Rivaroxaban - A Anticoagulant

Rivaroxaban is relatively newer anticoagulant used mainly as a preventive therapy for patients prone to stroke.

Image from wikipedia

Rivaroxaban is an oxazolidinone derivative optimized for inhibiting both free Factor Xa and Factor Xa bound in the prothrombinase complex. It is a highly selective direct Factor Xa inhibitor with oral bioavailability and rapid onset of action. Rivaroxaban does not inhibit thrombin (activated Factor II), and no effects on platelets have been demonstrated.

Mechanism of Action

Factor Xa inhibitor that inhibits platelet activation by selectively blocking the active site of factor Xa without requiring a cofactor (eg, antithrombin III) for activity
Blood coagulation cascade is dependent on the activation of factor X to factor Xa via the intrinsic and extrinsic pathways plays a central role in the blood coagulation cascade
Dose-dependent inhibition of factor Xa activity observed; antifactor Xa activity is also influenced by rivaroxaban; prolongs PT and aPTT and HepTest


Bioavailability: 80-100%
Peak plasma time: 2-4 hr


Metabolized by oxidative degradation catalyzed by CYP3A4/5 and CYP2J2; also metabolized by hydrolysis


Half-life: 5-9 hr; 11-13 hr (elderly)
Total body clearance: 10 L/hr (following IV administration)
Excretion: feces (21% as metabolites; 28% unchanged), urine (30% as metabolites; 36% unchanged)

Most Important Uses
  1. Prevention of stroke in patients with atrial fibrillation.
  2. Prophylaxis of deep vein thrombosis (DVT), which may lead to pulmonary embolism (PE) in patients undergoing knee or hip replacement surgery
  3. Treatment of DVT and PE and reduction in the risk of recurrence for DVT and PE following initial 6 months of treatment

Adverse Effects
  • Any bleeding event (5.8%)
  • Wound secretion (2.8%)
  • Pruritus (2.1%)
  • Extremity pain (1.7%)
  • Blister (1.4%)
  • Syncope (1.2%)
  • Atrial fibrillation
  • Major bleeding (5.6%)
  • Gastrointestinal bleeding (3.1%)
  • Bleeding resulting in transfusion (2.6%)
  • Bleeding into a critical organ (1.3%)

Some details taken from and Read in details on Medscape

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