From the Guidelines
Rivaroxaban works by inhibiting Factor Xa, a key enzyme in the blood clotting cascade, which prevents the formation of thrombin and subsequent clot development. This mechanism of action is supported by the study published in Circulation in 2016 1, which summarizes the randomized trials of non-vitamin K antagonist oral anticoagulants, including Rivaroxaban. The study highlights that Rivaroxaban is an antifactor Xa inhibitor, which is a distinct mechanism of action compared to other anticoagulants like Dabigatran, which is a direct thrombin inhibitor.
Key Points about Rivaroxaban
- Rivaroxaban is a direct oral anticoagulant (DOAC) medication used to prevent and treat blood clots
- The standard dose for atrial fibrillation is 20mg once daily with food, as indicated in the study 1
- Patients should take Rivaroxaban at the same time each day with food to enhance absorption
- Unlike warfarin, Rivaroxaban doesn't require routine blood monitoring, but kidney function should be assessed regularly as the drug is partially eliminated through the kidneys
- Common side effects include bleeding risk, which is its primary concern
Important Considerations
- Patients should avoid other blood thinners unless specifically directed by their doctor
- Patients should inform all healthcare providers about taking Rivaroxaban before any procedures or when starting new medications
- The study 1 provides a summary of the clinical trials and approved doses for Rivaroxaban, which can guide clinical decision-making.
From the FDA Drug Label
XARELTO is a selective inhibitor of FXa. It does not require a cofactor (such as Anti-thrombin III) for activity. Rivaroxaban inhibits free FXa and prothrombinase activity. Rivaroxaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, rivaroxaban decreases thrombin generation.
The mechanism of action of Rivaroxaban (Xarelto) is as a selective inhibitor of Factor Xa (FXa). It works by:
- Inhibiting free FXa and prothrombinase activity
- Indirectly inhibiting platelet aggregation induced by thrombin
- Decreasing thrombin generation This mechanism allows Rivaroxaban to prevent blood clot formation without requiring a cofactor like Anti-thrombin III 2.
From the Research
Mechanism of Action of Rivaroxaban
- Rivaroxaban is a direct factor Xa inhibitor, which means it works by inhibiting the activity of factor Xa in the coagulation cascade 3, 4, 5, 6, 7.
- By inhibiting factor Xa, rivaroxaban prevents the conversion of prothrombin to thrombin, thereby reducing the formation of blood clots 3, 5, 7.
- The mechanism of action of rivaroxaban is distinct from that of warfarin, which inhibits the production of vitamin K-dependent clotting factors 3, 4, 7.
Pharmacokinetics and Pharmacodynamics
- Rivaroxaban has a rapid onset of action and a predictable anticoagulant effect, which allows for fixed dosing without the need for routine coagulation monitoring 3, 4, 5.
- The pharmacokinetics of rivaroxaban are consistent and predictable across different doses and patient populations, with a moderate influence of age and renal function on clearance 5.
- The prothrombin time correlates almost linearly with plasma rivaroxaban concentrations, allowing for monitoring of anticoagulant activity if needed 5.
Clinical Implications
- Rivaroxaban has been shown to be non-inferior to warfarin in preventing stroke and systemic embolism in patients with non-valvular atrial fibrillation, with a similar tolerability profile 3, 6, 7.
- The use of rivaroxaban may offer advantages over warfarin, including a rapid onset of action, few drug interactions, and no requirement for routine coagulation monitoring 4, 7.
- However, important contraindications to rivaroxaban include valvular atrial fibrillation, prosthetic valves, and severe renal impairment 7.