礼来和Daiichi Sankyo公司共同推出的抗凝血药物Effient (prasugrel)已通过FDA批准，该药用于那些进行过血管修复术去除冠状动脉阻塞的患者，以降低他们的凝血风险，但药物标签需附带警示信息。

Effient获准的依据是一项13608名受试者参加的临床实验。在实验过程中，对比了这种药物和赛诺菲-安万特和百时美-施贵宝同类畅销药Plavix (clopidogrel)的疗效，受试者均为极有可能突发急性心脏病，需要接受血管修复术的高危患者。

将两组受试者的治疗情况进行对比之后发现，在减少患者非致命性心脏病发作几率上Effient疗效更胜一筹，其中Plavix受试组的发作几率为9.1%，而Effient受试组的发作几率则降到7%。然而，FDA称在死亡病例和心肌梗塞发作率方面，两个受试组的情况相当，而那些出现过心肌梗塞的患者使用Effient后再次发作的几率更高。

FDA还表明，在使用Effient治疗的患者当中，出现致命性出血风险的几率也更高，因此要求该药的标签信息中增加相应的警示说明。此外，FDA提醒那些伴有急性病理性出血、轻微中风/中风或急需进行手术治疗(包括冠状动脉搭桥术)的患者不宜使用这种药物进行治疗。FDA新药监管办公室负责人John Jenkins表示：“医生在确定哪些患者适宜采用Effient时，必须对药物疗效和潜在风险再三衡量。”

礼来首席执行官John Lechleiter称，今年2月份Effient已在欧洲获准，而现在又得到了FDA的认可，这对治疗急性动脉综合症来说是一个重要的进展。

Effient Description

Effient is a platelet aggregation inhibitor used to reduce the risk of having another serious heart or blood vessel problem (eg, heart attack, stroke, blood clots in your stent, death). It is intended for use in patients who have had a heart attack, angina, or a procedure called angioplasty.

Effient Directions

Follow the directions for using Effient provided by your doctor. Effient has a MEDICATION GUIDE approved by the U.S. Food and Drug Administration. Read it carefully. Ask your doctor, nurse, or pharmacist any questions that your may have about Effient. SWALLOW WHOLE. Do not break, crush, or chew before swallowing. Effient may be taken on an empty stomach or with food. YOU WILL ALSO NEED TO TAKE ASPIRIN while you take Effient. Check with your doctor about what dose of aspirin to take. STORE EFFIENT at 77 degrees F (25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store in the original container with the lid tightly closed. DO NOT REMOVE THE DESSICANT (gray cylinder) from the bottle. Store away from heat, moisture, and light. Do not store in the bathroom IF YOU MISS A DOSE OF EFFIENT, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. DO NOT take 2 doses at once.

Effient Cautions

DO NOT TAKE EFFIENT if you have had an allergic reaction to it or if you are allergic to any ingredient in this product. DO NOT EXCEED THE RECOMMENDED DOSE without checking with your doctor. DO NOT SUDDENLY STOP EFFIENT without checking with your doctor. This may increase the risk of severe heart problems or death. Laboratory and/or medical tests, including blood pressure, may be performed to monitor your progress or to check for side effects. KEEP ALL DOCTOR AND LABORATORY APPOINTMENTS while you are using/taking Effient. BEFORE YOU HAVE ANY MEDICAL OR DENTAL TREATMENTS, EMERGENCY CARE, OR SURGERY, tell the doctor or dentist that you are taking Effient. If possible, Effient should be stopped for at least 7 days before surgery. Effient may cause dizziness. DO NOT DRIVE, OPERATE MACHINERY, OR DO ANYTHING ELSE THAT COULD BE DANGEROUS until you know how you react to Effient. Using Effient alone, along with other medicines, or with alcohol may lessen your ability to drive or to perform other potentially dangerous tasks.EFFIENT MAY REDUCE THE NUMBER OF BLOOD CELLS THAT ARE NEEDED FOR CLOTTING. To prevent bleeding, avoid situations where bruising or injury may occur. EFFIENT MAY CAUSE A SERIOUS AND SOMETIMES FATAL CONDITION called thrombotic thrombocytopenic purpura (TTP). Contact your doctor right away if you develop purple patches on the skin, fever, weakness, unusually pale skin, yellowing of the skin or eyes, or change in the amount of urine produced. Discuss any questions with your doctor. BEFORE YOU BEGIN TAKING ANY NEW MEDICINE, either prescription or over-the-counter, check with your doctor or pharmacist. CAUTION IS ADVISED WHEN USING EFFIENT IN THE ELDERLY because they may be more sensitive to the effects of Effient, especially the risk of serious and sometimes fatal bleeding (including bleeding in the brain). Effient is usually not recommended in patients older than 74 years old except in high-risk situations (eg, diabetes, history of heart attack). FOR WOMEN: IF YOU PLAN ON BECOMING PREGNANT, discuss with your doctor the benefits and risks of using Effient during pregnancy. IT IS UNKNOWN IF EFFIENT IS EXCRETED in breast milk. IF YOU ARE OR WILL BE BREAST-FEEDING while you are using Effient, check with your doctor or pharmacist to discuss the risks to your baby.

Effient Side Effects

SIDE EFFECTS that may occur while taking Effient include back pain; cough; diarrhea; mild bruising or bleeding; nausea; nosebleeds; or tiredness. If they continue or are bothersome, check with your doctor. CONTACT YOUR DOCTOR IMMEDIATELY if you experience black, tarry, or bloody stools; change in the amount of urine; chest pain; confusion; coughing up blood; dark or bloody urine; dizziness; fast or irregular heartbeat; fever, chills, or persistent sore throat; one-sided weakness; pale skin; purple spots on the skin; seizure; severe or persistent headache; severe or persistent nosebleeds; shortness of breath; speech problems; stomach pain; unusual bruising; unusual or severe bleeding (eg, excessive bleeding from cuts, increased menstrual bleeding, unexplained vaginal bleeding, unusual bleeding from the gums when brushing); unusual tiredness or weakness; vision changes; vomit that contains blood or looks like coffee grounds; or yellowing of the skin or eyes. AN ALLERGIC REACTION to Effient is unlikely, but seek immediate medical attention if it occurs. Symptoms of an allergic reaction include rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue. This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects.

EFFIENT

Indications for EFFIENT

To reduce risk of thrombotic cardiovascular events in patients with acute coronary syndrome who are to be managed with percutaneous coronary intervention (patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI); patients with ST-elevation MI (STEMI) when managed with either primary or delayed PCI).

Adult dose for EFFIENT

Loading dose: 60mg once. Maintenance: 10mg once daily. <60kg: consider 5mg once daily. Take with aspirin (75mg–325mg daily).

Children's dosing for EFFIENT

Not recommended.

Contraindications for EFFIENT

Active pathological bleeding (eg, peptic ulcer, intracranial hemorrhage). Prior TIA or stroke. Do not start if patient likely to undergo urgent CABG.

Warnings/Precautions for EFFIENT

≥75yrs: usually not recommended. Weight <60kg, or CABG or other surgery or trauma, or severe hepatic dysfunction: increased risk of bleeding. Discontinue 7 days before surgery, and if TIA or stroke occurs. Premature discontinuation increases risk for cardiac events (eg, stent thrombosis, MI, death). Pregnancy (Cat.B). Nursing mothers.

Interactions for EFFIENT

Increased bleeding risk with heparin, warfarin, fibrinolytics, chronic NSAID use.

Adverse Reactions for EFFIENT

Bleeding (may be fatal), hyper- or hypotension, hyperlipidemia, headache, back pain, GI upset, dizziness, cough, chest pain, atrial fibrillation, leukopenia; rare: thrombotic thrombocytopenic purpura, thrombocytopenia, anemia, abnormal hepatic function, allergic reactions, angioedema.

How is EFFIENT supplied?

Tabs 5mg—7, 30
10mg—30, 90

Effient (普拉格雷，prasugrel)片

---------------------------------------------------------------
原产地英文商品名:
EFFIENT 10mg/tab 30tabs/box
原产地英文药品名:
PRASUGREL HYDROCHLORIDE
中文参考商品译名:
EFFIENT 10毫克/片 30片/盒
中文参考药品译名:
普拉格雷
生产厂家中文参考译名:
Lilly & Daiichi Sankyo
生产厂家英文名:
礼来&Daiichi Sankyo
---------------------------------------------------------------
原产地英文商品名:
EFFIENT 10mg/tab 90tabs/box
原产地英文药品名:
PRASUGREL HYDROCHLORIDE
中文参考商品译名:
EFFIENT 10毫克/片 90片/盒
中文参考药品译名:
普拉格雷
生产厂家中文参考译名:
Lilly & Daiichi Sankyo
生产厂家英文名:
礼来&Daiichi Sankyo
---------------------------------------------------------------
原产地英文商品名:
EFFIENT 5mg/tab 30tabs/box
原产地英文药品名:
PRASUGREL HYDROCHLORIDE
中文参考商品译名:
EFFIENT 5毫克/片 30片/盒
中文参考药品译名:
普拉格雷
生产厂家中文参考译名:
Lilly & Daiichi Sankyo
生产厂家英文名:
礼来&Daiichi Sankyo
---------------------------------------------------------------
原产地英文商品名:
EFFIENT 5mg/tab 7tabs/box
原产地英文药品名:
PRASUGREL HYDROCHLORIDE
中文参考商品译名:
EFFIENT 5毫克/片 7片/盒
中文参考药品译名:
普拉格雷
生产厂家中文参考译名:
Lilly & Daiichi Sankyo
生产厂家英文名:
礼来&Daiichi Sankyo
---------------------------------------------------------------

药品名称：普拉格雷
商品名为Efient
批准日期：欧盟EMEA 2009年2月25日，美国FDA2009年7月10日，公司：Daiichi Sankyo与Eli Lilly。

一般描述：

Effien含普拉格雷，为噻吩并吡啶类，是P2Y12 ADP受体介导血小板活化和集聚抑制剂。消旋普拉格雷盐酸盐化学名：5-[(1RS)-2-cyclopropyl-1-(2fluorophenyl) -2-oxoethyl]-4,5,6,7- tetrahydrothieno[3,2-c]pyridine-2-yl acetate hydrochloride。盐酸普拉格雷分子式：C20H20FNO3S?HCl，分子量：409.90。结构式：
 
——适应证——

Effient是P2Y12血小板抑制剂，适用于急性冠状动脉综合征患者用经皮冠状动脉介入疗法(PCI)减低血栓性心血管事件(包括支架血栓形成)：即不稳定性心绞痛或非-ST-升高心肌梗死(NSTEMI)；ST-升高心肌梗死(STEMI)用初期或延迟PCI处理患者

——剂量和用法——

起始负荷量与或无食物单次口服60 mg，继续每天1次10 mg；对< 60 kg患者每天1次5 mg；还应每天服用阿司匹林(75 mg至325 mg)。

——禁忌证——

1.活动性病理性出血。2.既往短暂缺血发作或卒中。

——不良反应——

出血，包括危及生命和致死性出血，是报道的最常见不良反应。
黑框警告：出血风险：可引起明显、有时致死出血；急性病理性出血或短暂缺血发作或卒中患者因增加致死和颅内出血及效益不确定不要使用本品；不推荐≥ 75岁患者使用本品，除高危患者(糖尿病或既往心肌梗死[MI])外，此时作用似乎较大可考虑使用；很可能进行冠状动脉旁路手术(CABG)时不要开始用本品。有可能时任何手术前7天中断Effient。以下情况增加出血风险：1.体重< 60 kg；2.出血倾向；3.同时使用增加出血风险药物。用本品时，任何低血压和近期进行冠状动脉血管造影、PCI、CABG或其它手术应怀疑出血。如可能处理出血，不停用。急性冠状动脉综合征后，特别是头几周后停用本品增加随后心血管事件风险。