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Apixaban (Eliquis)

Apixaban, marketed under the brand name Eliquis, is an oral anticoagulant used to prevent and treat blood clots. It belongs to a class of drugs known as direct oral anticoagulants (DOACs) or factor Xa inhibitors. Apixaban is widely prescribed due to its efficacy, predictable pharmacokinetics, and reduced need for routine monitoring compared to traditional anticoagulants like warfarin. This article provides a detailed overview of apixaban, including its mechanism of action, uses, dosage, side effects, precautions, drug interactions, and generic names, referencing authoritative sources such as the British National Formulary (BNF)Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.

Apixaban selectively inhibits factor Xa, a key enzyme in the coagulation cascade. The mechanism of action involves:

  1. Inhibition of Factor Xa:
    • Factor Xa plays a critical role in the conversion of prothrombin to thrombin, a key step in blood clot formation.
    • By inhibiting factor Xa, apixaban reduces thrombin generation, thereby preventing the formation of blood clots.
  2. Anticoagulant Effect:
    • Apixaban’s action is specific to factor Xa, making it a targeted anticoagulant with a lower risk of affecting other clotting factors.
    • It does not require antithrombin III (unlike heparin) for its activity.
  3. Predictable Pharmacokinetics:
    • Apixaban has a rapid onset of action, reaching peak plasma concentrations within 3–4 hours.
    • It has a half-life of approximately 12 hours, allowing for twice-daily dosing.

Apixaban is approved for the following conditions:

  1. Prevention of Stroke and Systemic Embolism in Atrial Fibrillation:
    • Used in patients with non-valvular atrial fibrillation (NVAF) to reduce the risk of stroke and systemic embolism.
  2. Treatment and Prevention of Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE):
    • Used for the treatment of acute DVT and PE.
    • Also used for the prevention of recurrent DVT and PE.
  3. Postoperative Thromboprophylaxis:
    • Used to prevent venous thromboembolism (VTE) in patients undergoing hip or knee replacement surgery.

the dosage of apixaban varies depending on the indication and patient-specific factors. Below are general guidelines:

  1. Atrial Fibrillation (Stroke Prevention):
    • Standard Dose: 5 mg taken orally twice daily.
    • Reduced Dose: 2.5 mg twice daily for patients with at least two of the following:
      • Age ≥ 80 years
      • Body weight ≤ 60 kg
      • Serum creatinine ≥ 1.5 mg/dL
  2. Treatment of DVT and PE:
    • Initial Dose: 10 mg taken orally twice daily for the first 7 days.
    • Maintenance Dose: 5 mg taken orally twice daily.
  3. Prevention of Recurrent DVT and PE:
    • Standard Dose: 2.5 mg taken orally twice daily.
  4. Postoperative Thromboprophylaxis:
    • Standard Dose: 2.5 mg taken orally twice daily, starting 12–24 hours after surgery.
    • Duration:
      • Hip replacement: 32–38 days.
      • Knee replacement: 10–14 days.
  5. Administration:
    • Apixaban can be taken with or without food.
    • Do not crush or chew the tablets.

Apixaban is generally well-tolerated, but some side effects may occur. These include:

  1. Common Side Effects:
    • Bleeding (e.g., nosebleeds, gum bleeding, bruising)
    • Nausea
    • Anemia
  2. Less Common Side Effects:
    • Headache
    • Rash
    • Elevated liver enzymes
  3. Rare but Serious Side Effects:
    • Major Bleeding: Gastrointestinal bleeding, intracranial hemorrhage.
    • Hypersensitivity Reactions: Rare cases of anaphylaxis or angioedema.
    • Spinal/Epidural Hematoma: Especially in patients undergoing spinal procedures.
  1. Contraindications:
    • Hypersensitivity to apixaban or any component of the formulation.
    • Active clinically significant bleeding.
    • Severe hepatic impairment (Child-Pugh class C).
  2. Warnings:
    • Bleeding Risk: Apixaban increases the risk of bleeding. Use with caution in patients with a history of bleeding disorders or conditions that predispose to bleeding.
    • Renal Impairment: Use with caution in patients with severe renal impairment (CrCl < 15 mL/min). Dose adjustment may be required.
    • Pregnancy and Lactation: Apixaban is not recommended during pregnancy or breastfeeding unless the benefits outweigh the risks.
  3. Monitoring:
    • Regular monitoring of renal function (serum creatinine).
    • Watch for signs of bleeding (e.g., unusual bruising, blood in stool or urine).

Apixaban interacts with several medications, including:

  1. Strong CYP3A4 and P-gp Inhibitors (e.g., ketoconazole, ritonavir): Increase apixaban levels, increasing the risk of bleeding. Avoid concurrent use or reduce the dose of apixaban.
  2. Strong CYP3A4 and P-gp Inducers (e.g., rifampin, carbamazepine): Decrease apixaban levels, reducing its efficacy. Avoid concurrent use.
  3. Other Anticoagulants (e.g., warfarin, heparin): Increased risk of bleeding.
  4. NSAIDs (e.g., ibuprofen): Increased risk of gastrointestinal bleeding.

Antiplatelet Agents (e.g., aspirin, clopidogrel): Increased risk of bleeding

Apixaban is available under its generic name as well as brand names. Some common formulations include:

  • Generic Name: Apixaban
  • Brand Name: Eliquis (commonly used worldwide).

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