Apixaban (Eliquis®) Considerations for Use*

US/FDA Approved Indications: Stroke Prevention in Non-valvular Atrial Fibrillation

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Black Box Warning* Discontinuing apixaban in patients with atrial fib and without adequate continuous anticoagulation increases the risk of thrombotic events.

Mechanism of Action

Direct factor Xa inhibitor

Dosing

Adult: 5 mg PO twice daily

With at least 2 of the following : age ≥ 80 years , body weight ≤ 60 kg, serum creatinine ≥ 1.5 mg/d L: 2.5 mg PO twice daily

With strong dual inhibitors of CYP3A4 and P-gp, (e.g., ketoconazole, itraconazole, ritonavir, or clarithromycin): decrease dose of apixaban to 2.5 mg twice daily or do not use apixaban

Hepatic Impairment: Not studied with severe hepatic impairment

Renal Impairment: CrCl < 15 mL/min or on dialysis: not recommended

Contraindications

Active pathological bleeding , prosthetic heart valve

Major Side Effects

Hemorrhagic event

Dosage forms and Strengths

PO: 2.5 , 5 mg tablets

Reversal

There is no rapid reversal agent for apixaban. Drug levels may persist for ~24 hours after last dose (i.e., 2 half lives).

  • Discontinue apixaban.
  • Because of the high plasma protein binding, dialysis may not remove apixaban.
  • Use of procoagulant reversal agents such as proth rombin complex concentrate , activated prothrombin complex concentrate , or recombinant factor VIIa may be considered, but has not been evaluated in clinical trials.
  • Activated oral charcoal reduces absorption of apixaban.
  • Surgery and interventions:
    If possible, discontinue at least 48 hours prior to procedure with moderate or high risk of significant bleeding. Discontinue at least 24 hours prior to procedure with low risk of bleeding or where the bleeding would be in non-critical location and easily controlled.

    Conversion to/from other drugs

    From apixaban to warfarin:

  • Apixaban affects INR, so INR measurements made during coadministration with warfarin may not be useful for determining the appropriate dose of warfarin.
  • Discontinue apixaban and begin both a parenteral anticoagulant and warfarin at the time the next dose of apix aban would have been taken.
  • From warfarin to apixaban:

  • Discontinue warfarin and start apix aban when INR < 2.
  • Switching between apixaban and an anticoagulant other than warfarin:

  • Discontinue one being taken and begin the other at the next scheduled dose
  • Special Notes

    Has many potential drug interactions.

  • Apixaban is a substrate of both CYP3A4 and P-gp. Inducers of CYP3 A4 and P - gp decrease exposure to apixaban and increase the risk of stroke. Inhibitors of CYP3A4 and P-gp increase exposure to apixaban and increase the risk of bleeding.
  • Do not use with drugs that are strong dual inducers of CYP3A4 and P-gp (e.g., rifampin, carbamazepine, phenytoin, St. John’s wort); decreases exposure to apixaban.
  • Decrease dose of apixaban to 2.5 mg twice daily or do not use apixaban with strong dual inhibitors of CYP3A4 and P-gp, (e. g., ketoconazole, itraconazole, ritonavir, or clarithromycin).
  • Do not use with drugs that are strong dual inhibitors of both CYP3A4 and P-gp, if already taking apixaban 2.5 mg twice daily.
  • Counseling

    Do not discontinue this medication without talking to the healthcare provider who prescribed it.

    Consult healthcare professional prior to using new drug (prescription, OTC, herbal). Report signs and symptoms of bleeding (e.g., unexpected bleeding or bleeding that lasts a long time; red or black, tarry stool; pink or brown urine; unusual bruising; coughing up blood; vomiting blood or vomit that looks like coffee grounds; unexplained pain, swelling, or joint pain; unusual headaches, dizziness, or weakness; recurring nose bleeds)

    Tell your healthcare professi onal if you have had or will have surgery to place a prosthetic heart valve.

    Tell your healthcare professional if you are pregnant or plan to become pregnant or are breastfeeding or plan to breastfeed during treatment.

    *Refer to prescribing information for more complete information.
    †Dosages given in the table may differ from those recommended by the manufacturers.


    Source:

    1. Eliquis® Prescribing information, 12/28/12 .