帕唑帕尼薄膜片Votrient tablets 400mg(Pazopanib)

药店国别:

产地国家:土耳其

处方药:

所属类别: 400毫克/片 60片/盒

包装规格: 400毫克/片 60片/盒

计价单位:

生产厂家中文参考译名:

生产厂家英文名:GLAXOSMITHKLINE

原产地英文商品名:VOTRIENT 400MG/TAB 60TABS/BOX

原产地英文药品名:

中文参考商品译名:VOTRIENT 400毫克/片 60片/盒

中文参考药品译名:盐酸帕唑帕尼

简介

部份中文帕唑帕尼处方资料(仅供参考)

商品名:VOTRIENT FILM-COATED

英文名:Pazopanib

中文名:帕唑帕尼膜衣錠

生产商:葛兰素史克、诺华制药

药理类別:抗癌药物

孕妇用药分级D级:在对照的人体研究试验中显示该药物对胚胎有不良影响,若此药能带来之效益远超过其它药物的使用,因此即使在其危险性的存在下,仍可接受此药物用于怀孕妇女上。

结构式:Pazopanib5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzolsulfonamide UpToDate UpToDate连接

药理作用

Pazopanib是一种多重酪胺酸酶抑制剂,作用目标包含血管内皮生长因子受主(vascular endothelial growth factor receptor)VEGFR-1、VEGFR -2、VEGFR -3,血小板衍生生长因子受主(platelet-derived growth factor receptor)PDGFR-α与-β,纤维母细胞生长因子受体(fibroblast growth factor receptor)FGFR-1与-3,细胞激素受主(cytokine receptor)(Kit),第二型介白素受主诱导T细胞激酶(interleukin-2 receptor inducible T-cell kinase)(Itk),白血球特定蛋白质酪胺酸酶(leukocyte-specific protein tyrosine kinase)(Lck),以及穿膜醣蛋白受主酪胺酸酶(transmembrane glycoprotein receptor tyrosine kinase)(c-Fms)。

体外试验发现,pazopanib可抑制VEGFR-2、Kit与PDGFR-β受主发生配体诱导的自体磷酸化。体内试验则显示,pazopanib可抑制小鼠肺部内由VEGF诱导的VEGFR-2磷酸化、小鼠的血管新生,以及小鼠体内人类肿瘤异体移植的生长。

适应症

晚期肾细胞癌之第一线治疗,或用于已接受细胞激素(cytokine)治疗失败之晚期肾细胞癌患者。

用法用量

VOTRIENT之建议剂量为一天一次,空腹时口服800 mg(至少于用餐前1小时或用餐后2小时。VOTRIENT之剂量不应超过800 mg。请勿压碎药锭,因为可能会增加吸收速率而影响全身暴露量。当漏服一剂时,如果与下次服药时间的间隔小于12个小时,请勿补服。

药动力学

吸收:口服pazopanib后达到最高血中浓度的时间中位数为2至4小时。每日剂量800 mg所得之几何平均AUC与Cmax分别为1,037 hr•μg/mL与58.1μg/mL(相当于132μM)。Pazopanib每日剂量超过800 mg时,AUC或Cmax并没有同时增加。服用单颗压碎的pazopanib 400 mg锭剂,相较于服用整颗完整的锭剂,会使AUC(0-72)增加46%,Cmax增加大约2倍,tmax则减少大约2小时。这些结果显示,锭剂压碎后服用会增加pazopanib的生体可用率与口服吸收速率。因此,为避免增加药物暴露量,VOTRIENT锭剂不应压碎服用。与食物并服会增加pazopanib的全身暴露量。Pazopanib与高脂或低脂食物并服,会使AUC与Cmax增加大约2倍。因此,pazopanib应于至少餐前1小时或餐后2小时服用。

分布:pazopanib与人体血浆蛋白结合比例超过99%。在10至100μg/mL之间,此结合比例不受浓度影响。体外试验结果显示pazopanib是P-醣蛋白(P-glycoprotein,P-gp)及乳癌阻抗蛋白质(breast cancer resistant protein,BCRP)的受质。

代谢:体外试验显示pazopanib主要由CYP3A4代谢,少部分由CYP1A2与CYP2C8。

排除:服用建议剂量800 mg pazopanib后,平均半衰期为30.9小时。主要是经由粪便排除,肾脏排除的部分仅占投予剂量的<4%。

副作用

VOTRIENT可能出现的严重不良反应包含:肝毒性、QT延长、Torsades de pointes(一种多态性心室心律不整)、出血事件、动脉血栓事件、胃肠道穿孔及瘘管。

互相作用

会抑制或诱发CYP450 3A4酵素的药物体外试验结果显示,pazopanib在人体肝脏微粒体内的氧化代谢主要受到CYP3A4的影响,CYP1A2与CYP2C8的影响较少。因此CYP3A4抑制剂及诱发剂可能会影响pazopanib的代谢。

CYP3A4抑制剂:并用pazopanib与强效CYP3A4抑制剂(例如:ketoconazole、ritonavir、clarithromycin)可能会增加pazopanib的浓度。若必须并用强效CYP3A4抑制剂,则应考虑降低VOTRIENT的剂量。葡萄柚汁会抑制CYP3A4的活性,可能因而增加pazopanib的血中浓度,故应避免饮用。

CYP3A4诱导剂:CYP3A4诱导剂(例如rifampin)可能会降低pazopanib的血中浓度。若无法避免而需长期服用强效CYP3A4诱导剂,则不应使用VOTRIENT。

禁忌:无。

给药规定

9.41.Pazopanib(如Votrient):

1.肾细胞癌:(1)可用于第一线治疗晚期或转移性肾细胞癌,其病理上为亮细胞癌(clear cell renal carcinoma)。(2)本品使用无效后,不得申请使用temsirolimus或其他酪胺酸激?阻断剂(tyrosine kinase inhibitor,TKI)等药品。(3)需经事前审查核准后使用,每次申请之疗程以三个月为限,送审时需检送图像数据,每三个月评价一次。(4)病人若对药物产生耐受性不佳(intolerance),则以原来药物减量为原则,若严重耐受性不佳,可以换其他TKI。

2.软组织肉瘤:(1)用于治疗先前曾接受化疗失败的晚期软组织肉瘤(STS)患者。其病情若能接受手术治疗者,须先经手术治疗。(2)须排除胃肠道基质瘤、脂肪恶性肉瘤、横纹肌恶性肉瘤、软骨恶性肉瘤、骨性恶性肉瘤、依文氏(Ewing’s sarcoma)恶性肉瘤、原发性神经外胚层肿瘤(primitive neuroectodermal tumor)、突起性表皮纤维恶性肿瘤(dermatofibrosarcoma protuberance)或具骨转移的患者。(3)须经事前审查核准后使用,每次申请疗程以三个月为限,每三个月需再次申请。

警语

临床试验中曾观察到严重且致命的肝毒性。应依建议监测肝功能,必要时应暂停使用、减量或停用药物。

过量处理

VOTRIENT用药过量的处理方式应包含一般的支持性疗法。目前尚无VOTRIENT用药过量时之特殊解毒剂。由于pazopanib主要并非由肾脏排出,且极易与血浆蛋白质结合,因此预期血液透析无法促进VOTRIENT的排除。

保存方式

请勿存于超过30°C处。

英文版说明书

IndicationVOTRIENT is a prescription medicine used to treat people with advanced renal cell cancer (RCC).It is not known if VOTRIENT is safe and effective in children under 18 years of age.Important Safety InformationBefore taking VOTRIENT, tell your healthcare provider if you have or had liver problems. Some people may develop liver damage while taking VOTRIENT. VOTRIENT can cause serious liver problems including death. Your healthcare provider will do blood tests to check your liver before you start and while you take VOTRIENT. Tell your healthcare provider right away if you have yellow eyes or skin, dark urine, tiredness, nausea or vomiting, loss of appetite, pain in the right upper side of your stomach area, or if you bruise easily. Your healthcare provider may need to prescribe a lower dose of VOTRIENT for you or tell you to stop taking VOTRIENT if you develop liver problems during treatment.•VOTRIENT may cause irregular or fast heartbeat or fainting.•VOTRIENT may cause heart failure; a condition where your heart does not pump as well as it should and may result in shortness of breath.•Heart attack and stroke can happen with VOTRIENT and may cause death. Tell your healthcare provider if you have heart problems. Call your healthcare provider right away if you have chest pain or pressure, pain in your arms, back, neck or jaw, shortness of breath, numbness or weakness on one side of your body, trouble talking, headache, or dizziness.•VOTRIENT may cause blood clots, which may form in a vein, especially in your legs. Pieces of a blood clot may travel to your lungs. This may be life-threatening and cause death. Call your healthcare provider right away if you have new chest pain, trouble breathing or sudden shortness of breath, leg pain, and swelling of the arms and hands, or legs and feet, a cool or pale arm or leg.•Thrombotic microangiopathy (TMA) including thrombotic thrombocytopenia purpura (TTP) and hemolytic uremic syndrome (HUS) is a condition involving blood clots that can happen while taking VOTRIENT. TMA is accompanied by a decrease in red blood cells and cells that are involved in clotting. TMA may harm organs such as the brain and kidneys.•VOTRIENT may cause bleeding problems, which may be severe and cause death. Tell your healthcare provider before taking VOTRIENT if you have a history of abnormal bleeding. If you experience unusual bleeding, bruising, or wounds that do not heal, call your healthcare provider right away.•VOTRIENT may cause a tear (called a perforation) in the stomach or intestinal wall. Fatal perforations have occurred. VOTRIENT may also cause an abnormal connection between two parts of your gastrointestinal system (called a fistula). Call your healthcare provider if you experience pain or swelling in the stomach area, vomiting blood, or black sticky stools.•Reversible Posterior Leukoencephalopathy Syndrome (RPLS) is a condition that can happen while taking VOTRIENT that may cause death. Symptoms may include headaches, seizures, lack of energy, confusion, high blood pressure, loss of speech, blindness or changes in vision, and problems thinking.•High blood pressure can happen with VOTRIENT, including a sudden and severe rise in blood pressure which may be life-threatening. These blood pressure increases usually happen in the first several months of treatment. Blood pressure should be well controlled before starting VOTRIENT. Your healthcare provider should test your blood pressure within 1 week of starting treatment with VOTRIENT and should check it often during treatment. Get medical help right away if you have symptoms of a severe increase in blood pressure, such as severe chest pain, severe headache, blurred vision, confusion, nausea and vomiting, severe anxiety, shortness of breath, or seizures, or if you pass out (become unconscious).•VOTRIENT may cause thyroid problems. Your healthcare provider should test your thyroid function during treatment with VOTRIENT.•VOTRIENT may affect wound healing. Tell your doctor if you had recent surgery (within the last 7 days) or are going to have surgery.•VOTRIENT may cause you to have too much protein in your urine. Your healthcare provider will check you for this problem. If there is too much protein in your urine, your healthcare provider may tell you to stop taking VOTRIENT.•Serious infections can happen with VOTRIENT and can cause death. Call your healthcare provider if you experience fever; cold symptoms, such as runny nose or a sore throat that does not go away; flu symptoms, such as cough, feeling tired, and body aches; pain when urinating; or cuts, scrapes, or wounds that are red, warm, swollen, or painful.•When used in combination with some other anti-cancer therapies, VOTRIENT has caused increased toxicity and even death. Tell your healthcare provider about all of the medicines you are taking, including other anti-cancer therapies.•VOTRIENT may harm an unborn baby (cause birth defects). Do not become pregnant while taking VOTRIENT. If you do become pregnant, tell your healthcare provider right away.•A collapsed lung can happen with VOTRIENT (called pneumothorax). This may cause shortness of breath. Call your healthcare provider right away if you experience shortness of breath.The most common side effects in people with advanced renal cell carcinoma who take VOTRIENT include:◦diarrheaDiarrheaFrequent and watery bowel movements.◦high blood pressure◦hair color changes◦nausea (feeling sick to your stomach) or vomiting◦loss of appetiteTell your healthcare provider right away if you have any side effects.VOTRIENT may affect the way other medicines work and other medicines may affect how VOTRIENT works. Tell your healthcare provider about all the medicines you take, including prescription and nonprescription medicines and herbal and dietary supplements.Do not eat grapefruit or drink grapefruit juice during treatment with VOTRIENT because it may affect how VOTRIENT works.

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