Indications for PRADAXA:

To reduce risk of stroke and systemic embolism in non-valvular atrial fibrillation (AF). Treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE) in patients treated with parenteral anticoagulant for 5–10 days. To reduce risk of recurrent DVT/PE in patients who have been previously treated.

Adult:

Swallow whole. Non-valvular AF: CrCl>30mL/min: 150mg twice daily. Severe renal impairment (CrCl 15–30mL/min): 75mg twice daily; CrCl<15mL/min or on dialysis: not recommended. Moderate renal impairment (CrCl 30–50mL/min) with concomitant dronedarone or systemic ketoconazole: consider reducing dose to 75mg twice daily. CrCl <30mL/min with concomitant P-gp inhibitors: avoid. DVT, PE: CrCl>30mL/min: 150mg twice daily after 5–10 days of parenteral anticoagulation. CrCl <30mL/min or on dialysis: not recommended. CrCl <50mL/min with concomitant P-gp inhibitors: avoid. Converting from/to warfarin, other anticoagulants: see full labeling. Take missed dose as soon as possible on same day; skip dose if it cannot be taken at least 6hrs before the next scheduled dose; do not double doses.

Children:

Not established.

Pharmacological Class:

Direct thrombin inhibitor.

Contraindications:

Active pathological bleeding. Mechanical prosthetic heart valve.

Warnings/Precautions:

Premature discontinuation increases risk of thrombotic events; if discontinued for reason other than bleeding or therapy completion, consider coverage with another anticoagulant. Increased risk of spinal/epidural hematoma in anticoagulated patients receiving neuraxial anesthesia or undergoing spinal puncture; monitor for signs/symptoms of neurological impairment. Increased risk of serious bleeding. Promptly eva luate signs/symptoms of blood loss (eg, a drop in hemoglobin and/or hematocrit or hypotension). Suspend treatment before invasive therapy or surgery, including dental procedures (see full labeling); restart promptly. Bioprosthetic heart valve: not recommended. Avoid lapses in therapy. Monitor renal function prior to initiation, then periodically as clinically indicated; discontinue if acute renal failure develops and consider alternate therapy. Bleeding risk can be assessed by ecarin clotting time (ECT), or if not available, aPTT. Severe renal impairment. Elderly (>75yrs). Labor & delivery. Pregnancy (Cat.C). Nursing mothers: not recommended.

Interactions:

Antagonized by P-gp inducers (eg, rifampin); avoid. Increased dabigatran levels in renal impairment with concomitant P-gp inhibitors (eg, [dronedarone, systemic ketoconazole; reduce dabigatran dose], verapamil, amiodarone, quinidine, clarithromycin). Concomitant NSAIDs, platelet inhibitors, heparin, fibrinolytic therapy: increased risk of bleeding. Switching to or from warfarin: monitor closely.

Adverse Reactions:

Gastritis-like symptoms (eg, GERD, esophagitis, erosive gastritis, gastric hemorrhage, ulcer), bleeding (may be fatal).

Metabolism:

Hepatic.

Elimination:

Renal.

How Supplied:

Caps—60


美国FDA批准Pradaxa(达比加群酯[dabigatran etexilate])胶囊
批准日期：2010年10月19日：公司：勃林格殷格翰Boehringer Ingelheim Pharmaceuticals, Inc.
译自：http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022512s000lbl.pdf和
http://www.drugs.com/newdrugs/fda-approves-pradaxa-prevent-stroke-atrial-fibrillation-2370.html
美国食品和药品监督管理局2010年10月19日批准Pradaxa胶囊(达比加群酯)为在有心律异常(心房颤动)患者中预防中风和凝血.
心房颤动累及超过200万美国人，涉及心脏上面两个腔室非常迅速和不协调收缩(心房)和心律异常的最常见类型之一。
美国FDA药物评价和研究中心心血管和肾产品室主任Norman Stockbridge, M.D., Ph.D.说：“心房颤动的人属于发生血凝块的高危人群，如凝块以致脑可中风致残”
Pradaxa是一种抗凝剂通过抑制凝血酶起作用，一种涉及血液凝固的酶。在一项临床试验比较Pradaxa与抗凝剂华法林[warfarin]研究Pradaxa的安全性和有效性。在试验中, 服用Pradaxa患者中风比用华法林患者较少。
Stockbridge说“与华法林不一样，前者需要患者定期进行监查血液检验，Pradaxa 不需要这类监查”。
如同其它被批准的抗凝血药，出血，包括危及生命和致命出血，是用Pradaxa治疗患者中报道的最常见不良反应。胃肠道症状，包括胃内不适感(消化不良), 胃痛, 恶心, 心灼热,和还报道胃气胀。
处方资料的重点
请参阅AFINITOR完整处方资料。
为口服用PRADAXA? (达比加群酯甲磺酸盐)胶囊
美国最初批准：2010
适应证和用途
PRADAXA是一种直接凝血酶抑制剂适用于有非瓣膜性心房颤动患者中减低中风和全身栓塞的风险(1)
剂量和给药方法
（1）对有CrCl >30 mL/min患者：150 mg口服，每天2次(2.1)
（2）对有CrCl 15-30 mL/min患者：75 mg口服，每天2次(2.1)
（3）指导患者不要咀嚼，弄碎，或打开胶囊(2.1)
（4）复习对转换至或从其它口服或非肠道抗凝剂的建议(2.2, 2.3)
（5）当可能时在损伤性或手术操作前暂时停止PRADAXA，然后立即在开始(2.4)
剂型和规格
胶囊：75 mg和150 mg (3)
禁忌证
（1）活动病理性出血(4)
（2）对PRADAXA严重超敏性反应史(4)
警告和注意事项
出血的风险：PRADAXA可能引起严重和，有时，致命出血。及时评价失血的征象和症状(5.1)
暂时停止：避免治疗中过失以缩小中风的风险(5.2)
P-gp诱导剂和抑制剂：避免利福平[rifampin]与PRADAXA同时给药因为对达比加群暴露的影响(5.3)
不良反应
最常见不良反应(>15%)是胃炎-样症状和出血 (6.1)
为报告怀疑的不良反应，联系Boehringer Ingelheim Pharmaceuticals, Inc.电话(800) 542-6257或(800) 459-9906 TTY或FDA电话1-800-FDA-1088或www.fda.gov/medwatch.
在特殊人群中的使用
老年人使用：出血的风险随年龄增加(8.5)
一般描述
达比加群酯甲磺酸盐，一种直接凝血酶抑制剂的化学名是β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl] amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate。经验式为C34H41N7O5  CH4O3S和分子量723.86(甲磺酸盐)，627.75(游离碱)结构式为：