英文药名: Emend(Aprepitant Capsules)

中文药名: 阿瑞吡坦胶囊

生产厂家: Merck & Co. Inc
药品名称

药品名称: 阿瑞吡坦
英文名: Aprepitant
别 名: Emend
药品类别: 止吐药和催吐药
规格

胶囊剂 80mg, 125mg
 
药理毒理

该药为选择性高亲和性P物质/神经激肽-1（NK1）受体抑制剂，对5-羟色胺（5HT3）、多巴胺和皮质激素受体的亲和力很低。该药可通过血脑屏障，与大脑中NK1受体结合。临床前及临床试验数据表明，该药与5HT3受体抑制剂昂丹司琼及皮质激素地塞米松合用后，可进一步增强后者抑制顺铂所致的急性及迟发性恶心、呕吐的临床疗效。

药动学

用度约为60％～65％，达峰时间（Tmax）为4小时，食物对该药的体内药代动力学影响不大。该药的药代动力学特性呈非线性，血浆蛋白结合率大于95％。该药分布容积大，主要通过药物代谢进行清除，代谢途径包括CYP3A4（主要途径）、CYP1A2和CYP2C19（次要途径）；经肾脏排泄较少。该药血浆清除率为62～90mL/min，半衰期为9～13小时。肝功能不全、肾功能不全以及终末期肾病（ESRD）患者无需调整给药剂量。
 
适应症

高致吐性抗癌化疗药物（包括大剂量顺铂治疗方案）所致的急性和迟发性恶心、呕吐。
用法用量

在化疗前1小时先口服1粒125mg规格胶囊；在随后进行化疗的两天中，每天早上口服1粒80mg规格胶囊。食物对该药吸收无太大影响。老年患者、肾功能不全患者以及正在进行血液透析的终末晚期肾病患者无需调整剂量。

不良反应

研究者曾在大约3300名患者群中对该药的总体安全性进行了评估。与安慰剂相比，该药发生率较高的不良反应包括碱性磷酸酶水平升高、血糖升高、血钠降低、白细胞数增高、红细胞尿及白细胞尿。在不同化疗周期，上述不良反应均有相似表现。在临床试验中，曾经出现过散在的因果关系不明确的严重不良反应病例，包括心动过缓、方向知觉的丧失以及十二指肠溃疡穿孔。曾报告有一位患者在服用该药后出现Stevens-Johnson综合征，而另一位患者曾经出现过血管性水肿和风疹。
注意事项

禁忌症:
该药为中等程度的CYP3A4抑制剂，最好不要与丁酰苯类精神病药匹募齐特（pimozide）、抗组胺药特非那定、阿司咪唑以及促胃肠道动力药西沙必利合用。这是因为抑制CYP3A4可能导致上述药物血浆浓度升高，从而引起严重，甚至是致命的不良的应。 应密切观察给药后化疗患者的临床表现，以防出现急性和迟发性恶心、呕吐。另外，还应注意患者是否存在药物不良反应的表现，如过敏反应、嗜睡和恶心。 应告知患者该药为一种止吐药，可预防和控制成年患者的恶心和呕吐。该药通过随其他药物一起使用，但无法阻止已经发生的恶心和呕吐。如果患者的肝脏存在问题，或者正在服用其他药物、维生素或植物补充剂，则应及早告知医生。应告知患者该药为胶囊剂，应随水一起吞服。应告知患者该药给药方案（见“剂量及用药”项）。食物对该药给药没有影响。该药最常见的副作用为疲乏、恶心、呃逆、便秘、腹泻及食欲减退。
药物相互作用

该药与其他药物（包括主要通过CYP3A4代谢的化疗药物）合用时应小心。该药对CYP3A4的抑制作用可能会导致合用药物的血浓度升高。该药对CYP3A4底物口服制剂的体人药代动力学的影响作用要大于对其静脉制剂的影响。

Emend Description
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.

Emend Directions
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

Emend Cautions
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.

Emend 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.
Emend Active Ingredients

包装规格：

·125mg*6 胶囊
·80mg *4 胶囊
·80mg (2粒) & 125mg (1粒) 3  胶囊