药理分类：
因子Xa抑制剂。

“活性成分”（词）：
阿哌沙班每公升2.5毫克，5毫克的药片。

公司
百百时美施贵宝公司和辉瑞公司
指示（S）：
为了降低非瓣膜性房颤（AF）患者中风和全身性栓塞的风险。

药理作用：
阿哌沙班是一种口服的，可逆的，选择性的活性位点抑制因子FXa的，它不需要抗凝血酶III，抗血栓活性。阿哌沙班抑制和血块结合的FXa，凝血酶原活动，对血小板聚集没有直接影响，但间接地抑制凝血酶诱导的血小板聚集，通过抑制FXa的，阿哌沙班降低凝血酶生成和血栓发展。

临床试验：
Eliquis的疗效和安全性的证据是来自亚里士多德，一个跨国企业，Eliquis和华法林的影响比较卒中和非中枢神经系统的全身性栓塞的风险与非瓣膜性房颤患者的双盲研究中。Eliquis优于华法林主要疗效终点卒中或全身性栓塞的相对风险降低了21％，超越华法林（1.27％/年和1.60％/年，HR = 0.79，P = 0.01），与华法林的优势，主要是由于减少出血行程转换为出血性中风和缺血性中风的。纯粹的缺血性中风的发生率相似，这两种药物。Eliquis优于华法林的主要安全终点的严重出血，相对危险度降低了31％（2.13％与3.09％/年/年，HR = 0.69，P <0.0001）。在AVERROES，这项研究的主要目的，是Eliquis，以确定是否优于阿司匹林不认为是候选人的华法林的房颤患者卒中或全身性栓塞的风险在减少。 Eliquis适度增加严重出血，与阿司匹林相比，呈现出显着降低卒中和全身性栓塞的一个预先设定的中期分析的基础上，AVERROES被提前终止。

法律分类：
接收

成人：
5毫克，每天两次，如果有任何以下内容：年龄≥80岁，体重≤60公斤，血肌酐≥神经病变：每公升2.5毫克，每天两次伴随强CYP3A4和P-gp的双重抑制剂（如酮康唑，伊曲康唑，利托那韦，克拉霉素）：每公升2.5毫克，每天两次，如果已经在每公升2.5毫克，每天两次，联合用药，应避免使用华法林的切换：停止华法林时开始Eliquis INR <2开关Eliquis华法林：停止Eliquis，并开始都是下一个剂量Eliquis已采取肠外抗凝和华法林，停止肠外抗凝INR达到可接受的范围内，Eliquis和比华法林等抗凝血剂之间切换：停止正在采取预定在明年剂量开始，停止在至少48小时在手术前与中度至出血或24小时的高风险，低风险的出血中度肝功能损害的程序：..剂量建议不能提供严重肝功能不全：不推荐使用。

儿童：
不成立的。

禁忌（S）：
主动病理性出血。

警告/注意事项：
。增加中风的风险，如果没有足够的连续抗凝治疗心脏瓣膜假体停止：不推荐妊娠劳动和交付（B类）哺乳母亲：不推荐。

互动（补）
。看成人剂量增强的CYP3A4和P-gp的拮抗双重抑制剂伴随强劲的双诱导CYP3A4和P-糖蛋白（如利福平，卡马西平，苯妥英，圣约翰麦芽汁）。避免伴出血的风险增加。阿司匹林，抗血小板剂，纤维蛋白溶解，其他抗凝血剂，肝素，溶栓药物，SSRIs类药物，SNRIs的，非甾体抗炎药。

不良反应（补）
出血。

如何提供：
标签-60，180

最后更新：
2013年2月25日

ELIQUIS
Pharmacological Class:
Factor Xa inhibitor.

Active Ingredient(s):
Apixaban 2.5mg, 5mg; tablets.

Company
Bristol-Myers Squibb and Pfizer
Indication(s):
To reduce risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation (AF).

Pharmacology:
Apixaban is an oral, reversible, and selective active site inhibitor of FXa. It does not require antithrombin III for antithrombotic activity. Apixaban inhibits free and clot-bound FXa, and prothrombinase activity. It has no direct effect on platelet aggregation, but indirectly in­hib­its platelet aggregation induced by thrombin. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development.

Clinical Trials:
Evidence for the efficacy and safety of Eliquis was derived from ARISTOTLE, a multinational, double-blind study in patients with nonvalvular AF comparing the effects of Eliquis and warfarin on the risk of stroke and non-CNS systemic embolism. Eliquis was superior to warfarin in the primary efficacy endpoint of stroke or systemic embolism, with a 21% relative risk reduction beyond warfarin (1.27%/year vs 1.60%/year, HR=0.79, p=0.01). Superiority to warfarin was primarily attributable to a reduction in hemorrhagic stroke and ischemic stroke that converted to hemorrhagic stroke. Purely ischemic strokes occurred with similar rates on both drugs. Eliquis was superior to warfarin for the primary safety endpoint of major bleeding, with a 31% relative risk reduction (2.13%/year versus 3.09%/year, HR=0.69, p<0.0001). In AVERROES, the primary objective of the study was to determine if Eliquis was superior to aspirin for reducing the risk of stroke or systemic embolism in AF patients thought not to be candidates for warfarin. AVERROES was stopped early on the basis of a prespecified interim analysis showing a significant reduction in stroke and systemic embolism for Eliquis compared to aspirin that was associated with a modest increase in major bleeding.

Legal Classification:
Rx

Adults:
5mg twice daily. If any two of the following: age ≥80 years; body weight ≤60kg, serum creatinine ≥1.5mg/dL: 2.5mg twice daily. Con­comitant strong dual inhibitors of CYP3A4 and P-gp (eg, ketoconazole, itraconazole, ritonavir, clarithromycin): 2.5mg twice daily; if already on 2.5mg twice daily, coadministration should be avoided. Switching from warfarin: discontinue warfarin, start Eliquis when INR is <2. Switching from Eliquis to warfarin: discontinue Eliquis and begin both parenteral anticoagulant and warfarin at the time the next dose of Eliquis would have been taken, discontinue parenteral anticoagulant when INR reaches acceptable range. Switching between Eliquis and anticoagulants other than warfarin: discontinue one being taken and begin the other at next scheduled dose. Dis­con­tinue at least 48 hours prior to surgery with moderate-to-high risk of bleeding or 24 hours for procedures with low risk of bleeding. Moderate hepatic impairment: dosing recommendation cannot be provided. Severe hepatic impairment: not recommended.

Children:
Not established.

Contraindication(s):
Active pathological bleeding.

Warnings/Precautions:
Increased risk of stroke if discontinued without adequate continuous anticoagulation. Prosthetic heart valve: not recommended. Labor & delivery. Pregnancy (Category B). Nursing mothers: not recommended.

Interaction(s)
See Adult dose. Potentiated by dual inhibitors of CYP3A4 and P-gp. Antagonized by concomitant strong dual inducers of CYP3A4 and P-gp (eg, rifampin, carbamazepine, phenyt­oin, St. John’s wort); avoid. Increased risk of bleeding with concomitant aspirin, antiplatelet agents, fibrinolytics, other anticoagulants, heparin, thrombolytic agents, SSRIs, SNRIs, NSAIDs.

Adverse Reaction(s)
Bleeding.

How Supplied:
Tabs—60, 180

LAST UPDATED:
2/25/2013