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先灵葆雅公司和Cor治疗公司宣布，美国食品与药品管理局（FDA）已批准了新剂型的Integrilin (eptifibatide)用于非急症的经皮冠脉介入术（PCI）放置冠脉内支架的治疗。
Integrilin现在适用于药物治疗或PCI治疗的急性冠脉综合症患者以及PCI术中的患者，后者包括进行冠脉内放置支架的患者。
新疗法是以ESPRIT试验资料为基础的。两家公司在联合声明中说，该试验表明三种剂量的疗法可显著降低心脏病、急性靶血管的血管再形成和死亡的发生率。该试验还表明三种剂量的疗法可减少PCI过程中取出血栓的必要性。这大大减少了副作用的发生。其具体使用方法为，首先以180 mcg/kg的大剂量注射Integrilin，随后立即以每分钟2.0 mcg/kg的剂量灌注，10分钟后再次以180 mcg/kg的大剂量注射。
据此，Integrilin的说明书也做了更改，认为肾功不全的患者应减小剂量，接受PCI的患者的肝素使用剂量也应进行调整，并补充了其它一些安全注意事项。Integrilin由新泽西Kenilworth的先灵葆雅公司和加州南旧金山的Cor治疗公司共同销售。先灵葆雅公司现在负责美国之外的销售，但他们同意以后与Cor治疗公司合作在欧洲共同推广该产品。
Integrilin
Generic Name: eptifibatide (ep ti FYE ba tide)
Brand Names: Integrilin
What is Integrilin?
Integrilin keeps the platelets in your blood from coagulating (clotting) to prevent unwanted blood clots that can occur with certain heart or blood vessel conditions.
Integrilin is used to prevent blood clots or heart attack in people with severe chest pain or other conditions, and in those who are undergoing a procedure called angioplasty (to open blocked arteries).
Integrilin may also be used for purposes other than those listed in this medication guide.
Important information about Integrilin
Do not receive Integrilin if you are allergic to eptifibatide, or to similar drugs such as abciximab (ReoPro) or tirofiban (Aggrastat).
Do not receive Integrilin if you have a stomach ulcer or ulcerative colitis, severe liver disease, severe high blood pressure, a bleeding or blood clotting disorder, a history of head injury, brain tumor, or blood clot in the brain (aneurysm), a stroke or any type of bleeding within the past 30 days, or any type of surgery, injury, or medical emergency within the past 6 weeks.
Integrilin is not expected to be harmful to an unborn baby. However, aspirin is sometimes given with Integrilin, and aspirin can cause bleeding when it is taken during the last 3 months of pregnancy. Aspirin can also cause side effects in a newborn baby.
Tell your doctor if you are pregnant or plan to become pregnant during treatment with Integrilin and aspirin.
Because Integrilin keeps your blood from coagulating (clotting) to prevent unwanted blood clots, it can also make it easier for you to bleed, even from a minor injury. Contact your doctor or seek emergency medical attention if you have bleeding that will not stop.
Before receiving Integrilin
Do not receive Integrilin if you are allergic to eptifibatide, if you have or will soon receive treatment with similar medications such as abciximab (ReoPro) or tirofiban (Aggrastat), or if you have:
kidney disease (or if you are on dialysis);
a severe form of hypertension (high blood pressure);
a bleeding or blood clotting disorder, such as hemophilia or thrombocytopenia;
a history of blood clot in the brain (aneurysm);
if you have had a stroke or any type of bleeding within the past 30 days; or
if you have had any type of surgery, injury, or medical emergency within the past 6 weeks.
Before using Integrilin, tell your doctor if you are allergic to any drugs
FDA Pregnancy Category B. Integrilin is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether Integrilin passes into breast milk or if it could harm a nursing baby. Do not receive Integrilin without telling your doctor if you are breast-feeding a baby.
How is Integrilin given?
Integrilin is given as an injection through a needle placed into a vein. You will receive this injection in a clinic or hospital setting.
If you are receiving this injection during an angioplasty procedure, the medicine will be given throughout the entire procedure and for up to 24 hours after the procedure.
Integrilin is usually given continuously for up to 4 days.
Integrilin is sometimes given together with aspirin.
To be sure Integrilin is not causing harmful effects, your blood will need to be tested on a regular basis. Do not miss any scheduled visits to your doctor.
Because Integrilin keeps your blood from coagulating (clotting) to prevent unwanted blood clots, it can also make it easier for you to bleed, even from a minor injury. Contact your doctor or seek emergency medical attention if you have bleeding that will not stop.
What happens if I miss a dose?
Since Integrilin is usually given in a hospital or clinic setting as needed, it is not likely that you will miss a dose.
What happens if I overdose?
Seek emergency medical attention if you think you have received too much of this medicine.
Symptoms of an Integrilin overdose may include severe bleeding.
What should I avoid while receiving Integrilin?
Integrilin lowers blood cells that help your blood clot. This can make it easier for you to bruise or bleed from an injury or minor cut. Avoid activities that increase your risk of a bruising or bleeding injury. Use extra caution to avoid cuts when brushing your teeth or shaving.
Avoid drinking alcohol while receiving Integrilin. Alcohol may increase your risk of bleeding in your stomach or intestines.
Integrilin side effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have any of these serious side effects:
nosebleed or other bleeding that will not stop;
black, bloody, or tarry stools;
coughing up blood or vomit that looks like coffee grounds;
feeling light-headed, fainting;
sudden numbness or weakness, especially on one side of the body;
sudden headache, confusion, problems with vision, speech, or balance;
fever, chills, body aches, flu symptoms; or
pale skin, easy bruising or bleeding, weakness, fever, and urinating more or less than usual.
Less serious side effects may also occur, such as:
nausea, stomach pain;
runny or stuffy nose, cough, sore throat; or
mild headache or dizziness.
Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.
What other drugs will affect Integrilin?
Before receiving Integrilin, tell your doctor if you are using any of the following drugs:
a blood thinner such as warfarin (Coumadin), heparin, ardeparin (Normiflo), dalteparin (Fragmin), danaparoid (Orgaran), enoxaparin (Lovenox), or tinzaparin (Innohep); or
any other medications used to prevent blood clots, such as alteplase (Activase), anistreplase (Eminase), clopidogrel (Plavix), dipyridamole (Persantine), streptokinase (Kabikinase, Streptase), ticlopidine (Ticlid), or urokinase (Abbokinase).
If you are using any of these drugs, you may not be able to receive Integrilin, or you may need dosage adjustments or special tests during treatment.
There may be other drugs not listed that can affect Integrilin. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.
Where can I get more information?
Your pharmacist has information about Integrilin written for health professionals that you may read.
What does my medication look like?
Eptifibatide is available with a prescription under the brand name Integrilin. Other brand or generic formulations may also be available. Ask your pharmacist any questions you have about Integrilin, especially if it is new to you.
Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.
英文名称: Eftifibatide
英文别名: Eptifibatide; Integrelin; Integrilin; Intrifiban;L-Cysteinamide, N6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl)-L-lysylglycyl-L-a-aspartyl-L-tryptophyl-L-prolyl-, cyclic (1->6)-disulfide
中文名称: 依菲巴特
中文别名: 依非巴特;埃替非巴肽;安普利肽
药理毒理: 利用枸橼酸盐抗凝剂评价，本品抑制血小板聚焦作用较其它非螯合型抗凝剂强 2 ～ 4 倍。本品可使急性冠脉综合征病人及进行 PCI 术病人的出血时间延长 2 ～ 4 倍（与其基线值相比），在停止输注本品后 1 小时内恢复正常。 本品经大鼠、兔和猴的安全性评价试验，未见毒性反应的迹象，给猴连续静脉输注 28 天，每天剂量高达 7.2mg/kg 也未见毒性表现。
适应症: 本品适用于治疗急性冠脉综合征，包括不稳定型心绞痛或无Q波心肌梗塞（既24小时内胸痛持续发作、心电图改变和/或心血管系统酶升高）；也可用于经皮冠脉介入疗法，包括血管成形术或动脉粥样斑块切除术。一般不用于无急性冠脉综合征的血管成形术。在专人监管下，本品可与阿司匹林或肝素辅用。
Integrilin vials should be stored refrigerated at 2-8 degreees celsius (36-46 degrees). Vials may be transferred to room temperature storage for a period not to exceed two months.
INTEGRILIN (eptifibatide) Injection, a potent GP IIb-IIIa inhibitor, helps prevent occlusion of the arteries supplying the heart muscle with oxygen to reduce the incidence of heart attack. INTEGRILIN prevents the aggregation of blood platelets that, when allowed to form clots, can obstruct the flow of blood through the coronary arteries.
INTEGRILIN can be administered upon diagnosis, including the emergency room setting, regardless of whether the patient ultimately undergoes PCI or drug therapy alone.
Treatment with INTEGRILIN has been shown to decrease the rate of a combined endpoint of death or new myocardial infarction (MI) in patients with ACS and the composite of death, MI, or urgent target vessel revascularization in patients undergoing PCI.
Indications:
For the treatment of patients with acute coronary syndrome (UA/NSTEMI), including patients who are to be managed medically and those undergoing percutaneous coronary intervention (PCI)
For the treatment of patients undergoing percutaneous coronary intervention (PCI), including those undergoing intracoronary stenting
Contraindications:
A history of bleeding diathesis, or evidence of active abnormal bleeding within the previous 30 days.
Severe hypertension (systolic blood pressure greater than 200 mm Hg or diastolic blood pressure greater than 110 mm Hg) not adequately controlled on antihypertensive therapy.
Major surgery within preceding 6 weeks.
History of stroke within 30 days or any history of hemorrhagic stroke.
Current or planned administration of another parenteral GP IIb-IIIa inhibitor.
Dependency on renal dialysis.
Known hypersensitivity to any component of the product.
Precautions and Warnings:
In patients undergoing PCI, INTEGRILIN® (eptifibatide) Injection is associated with an increase in major and minor bleeding at the site of arterial sheath placement. Special care should be employed to minimize the risk of bleeding among these patients.
If bleeding cannot be controlled with pressure, infusion of INTEGRILIN and concomitant heparin should be stopped immediately.
Because INTEGRILIN inhibits platelet aggregation, caution should be employed when it is used with drugs that affect hemostasis, including thrombolytics, oral anticoagulants, NSAIDs, and dipyridamole.
Use with other GP IIb-IIIa inhibitors should be avoided.
INTEGRILIN is cleared in part by the kidney and its plasma concentrations are doubled in patients with renal disease (creatinine clearance less than 50 mL/min). Therefore, the infusion dose of INTEGRILIN needs to be reduced to 1 mcg/kg/min in these patients. INTEGRILIN is contraindicated in patients who are dependent upon renal dialysis. If creatinine clearance is not available and serum creatinine is greater than 2 mg/dL, the infusion dose should be reduced to 1 mcg/kg/min.
Caution should be exercised when administering eptifibatide to patients with a platelet count less than 100,000/mm3.
Bleeding is the most common complication encountered during INTEGRILIN therapy. In the registration studies, the majority of excess major bleeding events were localized at the femoral artery access site. Oropharyngeal, genitourinary, gastrointestinal, and retroperitoneal bleeding were seen more commonly with INTEGRILIN compared with placebo. | 
