简介：

中文名称: 福沙吡坦二甲葡胺
英文名称: Fosaprepitant dimeglumine
英文同义词: Fosaprepitant dimeglumine;D-Glucitol, 1-deoxy-1-(methylamino)-, (3-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4- morpholinyl)methyl)-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl)phosphonate (2:1) (salt);Mk-0517;Phosphonic acid, (3-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4-morpholinyl)methyl)-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl)-, compd. with 1-deoxy-1-(methylamino)-D-glucitol (1:2);Unii-D35fm8T64x
FDA批准福沙吡坦二甲葡胺注射剂上市
FDA批准默克公司的福沙吡坦二甲葡胺注射剂（fosaprepitant dimeglumine，Emend）上市，与其他止吐药联合静脉注射，防治中等催吐和严重催吐抗癌药在化疗（包括大剂量顺铂）初始或反复用药时引起的急性和迟发性恶心和呕吐。本品是阿瑞吡坦（aprepitant）口服制剂的前体药物，注射后在体内迅速转化成阿瑞吡坦。
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.
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125 mg(1组)和阿瑞吡垣40mg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。
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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 (30minutes before chemotherapy) followed by a capsule of EMEND on Day2 and Day 3 
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