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 详细处方信息以本药内容附件PDF文件（20125623362414.pdf）的“原文Priscribing Information”为准
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部分中文Ivemend处方资料（仅供参考）

名称：福沙吡坦，又名福沙匹坦

药品名称：
通用名：福沙吡坦二甲葡胺注射剂fosaprepitant dimeglumine Injection
商品名：美国：Emend，在瑞典、捷克、葡萄牙和英国商品名为Ivemend
化学名称：1-Deoxy-1(methylamino)-D-glucitol[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)

剂 型：注射剂

规 格：115mg/10mL

类 别：化药3类

适应症：与其它止吐药联用静脉注射防治中等催吐和大剂量催吐的抗癌药化疗(包括大剂量顺铂)初始和反复用药引起的急性和迟后的恶心和呕吐。

用法用量：本品推荐剂量为115mg，给药方法为静脉注射(15分钟)。

专利情况：化合物专利2015年2月28日到期

专利号：95192860.

药 理：本品是阿瑞匹坦(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。福沙匹坦二甲葡胺与阿瑞匹坦属于称作人P物质/神经激肽1(NK-1)选择性高亲和性受体阻断剂，主要通过阻断大脑恶心和呕吐信号新颖的作用机制发挥作用。阿瑞匹坦对5-羟色胺(5-HT3)、多巴胺和糖皮质激素受体极微弱或无亲和性，用于治疗化疗诱导的恶心和呕吐及术后恶心和呕吐。

国外上市：2008年6月在美国获批上市。

市场前景：
　　由于铂类、阿霉素等多种抗肿瘤药物在使用过程中会产生严重的呕吐反应，急性剧烈的恶心、呕吐可能导致患者脱水、电解质紊乱、营养不良，严重者可能因消化道粘膜损伤而出血、感染甚至死亡，从而使患者的对化疗心存恐惧，依从性明显降低，结果导致化疗减量或中止治疗，严重影响治疗效果，因而止吐药物是抗肿瘤治疗重要的辅助治疗药物，特别是中、重度呕吐的治疗药物使用也主要集中在肿瘤的辅助治疗领域。同时，止吐药物也被用于术后呕吐的预防和治疗。 随着近代社会肿瘤发病率的不断提高，止吐药物的市场容量也水涨船高，一直呈增长态势。2005年止吐类药物的用药金额为2.5亿元，到2009年已经达到5.7亿元。目前其药物品种主要是5-HT3受体拮抗剂司琼类的药物。 NK-1受体拮抗剂具有全新的作用机制的止吐药物，抑制P物质向脑神经中枢发送一种产生恶心和呕吐的信号，从而起到止吐作用。2003年阿瑞匹坦作为第一个NK-1受体拮抗首次在美国上市，开启该领域新的研究方向。它可以明显有效的预防化疗引起的急性恶心和呕吐，而其突出优点是还可以同时预防化疗中的呕吐和延迟性呕吐。2009年默克公司阿瑞匹坦销售额为3.13亿美元，且自从其上市以来其用药金额就一直呈现良好的增长态势。而福沙匹坦是阿瑞匹坦的前体药物，他们在药效上是相当的，且是注射剂型。在治疗过程中，有时呕吐患者口服给药难以实现，这时就需要通过直肠或静脉给药的方式，所以福沙吡坦对于口服阿瑞匹坦来说是个很好的补充。

Ivemend：fosaprepitant
What is Ivemend?
Ivemend is a powder that is made up into a solution for infusion (drip into a vein). It contains the active substance fosaprepitant (115 or 150 mg).

What is Ivemend used for?
Ivemend is an anti‑emetic (a medicine that prevents nausea [feeling sick] and vomiting). It is used with other medicines to prevent nausea and vomiting caused by chemotherapy (medicines used to treat cancer) in adults (aged 18 years or over).

Ivemend works with chemotherapy containing cisplatin (a strong trigger of nausea and vomiting) and with chemotherapy that is a moderate trigger of nausea and vomiting (such as cyclophosphamide, doxorubicin or epirubicin). Ivemend makes chemotherapy more tolerable for the patient.

The medicine can only be obtained with a prescription.

How is Ivemend used?
Ivemend is given as an infusion around 30 minutes before the start of chemotherapy. It is only given on the first day of chemotherapy. The 115‑mg infusion lasts 15 minutes, and the 150‑mg infusion lasts 20 to 30 minutes.

Ivemend must always be given together with other medicines that prevent nausea and vomiting, including a corticosteroid (such as dexamethasone) and a ‘5HT3 antagonist’ (such as ondansetron). If after Ivemend. No aprepitant is given if the 150‑mg dose of Ivemend is used.

How does Ivemend work?
The active substance in Ivemend, fosaprepitant, is a ‘prodrug’ of aprepitant. This means that it is converted to aprepitant in the body. Aprepitant is a neurokinin 1 (NK1) receptor antagonist. It stops a chemical in the body called ‘substance P’ from attaching to the NK1 receptors. When substance P attaches to these receptors, it causes nausea and vomiting. By blocking these receptors, Ivemend can prevent nausea and vomiting, which often happens during and after chemotherapy. Aprepitant has been authorised in the European Union (EU) as Emend since 2003.

How has Ivemend been studied?
To support the use of the 115‑mg dose of Ivemend, the company presented information to show that an infusion of 115 mg Ivemend produces the same amount of aprepitant in the body as one 125‑mg Emend capsule taken by mouth. It also presented information from three studies used to support the authorisation of Emend, in which Emend 125‑mg capsules were used on the first day of chemotherapy in adults receiving chemotherapy including cisplatin or adults with breast cancer receiving cyclophosphamide.

To support the use of the 150‑mg dose of Ivemend, the company presented the results of one study comparing a single 150‑mg infusion of Ivemend with a three-day course of Emend capsules, both in combination with ondansetron and dexamethasone. The study involved over 2,000 adults with cancer who were receiving their first course of chemotherapy including cisplatin. The main measure of effectiveness was the number of patients who did not have any nausea or vomiting over the five days after receiving chemotherapy.

What benefit has Ivemend shown during the studies?
Because Emend 125‑mg capsules and the 115‑mg infusion of Ivemend produce equivalent levels of aprepitant in the body, the benefit shown by Emend in preventing nausea and vomiting when used on the first day of chemotherapy can be applied to this dose of Ivemend.

The study looking at the 150‑mg dose of Ivemend showed that a single 150‑mg infusion of Ivemend was as effective as a three-day course of Emend in preventing nausea and vomiting. Around 72% of both groups did not have any nausea or vomiting over the five days after receiving chemotherapy.

What is the risk associated with Ivemend?
The most common side effects with Ivemend (seen in between 1 and 10 patients in 100) are increased liver enzymes, headache, dizziness, hiccups, constipation, diarrhoea, dyspepsia (heartburn), eructation (burping), loss of appetite, and asthenia or fatigue (weakness or tiredness). For the full list of all side effects reported with Ivemend, see the package leaflet.

Ivemend should not be used in people who may be hypersensitive (allergic) to fosaprepitant or aprepitant, polysorbate 80 or any of the other ingredients. It must not be given at the same time as the following medicines:
pimozide (used to treat mental illness);
terfenadine, astemizole (commonly used to treat allergy symptoms - these medicines may be available without prescription);
cisapride (used to relieve certain stomach problems).

Caution is needed when Ivemend is given with some other medicines. See the package leaflet for full details.

Why has Ivemend been approved?
The CHMP decided that Ivemend’s benefits are greater than its risks and recommended that it be given marketing authorisation.

Other information about Ivemend
The European Commission granted a marketing authorisation valid throughout the European Union for Ivemend to Merck Sharp & Dohme Ltd on 11 January 2008. The marketing authorisation is valid for five years, after which it can be renewed.

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 详细处方信息以本药内容附件PDF文件（20125623362414.pdf）的“原文Priscribing Information”为准
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