阿昔单抗    Abciximab 
中文别名：  阿昔单抗、抗血小板凝聚单克隆抗体
英文别名：  Centorx、Reopro
生产企业：  
药品类别：  其它循环系统用药 
 
药理药动 
本品选择性阻断血小板糖蛋白Ⅱb／Ⅲa受体，而防止纤维蛋白元、血小板凝集因子(VWD)、玻璃体结合蛋白及纤维蛋白结合素与激活的血小板结合。
本品是一种带有精氨酸-甘氨酸-天门冬氨酸(RGD)合成的肽按顺序与血小板糖蛋白Ⅱb／Ⅲ受体结合。本品不是与RGD位点结合，而是阻断大分子进入受体(通过空间障碍和／或结构形态的作用)。
本品为嵌合性单克隆抗体7E3的碎片，它与血小板表面的糖蛋白Ⅱb／Ⅲa受体结合，以阻断纤维蛋白元，VWD因子和其它有粘性的分子与受体位点结合，从而抑制血小板聚集防止形成血栓，堵塞血流而致心肌急性缺血。 
药动学 
静脉注射本品后，游离血小板数量迅速下降，主要发生在第一个半衰期(10min)内和第二个半衰期(30min)内，作用快可能是因为该药与血小板糖蛋白Ⅱb／Ⅲa受体结合迅速。与以每分钟10mg阿司匹林给药的患者作对照，本品静脉滴注(0.25mg/kg)2小时后，抑制了90％以上的血小板凝集。给药10天后，仍出现少量的糖蛋白Ⅱb／Ⅲa受体阻断。 
适 应 症 
本品适用于经皮穿刺冠状血管成形术或动脉粥样化切除术，为防止病人突然发生冠状血管堵塞引起心肌急性缺血的辅助治疗。
处于突然发生堵塞的高危病人，至少要伴有以下情况之一：不稳定的心绞痛或无Q性心肌梗塞；在12小时内发作的急性Q性心肌梗塞；在扩张动脉时Ⅱ型血管损伤；至少65岁以上的妇女，在扩张动脉时Ⅰ型血管损伤；糖尿病人扩张动脉时Ⅰ型血管损伤或与7日内发生的心肌梗塞有关的血管成形术。在这些情况下，本品与阿司匹林和肝素是必须使用的。
本品对正在进行的血管成形术有抗血栓形成的活性并可预防血管再狭窄的发生。 
用法用量 

在血管成形术前10分钟，由静脉滴注本品按每公斤体重250μg，滴注1分钟以上，然后以每分钟滴入10μg，维持12小时。
[制剂与规格]静脉注射剂：每小瓶(5ml)含本品10mg。
[贮藏]本品应冷藏，但不可冻结或振摇。
不良反应 
给药后36小时出血是最常见的不良反应。因此，本品不应给予活动性出血或有出血倾向的病人。
其它不良反应包括低血压、恶心、呕吐、头痛、心动过缓、发热和血管功能障碍等。 
禁忌症 
给药后36小时出血是最常见的不良反应。因此，本品不应给予活动性出血或有出血倾向的病人。
本品还未经过动物遗传研究，因此尚不清楚用于孕妇时会否引起致命危害或影响胎儿。除非确实需要，才能将本品用于孕妇。本品对儿童及哺乳期妇女的安全情况尚未确定，故不宜使用。
由于本品会增加出血的危险，故有以下情况者禁用：急性内出血；近期内(6周内)胃肠道出血或泌尿道出血；2年内的脑意外损伤；脑损伤出现明显的神经系统缺陷；有出血倾向；7天内口服抗凝药(除非凝血时间低于对照组的1.2倍)；血小板减少症(＜100000 cells/ul)；近期内(6周内)作过大的外科手术或有严重损伤；颅内肿瘤；动静脉畸形或动脉瘤；严重的失控性高血压；有脉管炎史；经皮透腔血管成形手术前或手术中注射了右旋糖酐者；对本品或鼠蛋白过敏者。 
药物相互作用 
由于本品有抑制血小板凝集的作用，故在与其它影响凝血的药物合用时要谨慎。这些药物包括：溶血栓药、口服抗凝药、非甾体抗炎药及潘生丁等。本品不能与低分子右旋糖配合用，在11例既用本品又用低分子右旋糖酐的病例中，5例发生大出血，4例发生轻微出血，而5例以安慰剂合用低分子右旋糖酐的病人未出现出血。

Abciximab
Abciximab (ReoPro)
(ab- SIX-ih-mab)
Pregnancy Category: C ReoPro (Rx)

Classification: Antiplatelet agent

Action/Kinetics: Abciximab is the Fab fragment of the chimeric human-murine monoclonal antibody 7E3. It binds to a glycoprotein receptor on human platelets, thus inhibiting platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor, and other adhesive molecules to receptor sites on activated platelets. t 1/2, after IV bolus: 30 min. Recovery of platelet function: About 48 hr, although the drug remains in the circulation bound to platelets for up to 10 days. Following IV infusion, free drug levels in the plasma decrease rapidly for about 6 hr and then decline at a slower rate.

Uses: Inhibition of platelet aggregation. Adjunct to percutaneous transluminal coronary angioplasty or atherectomy for prophylaxis of acute cardiac ischemic complications in clients at high risk for abrupt closure of the treated coronary vessel. Used with aspirin and heparin. Adjunct with heparin to prevent cardiac ischemic complications in those undergoing PCI; also, for unstable angina clients not responding to conventional therapy when PCI is scheduled within 24 hr.

Contraindications: Due to a potential for drug-induced bleeding, abciximab is contraindicated as follows: history of CVA (within 2 years) or CVA with a significant residual neurologic deficit; active internal bleeding; within 6 weeks of GI or GU bleeding of clinical significance; bleeding diathesis; within 7 days of administration of oral anticoagulants unless the PT is less than 1.2 times control; thrombocytopenia (less than 100,000 cells/?within 6 weeks of major surgery or trauma; intracranial neoplasm; arteriovenous malformation or aneurysm; severe uncontrolled hypertension; presumed or documented history of vasculitis; use of IV dextran before atherectomy or intent to use it during atherectomy; hypersensitivity to murine proteins.

Special Concerns: Assess benefits versus the risk of increased bleeding in clients who weigh less than 75 kg, are 65 years of age or older, have a history of GI disease, are receiving thrombolytics, and are receiving heparin. The following conditions are also associated with an increased risk of bleeding in the angioplasty setting and which may be additive to that of abciximab: atherectomy within 12 hr of onset of symptoms for acute MI, atherectomy lasting more than 70 min, and failed atherectomy. Use with caution when abciximab is used with other drugs that affect hemostasis, including thrombolytics, oral anticoagulants, NSAIDs, dipyridamole, and ticlopidine. Use with caution during lactation. Safety and efficacy have not been determined in children.

Side Effects: CV: Increased bleeding tendencies hypotension, bradycardia, atrial fibrillation or flutter, vascular disorder, pulmonary edema, complete AV block supraventricular tachycardia, weak pulse, palpitations, intermittent claudication, pericardial effusion, limb embolism, pulmonary embolism, ventricular arrhythmia. GI:N&V, diarrhea, constipation, ileus. Hematologic: Thrombocytopenia, anemia, leukocytosis, hemolytic anemia, petechiae. CNS: Hypesthesia, confusion, abnormal thinking, dizziness, coma, brain ischemia insomnia. Respiratory: Pleural effusion, pleurisy, pneumonia. Musculoskeletal: Myopathy, cellulitis, myalgia. GU: Urinary tract infection, urinary retention, abnormal renal function. Miscellaneous: Pain, peripheral edema, abnormal vision, development of human antichimeric antibody, dysphonia, pruritus.

Drug Interactions: Bromelain / Potential for  bleeding risk Evening primrose oil / Potential for  antiplatelet effect Feverfew / Potential for  antiplatelet effect Garlic / Potential for  antiplatelet effect Ginger / Potential for  antiplatelet effect Ginkgo biloba / Potential for antiplatelet effect Ginseng / Potential for  antiplatelet effect Grapeseed extract / Potential for  antiplatelet effect

How Supplied: Injection: 2 mg/mL

Dosage
?IV Bolus Followed by IV Infusion Clients undergoing atherectomy with concomitant use of heparin and aspirin.
IV bolus: 0.25 mg/kg given 10-60 min before the start of atherectomy. This is followed by continuous IV infusion: 10 mcg/min for 12 hr.