Apixaban

Trade names

ELIQUIS

Actions

• Direct factor Xa inhibitor

Route of Administration

Oral

Bioavailability

66%

Plasma protein binding

~87%

Time to peak plasma concentration

2.5–4 h

Half-life

8–15 h

Duration of action

24 h

Metabolism

Hepatic

Enzymes involved

• CYP3A4
• CYP3A5
• CYP1A2

Elimination

Renal 25%

Interactions

CYP3Y4 and P-glycoprotein inhibitors increase the serum levels of apixaban.

CYP3Y4 inducers decrease the serum levels of apixabaan.

Recommended dose

Stroke prophylaxis in non-valvular AF or DVT prophylaxis:

5 mg twice daily

Reduce to 2.5 mg twice daily in patients with at least two of the following:

• age ≥80 years
• body weight ≤60 kg
• serum creatinine ≥1.5 mg/dL (133 µmol/l)

Renal impairment

In patients with creatinine clearance 15-29 ml/min the therapeutic dose of apixaban should be reduced to 2.5 mg twice daily.

Apixaban is not recommended in patients with creatinine clearance <15 ml/min or patients in dialysis.

Hepatic impairment

No dose adjustment is necessary in patients with mild to moderate hepatic impairment (Child-Pugh class A or B).

Apixaban is not recommended in patients with severe hepatic impairment.

Discontinuation before invasive procedures

If bleeding risk is low, abixaban can be discontinued 24 hours before an invasive procedure. If bleeding risk is moderate or high, abixaban should be discontinued at least 48 hours before the procedure.

Indwelling epidural or intrathecal catheters should not be removed earlier than 24 hours after the last administration of apixaban and the next dose should not be administered earlier than 5 hours after the removal of the catheter.

If traumatic puncture occurs, delay the administration of apixaban for 48 hours.

Bridging anticoagulation is generally not required.