Apixaban: Uses, Dosage & Side Effects
Apixaban is an oral anticoagulant (blood thinner) belonging to the class of Factor Xa inhibitors. It is used to prevent and treat blood clots in various medical conditions.
Things worth knowing about "Apixaban"
Apixaban is an oral anticoagulant (blood thinner) belonging to the class of Factor Xa inhibitors. It is used to prevent and treat blood clots in various medical conditions.
What is Apixaban?
Apixaban is a prescription medication classified as a direct oral anticoagulant (DOAC). It selectively inhibits coagulation Factor Xa, thereby preventing the formation of dangerous blood clots (thrombi). Apixaban is marketed under the brand name Eliquis and is one of the most widely prescribed anticoagulants in the world.
Indications
Apixaban is approved for several clinical conditions:
- Atrial fibrillation: Prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation.
- Deep vein thrombosis (DVT): Treatment and secondary prevention of blood clots in the deep veins of the legs.
- Pulmonary embolism (PE): Treatment and prevention of recurrent pulmonary embolism.
- Thromboprophylaxis after surgery: Prevention of blood clots following elective hip or knee replacement surgery.
Mechanism of Action
Apixaban acts as a direct Factor Xa inhibitor. Factor Xa is a key enzyme in the coagulation cascade that converts prothrombin into thrombin. Thrombin is then responsible for converting fibrinogen into fibrin, which forms the structural backbone of a blood clot.
By selectively and reversibly inhibiting Factor Xa, apixaban effectively interrupts this cascade without directly targeting thrombin. Unlike vitamin K antagonists (e.g., warfarin), apixaban does not require routine coagulation monitoring (INR testing), which makes it more convenient for long-term use.
Dosage
The dosage of apixaban varies depending on the indication:
- Atrial fibrillation: Typically 5 mg twice daily. A reduced dose of 2.5 mg twice daily is recommended for patients meeting at least two of the following criteria: age 80 or older, body weight 60 kg or less, or serum creatinine 1.5 mg/dL or higher.
- Treatment of DVT or PE: 10 mg twice daily for the first 7 days, followed by 5 mg twice daily.
- Post-surgical thromboprophylaxis: 2.5 mg twice daily.
Apixaban tablets can be taken with or without food.
Side Effects
The most common and clinically significant side effect of apixaban is an increased risk of bleeding. Potential bleeding complications include:
- Gastrointestinal bleeding (common)
- Bruising and mucosal bleeding (common)
- Nosebleeds and bleeding gums
- Rare but serious: intracranial bleeding (life-threatening)
Other possible side effects include nausea, anemia, and elevated liver enzyme levels. In cases of severe or life-threatening bleeding, andexanet alfa is available as a specific reversal agent for apixaban.
Interactions and Contraindications
Apixaban should not be used in patients with:
- Clinically significant active bleeding
- Severe hepatic impairment
- Pregnancy or breastfeeding
Important drug interactions occur with strong CYP3A4 and P-glycoprotein (P-gp) inhibitors (e.g., ketoconazole, ritonavir), which can increase apixaban plasma levels, and with strong inducers of these pathways (e.g., rifampicin, St. John's Wort), which can reduce its effectiveness. Concurrent use of other anticoagulants or non-steroidal anti-inflammatory drugs (NSAIDs) increases the risk of bleeding.
Important Notes
Before any planned surgical procedures or invasive interventions, apixaban should be temporarily discontinued in consultation with a healthcare provider. Patients should never stop taking apixaban on their own without medical advice, as this may significantly increase the risk of stroke or thromboembolic events.
References
- European Medicines Agency (EMA): Eliquis (Apixaban) - Summary of Product Characteristics (SmPC). Available at: www.ema.europa.eu
- Granger CB et al. - Apixaban versus Warfarin in Patients with Atrial Fibrillation. New England Journal of Medicine, 2011; 365:981-992.
- Agnelli G et al. - Oral Apixaban for the Treatment of Acute Venous Thromboembolism. New England Journal of Medicine, 2013; 369:799-808.
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