What is Apixaban (Eliquis)?

From the Guidelines

Apixaban (Eliquis) is a direct oral anticoagulant (DOAC) that is typically prescribed at 5 mg twice daily for most patients with atrial fibrillation or venous thromboembolism, with a reduced dose of 2.5 mg twice daily recommended for certain patients, such as those with age ≥80 years, weight ≤60 kg, or serum creatinine ≥1.5 mg/dL 1.

Key Characteristics of Apixaban

• Directly inhibits Factor Xa in the coagulation cascade, preventing thrombin formation and clot development
• Does not require routine INR monitoring, has fewer food and drug interactions, and offers more predictable anticoagulation compared to warfarin
• Common side effects include bleeding risk, bruising, and nausea
• Patients should avoid NSAIDs when possible and inform all healthcare providers about taking this medication before procedures ### Dosage and Administration
• Typically prescribed at 5 mg twice daily for most patients with atrial fibrillation or venous thromboembolism
• Reduced dose of 2.5 mg twice daily recommended for patients meeting at least two of the following criteria: age ≥80 years, weight ≤60 kg, or serum creatinine ≥1.5 mg/dL 1
• For DVT/PE treatment, patients usually start with 10 mg twice daily for 7 days, then continue with 5 mg twice daily
• Should be taken with or without food at approximately 12-hour intervals ### Clinical Evidence
• The Apixaban for Reduction in Stroke and Other Thromboembolic Events in Atrial Fibrillation (ARISTOTLE) trial compared apixaban 5 mg twice daily with adjusted-dose warfarin in 18,201 patients with nonvalvular atrial fibrillation, and found that apixaban was superior to warfarin in preventing stroke or systemic embolism, with a lower risk of major bleeding 2
• The Apixaban Versus Acetylsalicylic Acid to Prevent Strokes in Atrial Fibrillation Patients Who Have Failed or Are Unsuitable for Vitamin K Antagonist Treatment (AVERROES) trial compared apixaban 5 mg twice daily with aspirin 81-324 mg daily in 5,599 patients with nonvalvular atrial fibrillation, and found that apixaban was superior to aspirin in preventing stroke or systemic embolism, with a similar risk of major bleeding 2

From the FDA Drug Label

Apixaban, a factor Xa (FXa) inhibitor, is chemically described as 1-(4- methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4 c]pyridine-3-carboxamide. Apixaban is a white to off white crystalline powder. Apixaban tablets are available for oral administration in strengths of 2. 5 mg and 5 mg of apixaban with the following inactive ingredients: anhydrous lactose, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, and magnesium stearate. Apixaban is a selective inhibitor of FXa. It does not require antithrombin III for antithrombotic activity. Apixaban inhibits free and clot-bound FXa, and prothrombinase activity.

Apixaban (Eliquis) is a factor Xa inhibitor that works by inhibiting free and clot-bound FXa, and prothrombinase activity. It is available in oral administration in strengths of 2.5 mg and 5 mg. The main ingredients are apixaban and several inactive ingredients. Apixaban is used to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation, for the prophylaxis of deep vein thrombosis (DVT), and for the treatment of DVT and PE 3, 4, 5.

From the Research

What is Apixaban (Eliquis)

Apixaban, also known by its brand name Eliquis, is a factor Xa inhibitor anticoagulant used for the prevention of thromboembolic events in patients with atrial fibrillation and a high thrombotic risk 6. It has been authorized in the European Union for use in patients with non-valvular atrial fibrillation and a moderate or high risk of thrombosis.

Key Characteristics of Apixaban

• Apixaban is a direct factor Xa inhibitor, which means it works by inhibiting the activity of factor Xa in the coagulation cascade 7.
• It is approved by the US Food and Drug Administration (FDA) for the prevention of stroke and systemic embolism in nonvalvular atrial fibrillation 7.
• Apixaban has a lower risk of major bleeding events compared to warfarin, but a higher risk compared to aspirin 6.
• It is a substrate for various cytochrome P450 isoenzymes and for P-glycoprotein, which creates a risk of multiple drug-drug interactions 6.
• The anticoagulant action of apixaban is increased by renal failure, meaning that renal function must be regularly monitored 6.

Safety and Efficacy of Apixaban

• Studies have shown that apixaban is effective in preventing stroke and systemic embolism in patients with nonvalvular atrial fibrillation, with a lower risk of major bleeding events compared to warfarin 6, 8.
• Apixaban may be well-tolerated and effective in patients with nonvalvular atrial fibrillation weighing ≥ 120 kg, although more data is needed to confirm this 9.
• The safety and efficacy of apixaban in patients with severe renal impairment is limited, but studies suggest that it may be safe and effective in this population 8, 10.

Clinical Use of Apixaban

• Apixaban is typically prescribed at a dose of 5 mg twice daily, although a reduced dose of 2.5 mg twice daily may be used in patients with severe renal impairment or other factors that increase the risk of bleeding 7, 10.
• The use of apixaban must be monitored to ensure that FDA-approved dosing regimens are being prescribed and patients are not being underdosed 7.
• Apixaban is often prescribed in patients with nonvalvular atrial fibrillation who have a high risk of thrombosis, although it may also be used in patients with a moderate risk of thrombosis 6, 10.