Rivaroxaban: An oral direct inhibitor of factor Xa

• Published in: American journal of health-system pharmacy 2008-08, Vol.65 (16), p.1520-1529
• Main Authors: Gulseth, Michael P, Michaud, Jessica, Nutescu, Edith A
• Format: Article
• Language: English
• Subjects: Aging - metabolism; Anticoagulants (Medicine); Antithrombin III - pharmacokinetics; Antithrombin III - pharmacology; Antithrombin III - therapeutic use; Care and treatment; Clinical Trials as Topic; Complications and side effects; Dosage and administration; Drug Interactions; Fibrinolytic Agents - pharmacokinetics; Fibrinolytic Agents - pharmacology; Fibrinolytic Agents - therapeutic use; Health aspects; Hepatic Insufficiency - metabolism; Humans; Morpholines - pharmacokinetics; Morpholines - pharmacology; Morpholines - therapeutic use; Obesity - metabolism; Prevention; Prothrombin Time; Renal Insufficiency - metabolism; Rivaroxaban; Thiophenes - pharmacokinetics; Thiophenes - pharmacology; Thiophenes - therapeutic use; Thrombophlebitis; Venous Thromboembolism - prevention & control
• ISSN: 1079-2082; 1535-2900
• DOI: 10.2146/ajhp070624

The mechanism of action, pharmacodynamics, pharmacokinetics, efficacy in clinical trials, interactions, adverse effects and toxicity, and place in therapy of rivaroxaban are reviewed. Rivaroxaban, the first oral, direct factor Xa (FXa) inhibitor to reach Phase III trials, inhibits thrombin generation by both the intrinsic and the tissue factor pathways. It has shown predictable, reversible inhibition of FXa activity, and it may have the ability to inhibit clot-bound FXa. Rivaroxaban is being evaluated for prevention of venous thrombosis in patients undergoing hip or knee arthroplasty, treatment of venous thrombosis, long-term use for secondary prevention of venous thrombosis, and prevention of stroke in atrial fibrillation. To date, only short-term trials have been reported, but rivaroxaban's safety and efficacy appear to be at least equivalent to those of traditional anticoagulants. The results of four studies of primary prevention of venous thrombosis in patients undergoing orthopedic surgery suggest that rivaroxaban 10 mg daily is a promising alternative to low-molecular-weight heparins. Rivaroxaban appears to have a low potential for drug-drug or drug-food interactions. It offers the advantages of a fixed oral dose, rapid onset of action, and predictable and consistent anticoagulation effect, precluding the need for routine monitoring of anticoagulation. Rivaroxaban is a promising alternative to traditional anticoagulants for the prevention and treatment of venous thromboembolism and for stroke prevention in atrial fibrillation; it offers once-daily oral administration without the need for routine monitoring.