Pharm

Apixaban

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Apixaban, Eliquis

  • Mechanism
  1. Oral direct Xa inhibitor
  2. Factor Xa is the first step in the Common Clotting Cascade
  1. Alternative to Warfarin (where Pradaxa Dyspepsia not tolerated)
  2. Poor INR control on Warfarin
  3. Barriers to INR monitoring
  4. Warfarin Drug Interactions
  • Contraindications
  1. Acute bleeding
    1. Initial studies suggest less bleeding risk than Warfarin
  2. Mechanical Heart Valves or valvular Atrial Fibrillation
    1. Use Warfarin instead
  3. Moderate to severe hepatic Impairment
  4. Pregnancy or Lactation
  • Precautions
  1. No antidote for bleeding (until Andexxa released in 2018)
    1. Consider Prothrombin Complex Concentrate, activated PCC or recombinant factor VIIa
  2. Increased stroke risk if stopped abruptly without other Anticoagulation in nonvalvular Atrial Fibrillation
  • Pharmacokinetics
  1. Half-life: 8-15 hours (12 hour mean)
  2. Oral bioavailability: 58%
  3. Onset: 3-4 hours
  1. Standard dose
    1. Apixaban (Eliquis) 5 mg twice daily
  2. Half-dose indications (2.5 mg twice daily)
    1. See Renal Dosing below
  1. Venous Thromboembolism Treatment
    1. Initial: 10 mg orally twice daily for 7 days
    2. Maintenance: 5 mg orally twice daily
    3. Prevention of recurrence: 2.5 mg orally twice daily
  2. Venous Thromboembolism Prophylaxis after Surgery
    1. Hip Replacement: 2.5 mg orally twice daily for 35 days
    2. Knee Replacement: 2.5 mg orally twice daily for 12 days
  1. Renal Dosing (2.5 mg orally twice daily) is indicated if at least 2 of the following criteria are present
    1. Serum Creatinine >=1.5 mg/dl or higher
    2. Age >=80 years old
    3. Weight <=60 kg (or <132 lb)
  2. References
    1. https://packageinserts.bms.com/pi/pi_eliquis.pdf
  • Drug Interactions
  1. Strong Cytochrome P450 3A4 inducers
    1. Rifampin (also induces P-Glycoprotein)
    2. Phenytoin
    3. Carbamazepine
    4. Phenobarbital
  2. P-Glycoprotein Inhibitors
    1. Ketoconazole
    2. Itraconazole
    3. Voriconazole
    4. Ritonavir
    5. Conivaptan
  3. Other Anticoagulants and antiplatelet agents
    1. Aspirin and other antiplatelet agents (e.g. Clopidogrel)
    2. NSAIDs