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阿瑞匹坦胶囊EMEND Capsules 80mg(Aprepitant)

药店国别:

产地国家:日本

处方药:

所属类别: 80毫克/胶囊 6胶囊/盒

包装规格: 80毫克/胶囊 6胶囊/盒

计价单位:盒

生产厂家中文参考译名:

生产厂家英文名:Ono Pharmaceuticals

原产地英文商品名:EMEND80mg/cap 6caps/box

原产地英文药品名:Aprepitan

中文参考商品译名:EMEND80毫克/胶囊 6胶囊/盒

中文参考药品译名:阿瑞匹坦

简介

部分中文阿瑞吡坦处方资料(仅供参考)

英文名:Aprepitant

商标名:EMEND

中文名:阿瑞吡坦

生产商:小野制药

药品简介

药物分类名称:选择性NK1受体拮抗止吐药

批准日期:2009年12月

商標名:EMEND

一般名:アプレピタント(Aprepitant)

化学名:5-{[(2R,3S)-2-{(1R)-1-[3,5-Bis(trifluoromethyl)-phenyl]ethoxy}-3-(4-fluorophenyl)morpholin-4-yl]methyl}-1,2-dihydro-3H-1,2,4-triazol-3-one構造式

分子式:C23H21F7N4O3

分子量:534.43

性 状:本品为白色至灰白色粉末,微溶于乙醇(99.5),难溶于乙腈,难溶于水。

药用药理学

作用机制/药理作用

该药物是选择性神经激肽1(NK1)受体拮抗剂止吐药。

(1)神经激肽1(NK1)受体拮抗作用(体外)

1)NK1受体的亲和力抑制125I物质P与中国仓鼠卵巢来源细胞系中表达的人NK1受体的结合,其IC50值为0.1 nmol/L,Kd值为86 pmol/L(Hill 系数=1.1)。

2)对各种NK受体激动剂诱导的反应的作用它对物质PO-甲酯(NK1受体激动剂)诱导的回肠纵向肌肉收缩具有拮抗作用,其Ka值为0.09±0.02nmol/ L(n = 3),它是。 另一方面,对于由(Nle 10)- 神经激肽A(NK 2受体激动剂)诱导的气管收缩和Senseide(NK3受体激动剂)诱导诱导的上颈神经节去极化反应,在1μmol/ L浓度下的作用 没有表现出来。

(2)顺铂诱导的呕吐抑制作用

1)对顺铂诱导的呕吐反应的作用诱导并观察顺铂诱导的雄性雪貂的呕吐反应直至4小时。通过静脉内施用或1个小时顺铂之前口服给药3分钟前,这种药物呕吐反应物剂量依赖性地抑制,3毫克的剂量,在静脉内给药超过1毫克/千克,而在口服给药/kg几乎完全抑制了呕吐反应。

2)由动作顺铂用于反应(诱导24小时诱导的顺铂诱导的急性和延迟呕吐急性呕吐反应雄白鼬)和延迟呕吐反应(72小时后诱导的24小时)观察到。通过口服给药之前给予顺铂2小时后,这种药物抑制随着时间的延伸到第一催吐反应表达呕吐次,几乎完全抑制的剂量为16毫克/公斤的急性和延迟呕吐反应我做到了。

3)联合使用地塞米松和昂丹司琼(5-HT3受体拮抗止吐药)对顺铂诱导的呕吐反应的影响静脉注射0.1mg / kg顺铂和静脉注射地塞米松20 mg / kg或恩丹西酮0.1 通过与静脉内施用mg /kg组合,在施用顺铂后观察到的雄性雪貂的干呕和呕吐次数减少,显示出比每次施用更低的值。

(3)阿扑吗啡和吗啡诱导的呕吐抑制作用该药物通过3mg/kg单次口服给药抑制雪貂皮下给予阿扑吗啡或吗啡引起的中枢性呕吐反应。

适应症与抗肿瘤药

(顺铂等)给药相关的胃肠道症状(恶心,呕吐)(包括晚期)

用法与用量

与其他止吐药物组合,通常125mg抗肿瘤剂作为阿瑞吡坦在第一天给予12岁及以上的成人和儿童,并且从第二天开始每天给药一次或两次80mg。

包装

胶囊125毫克:3粒胶囊(PTP),6粒胶囊(PTP),30粒胶囊(PTP)80毫克:6粒胶囊(PTP),30粒胶囊(PTP)胶囊套装:(125毫克胶囊×1,80毫克胶囊×2)/片

阿瑞匹坦胶囊/板装英文版说明书

EMEND (APREPITANT)Emend InformationEmend is a popular medicine that is also generically known under the name of Aprepitant. This drug is known to block the actions of someharmful 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 IndicationsEmend 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 WarningsBefore 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 GuidelinesYou 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 DosageYou 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 OverdoseIf 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 DoseIf 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 effectsYou 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; theseinclude: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 ReactionsBefore 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.How to take EMENDEMEND, 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, in1 of2 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 33 capsules of EMEND—1 capsule on the day of chemotherapy (30 minutes before chemotherapy) followed

用药温馨提示:当您服用此药物时,需定期接受医疗专业人士的检查,以便随时针对其药效、副作用等情况进行监测。本网站所包含的信息旨在为患者提供帮助,不能代替医学建议和治疗。
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