Generic
Rivaroxaban
38 brands available in the market
At a glance
Rivaroxaban is a direct factor Xa inhibitor used as an anticoagulant to reduce the risk of stroke and systemic embolism in nonvalvular atrial fibrillation, for treatment of DVT and PE, for reducing the risk of recurrence of DVT and PE, and for prophylaxis of DVT following knee or hip replacement surgery.
Description
Rivaroxaban is a highly selective direct factor Xa inhibitor. Inhibition of factor Xa interrupts the intrinsic and extrinsic pathway of the blood coagulation cascade and inhibits thrombin formation. It does not inhibit thrombin and has no effects on platelets.
Indications
- Reduction of stroke and systemic embolism in nonvalvular atrial fibrillation
- Treatment of DVT and PE
- Reduction of risk of recurrence of DVT and PE
- Prophylaxis of DVT following knee or hip replacement surgery
Therapeutic class
Oral Anti-coagulants
Pharmacological class
Direct Factor Xa Inhibitor
Pharmacology
Rivaroxaban selectively inhibits factor Xa, disrupting the blood coagulation cascade and preventing thrombin formation. It does not require a cofactor such as antithrombin III. Dose-dependent inhibition of factor Xa activity is observed; it prolongs PT, aPTT, and HepTest.
Mechanism of action
Prevents thrombin formation and blood clotting by inhibiting factor Xa.
Dosage
Adult Dose (Oral):
- Nonvalvular AF (CrCl >50): 20 mg/day with evening meal
- Nonvalvular AF (CrCl 15-50): 15 mg/day
- DVT/PE treatment: 15 mg twice daily for 21 days, then 20 mg/day
- DVT/PE recurrence prevention: 20 mg/day
- Hip replacement: 10 mg/day for 35 days
- Knee replacement: 10 mg/day for 12 days
- ACS (2.5 mg): 2.5 mg twice daily + aspirin 75-100 mg/day
Administration
- Take with food (increases absorption)
- Take at the same time each day
- Swallow tablet whole; do not chew, crush, or break
Missed dose
If you miss a dose, take it as soon as possible; if almost time for next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Bleeding (nosebleeds, bruising, gum bleeding)
- Anemia
- Nausea
- Dizziness
- Spinal or epidural hematoma (with neuraxial anesthesia)
Precautions & warnings
- Bleeding risk: Caution in bleeding disorders, uncontrolled severe hypertension, GI disease
- Discontinuation increases risk of thrombotic events
- Spinal/epidural hematoma with neuraxial anesthesia
- May affect driving ability (dizziness or fainting)
Contraindications
- Active pathological bleeding
- Significant risk of major bleeding (peptic ulcer, esophageal varices, intracranial hemorrhage)
- Severe hepatic impairment (Child-Pugh B/C)
- Pregnancy and lactation
Drug interactions
- Strong CYP3A4 and P-gp inhibitors (ketoconazole, ritonavir, clarithromycin): Increased exposure; avoid
- Strong CYP3A4 inducers (rifampicin, phenytoin, carbamazepine): Decreased efficacy; avoid
- Antiplatelets, heparin, NSAIDs: Increased bleeding risk
Food interactions
Caution is advised when consuming alcohol with Rivaroxaban.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited human data suggests drug may pass into breast milk; consult your doctor.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: AF: CrCl 30-50: 20 mg/day; CrCl 15-50: 15 mg/day; CrCl <15: avoid; DVT/PE prophylaxis: CrCl 30-50: caution; CrCl <30: avoid; consult your doctor.
Hepatic Impairment: Avoid in moderate-severe hepatic impairment; avoid in any hepatic disease associated with coagulopathy; consult your doctor.
Overdose effects
Overdose may lead to hemorrhage; no specific antidote; activated charcoal to reduce absorption; partial reversal with plasma products.
Storage conditions
Store in a cool and dry place below 30°C, protected from light; keep out of reach of children.
Chemical structure
Rivaroxaban