Pharm 101: Rivaroxaban

Class

Direct oral anticoagulant (DOAC)


Pharmacodynamics
  • Direct factor Xa inhibitor (both free and prothrombinase-bound forms)

Pharmacokinetics
  • Bioavailability > 80%
  • Rapid onset and rapid offset
  • Maximal plasma levels 3 hours post-ingestion
  • Small volume of distribution (50L)
  • Highly protein bound
  • Elimination renal (predominant) and hepatic (CYP3A4)
  • Steady state half-life of 5-9 hours is prolonged with renal impairment

Clinical uses
  • Prevention of embolic stroke in patients with atrial fibrillation
  • Prevention of VTE following hip/knee surgery
  • Treatment of VTE
  • Offers advantages over warfarin:
    • More rapid onset/offset of action
    • More predictable effect, wider therapeutic index
    • INR monitoring not required
    • Fewer drug and dietary interactions

Adverse effects
  • Bleeding
  • Reversal is less straight forward than warfarin:
    • Andexanet alfa is a factor Xa “decoy” molecule without procoagulant activity that competes for binding to anti-Xa drugs and rapidly decreases anti-Xa effect

Precautions/contraindications
  • Dose adjustment in renal failure
  • Contraindicated in dialysis patients

Further Reading

Pharm 101 700

Pharmacology 101

Top 200 drugs

MBBS (UWA) CCPU (RCE, Biliary, DVT, E-FAST, AAA) Emergency Medicine Advanced Trainee in Melbourne, Australia. Special interests in diagnostic and procedural ultrasound, medical education, and ECG interpretation. Editor-in-chief of the LITFL ECG Library. Twitter: @rob_buttner

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