利伐沙班用于血栓栓塞性疾病的预防和治疗进展

利伐沙班为一种新型的口服直接Xa因子抑制剂,与传统的抗凝剂相比,利伐沙班具有可预测的药动学和药效学特征,较少发生药物-药物和食物-药物方面的相互作用,且不需要常规的凝血监测。但是,利伐沙班不宜与细胞色素P450 CYP3A4和转运体蛋白P-糖蛋白(P-glycoprotein,P-gp)的强抑制剂合用,可能出现药物之间的相互作用。利伐沙班的用药剂量因适应证不同而异,许多研究表明利伐沙班与传统抗凝治疗相比有着良好的受益-风险比。本文旨在概述利伐沙班在不同人群中的主要药动学和药效学特征,以及不同适应证而使用不同剂量的理论依据,为临床医生提供用药指导。

Progress in the prevention and treatment of thromboembolic diseases by rivaroxaban

Rivaroxaban is an oral inhibitor which directly inhibits Xa factor. Compared with the traditional anticoagulant, rivaroxaban has predictable pharmacokinetics and pharmacodynamic characteristics with few drug-drug and food-drug interactions. Routine coagulation monitoring is not needed as well. However, rivaroxaban is not suitable for combination with strong inhibitors of cytochrome P450 CYP3 A4 and P-glycoprotein(P-gp), which may cause drug-drug interaction. The dose regimen of the rivaroxaban varies by indication. Many of the clinical studies have shown that rivaroxaban has a good benefit-risk profile as compared to the traditional standard care. The purpose of this paper is to provide an overview of the main pharmacokinetic and pharmacodynamic characteristics of the rivaroxaban in different populations and the theoretical basis for the use of different dosage regimens in their licensed indications, as well as the practical guidance for professional health care personnel in charge of its application.