系统综述达比加群酯与心血管药物相互作用

Interactions between dabigatran etexilate and cardiovascular drugs: a systematic review

心房颤动患者除需长期使用口服抗凝药预防卒中外,还需要联用其他心血管药物。已知达比加群酯(DE)为P糖蛋白(P-gp)的底物,而许多常见的心血管药物可影响P-gp活性,从而改变DE的药动学,进而影响抗凝疗效。DE与许多常见心血管药物的相互作用已有部分临床研究及真实世界的探索,其中抗心律失常药物决奈达隆、奎尼丁、胺碘酮和维拉帕米会导致DE生物利用度增加,地尔硫?、地高辛和他汀类药物(除辛伐他汀和洛伐他汀)对DE药动学参数无显著影响,抗血小板药物、辛伐他汀和洛伐他汀会增加DE出血风险。临床上可根据患者肝、肾功能,病理状态及具体联合药物的情况选择调整DE剂量、更换药物或密切监测等措施。

In addition to the long-term use of oral anticoagulants to prevent stroke, atrial fibrillation patients also need to use other cardiovascular drugs. It is known that dabigatran etexilate(DE) is the substrate of p-glycoprotein(p-gp), and many cardiovascular drugs may affect the pharmacokinetics of DE and its anticoagulant effect by changing p-gp activity. The interaction of DE with many common cardiovascular drugs has been part of clinical research and real-world exploration. Among them, the antiarrhythmic drugs dronedarone, quinidine, amiodarone, and verapamil increase DE bioavailability. Diltiazem, digoxin, and statins(except simvastatin and lovastatin) have no significant effect on the pharmacokinetic parameters of DE. Antiplatelet drugs, simvastatin, and lovastatin increase the risk of bleeding of DE. Clinically, the measures can be chosen such as adjusting the DE dose, changing the drug or closely monitoring according to the liver and kidney function, pathological state and the specific combination of drugs of the patients.