Vranckx Pascal, Valgimigli Marco, Heidbuchel Hein
Hartcentrum Hasselt, Faculty of Medicine and Life Sciences, Hasselt UniversityHasselt, Belgium.
Swiss Cardiovascular Center Bern, Bern University HospitalBern, Switzerland.
Arrhythm Electrophysiol Rev. 2018 Mar;7(1):55-61. doi: 10.15420/aer.2017.50.1.
Vitamin K antagonists (VKAs) such as warfarin are the most commonly prescribed oral anticoagulants worldwide. However, factors affecting the pharmacokinetics of VKAs, such as food and drugs, can cause deviations from their narrow therapeutic window, increasing the bleeding or thrombosis risk and complicating their long-term use. The use of direct oral anticoagulants (DOACs) offers a safer and more convenient alternative to VKAs. However, it is important to be aware that plasma levels of DOACs are affected by drugs that alter the cell efflux transporter P-glycoprotein and/or cytochrome P450. In addition to these pharmacokinetic-based interactions, DOACs have the potential for pharmacodynamic interaction with antiplatelet agents and non-steroidal anti-inflammatory drugs. This is an important consideration in patient groups already at high risk of bleeding, such as patients with renal impairment.
维生素K拮抗剂(VKAs),如华法林,是全球最常用的口服抗凝剂。然而,影响VKAs药代动力学的因素,如食物和药物,可导致其偏离狭窄的治疗窗,增加出血或血栓形成风险,并使其长期使用复杂化。直接口服抗凝剂(DOACs)的使用为VKAs提供了一种更安全、更方便的替代方案。然而,必须注意的是,DOACs的血浆水平会受到改变细胞外排转运蛋白P-糖蛋白和/或细胞色素P450的药物影响。除了这些基于药代动力学的相互作用外,DOACs还可能与抗血小板药物和非甾体抗炎药发生药效学相互作用。对于已经有高出血风险的患者群体,如肾功能损害患者,这是一个重要的考虑因素。