ELIQUIS SPRINKLE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ELIQUIS SPRINKLE (ELIQUIS SPRINKLE).

How it works

Apixaban is a selective, reversible, direct inhibitor of factor Xa, inhibiting both free and clot-bound factor Xa, thereby reducing thrombin generation and thrombus formation.

What the body does with it

Metabolism	Apixaban is metabolized primarily via CYP3A4/5, with minor contributions from CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2J2. It is also a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP).
Excretion	Renal 27% unchanged; hepatic metabolism via CYP3A4/5 and CYP-independent hydrolysis, with fecal elimination as metabolites.
Half-life	Terminal half-life 12 hours (range 9-14h) in healthy adults; prolonged to approximately 24 hours in moderate renal impairment (CrCl 15-30 mL/min).
Protein binding	~87% bound to plasma proteins (primarily albumin).
Volume of Distribution	Vd ~0.3 L/kg, indicating low tissue distribution and primarily plasma compartment.
Bioavailability	Oral bioavailability ~50% for the 5 mg dose (60% for 2.5 mg dose) under fed conditions; slightly reduced with food but no significant clinical impact.
Onset of Action	Oral: 3-4 hours to peak effect (anti-Factor Xa activity); therapeutic anticoagulation established within 1-2 hours of initial dose.
Duration of Action	Approximately 12 hours after a single dose, consistent with trough levels at 12 hours; sustained anticoagulation with twice-daily dosing.

Classification & Brands

Dosing & administration

5 mg orally twice daily; for certain patients meeting criteria (age ≥80 years, body weight ≤60 kg, or serum creatinine ≥1.5 mg/dL), dose is 2.5 mg orally twice daily.

Dosage form	FOR SUSPENSION
Renal impairment	For CrCl 15–29 mL/min: 2.5 mg twice daily. CrCl <15 mL/min: not recommended. No adjustment for CrCl ≥30 mL/min.
Liver impairment	Contraindicated in patients with Child-Pugh B or C hepatic impairment. No dose adjustment for Child-Pugh A.
Pediatric use	For patients aged <18 years: safety and efficacy not established; not recommended.
Geriatric use	No specific age-based dose adjustment; use 2.5 mg twice daily if age ≥80 years and at least one of: body weight ≤60 kg or serum creatinine ≥1.5 mg/dL.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ELIQUIS SPRINKLE (ELIQUIS SPRINKLE).

Breastfeeding	Unknown if excreted in human breast milk. M/P ratio not available. Animal studies show excretion in rat milk. Caution advised due to potential for bleeding or thrombosis in nursing infant.
Teratogenic Risk	FDA Pregnancy Category B. Animal studies showed no evidence of fetal harm, but adequate human studies are lacking. Apixaban crosses the placenta. Risk of hemorrhage in fetus during labor and delivery. Avoid use in pregnancy unless clearly needed.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

ELIQUIS (apixaban) is not recommended for use in patients with prosthetic heart valves, including those with bioprosthetic valves.

Side Effect Profile

Common Effects	Anemia low number of red blood cells Blood in urine Bruise Nausea Nosebleeds Hematoma
Serious Effects

Absolute Contraindications

["Active pathological bleeding","Hypersensitivity to apixaban or any component of the formulation","Prosthetic heart valves (including bioprosthetic)","Moderate to severe mitral stenosis"]

Clinical Precautions

Precautions

["Increased risk of thrombotic events with abrupt discontinuation","Spinal/epidural hematoma with neuraxial anesthesia or spinal puncture","Bleeding risk","Use in patients with moderate to severe renal impairment","Use in patients with hepatic impairment","Concomitant use with other anticoagulants","Pregnancy and lactation","Patients with active cancer"]

Clinical Tips & Counseling

Drug interactions

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ELIQUIS SPRINKLE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ELIQUIS SPRINKLE (ELIQUIS SPRINKLE).

How it works

Apixaban is a selective, reversible, direct inhibitor of factor Xa, inhibiting both free and clot-bound factor Xa, thereby reducing thrombin generation and thrombus formation.

What the body does with it

Metabolism	Apixaban is metabolized primarily via CYP3A4/5, with minor contributions from CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2J2. It is also a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP).
Excretion	Renal 27% unchanged; hepatic metabolism via CYP3A4/5 and CYP-independent hydrolysis, with fecal elimination as metabolites.
Half-life	Terminal half-life 12 hours (range 9-14h) in healthy adults; prolonged to approximately 24 hours in moderate renal impairment (CrCl 15-30 mL/min).
Protein binding	~87% bound to plasma proteins (primarily albumin).
Volume of Distribution	Vd ~0.3 L/kg, indicating low tissue distribution and primarily plasma compartment.
Bioavailability	Oral bioavailability ~50% for the 5 mg dose (60% for 2.5 mg dose) under fed conditions; slightly reduced with food but no significant clinical impact.
Onset of Action	Oral: 3-4 hours to peak effect (anti-Factor Xa activity); therapeutic anticoagulation established within 1-2 hours of initial dose.
Duration of Action	Approximately 12 hours after a single dose, consistent with trough levels at 12 hours; sustained anticoagulation with twice-daily dosing.

Classification & Brands

Dosing & administration

5 mg orally twice daily; for certain patients meeting criteria (age ≥80 years, body weight ≤60 kg, or serum creatinine ≥1.5 mg/dL), dose is 2.5 mg orally twice daily.

Dosage form	FOR SUSPENSION
Renal impairment	For CrCl 15–29 mL/min: 2.5 mg twice daily. CrCl <15 mL/min: not recommended. No adjustment for CrCl ≥30 mL/min.
Liver impairment	Contraindicated in patients with Child-Pugh B or C hepatic impairment. No dose adjustment for Child-Pugh A.
Pediatric use	For patients aged <18 years: safety and efficacy not established; not recommended.
Geriatric use	No specific age-based dose adjustment; use 2.5 mg twice daily if age ≥80 years and at least one of: body weight ≤60 kg or serum creatinine ≥1.5 mg/dL.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ELIQUIS SPRINKLE (ELIQUIS SPRINKLE).

Breastfeeding	Unknown if excreted in human breast milk. M/P ratio not available. Animal studies show excretion in rat milk. Caution advised due to potential for bleeding or thrombosis in nursing infant.
Teratogenic Risk	FDA Pregnancy Category B. Animal studies showed no evidence of fetal harm, but adequate human studies are lacking. Apixaban crosses the placenta. Risk of hemorrhage in fetus during labor and delivery. Avoid use in pregnancy unless clearly needed.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

ELIQUIS (apixaban) is not recommended for use in patients with prosthetic heart valves, including those with bioprosthetic valves.

Side Effect Profile

Common Effects	Anemia low number of red blood cells Blood in urine Bruise Nausea Nosebleeds Hematoma
Serious Effects

Absolute Contraindications

["Active pathological bleeding","Hypersensitivity to apixaban or any component of the formulation","Prosthetic heart valves (including bioprosthetic)","Moderate to severe mitral stenosis"]