默克公司近日宣布，美国FDA已批准Emend（a prepitant、阿瑞吡坦）与其他止 吐药联用于刚开始或已多次采用致吐性抗癌药化疗的患者，防止抗癌药引起的恶心呕 吐，如采用高致吐性的铂类抗癌药物。 FDA的这个批准是以一项临床试验为依据，该试验的受试患者为866乳癌患者（其 中99.5%为女性）。在试验中，分别使用Emend（Emend+ 某种ondansetron+5 -HT3受体 拮抗剂+地塞米松+某种皮质类固醇药）和使用一种常规疗法（ondanset ron+地塞米松 ）对受试患者进行治疗，并对两种疗法的效果进行比较。 试验结果显示，使用常规疗法的患者只有51%的人出现了完全应答，而使用 Emend 治疗的患者当中，出现完全应答的人更多。此外，两者相比，Emend在防止患者日常生 活当中出现恶心呕吐的效果更好。 Emend作用模式不同于其它类止吐剂，不能作用于serotonin (5-HT3)、 dopamine和corticosteroid的接受器。它能阻止一种会引起恶心和呕吐的神经传递因子Substance P在脑部发生效用。 Emend仅用于预防化疗可能出现的呕吐，而不作为开始呕吐后的止吐用药。 处方信息摘要    （阿瑞）胶囊 美国初步批准：2003 适应症 校订®是P物质/神经激肽1（激肽1）受体拮抗剂，表示： 在与其他止吐剂的组合： 急性和延迟性恶心和呕吐的预防与高致吐性癌症化疗初期和重复课程（港灯）包括高剂量顺铂 恶心，呕吐的预防与癌症化疗致吐性中等（教育部）初始和重复的课程 对术后恶心和呕吐（PONV）预防 使用限制 没有研究的恶心和呕吐的既定治疗。 长期连续服用，不建议。   剂量和用法 化疗引起的恶心和呕吐的预防 校订，给出了三天，作为引起的恶心和呕吐（CINV之）疗程的化疗，其中包括类固醇和5 - HT3受体拮抗剂的一部分。 作者校订125毫克的建议剂量是前1小时口服化疗（第一天）和80毫克口服一次是在2和3的日子每天早上。 校订注射（福沙吡坦dimeglumine）可能代替口头订正（125毫克）第1天只作为化疗呕吐方案的一部分。 预防术后恶心和呕吐 推荐的校订口服剂量为术后恶心和呕吐（PONV）的标志是40前的3小时内麻醉诱导毫克。 剂型和优势 胶囊：40毫克，80毫克，125毫克 禁忌 过敏的任何这种药物的组成部分。 校订不应该同时使用与匹莫齐特，特非那丁，阿司咪唑，西沙必利或，由于受抑制CYP3A4的阿瑞可能会导致这些药物的血药浓度升高，可能造成严重或危及生命的反应。 注意事项： 与华法林（一CYP2C9的底物）阿瑞合用可能导致国际标准化比值临床显着降低凝血酶原时间（印度卢比）。  在28天期间和之后的最后一剂荷尔蒙避孕药校订疗效可能会减少。替代或避孕备份方法应该被使用。 校订是CYP3A4的剂量依赖性抑制，并应与接受的CYP3A4的代谢主要是通过合并用药的病人慎用。  行使时，应注意患者的肝功能损害严重管理。   不良反应 结合化疗呕吐的高度和中度致吐性化疗（发生率“10％）治疗的临床不良反应有：脱发，厌食，乏力/疲劳，便秘，腹泻，头痛，打嗝，恶心。 对于术后恶心呕吐方案（发生率“5％）临床不良反应有：便秘，低血压，恶心，瘙痒，发热。 药物相互作用 阿瑞是CYP3A4的底物，因此，校订合用药物抑制或诱导CYP3A4的活性，可能会导致阿瑞，分别增加或降低血浆浓度。 阿瑞是CYP2C9的诱导，因此，合用的订正是由CYP2C9的药物（如华法令，甲苯磺丁脲）代谢，可能会导致这些药物的血药浓度低。 适应症 预防化疗引起的恶心和呕吐（CINV之） EMEND1，与其他止吐药物制剂，被用于： 急性和延迟性恶心和呕吐的预防与高致吐性癌症化疗初期和重复课程（港灯），包括高剂量顺铂 恶心，呕吐的预防与癌症化疗致吐性中等。 ------------------------------------------------------------------------------------ How to take EMEND EMEND, in combination with other medicines, helps prevent CINV. EMEND is given on the first day of chemotherapy and for 2 days afterward. Take EMEND exactly as prescribed. Your doctor may prescribe EMEND, along with other medicines, in 1 of 2 ways: EMEND for Injection on the day of chemotherapy given by an I.V., followed by a capsule of EMEND on Day 2 and Day 3 3 capsules of EMEND—1 capsule on the day of chemotherapy (30 minutes before chemotherapy) followed by a capsule of EMEND on Day 2 and Day 3 EMEND (APREPITANT) Emend Information Emend is a popular medicine that is also generically known under the name of Aprepitant. This drug is known to block the actions of some harmful chemicals that are found in the patient’s organism and that usually trigger vomiting and nausea. Therefore, this medicine is widely used to prevent vomiting and nausea (these might be caused by cancer chemotherapy or surgery). This drug is unable to treat vomiting and nausea (it can only prevent them). Emend Indications Emend is a medicine that is usually prescribed to patients who are suffering from severe nausea and vomiting. However, this medicine might also be used to treat or to prevent some other medical disorders that have not been listed here. Emend Warnings Before you start taking Aprepitant, you must alert your doctor if you are suffering from liver disease. In this case, you may not be allowed to start taking this drug, or you might have to take in a lower dose of Emend. This drug is known to sometimes decrease the effectiveness of several birth-control pills, thus enabling the patient to become pregnant. During your treatment with this drug, you should use a non-hormonal birth control method (for example a diaphragm, spermicides or condoms). Emend is a category B FDA pregnancy drug. Therefore, even if it is taken during pregnancy, this medicine should not have harmful effects on a growing fetus. However, it is highly recommended that you consult with your personal physician before you start taking this medicine if you are pregnant or if you are planning to be pregnant soon. It is not known whether Emend’s main ingredients are able to pass into breast milk or not. You should consult with your doctor before you start a treatment with this medicine if you are currently breastfeeding your child.  Emend Intake Guidelines You should take this drug according to your personal doctor’s instructions. If you fail to understand some of them, you should ask a pharmacist, a doctor or a nurse for further explanations. You should carefully read the information in the medicine’s label for further instructions and advice. You must accompany each dose of Emend with a glass of water (8 ounces of liquid). The first dose of Aprepitant should be taken 3 hours before a major surgery or 1 hour before a chemotherapy treatment. Sometimes this drug is combined with some other medicines, in order to increase its effectiveness. Emend should be kept out of the children’s reach, away from heat, direct sunlight and moisture.   Emend Dosage You should ask your doctor to tell you the dose of Emend that should work best for you. This drug’s dosage is known to vary from one case to another, because it depends on a variety of factors such as age, general health condition, etc. You must not make any adjustments to the dose that you have been prescribed without asking your physician first. Emend Overdose If you suspect that you are suffering from overdose with Emend, you are in need of medical care. Overdose symptoms with this medicine usually include headache and drowsiness. Emend Missed Dose If you happen to miss one of your Emend doses, take it as soon as you remember. If it is time for another Aprepitant dose, you should skip the one that you have missed and proceed with your regular treatment. Do not take a double dose of this medicine without your physician’s approval. Emend side effects You should seek emergency medical help if you are experiencing any of these symptoms of an allergic reaction: difficulty breathing; hives; swelling of your face, tongue, lips, or throat. Alert your physician if you have any of these severe side effects: slow heart rate; light-headedness, fainting; pale skin, easy bleeding or bruising; burning or pain when you urinate. Some other, less severe side effects are also more common; these include: tiredness or weakness; nausea, vomiting, stomach pain, heartburn; diarrhea or constipation; hiccups; loss of appetite; dizziness; headache; increased thirst or dry, hot skin; ringing in your ears; fever, chills, flu-like symptoms,  body aches; Insomnia. Other side effects might also be triggered by a prolonged treatment with Emend. You should alert your physician if you experience anything unusual during your treatment with it. Emend Drug Reactions Before you start taking Emend, you should tell your personal doctor if you are also taking any of the following medicines: certain cancer drugs such as irinotecan (Camptosar), etoposide (VePesid), imatinib (Gleevec), ifosfamide (Ifex), vinblastine (Velban), vinorelbine (Navelbine), or vincristine (Oncovin, Vincasar); tolbutamide (Orinase); blood thinners like warfarin (Coumadin); phenytoin (Dilantin); steroid drugs such as methylprednisolone (Medapred, Solu-Medrol) , or dexamethasone (Decadron, Hexadrol); midazolam (Versed) or other similar drugs like Tranxene, Valium, Xanax, etc; antibiotics for example clarithromycin (Biaxin), ketoconazole (Nizoral), itraconazole (Sporanox), troleandomycin (Tao), rifampin (Rifater, Rifamate), etc; HIV drugs such as lopinavir/ritonavir (Kaletra), nelfinavir (Viracept), atazanavir (Reyataz), ritonavir (Norvir), or nelfnavir (Viracept); seizure drugs such as phenytoin (Dilantin) or carbamazepine (Tegretol, Carbatrol); antidepressants such as paroxetine (Paxil) or nefazodone (Serzone); diltiazem (Cardizem, Tiazac, Cartia). You should ask for your doctor’s consent before taking any other medicines, even if they are simple over-the-counter drugs like vitamins, minerals, herbal products, cold or cough medicines, etc.