Rivaroxaban
Unchecked
Rivaroxaban
Xarelto
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Summary
Common uses
Stroke prevention in nonvalvular atrial fibrillation0, VTE treatment0, VTE prophylaxis after hip/knee replacement0, Low-dose with aspirin in stable CAD/PAD0
Pharmacy
Starting dose
NVAF: 20 mg PO once daily with the evening meal (15 mg if CrCl 15-50); acute VTE: 15 mg BID for 21 days, then 20 mg daily; CAD/PAD: 2.5 mg BID with aspirin
Preparations
2.5, 10, 15, 20 mg tablets
US FDA Max
30 mg/d (acute VTE first 21 days as 15 mg BID); otherwise 20 mg/d
Pharmacology
Routes
Oral
Onset
Peak anticoagulant effect 2-4 hours
Duration
24 hours
Half-life
5-9 hours (elderly: 11-13 hours)[1]
Bioavailability
~80-100% with food at 15-20 mg doses (10 mg dose: ~80% without food); must be taken with food at therapeutic doses[1]
Pregnancy
Avoid in pregnancy; switch to LMWH. Crosses placenta; warfarin-class concerns about fetal hemorrhage and teratogenicity make heparins the preferred class.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Rivaroxaban is a selective reversible direct inhibitor of activated factor X (Xa); blocking Xa interrupts thrombin generation at a stoichiometrically efficient point in the coagulation cascade, producing predictable anticoagulation without routine monitoring.0 CYP3A4 (primary) and P-glycoprotein substrate; strong dual inhibitors or inducers materially shift exposure. Reversal: andexanet alfa for life-threatening bleeding; 4F-PCC commonly used off-label when andexanet unavailable[1].
References
[edit | edit source]- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Xarelto (rivaroxaban), Janssen, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/202439s037lbl.pdf