Abstract
Direct oral anticoagulants (DOACs) have predictable pharmacokinetics and pharmacodynamics, limited potential for drug to drug interactions, and can be given at fixed doses without the need for routine coagulation monitoring, which makes them a very attractive alternative to vitamin K antagonists. DOACs act by specifically targeting a single coagulation factor, such as Factor Xa or thrombin. Rivaroxaban is a direct Factor Xa inhibitor and has been approved for use in several thromboembolic disorders, such as the prevention of stroke and systemic embolism in adults with non-valvular atrial fibrillation and the prevention of recurrent deep vein thrombosis and pulmonary embolism in adult patients. This review aimed to provide an overview of the mechanism of action of rivaroxaban and outline its pharmacokinetic properties (absorption, distribution, metabolism, and excretion) in healthy adult subjects.
Highlights
BackgroundDirect oral anticoagulants (DOACs) have recently been developed to overcome the limitations of established oral anticoagulants such as vitamin K antagonists (VKAs)
The aim of this review is to provide an overview of the mechanism of action of rivaroxaban and outline its pharmacokinetic properties in healthy subjects
The mean area under the curve (AUC) and Cmax of the 20 mg dose increased by 39% and 76%, respectively with food compared to fasted
Summary
Direct oral anticoagulants (DOACs) have recently been developed to overcome the limitations of established oral anticoagulants such as vitamin K antagonists (VKAs). Rivaroxaban’s moderate tissue affinity could be due to its moderate lipophilicity, as reflected in its partition coefficient value (logP=1.5) [1] This might explain the insignificant effect of body weight on the pharmacokinetics of rivaroxaban (and the fixed-dosing regimens regardless of body weight), as it is unlikely that total vascular bed size and blood volume will vary as much between subjects as body weight itself, which is mainly affected by the amount of body fat [11]. A limitation of this study was once again the small sample size (n=34), but an important strength in contrast to the other studies, was the equal representation of both genders, as well as the greater range of BMIs. The above is in agreement with studies in patients with renal impairment, which have demonstrated that renal impairment results in decreased renal clearance of a single rivaroxaban 10 mg oral dose and increased overall exposure to the drug [25]
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