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甲磺酸伊马替尼片(IMATINIB MESYLATE 商品名:格列卫GLEEVEC)

2011-07-24 17:38:04  作者:新特药房  来源:中国新特药网天津分站  浏览次数:540  文字大小:【】【】【
简介: 【通用名称】:甲磺酸伊马替尼片【商品名称】:格列卫片【英文名称】:Gleevec 【性状】:甲磺酸伊马替尼的化学名称为4-[(4-甲基-1-哌嗪)甲基]-N-[4-甲基-3-[[4-(3-吡啶)-2-嘧啶]氨基]苯基]-苯 ...

【通用名称】:甲磺酸伊马替尼片
【商品名称】:格列卫片
【英文名称】:Gleevec      
【性状】:
甲磺酸伊马替尼的化学名称为4-[(4-甲基-1-哌嗪)甲基]-N-[4-甲基-3-[[4-(3-吡啶)-2-嘧啶]氨基]苯基]-苯胺甲磺酸盐,分子式为C29H31N7O·CH4SO3,分子量为589.7。
本品胶囊内容物为白色至类白色粉末。 
【药理作用】:
甲磺酸伊马替尼在体内外均可在细胞水平上抑制Bcr-Abl酪氨酸激酶,能选择性抑制Bcr-Abl阳性细胞系细胞、Ph染色体阳性的慢性粒细胞白血病和急性淋巴细胞白血病病人的新鲜细胞的增殖和诱导其凋亡。此外,甲磺酸伊马替尼还可抑制血小板衍化生长因子(PDGF)受体、干细胞因子(SCF),c-Kit受体的酪氨酸激酶,从而抑制由PDGF和干细胞因子介导的细胞行为。
临床前和临床数据提示,有些病人可通过不同的机制产生耐药性。
【临床研究】
注1:细胞遗传学反应指标:相应细胞遗传学疗效包括完全反应和部分反应。完全反应 :分裂细胞中Ph染色体阳性细胞消失。部分反应 :分裂细胞中,Ph染色体阳性细胞为1-35%。
对Ph染色体阳性的慢性粒细胞白血病急变期(髓性原始细胞危象)、加速期和经α-干扰素治疗失败的慢性期患者进行了三组开放、非对照性的II期临床研究。
临床研究病例中,40%患者的年龄≥ (greater than or equal to) 60岁,10-12%≥ (greater than or equal to) 70岁。
加速期 :(235例,其中63%患者在加速期已接受过其他治疗,235例患者中77例接受甲磺酸伊马替尼400 mg,每日1次 ;158例接受600 mg,每日1次)。结果63%患者获得确切的血液学反应,28%患者获得完全血液学反应,21%患者获得主要细胞遗传学反应(即分裂中Ph染色体阳性细胞减少到<35%,14%获得完全细胞遗传学缓解。以血液学缓解为主要终点的分析,发现400 mg和600 mg剂量组之间无明显差异,但600 mg剂量组的细胞遗传学反应改善更明显,其持续时间更长。本研究中,600 mg剂量组的疾病出现进展所需的时间明显不同。
急变期(髓性原始细胞危象):(260例,95例[37%]在进入加速期或急变期后均已接受过化疗,另165例[63%]此前未接受过化疗。223例开始治疗的剂量为600 mg, 每日1次)。以不同的完全血液学反应作为主要疗效进行统计,26%获得了肯定的血液学反应(未接受过治疗患者为30%,经过治疗的患者为19%),13.5%患者观察到主要细胞遗传学反应。未接受和接受过治疗的患者的中位存活时间分别为7.1和5.2个月。
干扰素治疗失败的患者(慢性期):(532例,开始剂量400 mg,每日1次)患者的49%获得了主要细胞遗传学反应,30%获得了完全反应,88%获得了完全血液学反应。
【药代动力学】   
本研究的药代动力学系单剂量口服25-1000 mg甲磺酸伊马替尼并达稳态后测定。
甲磺酸伊马替尼剂量在25-1000 mg范围内,其平均曲线下面积(AUC)的增加与剂量间存在比例性关系。重复给药的药物累积量可达稳态时的1.5-2.5倍。成人人群药代动力学研究表明,性别对药代动力学无影响,体重的影响也可忽略而不计。
吸收
胶囊剂的平均绝对生物利用度为98%,口服1次甲磺酸伊马替尼后血浆AUC的变异系数波动在40-60%之间。与空腹时比较,高脂饮食后本药吸收率减少甚微(Cmax减少11%,Tmax延长),AUC略减少(7.4%)。
分布
约95%与血浆蛋白结合,绝大多数是与白蛋白结合,少部分与α-酸性糖蛋白结合,只有极少部分与脂蛋白结合。整个机体内的总体分布浓度较高,分布容量为4.9 L/kg体重,但红细胞内分布比率较低。体内组织中有关药物分布情况仅来源于临床前的资料。肾上腺和性腺中摄取水平高,中枢神经系统中摄取水平低。
代谢
人体内主要循环代谢产物是N-去甲基哌嗪衍生物,在体外其药效与原药相似。该代谢物的血浆AUC是原药甲磺酸伊马替尼AUC的16%。甲磺酸伊马替尼是CYP3A4的底物,又是CYP3A4、CYP2D6、CYP2C9和CYP2C19的抑制剂,因此,可影响同时给予药物的代谢。
排泄
甲磺酸伊马替尼的清除半衰期为18小时,其活性代谢产物半衰期为40小时,7天内约可排泄所给药物剂量的81%,其中从大便中排泄68%,尿中排泄13%。约25%为原药(尿中5%,大便中20%),其余为代谢产物,大便和尿中活性代谢产物和原药的比例相似。
肝肾功能衰竭
对肝、肾功能衰竭病人未进行过临床研究,这些患者应用甲磺酸伊马替尼时要谨慎。已知甲磺酸伊马替尼的排泄很少经肾脏,估计肾功能衰竭患者服用不会出现问题。 
【适应症】   
用于治疗慢性粒细胞白血病(CML)急变期、加速期或α-干扰素治疗失败后的慢性期患者;不能手术切除或发生转移的恶性胃肠道间质肿瘤(GIST)患者。 
【用法用量】   
开始剂量:对慢性粒细胞白血病急变期和加速期患者,甲磺酸伊马替尼的推荐剂量为600 mg/日 ;对干扰素治疗失败的慢性期患者,以及不能手术切除或发生转移的恶性胃肠道间质肿瘤(GIST)患者,推荐剂量为400 mg/日,均为每日1次口服,宜在进餐时服药,并饮一大杯水,只要有效,就应持续服用。
如果血象许可,没有严重药物不良反应,在下列情况下剂量可考虑从400 mg/日增加到600 mg/日,或从600 mg/日增加到800 mg/日(400 mg,分2次服用):疾病进展、治疗至少3个月后未能获得满意的血液学反应,已取得的血液学反应重新消失。
下列情况中必须调整剂量:如治疗过程中出现严重非血液学不良反应(如严重水潴留),宜停药,直到不良反应消失,随后再根据该不良反应的严重程度调整剂量。
严重肝脏毒副作用时剂量的调整:如胆红质升高超过正常范围上限3倍或转氨酶升高超过正常范围上限5倍,宜停药,直到上述指标分别降到正常范围上限的1.5或2.5倍以下。
中性粒细胞减少或血小板减少时剂量的调整:加速期或急变期 :如果出现严重中性粒细胞和血小板减少(中性粒细胞<0.5×109/L和/或血小板<10×109/L,建议剂量减少到400 mg/日。如果血细胞持续减少2周,则进一步减少剂量到300 mg/日,如血细胞持续减少4周,宜停药,直到中性粒细胞≥ (greater than or equal to) 1.0×109/L和血小板≥ (greater than or equal to) 20×109/L。再用时剂量为300 mg/日。
α-干扰素治疗失败后慢性期患者 :当中性粒细胞<1.0×109/L和/或血小板<50×109/L时宜停药,仅在中性粒细胞≥ (greater than or equal to) 1.5×109/L和血小板≥ (greater than or equal to) 75×109/L时再恢复用药,剂量为400 mg/日,如中性粒细胞或血小板重新减少到上述数值时,再恢复用药时剂量减至300 mg/日。
儿童和青少年:尚无18岁以下患者使用甲磺酸伊马替尼治疗的安全性和有效性临床资料。
肝功能衰竭患者的剂量:有肝功能损害者甲磺酸伊马替尼的血浆浓度可以升高,因此这些患者用本药时要谨慎,目前尚无肝功能损害患者使用甲磺酸伊马替尼的临床资料,无法提出剂量调整的建议。
肾功能衰竭和老年患者的剂量:已知肌酐清除率可随年龄老化而降低,而年龄对甲磺酸伊马替尼的药代动力学无明显影响,由于尚未在肾功能损害患者中进行过临床试验,故无法提出剂量调整的建议。 
【不良反应】   
多数患者在服用甲磺酸伊马替尼期间会出现一些不良反应,但绝大多数属轻到中度。考虑到疾病本身也会产生症状,常难以明确他们的因果关系。临床试验过程中,因药物相关的不良反应而停药者,在α-干扰素治疗失败的慢粒慢性期患者中仅占1%,加速期中约占2%,慢粒急变期占5%。
最常见与药物治疗相关的不良事件有轻度恶心(50-60%),呕吐,腹泻、肌痛及肌痉挛,这些不良事件均容易处理。所有研究中均报告有浮肿和水潴留,发生率分别为47-59%和7-13%,其中严重者分别为1-3%和1-2%。大多数患者的浮肿表现为眶周和下肢浮肿,也有报告为胸水、腹水、肺水肿和体重迅速增加的,此时通常暂停药,用利尿剂或给予某些支持治疗。个别患者情况严重,甚至威胁生命。有1例慢粒急变患者因并发胸水、充血性心力衰竭和肾功能衰竭的复杂临床情况而死亡。这些不良反应的发生率与剂量有一定关系,多见于每天≥ (greater than or equal to) 600 mg时。
按系统器官分类及发生的频度,将不只是发生于个别患者的不良反应罗列如下。频度的定义为很常见>10%,常见>1%≤ (smaller than or equal to) 10%,偶见>0.1%≤ (smaller than or equal to) 1%,罕见>0.01%≤ (smaller than or equal to) 0.1%,非常罕见≤ (smaller than or equal to) 0.01%(CIOMS分类法)。
全身性异常:
很常见 :水潴留(10%)和周身浮肿(两者共51%)。
常见 :发热、疲劳、乏力、畏寒和体重增加。
不常见 :不适、出血和体重减轻。
传染病/感染:
不常见 :败血症、肺炎、单纯疱疹、带状疱疹和上呼吸道感染。
血液与淋巴系统异常:
很常见 :中性粒细胞减少(14%)、血小板减少(14%)和贫血(11%)。
常见 :发热性中性粒细胞减少、全血细胞减少。
代谢和营养失衡:
常见 :食欲不振。
不常见 :脱水、高尿酸血症、低钾血症、高钾血症,低钠血症、食欲增加。
精神异常:
不常见 :抑郁症。
神经系统异常:
很常见 :头痛(11%)。
常见 :头晕、味觉障碍、感觉异常、失眠。
不常见 :出血性卒中、晕厥、周围神经病变、感觉减退、嗜唾、偏头痛。
眼异常 :
常见 :结膜炎、流泪增多。
不常见 :眼刺激症状、视力模糊、结膜出血、眼干、眶周浮肿。
耳和迷路异常:
不常见 :头晕。
心脏异常:
不常见 :心力衰竭、肺水肿、心动过速。
血管异常:
不常见 :血肿、高血压、低血压、潮红、四肢发冷。
呼吸道、胸和纵隔异常:
常见 :胸水、鼻衄。
不常见 :呼吸困难、咳嗽。
消化系统异常:
很常见 :恶心(56%)、呕吐(33%)、腹泻(24%)、消化不良(12%)。
常见 :腹痛、腹胀、胀气、便秘、口干。
不常见 :胃肠道出血、黑便、腹水、胃溃疡、胃炎、胃食道反流、口腔溃疡。
肝胆系统异常:
不常见 :黄疸、肝酶升高、高胆红质血症。
皮肤和皮下组织异常:
很常见 :周身浮肿(30%)、皮炎/湿疹/皮疹(共25%)。
常见 :脸肿、眶周肿、瘙痒、红皮症、皮肤干燥、脱发、盗汗。
不常见 :瘀斑、多汗、荨麻疹、指甲断裂、光过敏反应、紫癜。
骨骼肌、结缔组织和骨异常:
很常见 :肌痉挛、疼痛性肌痉挛(33%)、骨骼肌肉痛包括关节肿胀(25%)。
不常见 :坐骨神经痛。
肾和泌尿系统异常:
不常见 :肾衰、肌酐升高。
生殖系和乳房异常:
不常见 :男性乳房女性化、乳房肿大、阴囊水肿。
实验室检查异常
所有研究均报告有血细胞减少,尤其是中性粒细胞和血小板减少,以≥ (greater than or equal to) 750 mg/日的大剂量时发生率为高(I期研究),然而血细胞减少的发生率也明显取决于病期,3或4度的中性粒细胞减少(ANC<1.0×109/L)和血小板减少(<50×109/L),在急变期和加速期发生率分别为58-62%和42-58%,相比之下在慢性期分别只有33%和17%,前者为后者的2-3倍。4度中性粒细胞减少(ANC<0.5×109/L)和血小板减少(<10×109/L)发生率分别只有8%和1%。中性粒细胞和血小板减少发生的中位数持续时间分别为2-3周和3-4周,仅少数病例需为此而长期停药。
严重的转氨酶或胆红质升高少见(<3%病例,常需减量或停药(中位数持续时间约为1周),只有不到0.5%患者由此而长期停药。有1例加速期患者死于急性肝功能衰竭,但该例患者尚不能排除大剂量扑热息痛与甲磺酸伊马替尼的药物相互反应的结果。 
【禁忌症】:对本药活性物质或任何赋形剂成份过敏者禁用。 
【注意事项】:   
一开始治疗就应由对慢性粒细胞白血病有治疗经验的医师进行。
大约有1-2%服用甲磺酸伊马替尼的患者发生严重水潴留(胸水、浮肿、肺水肿和腹水),因此建议定期监测体重,如用药过程中体重出乎意料地快速增加,应作详细检查,必要时采取适当支持治疗和处理措施。
水潴留可以加重或导致心衰,目前尚无严重心衰者(按纽约心脏学会分类法的III-IV级)临床应用甲磺酸伊马替尼的经验。对这些患者用本药要谨慎。
肝功能衰竭患者甲磺酸伊马替尼的量可能会增加,有肝功损害者慎用本药。
有关本药安全性和有效性的长期临床资料尚有限。
临床前研究表明,甲磺酸伊马替尼不易通过血脑屏障。尚未在人体进行过研究。
甲磺酸伊马替尼治疗第1个月宜每周查1次全血象,第2个月每2周查1次,以后则视需要而定(如每2-3个月查1次)。若发生严重中性粒细胞或血小板减少,应调整剂量。
开始治疗前应检查肝功能(包括转氨酶、胆红质和碱性磷酸酶),随后每月查1次或根据临床情况决定,必要时宜调整剂量。
对驾驶员和机器操纵者能力的影响尚无有关对驾驶员或机器操纵者能力可能发生的影响的信息和资料。 
【孕妇及哺乳期妇女用药】   
妊娠 :动物研究表明本药对生殖系统有毒性作用,但目前尚缺乏孕妇使用的资料,对胎儿可能的毒性目前不详。除非使用后可能的好处大于对胎儿/婴儿的危害,否则妊娠期间不宜应用。如妊娠期间服用甲磺酸伊马替尼,必须告诉其对胎儿可能的危害。生育期妇女在服用甲磺酸伊马替尼期间应劝其同时进行有效的避孕。
哺乳 :在动物实验中,甲磺酸伊马替尼及其代谢产物大量从乳汁中排出,但未进行过人体研究,用甲磺酸伊马替尼的妇女不应哺乳。
【儿童用药】   
个别样本中,儿童血浆浓度可升高1.5- 2倍,这一数据尚不足以作为推荐儿童药物剂量的依据。
【老年患者用药】   
已知肌酐清除率可随年龄老化而降低,而年龄对甲磺酸伊马替尼的药代动力学无明显影响。 
【药物相互作用】
可改变甲磺酸伊马替尼血浆浓度的药物
CYP3A4抑制剂 :健康志愿者同时服用单剂酮康唑(CYP3A4抑制剂)后,甲磺酸伊马替尼的药物暴露量大大增加(平均最高血浆浓度和曲线下面积可分别增加26%和40%,因此同时服用甲磺酸伊马替尼和CYP3A4抑制剂(如酮康唑、伊曲康唑、红霉素和克拉仙)时必须谨慎。
CYP3A4诱导剂 :在临床研究中发现,同时给予苯妥英药物后,甲磺酸伊马替尼的血浆浓度降低,疗效减低。其它诱导剂如地塞米松、卡他咪嗪、利福平、苯巴比妥和含有St John麦汁浸膏制剂等,可能有类似问题,但尚未进行专门研究,因此同时服用这些药物时须谨慎。
甲磺酸伊马替尼可使下列药物改变血浆浓度甲磺酸伊马替尼使辛伐他丁(CYP3A4底物)的平均Cmax和AUC分别增加2倍和3.5倍。
当同时服用本药和治疗窗狭窄的CYP3A4底物(如环孢素、哌咪清)时应谨慎。甲磺酸伊马替尼可增加经CYP3A4代谢的其他药物(如苯二氮类、双氢吡啶、钙离子拮抗剂、和HMG-COA还原酶抑制剂等)的血浆浓度。
在与抑制CYP3A4活性相似的浓度下,甲磺酸伊马替尼还可在体外抑制细胞色素P450异构酶CYP2D6的活性,因此在与甲磺酸伊马替尼同时服用时,有可能增加全身与CYP2D6底物的接触量,尽管尚未作专门研究,用药时仍应谨慎。
甲磺酸伊马替尼在体外还可抑制CYD2C9和CYD2C19的活性,同时服用华法令后可见到凝血酶原时间延长。因此在甲磺酸伊马替尼治疗的始末或更改剂量时,若同时在用双香豆素,宜短期监测凝血酶原时间。
应告知病人避免使用含有扑热息痛的非处方药和处方药。 
【药物过量】:   
剂量超过800 mg的经验尚少,也无剂量过量的病例报告。若发生过量,应密切观察病人,并给予适当的支持治疗。 
【贮藏/有效期】:宜保存在30°C以下。有效期2年。

【原产地英文商品名】GLEEVEC 400mg/Tablet,30Tablets/bottle
【原产地英文药品名】IMATINIB MESYLATE
【中文参考商品译名】
注:以下产品不同规格和不同价格,购买时请以电话咨询为准!
·格列卫片 100毫克/片 90片/瓶
·格列卫片 400毫克/片 30片/瓶
【中文参考药品译名】甲磺酸伊马替尼
【生产厂家中文参考译名】诺华制药
【生产厂家英文名:Novartis

Important information

 

GLEEVEC® is available only by prescription.

GLEEVEC® Indications

GLEEVEC® (imatinib mesylate) tablets are indicated for:

  • Newly diagnosed adult and pediatric patients with Philadelphia chromosome–positive chronic myeloid leukemia (Ph+ CML) in the chronic phase
  • Patients with Ph+ CML in blast crisis (BC), accelerated phase (AP), or in the chronic phase (CP) after failure of interferon-alpha therapy

SAFETY: Important product information (Click here for full Prescribing Information)

Who should NOT take GLEEVEC

  • Women who are or could be pregnant. Fetal harm can occur when administered to pregnant women; therefore, women should not become pregnant, as well as be advised of the potential risk to the unborn child if GLEEVEC is used during pregnancy
  • Women who are breast-feeding because of the potential for serious adverse reactions in nursing infants
  • Sexually active females should use adequate birth control while taking GLEEVEC

Be sure to talk to your doctor and/or healthcare professional about these issues before taking GLEEVEC.

Warnings and precautions

  • GLEEVEC is often associated with edema (swelling) and serious fluid retention. It is important that patients be weighed and monitored regularly for signs and symptoms of serious fluid retention, or unexpected weight gain. Patients experiencing unexpected rapid weight gain should speak to their doctor about appropriate supportive care treatment. Studies have shown that edema (swelling) tended to occur more often among patients who are 65 and older or those taking higher doses of GLEEVEC. If you experience severe fluid retention, your doctor may treat you with diuretics and may stop your GLEEVEC treatment until the fluid retention has been managed
  • Cytopenias (reduction or lack of certain cell elements in blood circulation), such as anemia, have occurred. Your doctor will perform complete blood counts weekly for the first month, biweekly for the second month, and periodically thereafter. In most cases, your doctor will reduce or interrupt your GLEEVEC therapy; in rare cases, your doctor may discontinue treatment. If the cytopenia is severe, your doctor may reduce your dose or temporarily stop your treatment with GLEEVEC
  • Severe congestive heart failure and left ventricle dysfunction have been reported, particularly in patients with other health issues and risk factors. Patients with heart disease or risk factors will be monitored and treated for the condition
  • Severe liver problems (hepatotoxicity) may occur. Cases of fatal liver failure and severe liver injury requiring liver transplants have been reported with both short-term and long-term use of GLEEVEC. Your doctor will check your liver function before beginning treatment and continue to monitor liver function as needed. If you experience severe liver problems, your doctor may stop your treatment with GLEEVEC until the liver problem has been managed
  • Bleeding may occur. Severe gastrointestinal (GI) bleeding has been reported in patients with Ph+ CML
  • In patients with hypereosinophilic syndrome (a condition with increased eosinophils, which are a type of white blood cell) and heart involvement, cases of heart disease (cardiogenic shock/left ventricular dysfunction) have been associated with the initiation of GLEEVEC therapy. Speak to your doctor regarding appropriate supportive care or discontinuing GLEEVEC
  • Skin reactions, such as fluid-filled blisters, have been reported with the use of GLEEVEC
  • Clinical cases of hypothyroidism (reduction in thyroid hormones) have been reported in patients taking levothyroxine replacement during treatment with GLEEVEC. Your doctor should closely monitor your thyroid hormone levels
  • Long-term use may result in potential liver, kidney, and/or heart toxicities; immune system suppression may also result from long-term use
  • GLEEVEC can cause fetal harm when administered to a pregnant woman. Women should be aware of the potential harm to the fetus. Be sure to inform your doctor if you are or think you may be pregnant. You should not breast-feed while taking GLEEVEC
  • GI perforation (small holes or tears in the walls of the stomach or intestine), in some cases fatal, has been reported
  • Growth retardation has been reported in children taking GLEEVEC. The long-term effects of extended treatment with GLEEVEC on growth in children are unknown. Growth retardation may be monitored in children receiving treatment
  • Cases of tumor lysis syndrome (TLS), which refers to a metabolic and electrolyte disturbance caused by the breakdown of tumor cells, have been reported and can be life-threatening in some cases. The patients at risk of TLS are those that have a higher amount of tumor cells and whose tumors are fast-growing before beginning therapy. Your doctor should monitor you closely and take appropriate precautions

Important safety information

The following serious side effects have been reported in patients taking GLEEVEC:

  • Severe fluid retention, which can cause swelling around the eyes or swelling of the lower legs, lungs, and heart; fatal in rare cases
  • Increased pressure in the heart or brain; fatal in rare cases
  • Low levels of certain blood cells
  • Heart failure/cardiogenic shock
  • Liver problems
  • Hemorrhage (abnormal bleeding)
  • Skin blistering
  • Low levels of thyroid hormone

Your doctor will check you closely for any side effects to stop more serious complications from occurring. Patients with heart disease or risk factors for heart failure should also be monitored carefully.

GLEEVEC is sometimes associated with stomach or intestinal irritation. GLEEVEC should be taken with food and a large glass of water to minimize this problem. There have been rare reports, including deaths, of stomach or intestinal perforation (a small hole or tear).

If you are experiencing any of the above-mentioned side effects, please be sure to speak with your doctor immediately.

Common side effects of GLEEVEC

Almost all patients treated with GLEEVEC experience side effects at some time. Most side effects are mild to moderate in severity. Some common side effects you may experience include:

  • Fluid retention
  • Diarrhea
  • Fatigue
  • Muscle cramps or pain and bone pain
  • Decreased
    hemoglobin
  • Rash
  • Vomiting
  • Nausea
  • Anorexia (loss
    of appetite)

If you are experiencing any of the above-mentioned side effects, please be sure to speak with your doctor immediately.

The severity of some side effects may be reduced with the help of other medicines and advice from your doctor, while others may require stopping GLEEVEC therapy for a while or changing the dose. However, in some cases, GLEEVEC therapy may need to be discontinued.

Tell your doctor if you experience side effects during therapy with GLEEVEC, including fever, shortness of breath, blood in your stools, jaundice (yellowing of the skin and/or eyes), sudden weight gain, symptoms of heart failure, or if you have a history of heart disease or risk factors for heart disease.

After the approval of GLEEVEC, the following adverse events have been reported in patients treated with GLEEVEC: compression of the heart due to increased fluid, swelling of the brain, GI perforation (holes in the stomach or intestine), and sudden lung failure.

These events, including some fatalities, may or may not have been drug related.

Take GLEEVEC exactly as prescribed. Do not change your dose or stop taking GLEEVEC unless you are told to do so by your doctor. If you miss a dose, take your dose as soon as possible, unless it is almost time for your next dose. In this case, your missed dose should not be taken. A double dose should not be taken to make up for any missed dose. You should take GLEEVEC with a meal and a large glass of water.

Do not take any other medications without talking to your doctor or pharmacist first, including over-the-counter medications such as Tylenol® (acetaminophen); herbal products (St. John's wort, Hypericum perforatum); Coumadin® (warfarin sodium); rifampin; erythromycin; metoprolol; ketoconazole; and Dilantin® (phenytoin). Taking these with GLEEVEC may affect how they work, or affect how GLEEVEC works.

You should also tell your doctor if you are taking or plan to take iron supplements. Patients should also avoid grapefruit juice and other foods that may affect how GLEEVEC works.

责任编辑:admin


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