房颤卒中预防:了解新的口服抗凝剂达比加群、利伐沙班和阿哌沙班。

Thrombosis Pub Date : 2012-01-01 Epub Date: 2012-09-10 DOI:10.1155/2012/108983
Tan Ru San, Mark Yan Yee Chan, Teo Wee Siong, Tang Kok Foo, Ng Kheng Siang, Sze Huar Lee, Ching Chi Keong
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引用次数: 19

摘要

与维生素K拮抗剂(VKA)不同,新的口服抗凝剂(NOAC)-直接凝血酶抑制剂达比加群和直接激活因子X抑制剂利伐沙班和阿哌沙班不需要常规INR监测。与VKAs相比,它们具有相对快速的起效和较短的半衰期,但在肾脏排泄的相对程度以及与p-糖蛋白膜转运蛋白和肝脏细胞色素P450代谢酶的相互作用方面有所不同。最近完成的比较NOAC和VKAs预防心房颤动(AF)中风的III期试验——RE-LY、ROCKET AF和ARISTOTLE试验至少证明了非劣效性,主要是由于出血性中风的显著减少。与VKA相比,主要和非主要临床相关出血率是可接受的。值得注意的是,与VKA相比,NOAC引起的颅内出血事件明显较少,其机制尚不完全清楚。通过方便的固定剂量给药,NOAC有助于社区AF的抗凝管理,而社区AF迄今尚未得到充分利用。指导方针应该朝着简单的方向发展,以期在初级保健医生中更多地使用NOAC。同时,应强调在肾功能严重受损的患者中谨慎使用它们的必要性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Stroke prevention in atrial fibrillation: understanding the new oral anticoagulants dabigatran, rivaroxaban, and apixaban.

Stroke prevention in atrial fibrillation: understanding the new oral anticoagulants dabigatran, rivaroxaban, and apixaban.

Unlike vitamin K antagonists (VKAs), the new oral anticoagulants (NOACs)-direct thrombin inhibitor, dabigatran, and direct activated factor X inhibitors, rivaroxaban, and apixaban-do not require routine INR monitoring. Compared to VKAs, they possess relatively rapid onset of action and short halflives, but vary in relative degrees of renal excretion as well as interaction with p-glycoprotein membrane transporters and liver cytochrome P450 metabolic enzymes. Recent completed phase III trials comparing NOACs with VKAs for stroke prevention in atrial fibrillation (AF)-the RE-LY, ROCKET AF, and ARISTOTLE trials-demonstrated at least noninferior efficacy, largely driven by significant reductions in haemorrhagic stroke. Major and nonmajor clinically relevant bleeding rates were acceptable compared to VKAs. Of note, the NOACs caused significantly less intracranial haemorrhagic events compared to VKAs, the mechanisms of which are not completely clear. With convenient fixed-dose administration, the NOACs facilitate anticoagulant management in AF in the community, which has hitherto been grossly underutilised. Guidelines should evolve towards simplicity in anticipation of greater use of NOACs among primary care physicians. At the same time, the need for caution with their use in patients with severely impaired renal function should be emphasised.

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