Anticoagulant · Factor Xa inhibitor

Apixaban (Eliquis)

Also called Eliquis

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Indications

Stroke prevention in nonvalvular atrial fibrillation
Treatment of DVT and PE, and prevention of recurrence
VTE prophylaxis after hip or knee replacement
Cancer-associated VTE
Stable HIT, in place of warfarin (off-label)
VTE in children from birth, after at least 5 days of initial anticoagulation

Mechanism of action

Apixaban binds the active site of factor Xa directly and reversibly, with no need for antithrombin. It inhibits free Xa, Xa assembled in the prothrombinase complex on platelet membranes and clot-bound Xa, which the heparin–antithrombin complex reaches poorly. Because each Xa molecule generates many thrombin molecules, this blunts the thrombin burst; apixaban has no direct effect on platelets but reduces thrombin-induced aggregation.

Pharmacology

Hematologic: anti-Xa activity tracks the plasma level, peaking 3–4 h after a dose
Hematologic: PT, INR and aPTT change little, so a normal PT does not exclude a meaningful level; use a drug-calibrated anti-Xa (heparin-calibrated assays read high for 2–3 days)
Hematologic: in ARISTOTLE (NEJM 2011) it beat warfarin on stroke and systemic embolism (1.27% vs 1.60% per year) with less major bleeding (2.1% vs 3.1%)

Pharmacokinetics

Onset and peak	Oral; peak 3–4 h
Duration	About 24 h; most procedures need a 1–2 day hold (PAUSE)
Half-life	About 12 h orally but about 5 h after IV dosing, so absorption sets the oral value
Bioavailability	About 50%; no food effect
Distribution	Vd about 21 L; 87% protein-bound
Metabolism	Mainly CYP3A4/5, minor 1A2, 2C8, 2C9, 2C19 and 2J2; no active metabolites; P-gp and BCRP substrate
Elimination	Kidneys about 27% of clearance, the lowest DOAC share; the rest via bile and intestine to feces
Organ failure	Allowed on dialysis; the AF dose is halved with 2 of: age ≥80, weight ≤60 kg, creatinine ≥1.5 mg/dL; avoid in Child-Pugh C
Dialysis	Clearance about 18 mL/min: not meaningfully removed
Routes	Whole or crushed in water, D5W, apple juice or applesauce, or crushed in D5W via NG tube

Chemistry

Pyrazolopyridinone carboxamide: a tetrahydro-pyrazolo[3,4-c]pyridin-7-one core with a 4-methoxyphenyl and a 2-oxopiperidinyl-phenyl lactam; MW 459.5
Its neutral p-methoxyphenyl group fills the S1 pocket that early Xa inhibitors filled with charged amidines, keeping potency with good oral bioavailability (Pinto 2007)
Achiral; does not ionize between pH 1.2 and 6.8; water solubility about 0.04 mg/mL; XLogP 2.2
Film-coated 2.5 mg (yellow) and 5 mg (pink) tablets; pediatric 0.5 mg tablets for suspension and 0.15 mg sprinkle capsules

Adverse effects and cautions

In the one-pagers

Pulmonary EmbolismAnticoagulation: choice, dosing and timing: Apixaban: 10 mg twice daily for 7 days, then 5 mg twice daily: No heparin lead-in; 2.5 mg twice daily if extended

Practice Pulmonary Embolism questions free8 exam-style questions with rationales on the topic where Apixaban comes up most. No account or download needed.

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Massive Hemoptysis

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Sources

FDA label: Eliquis (2025)
Byon et al., Clin Pharmacokinet (2019)
ARISTOTLE, NEJM (2011)
FDA safety communication: andexanet (2025)

For education and exam preparation only. Follow your institution’s protocols. Typical adult values for study. Follow your local protocols and medical direction.