THERAPEUTICS

Brands

• Xarelto

Generic?

• No

Class

• Anticoagulant

Commonly Prescribed for

(FDA approved in bold)

• Reduction in the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation (NVAF)

• Treatment of deep vein thrombosis (DVT), pulmonary embolism (PE), and reduction in the risk of recurrence of DVT and of PE

• Prophylaxis of DVT, which may lead to PE in patients undergoing knee or hip replacement surgery

• Ventricular dysfunction due to hypertrophic cardiomyopathy

• Hypertensive heart disease

How the Drug Works

• Rivaroxaban is a selective reversible inhibitor of both free factor Xa and prothrombinase activity, thereby reducing the conversion of prothrombin to thrombin and thrombus formation. Thrombin-induced platelet aggregation is also inhibited

How Long Until It Works

• Peak concentration in 2–4 hours

If It Works

• Monitor for signs of bleeding. Assess liver and kidney function periodically as clinically indicated

If It Doesn't Work

• Correct the underlying disorder. Use full dose or switch to anticoagulant of different class

Best Augmenting Combos for Partial Response or Treatment-Resistance

• None

Tests

• The degree of anticoagulation does not need to be assessed. Prolonged PT may indicate greater bleeding risk

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• Reduced coagulation due to inhibited thrombin formation

Notable AEs

• Bleeding

Life-Threatening or Dangerous AEs

• Fatal bleeding (< 0.4%), major bleeding (0.3–5.6%), anaphylaxis

Weight Gain

• Unusual

Sedation

• Unusual

What to Do About AEs

• Discontinue treatment, supportive care. Prothrombin complex concentrates. Activated charcoal reduces absorption. Not effective: vitamin K, protamine sulfate, hemodialysis

Best Augmenting Agents to Reduce AEs

• Antiplatelet agent, fibrinolytic agent, other anticoagulants, long-term NSAID, CYP3A4/ P-glycoprotein (P-gp) inhibitors

DOSING AND USE

Usual Dosage Range

• 10–20mg

Dosage Forms

• Tablet: 10, 15, 20mg

How to Dose

Treatment of NVAF: