繁体中文
设为首页
加入收藏
当前位置:药品说明书与价格首页 >> 抗肿瘤药 >> 新药推荐 >> 希罗达(卡培他滨片)Xeloda(Capecitabine Tablets)

希罗达(卡培他滨片)Xeloda(Capecitabine Tablets)

2012-07-21 23:20:57  作者:新特药房  来源:本站原创  浏览次数:696  文字大小:【】【】【
简介:英文药名: Xeloda(Capecitabine Tablets) 中文药名: 希罗达(卡培他滨片) 品牌药生产厂家: Hoffman-La-Roche 产品简介 卡培他滨是一种对肿瘤细胞有选择性活性的口服细胞毒性制剂。卡培他滨本身无细胞毒性 ...

英文药名: Xeloda(Capecitabine Tablets)

中文药名: 希罗达(卡培他滨片)

品牌药生产厂家: Hoffman-La-Roche

产品简介

卡培他滨片适用于紫杉醇和包括有蒽环类抗生素化疗方案治疗无效的晚期原发性或转移性乳腺癌的进一步治疗。适用于结、直肠癌的治疗,有希罗达严重副反应或对氟脲嘧啶(卡培他滨的代谢产物)有过敏史者禁用,需限制剂量的毒性包括:腹泻、腹痛、恶心、胃炎及手足综合征。

药物名称和成分

商品名:希罗达
通用名:卡培他滨片
成分: 卡培他滨
 
药理作用

卡培他滨是一种对肿瘤细胞有选择性活性的口服细胞毒性制剂。卡培他滨本身无细胞毒性,但可转化为具有细胞毒性的5氟尿嘧啶,其结构通过肿瘤相关性血管因子胸苷磷酸化酶在肿瘤所在部位转化而成,从而最大程度的降低了5-氟尿嘧啶对正常人体细胞的损害。
药代动力学

通过以502-3514 mg/m2/天的剂量范围对卡培他滨进行的药代动力学研究表明,用药第1天和第14天时,卡培他滨,5’-脱氧-5-氟胞苷和5‘-脱氧-5-氟尿苷的药代动力学参数相同。第14天时,5-氟尿嘧啶的血药浓度比第一天高30%,但在第22天时其浓度无继续增加。使用治疗剂量时,除5-氟尿嘧啶外,卡培他滨及其代谢产物的药代动力学参数与剂量比例相称。
吸收:口服后卡培他滨以完整的分子穿过肠粘膜而完全迅速的被人体吸收,进而完全转化为5‘ -脱氧-5-氟胞苷及5’ -脱氧-5-氟尿苷。饭中服用卡培他滨会影响其吸收率,但对5’ -脱氧-5-氟尿苷及其次级代谢产物5-氟尿嘧啶的曲线下面积的影响甚小。
分布:对人类血清的体外研究表明,卡培他滨,5‘-脱氧-5-氟胞苷,5’-脱氧-5氟尿苷与蛋白(主要是白蛋白)结合的比率分别为54%、10%和62%。
代谢:卡培他滨主要在肝脏和肿瘤组织内首先通过羧酸脂酶转化为5‘ -脱氧-5-氟胞苷然后再通过胞苷脱氨酶转化为5’ -脱氧-5-氟尿苷,在肿瘤细胞内的肿瘤相关性血管因子胸苷磷酸化酶的作用下转化为5-氟尿嘧啶,从而最大程度地降低了5-氟尿嘧啶对正常组织的损害。使用所推荐的剂量时,卡培他滨,5’ -脱氧-5-氟胞苷,5‘ -脱氧-5-氟尿苷和5-氟尿嘧啶的平均血清曲线下面积分别为7.40 mg?hr/mL、5.21 mg?hr/mL、21.7 mg?hr/mL和1.63 mg?hr/mL。5-氟尿嘧啶的血清曲线下面积大约比静脉注射(剂量为600 mg/m2)后低10倍。尚未发现有别于5-氟尿嘧啶的其他细胞毒性,用药2小时后,卡培他滨,5‘ -脱氧-5-氟胞苷,5’ -脱氧-5-氟尿苷的血药浓度达到峰值。然后以半衰期为0.7-1.14小时的指数逐渐降低。用药3小时后,5-氟尿嘧啶的分解产物α-氟-β-丙氨酸达到峰值,其半衰期为3-4小时。
清除:卡培他滨的代谢产物主要由肾脏排除,71%在尿中恢复原形,α-氟-β-丙氨酸为其主要代谢产物(52%)。
适应症

联合多西紫杉醇治疗包括蒽环类抗生素化疗失败的转移性乳腺癌;单药一线治疗转移性直肠癌。
用法用量

推荐剂量:每日2.5 g/m2,连用2周,休息1周。每日总剂量分早晚2次于饭后半小时用水吞服。如病情继续恶化或产生不能耐受的毒性时应停止治疗。
治疗中剂量调整 :本品所引起的毒性有时需要做对症处理或对剂量进行调整(停药或减量)。一旦减量,以后不能再增加剂量。
以下是对毒性进行剂量调整时的推荐剂量(根据加拿大国家癌症研究所制定的常见毒性标准)。
1 级:维持剂量。
2 级:
第一次出现:停止治疗,直到恢复至0-1级水平时,按维持剂量的100%进行下一疗程治疗。
第二次出现:停止治疗,直到恢复至0-1级水平时,按推荐剂量的75%进行下一疗程治疗。
第三次出现:停止治疗,直到恢复至0-1级水平时,按推荐剂量的50%进行下一疗程治疗。
第四次出现:永久停止治疗。
3 级:
第一次出现:停止治疗,直到恢复至0-1级水平时,按推荐剂量的75%进行下一疗程治疗。
第二次出现:停止治疗,直到恢复至0-1级水平时,按推荐剂量的50%进行下一疗程治疗。
第三次出现:永久停止使用。
4 级:永久停止治疗。
如停药后需继续治疗,则应考虑到病人的最大益处,且在毒性症状恢复至0-1级水平时以推荐剂量的50%进行使用。
特殊人群的剂量调整:
肝功能不全:对肝转移引起的轻度至中度肝功能不全的病人所进行的本品药代动力学研究表明,无须对这类病人作剂量调整。
肾功能不全:尚未对肾功能不全者(指血清肌酐升高)进行本品药代动力学研究。
儿童:尚未在儿童中进行本品的疗效与安全性研究。
老年人:无须作剂量调整。但老年人(65岁以上)比年轻人更易对卡培他滨产生毒性,故应对其进行密切监测。
任何疑问,请遵医嘱!

不良反应

本品的副反应可能与以下情况有关:
消化系统:最常见的副反应为可逆性胃肠道反应,如腹泻、恶心、呕吐、腹痛、口炎等。严重的(3-4级)副反应相对少见。
皮肤:在几乎一半使用本品的病人中发生手足综合征:表现为麻木、感觉迟钝、感觉异常、麻刺感、无痛感或疼痛感,皮肤肿胀或红斑,脱屑、水泡或严重的疼痛。皮炎和脱发较常见,但严重者很少见。
全身不良反应:常有疲乏但严重者极少见。其他常见的副反应为粘膜炎、发热、虚弱、嗜睡等,但均不严重。
神经系统:头痛、感觉异常、味觉障碍、眩晕、失眠等较常见,但严重者少见。
心血管系统:下肢水肿较轻且不常见。尚未见其他心血管系统副作用。
血液系统:少见中性粒细胞减少,极少见贫血,但都不严重。
其他:常见厌食及脱水,但重者极少见。
禁忌症

曾经出现本品严重副反应或对氟嘧啶(卡培他滨的代谢产物)有过敏史者禁用。

注意事项

需限制剂量的毒性包括:腹泻、腹痛、恶心、胃炎及手足综合征。近半数接受本品治疗者会诱发腹泻,对发生脱水的严重腹泻者应严密监测并给予补液治疗。每日腹泻4-6次或有夜间腹泻者为2级腹泻,每日腹泻7-9次或大便失禁和吸收障碍者为3级腹泻,每日腹泻10次以上或者有肉眼血便和需静脉补液者为4级腹泻。如发生2、3或4级腹泻,则应停用本品,直到腹泻停止或腹泻次数减少到1级时再恢复使用。3级或4级腹泻后再使用本品时应减少用量。几乎近一半使用本品的病人发生手足综合征,但多为1-2级,3级综合征者不多见。多数副反应可以消失,但需要暂时停止用药或减少用量,无须长期停止治疗。

孕妇及哺乳期妇女用药

尚未在妊娠妇女中进行本品临床研究,但必须要考虑到如果在这类病人中使用本品,可能会引起胎儿损伤。动物实验表明,卡培他滨能导致胎儿死亡或畸形。这些发现预示卡培他滨衍生物也具有这种作用,因此不能在妊娠妇女中使用本品。如在妊娠期间使用本品或在使用本品间发生妊娠时,必须考虑到该药对胎儿损伤或致畸的潜在危险性。生育期妇女使用本品时必须采取避孕措施。
尽管尚不知本品是否能分泌于母乳中,但由于许多药物能在母乳中分泌而有对哺乳的婴儿造成严重副反应的潜在危险性,因此建议使用本品的妇女停止哺乳。

药物相互作用

联合用药:本品与大量药物,如抗组胺药、非甾体抗炎药、吗啡、扑热息痛、阿斯匹林、止吐药、H2受体拮抗剂等合用,未见具有临床意义的副作用。
蛋白结合:卡培他滨与血清蛋白结合率较低(64%),通过置换能与蛋白紧密结合的药物发生相互作用的可能性尚无法预测。
与细胞色素P450酶间的相互作用:在体外实验中,未发现卡培他滨对人类肝微粒体P450酶产生影响。
 
药物过量

本品的临床试验中,未发现由于药物过量而引起的副反应。但动物实验(对猴类以25.679 g/m2/天的积极治疗)以及对人以最大耐受剂量(3.514 g/m2/天)的治疗中,药物过量的表现为恶心、呕吐、腹泻、胃肠激惹、肠胃出血和骨髓抑制等。

 
Xeloda is used in the treatment of colorectal cancer; stomach cancer; pancreatic cancer; breast cancer; breast cancer, metastatic (and more), and belongs to the drug class antimetabolites. There is positive evidence of human fetal risk during pregnancy.
Xeloda Description
This medicine is an antimetabolite used to treat colon cancer and breast cancer that has not responded to other treatments. It may also be used to treat other conditions as determined by your doctor.
Xeloda Directions
Follow the directions for using this medicine provided by your doctor. THIS MEDICINE COMES WITH A PATIENT INFORMATION LEAFLET. Read it carefully. Ask your doctor, nurse, or pharmacist any questions that you may have about this medicine. TAKE THIS MEDICINE with water after meals. STORE THIS MEDICINE at room temperature below 77 degrees F (25 degrees C) in a tightly-closed container, away from heat, moisture, and light. IF YOU MISS A DOSE OF THIS MEDICINE, skip the missed dose and go back to your regular dosing schedule. Do NOT take 2 doses at once.
Xeloda Cautions
KEEP ALL DOCTOR AND LABORATORY APPOINTMENTS while you are using this medicine. BEFORE YOU HAVE ANY MEDICAL OR DENTAL TREATMENTS, EMERGENCY CARE, OR SURGERY, tell the doctor or dentist that you are using this medicine. THIS MEDICINE MAY LOWER YOUR RESISTANCE TO INFECTION. Prevent infection by avoiding contact with people who have colds or other infections. Do not touch your eyes or the inside of your nose unless you have thoroughly washed your hands first. CHECK WITH YOUR DOCTOR BEFORE HAVING IMMUNIZATIONS (VACCINATIONS) while you are using this medicine. THIS MEDICINE HAS BEEN SHOWN TO CAUSE HARM to the human fetus. IF YOU PLAN ON BECOMING PREGNANT, discuss with your doctor the benefits and risks of using this medicine during pregnancy. IT IS UNKNOWN IF THIS MEDICINE IS EXCRETED in breast milk. DO NOT BREAST-FEED while taking this medicine.
Xeloda Side Effects
SIDE EFFECTS that may occur while taking this medicine include mild diarrhea (less than 4 stools a day), fatigue, headache, vomiting, dizziness, weakness, constipation, rash, or dry or itchy skin. If they continue or are bothersome, check with your doctor. CHECK WITH YOUR DOCTOR AS SOON AS POSSIBLE if you experience diarrhea more than 4 times a day or diarrhea at night; repeated vomiting; nausea which prevents you from eating; pain, redness, swelling, or sores in your mouth; sore throat or fever; unusual bleeding or bruising; or pain, swelling, or redness of hands or feet. If you notice other effects not listed above, contact your doctor, nurse, or pharmacist. This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your healthcare provider. Call your doctor for medical advice about side effects.
Xeloda Active Ingredients
------------------------------------------------------------------
What is Xeloda (CAPECITABINE)?
Xeloda (CAPECITABINE) is a cancer medication that interferes with the growth of cancer cells and slows their spread in the bodyXeloda (CAPECITABINE) is used to treat breast cancer and colon or rectum cancer that has spread to other parts of the body.Xeloda (CAPECITABINE) may also be used for other purposes not listed in this medication guide.
What is the most important information I should know about Xeloda (CAPECITABINE)?
You should not take this medication if you are allergic to Xeloda (CAPECITABINE) or fluorouracil (Adrucil), or if you have severe kidney disease or a metabolic disorder called DPD (dihydropyrimidine dehydrogenase) deficiency. Do not use Xeloda (CAPECITABINE) if you are pregnant. It could harm the unborn baby. Use effective birth control while you are taking Xeloda (CAPECITABINE), whether you are a man or a woman. Tell your doctor if a pregnancy occurs during treatment. You should not breast-feed while you are taking Xeloda (CAPECITABINE). Before you take Xeloda (CAPECITABINE), tell your doctor if you have liver or kidney disease, a history of coronary artery disease, or if you are also taking folic acid (contained in many vitamin and mineral supplements), leucovorin (Wellcovorin), phenytoin (Dilantin), or a blood thinner (warfarin, Coumadin).While taking Xeloda (CAPECITABINE), you will need blood tests at your doctor's office on a regular basis. Do not miss any appointments.
You must remain under the care of a doctor while you are taking Xeloda (CAPECITABINE).Call your doctor at once if you have a serious side effect such as severe vomiting or diarrhea, fever or flu symptoms, pain or redness of your hands or feet, jaundice (yellowing of the skin or eyes), chest pain, sudden numbness or weakness, or fainting.
What should I discuss with my healthcare provider before taking Xeloda (CAPECITABINE)?
You should not take this medication if you are allergic to Xeloda (CAPECITABINE) or fluorouracil (Adrucil), or if you have: severe kidney disease; or a metabolic disorder called DPD (dihydropyrimidine dehydrogenase) deficiency.If you have any of these other conditions, you may need a dose adjustment or special tests to safely use Xeloda (CAPECITABINE):kidney disease; liver disease; a history of coronary artery disease; orif you are also taking folic acid (contained in many vitamin and mineral supplements), leucovorin (Wellcovorin), phenytoin (Dilantin), or a blood thinner (warfarin, Coumadin).Use birth control to prevent pregnancy while you are taking Xeloda (CAPECITABINE), whether you are a man or a woman. Tell your doctor if a pregnancy occurs during treatment.It is not known whether Xeloda (CAPECITABINE) passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are taking Xeloda (CAPECITABINE). People over 80 years old may be more likely to have certain side effects from this medication.
How should I take Xeloda (CAPECITABINE)?
Take this medication exactly as prescribed by your doctor. Do not take it in larger amounts or for longer than recommended. Follow the directions on your prescription label.Xeloda (CAPECITABINE) is usually given in a treatment cycle of 2 weeks on and 1 week off. This 3-week cycle is repeated up to 8 times (24 weeks). Your Xeloda (CAPECITABINE) dosage may be different. Follow your doctor's instructions.During the weeks when you take Xeloda (CAPECITABINE), take the medication once in the morning and once in the evening, unless your doctor tells you otherwise. You may also be given other medications as part of a combination cancer treatment.Xeloda (CAPECITABINE) should be taken with food or within 30 minutes after eating a meal. Take this medication with a full glass (8 ounces) of water. To be sure this medication is not causing harmful effects, your blood may need to be tested on a regular basis. Your kidney and liver function may also need to be tested. Do not miss any follow-up visits. You must remain under the care of a doctor while you are taking Xeloda (CAPECITABINE).
Store Xeloda (CAPECITABINE) at room temperature away from moisture and heat. Keep the bottle tightly closed when not in use.
What happens if I miss a dose?
Take the missed dose as soon as you remember. If it is almost time for your next dose, wait until then to take the medicine and skip the missed dose. Do not take extra medicine to make up the missed dose.
What happens if I overdose?
Seek emergency medical attention if you think you have used too much of this medicine. Overdose symptoms may include fever, nausea, vomiting, diarrhea, blood in your stools, coughing up blood.
What should I avoid while taking Xeloda (CAPECITABINE)?
Avoid using antacids without your doctor's advice. Use only the specific type of antacid your doctor recommends.Xeloda (CAPECITABINE) side effectsGet emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Call your doctor at once if you have a serious side effect such as:
severe diarrhea (more than 4 times per day, or during the night);vomiting (more than once in 24 hours);nausea, loss of appetite, eating much less than usual;weakness, feeling light-headed, hot or dry skin;pain, tenderness, redness, swelling, blistering, or peeling skin on your hands or feet;fever, chills, body aches, flu symptoms;swelling, white patches, or sores in your mouth or throat;jaundice (yellowing of the skin or eyes);chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;sudden numbness, weakness, headache, confusion, or problems with vision, speech, or balance; orslow heart rate, weak pulse, fainting, slow breathing (breathing may stop).
Less serious side effects may include:
stomach pain or upset, constipation;tired feeling;temporary hair loss;mild skin rash;headache, dizziness;altered sense of taste;back pain, joint or muscle pain;eye irritation.
What other drugs will affect Xeloda (CAPECITABINE)?
Tell your doctor about all other medications you use, especially:bosentan (Tracleer);fluoxetine (Prozac);fosphenytoin (Cerebyx);montelukast (Singulair) or zafirlukast (Accolate);rifampin (Rifater, Rifadin, Rifamate);selegiline (Eldepryl, Emsam, Zelapar);voriconazole (Vfend);cancer medication such as paclitaxel (Taxol) or tamoxifen (Soltamox);heart or blood pressure medications such as amiodarone (Cordarone, Pacerone), carvedilol (Coreg), losartan (Hyzaar, Cozaar), or torsemide (Demadex);type 2 diabetes medications such as glimepiride (Amaryl), glipizide (Glucotrol), nateglinide (Starlix), pioglitazone (Actos, Actoplus Met), repaglinide (Prandin), rosiglitazone (Avandia, Avandamet), or tolbutamide (Orinase); orsulfa drugs (Bactrim, Gantanol, Gantrisin, Septra, SMX-TMP, and others).This list is not complete and there may be other drugs that can interact with Xeloda (CAPECITABINE). Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.

责任编辑:admin


相关文章
Selincro(nalmefen film-coated tablets)
VALSARTAN TABLETS(缬沙坦片)
VICCILLIN-S COMBINATION TABLETS(氨苄西林/氯唑西林钠复合片)
ABILIFY OD tablets(阿立哌唑口腔崩解片)
非诺贝特片|LIPIDIL(Fenofibrate Tablets)
TAKELDA Combination Tablets(阿司匹林/兰索拉唑配合錠)
Valsartan Tablets(缬沙坦片)
RILUZOLE TABLETS(Riluzole)利鲁唑片
METHOTREXATE Tablets(氨甲喋呤片)
Azunol ST Tablets(呱仑酸钠片)
富马酸沃诺拉赞|Takecab Tablets((Vonoprazan,TAK-438)
 

最新文章

更多

· Removab(Catumaxomab)...
· 希罗达(卡培他滨片)Xe...
· ZOLINZA(vorinostat,伏...
· 聚乙二醇干扰素(SYLATRO...
· 苹果酸舒尼替尼胶囊|Sut...
· 地尼白介素-2(DENILEUK...
· GARDASIL(基因重组四价...
· Jakafi(Ruxolitinib)片
· INFED(IRON DEXTRAN COM...
· 格拉司琼透皮贴片(gran...

推荐文章

更多

· Removab(Catumaxomab)...
· 希罗达(卡培他滨片)Xe...
· ZOLINZA(vorinostat,伏...
· 聚乙二醇干扰素(SYLATRO...
· 苹果酸舒尼替尼胶囊|Sut...
· 地尼白介素-2(DENILEUK...
· GARDASIL(基因重组四价...
· Jakafi(Ruxolitinib)片
· INFED(IRON DEXTRAN COM...
· 格拉司琼透皮贴片(gran...

热点文章

更多