Emend(Aprepitant)-阿瑞吡坦 【中文品名】阿瑞吡坦 【药效类别】抗抑郁药，镇吐药 【通用药名】Aprepitant 【别　　名】MK-0869 【化学名称】 3H-1,2,4-Triazol-3-one, 5-[[[2R,3S]-2-[[1R]-1-[3,5-bis[trifluoromethyl]phenyl]ethoxy]-3-[4-fluorophenyl]-4-morpholinyl]methyl]-1,2-dihydro- 【CA登记号】[170729-80-3] 【结 构 式】 【分 子 式】C23H21F7N4O3 【分 子 量】534.43 【收录药典】USP2000 【开发单位】Merck 【首次上市】2000 【靶      点】为P/神经激肽受体拮抗剂。 【作用机制】为P/神经激肽受体拮抗剂，它是由FDA批准的第一种可帮助患者避免恶心及呕吐-通常在患者接受极易引起呕吐的化疗法治疗后第一天即发生，并可持续几天-这种症状持续发生的药物 【临床阶段】2003年3月美国FDA批准上市 【用法用量】Emend为口服胶囊剂，临床上用于与其它止吐药联合用药。连续三天，每日一次剂量，推荐剂量为化疗前1小时，口服125mg,第二，三天清晨各80mg,无论与食物是否同服均可。 【适 应 症】化疗呕吐 【贮藏条件】常温避光。 【剂    型】胶囊剂。 阿瑞吡坦可预防术后恶心呕吐 美国杜克大学医学中心麻醉科Gan医师报告,NK-1受体拮抗剂阿瑞吡坦(aprepitant)较之常用的镇吐药物昂丹司琼(枢复宁)对减少患者术后呕吐更有效。(Anesthesiology 2005; 103: A769) 该多中心临床试验纳入805例因腹部手术而接受全身麻醉的住院患者。这些患者随机分成三组:口服阿瑞吡坦125mg(1组)和阿瑞吡垣40 mg组(2组),以及静脉注射昂丹司琼4 mg组(3组)。均为术前单次给药,并采用双盲法。 术后最初48小时内,患者在麻醉复苏室接受持续监测,多时点记录呕吐次数,补救治疗恶心或呕吐的次数,以及恶心的严重程度。主要观察终点为术后0~24小时内完全有效(无呕吐及补救治疗)。次要观察终点包括0~24小时内无呕吐、无补救治疗以及0~48小时无呕吐。通过报告的不良事件、体格及实验室检查、苏醒时间以及麻醉后的恢复时间评估耐受性。 结果显示,阿瑞吡坦1组95%和2组90%的患者术后24小时没有发生呕吐,而3组只有74%的患者没有发生呕吐(P<0.001)。相应的术后48小时呕吐发生率分别为93%、85%和67%。三组患者的耐受性差别无显著性,患者对阿瑞吡坦40mg和125 mg均有良好的耐受性。该结果表明阿瑞吡垣预防术后呕吐的作用显著好于昂丹司琼,较大剂量的阿瑞吡坦效果更佳。 Gan医师认为,这个结果非常重要。他说,很多患者都害怕呕吐超过术后疼痛。这是第一次有一种镇吐药可以使超过90%的患者获得持久的镇吐效果。 Medication name Generic name: Aprepitant - Oral Brand name(s): Emend Uses Aprepitant is used with other medications to help prevent nausea and vomiting caused by cancer drug treatment (chemotherapy). This medication is also used to prevent nausea and vomiting after surgery. Aprepitant works by blocking one of the body's natural substances (substance P/neurokinin 1) that causes vomiting.This medication will not treat nausea or vomiting if you already have it. Contact your doctor for further instructions if you are experiencing nausea or vomiting. How to use Read the Patient Information Leaflet available from your pharmacist before you start taking this medication and each time you get a refill. If you have any questions, consult your doctor or pharmacist.Take this medication by mouth, with or without food. To prevent nausea and vomiting caused by cancer chemotherapy, you will usually take the first dose 1 hour before treatment. On the following 2 days, you will usually take the dose once daily in the morning or as directed by your doctor. If you are taking this medication to prevent nausea and vomiting after surgery, you will usually take one dose of 40 milligrams before surgery.Dosage is based on your medical condition (depending on whether you are taking this medication before cancer chemotherapy or surgery) and response to treatment. It is important to follow your doctor's instructions for when to take each dose, how long to keep taking it, and the strength (number of milligrams) of each dose. If you have any questions, consult your doctor or pharmacist.Tell your doctor if you develop nausea or vomiting. Precautions Before using aprepitant, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver problems.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is not known if this drug passes into breast milk. Consult your doctor before breast-feeding. Drug interactions Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.This drug should not be used with the following medications because very serious (possibly fatal) interactions may occur: cisapride, pimozide.If you are currently using either of these medications listed above, tell your doctor or pharmacist before starting aprepitant.Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: drugs affecting liver enzymes that remove aprepitant from your body (such as azole antifungals including itraconazole, macrolide antibiotics including erythromycin, cimetidine, rifamycins including rifabutin, St. John's wort, certain anti-seizure medicines including carbamazepine/phenytoin, certain cancer chemotherapy drugs including ifosfamide/vinblastine/vincristine).Aprepitant can both speed up and slow down the removal of other drugs from your body, thereby affecting how they work. These affected drugs include (not a complete list): benzodiazepines (e.g., alprazolam, midazolam, triazolam), simvastatin, drugs to treat erectile dysfunction-ED or pulmonary hypertension (e.g., sildenafil, tadalafil).If you take warfarin, this drug may affect how well warfarin works in your body. Therefore, your doctor should test your blood during the 2 weeks after your aprepitant treatment to measure how well warfarin is working.This medication may decrease the effectiveness of hormonal birth control such as pills, patch, or ring. This could cause pregnancy. Discuss with your doctor or pharmacist if you should use additional reliable birth control methods while using this medication and for 1 month after stopping this medication. Also tell your doctor if you have any new spotting or breakthrough bleeding, because these may be signs that your birth control is not working well.This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Side effects Tiredness and hiccups may occur. If either of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms of a serious allergic reaction: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345. Missed dose It is important that you take each dose according to the prescribed schedule. If you miss a dose, contact your doctor or pharmacist immediately to establish a new dosing schedule. Overdose If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center. Notes Do not share this medication with others. Storage Store at room temperature between 68-77 degrees F (20-25 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product. Photos by medication strength Click the "Photos" link to see sample photographs for a specific medication strength. Common strengths Emend 125 mg (1)-80 mg (1)-80 mg(1) capsules in a dose pack Emend 125 mg capsule Emend 40 mg capsule Emend 80 mg capsule *The photos shown are samples only. Not all photos of the drug may be displayed. Your medication may look different. If you have questions, ask your pharmacist. Important note HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs. Information last revised July 2012. Copyright(c) 2012 First Databank, Inc. Oral capsule,dose pack Aprepitant| Postoperative Nausea and Vomiting Prophylaxis|Postop Nausea and Vomiting Prophylaxis|Cancer Chemotherapy-Induced Nausea & Vomiting Prophylaxis| Prevent Nausea and Vomiting After Surgery|Prevent Nausea and Vomiting from Cancer Chemotherapy| Selected from NATIONAL DRUG DATA FILE (NDDF) data included with permission and copyrighted by First DataBank, Inc., 2012. This copyrighted material has been downloaded from a licensed data provider. The above information is intended to supplement, not substitute for, the expertise and judgment of your health care professional. You should consult your health care professional before taking any drug, changing your diet, or commencing or discontinuing any course of treatment. 附件: 2011101000141422.PDF -------------------------------------------------------- 产地国家: 土耳其 原产地英文商品名: Emend Tripack 3Cap/box(1*125mg+2*80mg) 原产地英文药品名: Aprepitant 中文参考商品译名: Emend Tripack 3胶囊/盒(1*125毫克+2*80毫克) 中文参考药品译名: 阿瑞吡坦 生产厂家中文参考译名: 默克 生产厂家英文名: Merck Emend(Aprepitant)