Eliquis (apixaban) is a next-generation oral anticoagulant specifically engineered to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. It represents a significant advancement in antithrombotic therapy, offering a predictable anticoagulant effect with a fixed dosing regimen and no requirement for routine coagulation monitoring. By directly inhibiting Factor Xa, a key component in the blood coagulation cascade, Eliquis provides effective protection against thrombotic events while maintaining a favorable safety profile concerning major bleeding compared to older therapies like warfarin. Its clinical efficacy is robustly supported by extensive trial data, making it a cornerstone in modern management strategies for thromboembolic disorders.

Features

• Active Ingredient: Apixaban, a highly selective direct Factor Xa inhibitor.
• Mechanism of Action: Prevents thrombus formation by inhibiting free and clot-bound Factor Xa, and prothrombinase activity.
• Dosage Forms: Available as film-coated tablets in 2.5 mg and 5 mg strengths.
• Pharmacokinetics: Rapid oral absorption with peak plasma concentrations achieved in 3-4 hours; bioavailability approximately 50%.
• Half-life: Approximately 12 hours, supporting twice-daily dosing.
• Renal Elimination: Approximately 27% of the dose is excreted renally; no dose adjustment required in mild-to-moderate renal impairment.
• No Routine Monitoring: Does not require regular INR (International Normalized Ratio) testing.

Benefits

• Superior Stroke Reduction: Demonstrated significant reduction in the risk of stroke and systemic embolism compared to warfarin in patients with nonvalvular atrial fibrillation.
• Lower Major Bleeding Risk: Associated with significantly fewer major bleeding events, including intracranial hemorrhage, than warfarin.
• Fixed Dosing Convenience: Eliminates the need for frequent blood tests and dose adjustments, enhancing patient adherence and quality of life.
• Rapid Onset and Offset: Provides predictable anticoagulation without the need for bridging therapy with parenteral anticoagulants.
• Fewer Dietary Restrictions: Unlike vitamin K antagonists, no specific dietary limitations regarding vitamin K intake.
• Reduced Drug Interactions: Lower potential for interactions compared to warfarin, though significant interactions still exist and require vigilance.

Common use

Eliquis is primarily indicated for:

• Reducing the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation.
• Prophylaxis of deep vein thrombosis (DVT), which may lead to pulmonary embolism (PE), in patients who have undergone hip or knee replacement surgery.
• Treatment of DVT and PE.
• Reduction in the risk of recurrent DVT and PE following initial therapy.

Dosage and direction

For nonvalvular atrial fibrillation:

• The recommended dose is 5 mg taken orally twice daily.
• For patients with at least two of the following characteristics: age ≥80 years, body weight ≤60 kg, or serum creatinine ≥1.5 mg/dL, the recommended dose is 2.5 mg twice daily.

For hip replacement surgery prophylaxis:

• 2.5 mg twice daily, initiated 12 to 24 hours postoperatively, for 35 days.

For knee replacement surgery prophylaxis:

• 2.5 mg twice daily, initiated 12 to 24 hours postoperatively, for 12 days.

For treatment and risk reduction of DVT/PE:

• Following 7 days of initial therapy, the recommended dose is 5 mg twice daily for DVT/PE treatment, and 2.5 mg twice daily after at least 6 months of treatment for reduction in the risk of recurrent DVT/PE.

Tablets should be swallowed whole, with or without food. Do not crush or break tablets.

Precautions

• Bleeding Risk: Eliquis increases the risk of bleeding and can cause serious, potentially fatal, bleeding. Promptly evaluate any signs or symptoms of blood loss.
• Spinal/Epidural Hematoma: Patients undergoing spinal puncture or neuraxial anesthesia are at risk of epidural or spinal hematoma, which can result in long-term or permanent paralysis.
• Renal Impairment: Use with caution in severe renal impairment (CrCl 15-29 mL/min); avoid use in patients with CrCl <15 mL/min or on dialysis.
• Hepatic Impairment: Avoid use in patients with severe hepatic impairment; use with caution in moderate impairment.
• Prosthetic Heart Valves: Not recommended in patients with mechanical prosthetic heart valves.
• Pregnancy and Lactation: Use only if potential benefit justifies potential risk to the fetus; apixaban is excreted in human milk—use is not recommended while breastfeeding.

Contraindications

• Active pathological bleeding.
• Severe hypersensitivity reaction to apixaban or any excipient in the formulation.

Possible side effect

Common adverse reactions (≥1%) include:

• Hemorrhage (including gastrointestinal, intracranial, and other sites)
• Nausea
• Anemia
• Bruising
• Rash

Serious side effects may include:

• Serious bleeding events
• Allergic reactions (including anaphylaxis)
• Thrombocytopenia (rare)

Drug interaction

• Strong Dual Inhibitors of CYP3A4 and P-gp: Drugs like ketoconazole, itraconazole, ritonavir, or clarithromycin increase apixaban exposure—avoid concomitant use.
• Anticoagulants and Antiplatelets: Concomitant use with other anticoagulants (e.g., warfarin, heparin), NSAIDs, aspirin, or other antiplatelet drugs increases bleeding risk.
• Strong Inducers of CYP3A4 and P-gp: Drugs like rifampin, carbamazepine, phenytoin, or St. John’s wort decrease apixaban exposure and may reduce efficacy—avoid coadministration.

Missed dose

If a dose is missed, the patient should take it as soon as possible on the same day and resume the twice-daily regimen. Do not double the dose to make up for a missed one.

Overdose

Overdose may lead to hemorrhagic complications. There is no specific antidote; management consists of discontinuation and supportive care. Activated charcoal may reduce absorption if given shortly after ingestion. In life-threatening bleeding, consider procoagulant agents (e.g., prothrombin complex concentrate, activated prothrombin complex concentrate, or recombinant Factor VIIa), though their utility has not been fully established in clinical trials. Dialysis is not expected to enhance elimination.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Keep in the original bottle or blister pack to protect from moisture and light. Keep out of reach of children.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional for diagnosis and individualized treatment recommendations. Do not initiate, adjust, or discontinue any medication without professional guidance.

Reviews

Clinical trials and post-marketing surveillance have consistently demonstrated Eliquis’s efficacy in stroke prevention and venous thromboembolism management, with a bleeding risk profile favorable to warfarin. Many clinicians regard it as a first-line option for appropriate patients due to its convenience and evidence-based benefits. Patient satisfaction is often high owing to the lack of dietary restrictions and monitoring requirements. However, cost and insurance coverage can be barriers to access in some regions.