Divisions of Clinical Pharmacology (TAD) and Cardiovascular Medicine (RCB) Duke University Medical Center, Duke Clinical Research Institute (RCB), Durham, NC, USA,
J Thromb Thrombolysis. 2014;37(2):217-33. doi: 10.1007/s11239-013-0967-z.
Anticoagulation for the prevention of stroke is an important aspect of the management of atrial fibrillation. Novel anticoagulants including oral factor Xa inhibitors rivaroxaban and apixaban and the direct thrombin inhibitor dabigatran have emerged as important therapeutic treatment options for prevention of stroke in non-valvular atrial fibrillation. These agents offer practical advantages over traditional vitamin K antagonists, however an understanding of their individual pharmacokinetic and other agent-specific differences is essential for identifying appropriate candidates for therapy, and for selecting the appropriate agent that will be effective and safe. Here, we review the pharmacokinetic process of oral medication use, summarize the newer anticoagulants, their pharmacology, individual pharmacokinetic features, and explore possible explanations for the differences in bleeding outcomes observed in the clinical trials.
抗凝治疗预防中风是心房颤动管理的一个重要方面。新型抗凝药物,包括口服因子 Xa 抑制剂利伐沙班和阿哌沙班以及直接凝血酶抑制剂达比加群,已成为预防非瓣膜性心房颤动中风的重要治疗选择。这些药物在实际应用方面优于传统维生素 K 拮抗剂,然而,为了确定合适的治疗候选者,以及选择将有效且安全的合适药物,了解其个体药代动力学和其他特定药物差异是至关重要的。在这里,我们回顾了口服药物使用的药代动力学过程,总结了新型抗凝药物的药理学、个体药代动力学特征,并探讨了临床试验中观察到的出血结局差异的可能解释。