岁儿科患者每日一次25mg。肝功能损害患者和一些东亚血统患者需要减少剂量。调整以维持血小板计数大于或等于50 x 10 9 / L。每天不要超过75毫克。

慢性丙型肝炎相关血小板减少症：起始 PROMACTA 25mg，每日一次，适用于所有患者。调整以达到启动抗病毒治疗所需的目标血小板计数。不要超过每日100毫克的剂量。

严重再生障碍性贫血：每日一次以50mg开始PROMACTA治疗大多数患者。调整以维持血小板计数大于50 x 10 9 / L。每天不要超过150毫克。

【艾曲博帕剂型包装】

片剂：12.5mg，25mg，50mg，75mg和100mg

口服悬液：25mg

【艾曲博帕警告和注意事项】

肝毒性：在治疗前和治疗期间监测肝功能。

死亡风险增加和骨髓增生异常综合征进展为急性髓系白血病。

血栓/血栓栓塞并发症：慢性肝病患者接受PROMACTA的门静脉血栓形成已有报道。定期监测血小板计数。

【艾曲博帕不良反应】

在成人ITP患者中，最常见的不良反应（大于或等于5％，大于安慰剂）为：恶心，腹泻，上呼吸道感染，呕吐，ALT升高，肌痛和尿路感染。

在ITP年龄≥1岁的儿科患者中，最常见的不良反应（大于或等于10％，大于安慰剂）为上呼吸道感染和鼻咽炎。

在慢性丙型肝炎相关血小板减少症患者中，最常见的不良反应（大于或等于10％，大于安慰剂）为：贫血，发热，疲劳，头痛，恶心，腹泻，食欲下降，流感样疾病，虚弱，失眠，咳嗽，瘙痒，寒战，肌痛，脱发和周围性水肿。

在严重再生障碍性贫血患者中，最常见的不良反应（大于或等于20％）为：恶心，乏力，咳嗽，腹泻和头痛。

【药物相互作用】

服用任何含有多价阳离子的药物或产品（如抗酸剂，富含钙的食物和矿物质补充剂）之前至少2小时或4小时服用PROMACTA。

【在特定人群中使用】

怀孕：根据动物数据，PROMACTA可能会对胎儿造成伤害。

护理母亲：应考虑PROMACTA对母亲的重要性，决定终止PROMACTA或护理。

艾曲博帕英文说明书

Eltrombopag uses

Eltrombopag is used for low platelet count due to ITP or HCV infection. It is used to treat low platelet count due to chronic immune (idiopathic) thrombocytopenic purpura (ITP) or chronic hepatitis C virus (HCV) infection. It’s also used to treat severe aplastic anemia.

How eltrombopag works

Eltrombopag is a thrombopoietin agonist. It works by stimulating the formation of new platelets in the blood. Platelets help to reduce or prevent bleeding.

Common side effects of eltrombopag

Nausea, Diarrhea, Upper respiratory tract infection, Vomiting, Increased liver enzymes, Muscle pain, Urinary tract infection

Eltrombopag

生物活性

产品描述	Eltrombopag, an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity, binds to and stimulates the platelet thrombopoietin receptor (TPO-R or CD110).
靶点活性	Thrombopoietin receptor,
体外活性	Eltrombopag demonstrates a half maximal effective concentration (EC50) of 0.27 μM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR). Eltrombopag activates the receptor by association with metal ions (i.e., Zn2+) and specific amino acids within the transmembrane and juxtamembrane domains of the TpoR. Eltrombopag (30 μM) results in activation of STAT5 in N2C-Tpo cells, as detected with an antiphospho-STAT5 antibody on Western blots. Eltrombopag stimulates proliferation after a 2-day incubation with an EC50 of 0.03 μM in a BrdU assay conducted in BAF3/hTpoR cells. Eltrombopag also induces differentiation of hematopoietic stem cells into committed megakaryocyte progenitor cells. Eltrombopag increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes in a dose-dependent manner with an EC50 of 0.1 μM. [1] Eltrombopag inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL.[2] Eltrombopag (20 μg/mL) leads to a decreased cell division rate, a block in G(1) phase of cell cycle, and increased differentiation in human and murine leukemia cells. Eltrombopag (5 μg/mL) shows clear signs of differentiation, significant changes in the organization of the nuclear contents, and an increase in the cytoplasm/nucleus ratio in HL60 cells. Eltrombopag (5 μg/mL) causes an increase in CD11b, which is consistent with a premacrophage state in U937 cells, and also causes an increase in CD11b in URE cells. Eltrombopag leads to a reduction in free intracellular iron in leukemic cells in a dose-dependent manner in HL60 cells. [3]
体内活性	Eltrombopag (10 mg/kg per day) increases platelet counts over twofold approximately 1 week after the last dose for one chimpanzee and approximately 1.5-fold for the other two chimpanzees. [1] Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia. [3]

化学信息

分子量	442.47
分子式	C25H22N4O4
CAS	496775-61-2
溶解度	DMSO: 25 mg/mL (56.5 mM) Ethanol: <1 mg/mL Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )
储存条件	store at -80°C
备注	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.