Apixaban

What it is and how it works

Mechanism of Action 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 has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development.

Mechanism class: Factor Xa Inhibitors

Indications

Apixaban tablets are a factor Xa inhibitor indicated: to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. for the prophylaxis of deep vein thrombosis (DVT), which may lead to pulmonary embolism (PE), in patients who have undergone hip or knee replacement surgery. for the treatment of DVT and PE, and for the reduction in the risk of recurrent DVT and PE following initial therapy. (1.3 , 1.4 , 1.5) Reduction of Risk of Stroke and Systemic Embolism in Nonvalvular Atrial Fibrillation Apixaban tablets are indicated to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. Prophylaxis of Deep Vein Thrombosis Following Hip or Knee Replacement Surgery Apixaban tablets are indicated for the 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 Deep Vein Thrombosis Apixaban tablets are indicated for the treatment of DVT.

Dosage and administration (summary)

Reduction of risk of stroke and systemic embolism in nonvalvular atrial fibrillation: The recommended dose is 5 mg orally twice daily. In patients with at least 2 of the following characteristics: age greater than or equal to 80 years, body weight less than or equal to 60 kg, or serum creatinine greater than or equal to 1.5 mg/dL, the recommended dose is 2.5 mg orally twice daily. Prophylaxis of DVT following hip or knee replacement surgery: The recommended dose is 2.5 mg orally twice daily. Treatment of DVT and PE: The recommended dose is 10 mg taken orally twice daily for 7 days, followed by 5 mg taken orally twice daily.

Contraindications

Apixaban is contraindicated in patients with the following conditions: Active pathological bleeding Severe hypersensitivity reaction to apixaban (e.g., anaphylactic reactions) Active pathological bleeding. Severe hypersensitivity to apixaban.

Warnings and precautions

Apixaban tablets can cause serious, potentially fatal, bleeding. Promptly evaluate signs and symptoms of blood loss. An agent to reverse the anti-factor Xa activity of apixaban is available. Prosthetic heart valves: Apixaban use not recommended. Increased Risk of Thrombosis in Patients with Triple Positive Antiphospholipid Syndrome: Apixaban use not recommended.

Pregnancy

Pregnancy Risk Summary The limited available data on apixaban use in pregnant women are insufficient to inform drug-associated risks of major birth defects, miscarriage, or adverse developmental outcomes. Treatment may increase the risk of bleeding during pregnancy and delivery.

Storage and supply

Storage and Handling Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F to 86°F) . Storage and Handling Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F to 86°F) .

Source: Apixaban (Apixaban) — US FDA prescribing information, 2024-05-23, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.