U&Y Apixaban Tablets

1. Indications and Usage
Atrial Fibrillation: Indicated to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation.
Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE): Indicated for the treatment of DVT and PE.
Post-Operative Prophylaxis: Indicated for the prevention of DVT following elective hip or knee replacement surgery.
2. Dosage and Administration
Atrial Fibrillation: The usual dose is 5 mg twice daily. This may be reduced to 2.5 mg twice daily if the patient meets at least two of the following criteria: age ≥80 years, body weight ≤60 kg, or serum creatinine ≥1.5 mg/dL.
DVT/PE Treatment: The recommended dose is 10 mg twice daily for 7 days, followed by 5 mg twice daily for continued treatment.
Post-Operative Prophylaxis: The usual dose is 2.5 mg twice daily, initiated 12–24 hours post-surgery.
Administration: Can be taken with or without food. If unable to swallow tablets, apixaban may be dispersed in water, apple juice, or orange juice and administered orally or via a gastric tube.
3. Mechanism of Action
Factor Xa Inhibition: Apixaban is a highly selective, reversible, and direct inhibitor of Factor Xa.
Thrombin Inhibition: By binding directly to the active site of Factor Xa, it blocks the conversion of prothrombin to thrombin, thereby reducing thrombus formation and impairing clot propagation.
4. Safety and Warnings
Bleeding Risk: The most significant risk is serious or fatal bleeding. It is contraindicated in patients with active pathological bleeding or a history of severe hypersensitivity.
Neuraxal Anesthesia: In patients receiving neuraxal (epidural/spinal) anesthesia, apixaban increases the risk of spinal or epidural hematomas, which can result in long-term or permanent paralysis.
Discontinuation: To reduce bleeding risk, it should be discontinued prior to elective surgery if anti-clotting effect is not desired.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: Bleeding events (epistaxis, hematuria, Gingival bleeding), anemia, and bruising.
Serious Adverse Reactions: Intracranial hemorrhage and gastrointestinal bleeding.
Clinical Findings: Clinical trials (e.g., ARISTOTLE trial) demonstrated that apixaban was superior to warfarin in reducing stroke and systemic embolism and had a lower risk of major bleeding.
6. Drug Interactions
Strong Dual Inhibitors: Concomitant use with strong dual inhibitors of both CYP3A4 and P-gp (e.g., ketoconazole, ritonavir) is contraindicated as it significantly increases apixaban exposure.
Strong Inducers: Concomitant use with strong inducers (e.g., rifampin, phenytoin) may decrease apixaban exposure and anti-clotting effect.
Antiplatelet/NSAIDs: Concurrent use with aspirin, NSAIDs, or other antiplatelet agents increases the risk of bleeding.
7. Pharmaceutical Information
Active Ingredient: Apixaban.
Strengths: Typically available as 2.5 mg and 5 mg tablets.
Appearance: Orange, biconvex, round film-coated tablets, imprinted with “LG” and “723” on one side and blank on the reverse.
Storage: Store at 25°C (77°F), with excursions permitted to 15°C–30°C (59°F–86°F).