英文药名: Gleevec(Imatinib Mesylate Capsules) 中文药名: 格列卫（伊马替尼胶囊） 品牌药生产厂家: Novartis诺华公司 药物名称 [商品名]格列卫 [通用名]甲磺酸伊马替尼胶囊   适应症 用于治疗慢性髓性白血病(CML) 急变期、加速期或α-干扰素治疗失败后的慢性期患者。用于治疗不能切除和/或发生转移的恶性胃肠道间质肿瘤(GIST)的成人患者。 用法用量 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。 对急变期和加速期患者甲磺酸伊马替尼的推荐剂量为600mg/日，对干扰素治疗失败的慢性期患者为400mg/日，均为每日一次口服，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400mg/日增加到600mg/日，或从600mg/日增加到800mg/日（400mg，口服，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。 如果您有任何疑问，请遵医嘱。 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。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. 禁忌 对本药活性物质或任何赋形剂成份过敏者禁用。 注意事项 大约有1~2％服用本品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, 应仔细评价体重的增加，必要时采取适当的支持治疗。特别是儿童患者，水潴留可能不出现可以识别的水肿.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）临床应用本品的经验。对这些患者用本药要谨慎，青光眼的患者也应慎用（见不良反应）。 GIST临床试验中，报告有8例病人（5.4%）出现胃肠道出血和4例病人（2.7%）出现肿瘤内出血。根据肿瘤的部位不同，肿瘤内出血可能发生在腹腔内，也可能发生在肝内。这类病人的肿瘤内出血也有可能表现为胃肠道出血，因此，在治疗开始阶段应监测病人的胃肠道症状。同时服用本品和CYP3A4诱导剂（见相互作用）可显著降低伊马替尼的总暴露量，因此增加潜在治疗失败的危险。因此应避免本品与CYP3A4诱导剂合用。肝功能衰竭患者本品的暴露量可能会增加，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。本品治疗第一个月宜每周查一次全血象，第二个月每两周查一次，以后则视需要而定（如每2－3个月查一次）。若发生严重中性粒细胞或血小板减少，应调整剂量（见用法用量）。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），随后每月查一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。 老人用药 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。 贮藏 本药宜保存在30°C以下。 包装规格： ·100mg *60 胶囊 ·400mg *30 胶囊 ·100mg 10 胶囊 ·400mg 10 胶囊 FDA Approves Updated Indication for Gleevec New Labeling Extends Treatment to 36 Months for Certain GIST Patients After Surgery On Jan. 31, the FDA approved a new indication for Gleevec (imatinib mesylate, Novartis) for use in certain adult patients following surgical removal of KIT (CD117)-positive gastrointestinal stromal tumors (GIST). The new labeling recommends 36 months of treatment with Gleevec after surgery in adult patients with KIT-positive GIST who meet the risk for recurrence inclusion criteria of the pivotal trial. The 36-month treatment regimen was shown to improve recurrence-free survival (RFS) and overall survival (OS) in patients with KIT-positive GIST compared with 12 months of treatment. The new approval is based on data from an international, multicenter, open-label Phase III clinical trial (SSG XVIII) conducted by the Scandinavian Sarcoma Group and the Sarcoma Group of the Arbeitsgemeinschaft Internistische Onkologie. Gleevec manufacturer Novartis provided funding for the study. The primary end point of the study was to compare, within the first five years, RFS in patients with a greater than 50% estimated risk for GIST recurrence following diagnosis and treatment with adjuvant Gleevec for either 12 or 36 months. Results of the study revealed that RFS was longer for patients assigned to receive 36 months of Gleevec after surgery compared with those who received 12 months of treatment, for a 54% reduction in risk for GIST recurrence (hazard ratio [HR], 0.46; 95% confidence interval [CI], 0.32-0.65; P<0.0001). Additionally, OS was longer in the 36-month treatment group, which resulted in a 55% reduction in the risk for death (HR, 0.45; 95% CI, 0.22-0.89; P=0.0187). Gleevec was originally granted accelerated approval for the treatment of advanced or metastatic GIST in 2002. In 2008, Gleevec was granted accelerated approval for adjuvant use for the treatment of patients with GIST who had had potentially curative resection (surgical removal) of GIST, but who had an increased risk for recurrence. Approval for the metastatic GIST indication also was granted in 2008. “The development of Gleevec over the past decade highlights the need to further study drugs after approval to truly characterize their benefits,” said Richard Pazdur, MD, director of the Office of Hematology and Oncology Products in the FDA’s Center for Drug Evaluation and Research, in a press release. “Although originally approved in the metastatic disease setting, this subsequent trial has demonstrated that longer use of Gleevec can prolong patients’ lives in earlier disease settings.” GIST is a rare form of cancer that originates in cells found in the wall of the gastrointestinal tract. These cells, known as interstitial cells of Cajal, are part of the autonomic nervous system, which regulates body processes such as food digestion. The major cause of GIST is an abnormal form of the protein KIT, which causes cells to grow uncontrollably and become cancerous. Gleevec is indicated for the treatment of patients with KIT-positive GIST that are cancerous, cannot be surgically removed and/or have spread to other parts of the body. The drug also is approved for use after surgery in patients who have had KIT-positive GIST completely removed. Additionally, Gleevec is approved for the treatment of other cancers; it was first approved by the FDA in 2001 to treat patients with advanced Philadelphia chromosome-positive chronic myeloid leukemia, a blood and bone marrow disease linked to a genetic abnormality. -------------------------------------------------------------------- Gleevec Generic Name: Imatinib (i-MA-tin-ib)Brand Name: Gleevec Gleevec is used for: Treating certain types of leukemia (eg, chronic myeloid leukemia, Philadelphia chromosome positive chronic myeloid leukemia [CML]), bone marrow diseases, certain types of skin cancer, and certain intestinal tumors (eg, gastrointestinal stromal tumors [GIST]). It may also be used to prevent cancer from growing in patients after surgical removal of GIST. It is also used to treat mastocytosis (a buildup of large amounts of mast cells in certain parts of the body). It may also be used for other conditions as determined by your doctor. Gleevec is a protein-tyrosine kinase inhibitor. It works by preventing the growth of cancer cells. Do NOT use Gleevec if: you are allergic to any ingredient in Gleevec you take warfarin Contact your doctor or health care provider right away if any of these apply to you. Before using Gleevec : Some medical conditions may interact with Gleevec . Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you: if you are pregnant, planning to become pregnant, or are breast-feeding if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement if you have allergies to medicines, foods, or other substances if you have liver or kidney problems, heart problems, or lung problems if you have had your thyroid gland removed if you have bone marrow problems, low white blood cell levels, or low blood platelet levels if you have a history of swelling (edema) or fluid retention if you are or will be taking an iron supplement Some MEDICINES MAY INTERACT with Gleevec . Tell your health care provider if you are taking any other medicines, especially any of the following: Warfarin because side effects, including the risk of bleeding, may be increased Azole antifungals (eg, itraconazole, ketoconazole), ketolide antibiotics (eg, telithromycin), macrolide antibiotics (eg, clarithromycin, erythromycin), nefazodone, or protease inhibitors (eg, ritonavir) because they may increase the risk of Gleevec 's side effects Barbiturates (eg, phenobarbital), carbamazepine, dexamethasone, hydantoins (eg, phenytoin), rifampin, or St. John's wort because they may decrease Gleevec 's effectiveness Acetaminophen, alfentanil, benzodiazepines (eg, alprazolam), calcium channel blockers (eg, nifedipine), cyclosporine, ergot derivatives (eg, ergotamine), fentanyl, HMG-CoA reductase inhibitors (eg, simvastatin), pimozide, quinidine, sirolimus, or tacrolimus because the risk of their side effects may be increased by Gleevec Levothyroxine because its effectiveness may be decreased by Gleevec This may not be a complete list of all interactions that may occur. Ask your health care provider if Gleevec may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine. How to use Gleevec : Use Gleevec as directed by your doctor. Check the label on the medicine for exact dosing instructions. Take Gleevec by mouth with a meal and a full glass of water (8 oz/240 mL). If you have trouble swallowing tablets whole, talk with your doctor or pharmacist. You may dissolve your dose in a glass of water or apple juice. The amount of liquid will vary depending on your dose. Ask your doctor or pharmacist for instructions. Stir the mixture well and drink immediately. Do not eat grapefruit or drink grapefruit juice while you use Gleevec . Take Gleevec on a regular schedule to get the most benefit from it. Taking Gleevec at the same time each day will help you to remember to take it. If you miss a dose of Gleevec , take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once. Ask your health care provider any questions you may have about how to use Gleevec . Important safety information: Gleevec may cause dizziness. These effects may be worse if you take it with alcohol or certain medicines. Use Gleevec with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it. Do NOT take more than the recommended dose or take for longer than prescribed without checking with your doctor. Tell your doctor or dentist that you take Gleevec before you receive any medical or dental care, emergency care, or surgery. Gleevec may reduce the number of clot-forming cells (platelets) in your blood. Avoid activities that may cause bruising or injury. Tell your doctor if you have unusual bruising or bleeding. Tell your doctor if you have dark, tarry, or bloody stools. Gleevec may lower the ability of your body to fight infection. Avoid contact with people who have colds or infections. Tell your doctor if you notice signs of infection like fever, sore throat, rash, or chills. Do not receive a live vaccine (eg, measles, mumps) while you are taking Gleevec . Talk with your doctor before you receive any vaccine. Check your weight every morning and keep a log. Report any 3- to 5-pound weight gain to your doctor. Gleevec may cause you to become sunburned more easily. Avoid the sun, sunlamps, or tanning booths until you know how you react to Gleevec . Use a sunscreen or wear protective clothing if you must be outside for more than a short time. If vomiting or diarrhea occurs, you will need to take care not to become dehydrated. Contact your doctor for instructions. If you may become pregnant, you must use an effective form of birth control while you take Gleevec . If you have questions about effective birth control, talk with your doctor. Lab tests, including liver function, kidney function, and complete blood cell counts, may be performed while you use Gleevec . These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments. Use Gleevec with caution in the ELDERLY; they may be more sensitive to its effects, especially swelling and fluid retention. Gleevec should be used with extreme caution in CHILDREN younger than 2 years old; safety and effectiveness in these children have not been confirmed. PREGNANCY and BREAST-FEEDING: Gleevec may cause harm to the fetus. Do not become pregnant while you are using it. If you think you may be pregnant, contact your doctor. You will need to discuss the benefits and risks of using Gleevec while you are pregnant. Gleevec is found in breast milk. Do not breast-feed while taking Gleevec . Possible side effects of Gleevec : All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome: Anxiety; bone pain; constipation; cough; diarrhea; dizziness; gas; hair loss; headache; increased tear production; loss of appetite; muscle cramps; muscle or joint pain; nausea; night sweats; nose and throat irritation; stomach pain or upset; taste changes; tiredness; trouble sleeping; vomiting; weakness. Seek medical attention right away if any of these SEVERE side effects occur: Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); black, bloody, or tarry stools; bone pain; change in the amount of urine produced; chest pain; chills, fever, or sore throat; confusion; dark urine; depression; fast or irregular heartbeat; mouth pain, sores, or swelling; pale stools; red, swollen, blistered, or peeling skin; severe or persistent headache; severe stomach pain; severe tiredness or weakness; shortness of breath; slurred speech; sudden, unusual weight gain; swelling of the hands, feet, ankles, or around the eyes; trouble swallowing or talking; unusual bruising or bleeding; vision problems; vomit that looks like coffee grounds; yellowing of the eyes or skin. This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch. If OVERDOSE is suspected: Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center (http://www.aapcc.org), or emergency room immediately. Symptoms may include diarrhea; fever; headache; loss of appetite; muscle pain or spasms; nausea; stomach pain; swelling; unusual bruising or bleeding; unusual tiredness or weakness; vomiting. Proper storage of Gleevec : Store Gleevec at 77 degrees F (25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Gleevec out of the reach of children and away from pets. General information: If you have any questions about Gleevec , please talk with your doctor, pharmacist, or other health care provider. Gleevec is to be used only by the patient for whom it is prescribed. Do not share it with other people. If your symptoms do not improve or if they become worse, check with your doctor. This information is a summary only. It does not contain all information about Gleevec . If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.