Gegu Marine, Chevalet Pascal, Piloquet François-Xavier, Berrut Gilles, De Decker Laure
Service de médecine polyvalente gériatrique, Hôpital Bellier, CHU de Nantes, France.
Geriatr Psychol Neuropsychiatr Vieil. 2013 Dec;11(1 Suppl):4-9. doi: 10.1684/pnv.2013.0446.
Treatment with vitamin K antagonists are subject to a common iatrogenic mainly characterized by hemorrhagic stroke. Their narrow therapeutic range associated with variability largely explains this phenomenon. New oral anticoagulants (NOAC) are now available. dabigatran (Pradaxa®) is a direct and specific thrombin inhibitor. It is excreted mainly by the kidney and is the only which can be dialyzed. Rivaroxaban (Xarelto®) and apixaban (Eliquis®) are factor X activated direct inhibitors. They are highly bound to plasma proteins and are metabolized mainly by the liver, via CYP3A4. All NOAC are substrates of P-glycoprotein (P-gp). Due to pharmacological changes, some populations at risk were identified: patients with hepatic impairment, renal impairment, elderly patients or low weight. Some pharmacokinetic or pharmacodynamic drug interactions alter the concentration and the expected impact of NOAC. The NOAC does not require biological monitoring. They interfere with the routine coagulation tests which should be interpreted with caution. Specific tests exist and can be used in case of emergencies. Currently, no antidote is available. The new oral anticoagulant look promising in the elderly. However, certain rules must be followed to reduce the risk of iatrogenic.
维生素K拮抗剂治疗存在一种常见的医源性问题,主要特征为出血性中风。其狭窄的治疗窗以及较大的变异性在很大程度上解释了这一现象。新型口服抗凝药(NOAC)现已上市。达比加群(Pradaxa®)是一种直接且特异性的凝血酶抑制剂。它主要通过肾脏排泄,是唯一可进行透析的药物。利伐沙班(Xarelto®)和阿哌沙班(Eliquis®)是活化X因子直接抑制剂。它们与血浆蛋白高度结合,主要通过肝脏经CYP3A4代谢。所有NOAC都是P-糖蛋白(P-gp)的底物。由于药理学变化,已确定了一些高危人群:肝功能损害患者、肾功能损害患者、老年患者或体重过低者。一些药代动力学或药效学药物相互作用会改变NOAC的浓度和预期效果。NOAC不需要进行生物监测。它们会干扰常规凝血试验,对此应谨慎解读。存在特定检测方法,可在紧急情况下使用。目前尚无解毒剂。新型口服抗凝药在老年人中前景看好。然而,必须遵循某些规则以降低医源性风险。