Product: Xarelto

Company: Janssen

Pharmacologic class: Factor Xa inhibitor

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Active ingredient: Rivaroxaban 10 mg; tablets.

Indication: Prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism in patients undergoing knee- or hip-replacement surgery.

Pharmacology: Rivaroxaban is an orally bioavailable factor Xa inhibitor that selectively blocks the active site of factor Xa and does not require a cofactor (e.g., Antithrombin III) for activity. Activation of factor X to factor Xa via the intrinsic and extrinsic pathways plays a central role in the cascade of blood coagulation.

Clinical trials: Three trials were conducted to evaluate the safety and efficacy of rivaroxaban.

Two randomized, double-blind, studies (RECORD 1 and 2) involving patients undergoing elective total hip replacement surgery compared rivaroxaban 10 mg once daily starting at least six to eight hours after wound closure versus enoxaparin 40 mg once daily starting 12 hours preoperatively.

In RECORD 1, 1,513 patients received rivaroxaban; 1,473 patients received enoxaparin. The total percentage of patients experiencing venous thromboembolism (VTE) was 1.1% for the rivaroxaban group compared with 3.9% for the enoxaparin group; relative risk reduction (RRR) was 71%.

In RECORD 2, 834 patients received rivaroxaban; 835 patients received enoxaparin. In this study the treatment duration differed between study arms (rivaroxaban: 33.5 +/- 6.9 days; enoxaparin: 12.4 +/- 2.9 days). The total percentage of patients experiencing VTE was 2% for the rivaroxaban group compared with 8.4% for the enoxaparin group; RRR was 76%.

The RECORD 3 trial was conducted in patients undergoing elective total-knee-replacement surgery. Patients were given either rivaroxaban 10 mg once daily (813) or enoxaparin 40 mg once daily (871). In the rivaroxaban group, the percentage of total VTE was 9.7%; the enoxaparin group had 18.8%; RRR was 48%.

Adults: Take six to 10 hours after surgery once hemostasis is established. 10 mg once daily; may increase to 20 mg once daily with food if necessary. Hip: treat for 35 days. Knee: treat for 12 days.

Children: Not recommended.

Contraindications: Active major bleeding.

Warnings/Precautions: Increased risk of spinal/epidural hematoma in anticoagulated patients receiving neuraxial anesthesia or undergoing spinal puncture; monitor for signs/symptoms of neurological impairment. Conditions with increased risk of hemorrhage. Severe renal impairment (creatinine clearance <30 mL/min), moderate or severe hepatic impairment, hepatic disease associated with coagulopathy: avoid. Monitor closely for blood loss with moderate renal impairment; discontinue if acute renal failure develops. Elderly. Labor & delivery. Pregnancy (Cat. C); use with caution, risk of pregnancy-related hemorrhage. Nursing mothers: not recommended.

Interactions: See Adult dose. Increased risk of bleeding with concomitant platelet aggregation inhibitors, other antithrombotic agents, fibrinolytic therapy, thienopyridines, chronic use of nonsteroidal anti-inflammatory drugs. Avoid with concomitant combined P-glycoprotein (gp) and strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, lopinavir/ritonavir, ritonavir, indinavir/ritonavir, conivaptan). May be potentiated with concomitant renal impairment and combined P-gp and weak or moderate CYP3A4 inhibitors (e.g., erythromycin, azithromycin, diltiazem, verapamil, quinidine, ranolazine, dronedarone, amiodarone, felodipine).

Adverse reactions: Bleeding, wound secretion, pain in extremity, muscle spasm, syncope, pruritus, blister.

How supplied: Tabs — 30, 100 (10X10 blister cards)

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