Pronunciation:
a-pix-a-ban
Trade Name(s)
Ther. Class.
Pharm. Class.
factor xa inhibitors
Acts as a selective, reversible site inhibitor of factor Xa, inhibiting both free and bound factor. Does not affect platelet aggregation directly, but does inhibit thrombin-induced platelet aggregation. Decreases thrombin generation and thrombus development.
Therapeutic Effect(s):
Treatment and prevention of thromboembolic events.
Absorption: 50% absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: Primarily metabolized by the liver by the CYP3A4 isoenzyme; excreted in urine and feces. Biliary and direct intestinal excretion account for fecal elimination.
Half-life: 6 hr (12 hr after repeated dosing due to prolonged absorption).
TIME/ACTION PROFILE (effect on hemostasis)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
PO | unknown | 3–4 hr† | 24 hr |
Contraindicated in:
Use Cautiously in:
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Pedi: Safety and effectiveness not established in children.Hemat: BLEEDING
Misc: HYPERSENSITIVITY REACTIONS (including anaphylaxis)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Drug-Drug
Drug-Natural Products:
Concurrent use St. John's wort , a strong dual inducer of the CYP3A4 and P-gp enzyme systems can ↓ levels and ↑ risk of thromboses and should be avoided.
Reduction in Risk of Stroke/Systemic Embolism in Nonvalvular Atrial Fibrillation
PO (Adults): 5 mg twice daily; Any 2 of the following: age ≥80 yr, weight ≤60 kg, serum creatinine ≥1.5 mg/dL: 2.5 mg twice daily; Concurrent use of strong inhibitors of both CYP3A4 and P-gp: 2.5 mg twice daily; if patient already taking 2.5 mg twice daily, avoid concomitant use.
Renal Impairment
PO (Adults): Hemodialysis: 5 mg twice daily; HD and either age ≥80 yr or weight ≤60 kg: 2.5 mg twice daily.
Prevention of Deep Vein Thrombosis Following Knee or Hip Replacement Surgery
PO (Adults): 2.5 mg twice daily, initiated 12–24 hr postoperatively (when hemostasis is achieved) continued for 35 days after hip replacement or 12 days after knee replacement; Concurrent use of strong inhibitors of both CYP3A4 and P-gp: Avoid concomitant use.
Treatment of Deep Vein Thrombosis or Pulmonary Embolism
PO (Adults): 10 mg twice daily for 7 days, then 5 mg twice daily; Concurrent use of strong inhibitors of both CYP3A4 and P-gp: 2.5 mg twice daily
Reduction in Risk of Recurrence of Deep Vein Thrombosis or Pulmonary Embolism
PO (Adults): 2.5 mg twice daily after ≥6 mo of treatment of DVT or PE; Concurrent use of strong inhibitors of both CYP3A4 and P-gp: Avoid concomitant use.
Tablets: 2.5 mg, 5 mg
Toxicity and Overdose:
Antidote is andexanet alfa. Effects persist for at least 24 hrs after last dose. Oral activated charcoal decreases apixaban absorption, lowering plasma concentrations. Other agents and hemodialysis do not have a significant effect.
High Alert: Do not confuse apixaban with axitinib.
Inform patient that they may bruise and bleed more easily or longer than usual. Advise patient to notify health care professional immediately if signs of bleeding (unusual bruising, pink or brown urine, red or black, tarry stools, coughing up blood, vomiting blood, pain or swelling in a joint, headache, dizziness, weakness, recurring nose bleeds, unusual bleeding from gums, heavier than normal menstrual bleeding, dyspepsia, abdominal pain, epigastric pain) occurs or if injury occurs, especially head injury.
Caution patient to notify health care professional if skin rash or signs of severe allergic reaction (chest pain or tightness, swelling of face or tongue, trouble breathing or wheezing, feeling dizzy or faint) occur.
Reduction in the risk and treatment of stroke and systemic embolism.