Clopidogrel(氯吡格雷/阿司匹林复方片)-为新一代的抗血小板药物 作用机制 被活化后的血小板,会释放促血栓性和发炎性的分子:如ADP(腺核甘二磷酸)、血纤维蛋白(Fibrinogen)、血栓素TXA2,且血小板还会在表面表现出活化糖蛋白GP IIb/IIIa receptor。GP IIb/IIIa receptor (血小板上的主要 Fibrinogen receptor)构造的改变使Fibrinogen可键结,促进血小板相互连结,造成血小板凝集体。 Clopidogrel的作用机转为选择性的抑制血小板上ADP受体与ADP之结合,抑制经由ADP媒介的GP IIb/IIIa复合体的活化作用,进而抑制血小板凝集。 Clopidogrel须先经过生体转换才可产生抑制血小板凝集的作用。 除了ADP之外,对于其他可活化血小板的ADP拟似剂,Clopidogrel亦有抑制血小板凝集的作用。 临床效果 具优异的心血管保护作用 CAPRIE试验研究19,185位有粥状动脉硬化和粥状动脉栓塞病史,且最近发生心肌梗塞(<35天)、最近发生中风(介于7天到6个月内)或确定有周边动脉疾病(PAD )的病人。受试者以随机分配方式分成两组,一组每天服用75mg的Clopidogrel,另一组每天服用325mg的Aspirin,追踪1~3年。和Aspirin比较,Clopidogrel明显降低新的血管缺血事件的发生率(心肌梗塞、缺血性中风或其他因血管病变引起的死亡之总合)。将CAPRIE试验分组分析(将心肌梗塞、缺血性中风和周边动脉疾病三组病人分组分析)发现,Clopidogrel与Aspirin相比,对于周边动脉疾病相对危险性降低23.7%,对于缺血性中风相对危险性降低7.3%。针对合并有糖尿病及高血脂病人,Clopidogrel亦有较低的相对危险性。 副作用 更少胃肠道出血副作用 根据CAPRIE之临床试验,Clopidogrel(n=9,599)其安全性和Aspirin(n=9,586)比较,追踪时间1-3年,Clopidogrel 比Aspirin在胃肠道消化不良/恶心/呕吐副作用相对降低15%,胃肠道出血相对降低26%,颅内出血相对降低29%,肝功能不正常相对降低6%。所以很明显地Clopidogrel 75mg/day对胃肠道副作用影响较小。 Coplavix 75mg/100mg 30 Tablets CoPlavix - Concise Prescribing InformationManufacturer: sanofi-aventis Contents: Clopidogrel 75mg, acetylsalicylic acid 100mg Indications:Prevention of atherothrombotic events in patients suffering from non-ST segment elevation acute coronary syndrome (unstable angina/non-Q-wave MI); ST segment elevation acute MI in medically treated patients eligible for thrombolytic therapy. Dosage: Adult &elderly 1 tab as single daily dose. Non-ST segment elevation acute coronary syndrome (unstable angina/non-Q-wave MI) Initially 300 mg as single dose of clopidogrel & an appropriate dose of ASA, then CoPlavix 1 tab once daily for 12 mth. ST segment elevation acute MI Therapy should be started as soon as symptoms start, then continued for at least 4 wk. Overdosage: View CoPlavix overdosage for action to be taken in the event of an overdose. Administration:May be taken with or without food (May be taken w/ meals to reduce GI discomfort.). Contraindications: Severe renal & hepatic impairment, active pathological bleeding eg peptic ulcer/intracranial haemorrhage; allergy to NSAID, patients w/ asthma, rhinitis & nasal polyps; history of peptic ulcer, haemophilia & other bleeding disorders. Galactose intolerance, Lapp lactase deficiency/glucose-galactose malabsorption. Special Precautions:Monitor blood cell count. Patient at risk of increased bleeding from trauma, surgery or other pathological conditions. Discontinue use 7 days prior to surgery. Lesions w/ a propensity to bleed. Recent transient ischaemic attack or stroke. Mild to moderate renal impairment. Moderate hepatic disease. Asthma or allergic disorders, gout, HTN; history of peptic ulcer/gastroduodenal hemorrhage/minor upper GI symptoms. Pregnancy & lactation. Childn. Adverse Drug Reactions:GI bleeding, purpura/bruising & epistaxis. Severe neutropenia & thrombocytopenia. Diarrhoea, abdominal pain & dyspepsia. View ADR Monitoring Form Drug Interactions:Oral anticoagulants, glycoprotein IIb/IIIa inhibitors, heparin, thrombolytics, NSAIDs, uricosurics, methotrexate, ACE inhibitors, acetazolamide, anticonvulsants, β-blockers, diuretics & oral hypoglycemic agents. View more drug interactions with CoPlavix Storage:View CoPlavix storage conditions for details to ensure optimal shelf-life. Description:View CoPlavix description for details of the chemical structure and excipients (inactive components). Mechanism of Action:View CoPlavix mechanism of action for pharmacodynamics and pharmacokinetics details. MIMS Class:Anticoagulants, Antiplatelets & Fibrinolytics (Thrombolytics) ATC Classification:B01AC04 - clopidogrel ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis. Poison Schedule:POM ------------------------------------------------------- 产地国家: 澳大利亚 原产地英文商品名: COPLAVIX (75mg/100mg)/tab 30tabs/box 原产地英文药品名: CLOPIDOGREL/ASPIRIN 中文参考商品译名: COPLAVIX (75毫克/100毫克)/片 30片/盒 中文参考药品译名: 氯吡格雷/阿司匹林 生产厂家中文参考译名: 赛诺菲安万特 生产厂家英文名: Sanofi Aventis |