英文药名: Integrilin(Eptifibatide Injection)

中文药名: 依非巴特注射液

生产厂家: Glaxo Smith Kline

药品简介
药品英文名
Eptifibatide

药品别名
依替巴肽、埃替非巴肽、依非巴肽、Integrelin、Integrilin

药理作用
本品为糖蛋白(GP)Ⅱb/Ⅲa受体(血小板凝血因子Ⅰ受体)拮抗药。通过选择性、可逆性抑制血小板聚集的最终共同通路(血浆凝血因子Ⅰ与GPⅡb/Ⅲa结合)，可逆转因血栓形成而导致的缺血状态。

药动学
本品静注后5min可达血药浓度峰值。静脉给药后lh，可显著抑制血小板功能，作用可持续2～4h，药时曲线下面积为1.06μg·h/ml。分布容积约为185ml/kg，分布半衰期为5min。总蛋白结合率为25%。代谢产物脱氨基依替非巴肽和极性代谢物均无活性。本品肾脏清除率为3.79L/h，总体清除率为55～58L/(kg·h)。肾脏排泄率为71.4%，经呼吸排泄不到1%，经粪便排泄不到1.5%。消除半衰期为1.13～2.5h，本品可经血液透析清除。

适应证
用于急性冠脉综合征及经皮冠状动脉介入治疗。

禁忌证
以下患者禁用。
1．对本品过敏者。
2．近30日内有异常出血或有出血倾向者。
3．有出血性脑卒中的病史或近30日内发生脑卒中的患者。
4．肾透析患者。
5．难以控制的严重高血压患者，收缩压大于26.7kPa(200mmHg)或舒张压大于14.7kPa(110mmHg)。6．近6周内做过大手术的患者。
7．血肌酸酐大于或等于4mg/dl者。
8．血小板计数低于100×109/L者。
9．同时胃肠外使用其他糖蛋白Ⅱb/Ⅲa抑制药的患者。
注意事项
1．老人无需调整剂量，但体重小于50kg者，有加重出血的危险性。
2．本品妊娠安全分级为B级。
3．宜尽量减少血管及其他部位创伤，避免在不易压迫止血部位静脉给药。
4．股动脉穿刺部位止血后及患者停用本品和肝素后，应至少观察4h。
5．只有活化部分凝血激酶时间(APTT)小于45s时，才可拔掉动脉导管鞘。接受PCI的患者，应在停用肝素并使其药效消失后才可拔掉动脉导管鞘。
6．如发生不能控制的出血，应立即停用本品和肝素。7．2～8℃保存。
不良反应
l．心血管系统：可出现血压降低。
2．血液：可见淤斑(7%)、血肿(6%)、血尿(0.6%)、血小板减少。有报道，可出现股动脉穿刺部位的大出血(5%～11%)、胃肠道出血(8%)、泌尿生殖道出血(4%)、颅内出血(2%)。
3．中枢神经系统：可出现脑卒中，多为非出血性(脑梗死)，尤其是心率过快、年龄偏大、曾患前壁心肌梗死、暂时性脑缺血或脑卒中、糖尿病病史者。
用法用量
静脉给药。
1．急性冠脉综合征：推荐剂量为180μg/kg，静注，然后以2μg/(kg·min)静滴，直至患者出院或者开始进行冠状动脉旁路移植(CABG)手术，最多持续72h。
2．经皮冠脉介入治疗(PCI)：推荐剂量为手术前180μg/kg，静注，然后以2μg/(kg·min)静滴，并于第1次静注后10min，再次给予180μg/kg静注。滴注时间应维持18～24h(至少12h)。极量：体重超过121kg者，每次静注的最大用量为22．6mg，静滴速度最大为15mg/h。肾功能不全时(血肌酸酐为2～4mg/dl)的急性冠脉综合征：先给予180μg/kg静注，然后以1μg/(kg·min)静滴。PCI患者，先给予180μg/kg静注，然后以1μg/(kg·min)静滴，并于第1次静注后10min，再次给予180μg/kg静注。体重超过121kg者，每次静注的最大用量为22.6mg，静滴速度最大为7.5mg/h。
药物相应作用
1．与阿加曲班、噻氯匹定、双嘧达莫、低分子肝素、萃布地尼(Treprostinil)、尕古树脂(Guggul)、维生素A、软骨素、多昔单抗、非甾体类抗炎药(如阿司匹林)、抗凝药、溶栓药合用，有增加出血的危险性。
2．与当归、茴香、山金车、小槲树、月见草、绣线菊、小白菊、越橘、红醋栗、墨角藻、睡菜、波多、琉璃苣、猫爪草、芹菜、姜黄素、大蒜、黄芪、辣椒素、生姜、蒲公英、银杏、丁香油、卡法(KAVA)、山楂、甘草、益母草、黄芩、丹参、大黄、红花油合用，有增加出血的危险性。
3．本品与呋塞米存在配伍禁忌，但可与阿替普酶、阿托品、多巴酚丁胺、利多卡因、哌替啶、美托洛尔、咪达唑仑、吗啡、硝酸甘油、氯化钾、葡萄糖、氯化钠配伍.

Integrilin Generic Name: Eptifibatide (ep-ti-FIB-ih-tide)Brand Name: Integrilin
Integrilin is used for:
Treating unstable angina (chest pain) or certain types of heart attacks. It may also be used to treat patients undergoing a certain type of procedure (percutaneous coronary intervention [PCI]). It may also be used to treat certain conditions as determined by your doctor that may not be listed in the professional package insert.

Integrilin is a platelet aggregation inhibitor. It works by preventing blood platelets from sticking together and forming blood clots.

Do NOT use Integrilin if:
you are allergic to any ingredient in Integrilin
you have a history of bleeding problems, active bleeding within the past 30 days, stroke or bleeding in the brain, or major surgery or severe injury within the past 6 weeks
you have uncontrolled severe high blood pressure or if you must have kidney dialysis
you are or will be taking another medicine similar to this one
Contact your doctor or health care provider right away if any of these apply to you.

Before using Integrilin :
Some medical conditions may interact with Integrilin . Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

if you are pregnant, planning to become pregnant, or are breast-feeding
if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
if you have allergies to medicines, foods, or other substances
if you have kidney problems or high serum creatinine levels, high blood pressure, or low blood platelet levels (eg, thrombocytopenia)
Some MEDICINES MAY INTERACT with Integrilin . Tell your health care provider if you are taking any other medicines, especially any of the following:

Anticoagulants (eg, warfarin, heparin), aspirin, dipyridamole, nonsteroidal anti-inflammatory drugs (NSAIDs) (eg, ibuprofen), or thrombolytics (eg, alteplase) because risk of bleeding may be increased
This may not be a complete list of all interactions that may occur. Ask your health care provider if Integrilin may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Integrilin :
Use Integrilin as directed by your doctor. Check the label on the medicine for exact dosing instructions. Check the label on the medicine for exact dosing instructions.

Integrilin will be administered as an injection at a hospital. Ask your doctor any questions that you may have about Integrilin .
If you miss a dose of Integrilin , contact your doctor right away.
Ask your health care provider any questions you may have about how to use Integrilin .

Important safety information:
Integrilin may reduce the number of blood cells that are needed for clotting. To prevent bleeding, avoid situations where bruising or injury may occur. Report any unusual bleeding, bruising, blood in stools, or dark tarry stools to your doctor.
After using Integrilin , your doctor may prescribe other medicines to continue your treatment at home. If so, be sure to fill your prescriptions promptly.
Before you have any medical or dental treatments, emergency care, or surgery, tell the doctor or dentist that you are using Integrilin .
LAB TESTS, including platelet counts, blood cell counts, and serum creatinine levels, will be performed to monitor your progress. Be sure to keep all doctor and lab appointments.
Use Integrilin with caution in the ELDERLY because they may be more sensitive to its effects, especially the risk of bleeding.
Integrilin is not recommended for use in CHILDREN; safety and effectiveness have not been confirmed.
PREGNANCY and BREAST-FEEDING: If you plan on becoming pregnant, discuss with your doctor the benefits and risks of using Integrilin during pregnancy. It is unknown if Integrilin is excreted in breast milk. If you are or will be breast-feeding while you are using Integrilin , check with your doctor or pharmacist to discuss the risks to your baby.
Possible side effects of Integrilin :
All medicines may cause side effects, but many people have no, or minor, side effects. When used in small doses, no COMMON side effects have been reported with this product. Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); black, tarry stools; bleeding from gums when brushing or flossing teeth; coughing up blood; excessive bleeding from cuts; increased menstrual bleeding; major bleeding episodes; nosebleeds; one-sided weakness; red urine; redness or pain after an injection; severe headache; stomach pain or swelling; unexplained vaginal bleeding; unusual bruising; vision or speech changes; vomiting blood or material that looks like coffee grounds.

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. You may report side effects to FDA at 1-800-FDA-1088. You may also report side effects at .

If OVERDOSE is suspected:
Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center , or emergency room immediately.

Proper storage of Integrilin :
Vials should be stored refrigerated at 36 to 46 degrees F (2 to 8 degrees C). Protect from light until time of use. Vials may be stored at room temperature between 59 and 86 degrees F (15 and 30 degrees C) for a period of 2 months or less. Do not use past the expiration date. Discard any unused portion left in the vial. Keep Integrilin out of the reach of children and away from pets.

General information:
If you have any questions about Integrilin , please talk with your doctor, pharmacist, or other health care provider.
Integrilin is to be used only by the patient for whom it is prescribed. Do not share it with other people.
If your symptoms do not improve or if they become worse, check with your doctor.
This information is a summary only. It does not contain all information about Integrilin . If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Generic Name for INTEGRILIN
Eptifibatide 0.75mg/mL, 2mg/mL; soln for IV inj.

Legal Classification:
Rx
Pharmacological Class for INTEGRILIN
Antiplatelet (GP IIb/IIIa blocker).

Manufacturer of INTEGRILIN
Merck & Co., Inc.

Indications for INTEGRILIN
For acute coronary syndrome, including patients who are to be managed medically and those undergoing percutaneous coronary intervention (PCI), including those undergoing intracoronary stenting.

Adult dose for INTEGRILIN
See literature. Use in combination with aspirin and heparin. ACS: 180micrograms/kg IV bolus, followed by a continuous IV infusion of 2micrograms/kg/min until discharge or CABG surgery, up to 72 hours. If PCI planned, continue infusion until discharge, or for up to 18–24hrs after procedure, whichever comes first, allowing up to 96hrs of therapy. PCI: 180micrograms/kg IV bolus followed by 2micrograms/kg/min infusion; repeat 180micrograms/kg IV bolus 10minutes after the 1st bolus; continue infusion until discharge, or for up to 18–24hrs, whichever comes first, minimum 12hr-infusion recommended. CrCl <50mL/min: reduce infusion rate to 1microgram/kg/min.

Children's dosing for INTEGRILIN
Not recommended.

Contraindications for INTEGRILIN
Bleeding diathesis or active abnormal bleeding within previous 30 days. Severe uncontrolled hypertension. Major surgery within previous 6 weeks. History of stroke within 30 days or any history of hemorrhagic stroke. Concomitant parenteral GP IIb/IIIa inhibitors. Renal dialysis.

Warnings/Precautions for INTEGRILIN
See literature. Discontinue if uncontrolled bleeding occurs. Platelet count <100,000/mm3. Properly care for femoral artery access site to minimize bleeding. Minimize other arterial and venous punctures, IM inj, catheter use, intubation, NG tubes, to lower bleeding risk; avoid use of non-compressible IV access sites. Do baseline platelet counts, hemoglobin, hematocrit, others and monitor during therapy (see literature). Discontinue if confirmed thrombocytopenia occurs. Renal insufficiency. Pregnancy (Cat.B). Nursing mothers: not recommended.

Interactions for INTEGRILIN
Antiplatelet effects may be potentiated by thrombolytics, oral anticoagulants, NSAIDs, and dipyridamole.

Adverse Reactions for INTEGRILIN
Bleeding, intracranial hemorrhage, stroke, thrombocytopenia, hypersensitivity reactions, hypotension.

How is INTEGRILIN supplied?
Vial 0.75mg/mL (100mL)—1
2mg/mL (10mL, 100mL)—1

相关资料附件：http://www.dailymedplus.com/monograph/view/setid/5ad82e30-50d8-450c-8a2a-b4b507ed1ce2