ASPRUZYO SPRINKLE

Clinical safety rating: caution

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

How it works

ASPRUZYO SPRINKLE (lacosamide) enhances slow inactivation of voltage-gated sodium channels, stabilizing neuronal membranes and inhibiting repetitive neuronal firing.

What the body does with it

Metabolism	Lacosamide is primarily metabolized by CYP2C19, CYP3A4, and to a lesser extent by CYP2C9, with less than 20% excreted unchanged in urine.
Excretion	Primarily hepatic metabolism via CYP3A4 and CYP2C9, with <2% excreted unchanged in urine. Biliary/fecal excretion accounts for >90% of metabolites.
Half-life	Terminal half-life is approximately 20-30 hours, allowing for once-daily dosing. Steady-state achieved within 5-7 days.
Protein binding	Approximately 99% bound to serum albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Vd is approximately 0.6-0.8 L/kg, suggesting distribution into total body water.
Bioavailability	Oral bioavailability is approximately 60-70% with the sprinkle formulation. Food may increase absorption.
Onset of Action	Oral (sprinkle): Clinical effect observed within 2-4 weeks, with maximal effect by 8-12 weeks.
Duration of Action	Duration of clinical effect supports once-daily dosing. Therapeutic drug monitoring recommended to maintain trough concentrations between 100-350 ng/mL.

Classification & Brands

Dosing & administration

Oral: 30 mg once daily, with or without food. Sprinkle capsules can be opened and contents mixed with soft food or liquid.

Dosage form	GRANULES, EXTENDED RELEASE
Renal impairment	eGFR 30-89 mL/min/1.73m2: No adjustment. eGFR 15-29: Reduce to 15 mg once daily. eGFR <15 or dialysis: Not recommended.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce to 15 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Not approved for pediatric use. Safety and efficacy not established.
Geriatric use	No specific dose adjustment; use caution due to potential renal impairment (monitor renal function).

Use during pregnancy

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

Clinical note

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

Breastfeeding	Bisoprolol is excreted in breast milk; milk-to-plasma ratio approximately 1.9. Monitor infant for bradycardia, hypotension, and hypoglycemia. Consider alternative treatments unless benefit to mother outweighs potential risk to infant.
Teratogenic Risk	ASPRUZYO SPRINKLE contains bisoprolol fumarate, a beta-blocker. First trimester: limited data, potential risk of fetal bradycardia and hypoglycemia. Second and third trimesters: associated with fetal growth restriction, bradycardia, hypoglycemia, and respiratory depression. Avoid use unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

There is no FDA boxed warning for lacosamide.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to lacosamide or any component of the formulation","Second- or third-degree AV block (unless pacemaker)"]

Clinical Precautions

Precautions	["Cardiac conduction abnormalities (PR interval prolongation, AV block, atrial fibrillation/flutter)","Suicidal ideation and behavior (antiepileptic drug class)","Dizziness and ataxia (especially at high doses)","Withdrawal seizures (abrupt discontinuation)","Serious dermatologic reactions (e.g., DRESS, Stevens-Johnson syndrome)"]
Food/Dietary	Avoid high-fiber foods within 1 hour of taking ASPRUZYO as they may impair enzyme activity. Do not mix with milk, ice cream, or other alkaline foods/drinks. Take with acidic foods like applesauce, pears, or fruit juice (pH < 5.5). Enteral tube feeding: do not mix with tube feed formulas; administration via tube is not recommended due to microsphere size.

Clinical Tips & Counseling

Drug interactions

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ASPRUZYO SPRINKLE

Clinical safety rating: caution

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

How it works

ASPRUZYO SPRINKLE (lacosamide) enhances slow inactivation of voltage-gated sodium channels, stabilizing neuronal membranes and inhibiting repetitive neuronal firing.

What the body does with it

Metabolism	Lacosamide is primarily metabolized by CYP2C19, CYP3A4, and to a lesser extent by CYP2C9, with less than 20% excreted unchanged in urine.
Excretion	Primarily hepatic metabolism via CYP3A4 and CYP2C9, with <2% excreted unchanged in urine. Biliary/fecal excretion accounts for >90% of metabolites.
Half-life	Terminal half-life is approximately 20-30 hours, allowing for once-daily dosing. Steady-state achieved within 5-7 days.
Protein binding	Approximately 99% bound to serum albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Vd is approximately 0.6-0.8 L/kg, suggesting distribution into total body water.
Bioavailability	Oral bioavailability is approximately 60-70% with the sprinkle formulation. Food may increase absorption.
Onset of Action	Oral (sprinkle): Clinical effect observed within 2-4 weeks, with maximal effect by 8-12 weeks.
Duration of Action	Duration of clinical effect supports once-daily dosing. Therapeutic drug monitoring recommended to maintain trough concentrations between 100-350 ng/mL.

Classification & Brands

Dosing & administration

Oral: 30 mg once daily, with or without food. Sprinkle capsules can be opened and contents mixed with soft food or liquid.

Dosage form	GRANULES, EXTENDED RELEASE
Renal impairment	eGFR 30-89 mL/min/1.73m2: No adjustment. eGFR 15-29: Reduce to 15 mg once daily. eGFR <15 or dialysis: Not recommended.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce to 15 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Not approved for pediatric use. Safety and efficacy not established.
Geriatric use	No specific dose adjustment; use caution due to potential renal impairment (monitor renal function).

Use during pregnancy

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

Clinical note

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

Breastfeeding	Bisoprolol is excreted in breast milk; milk-to-plasma ratio approximately 1.9. Monitor infant for bradycardia, hypotension, and hypoglycemia. Consider alternative treatments unless benefit to mother outweighs potential risk to infant.
Teratogenic Risk	ASPRUZYO SPRINKLE contains bisoprolol fumarate, a beta-blocker. First trimester: limited data, potential risk of fetal bradycardia and hypoglycemia. Second and third trimesters: associated with fetal growth restriction, bradycardia, hypoglycemia, and respiratory depression. Avoid use unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

There is no FDA boxed warning for lacosamide.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to lacosamide or any component of the formulation","Second- or third-degree AV block (unless pacemaker)"]

Clinical Precautions

Precautions	["Cardiac conduction abnormalities (PR interval prolongation, AV block, atrial fibrillation/flutter)","Suicidal ideation and behavior (antiepileptic drug class)","Dizziness and ataxia (especially at high doses)","Withdrawal seizures (abrupt discontinuation)","Serious dermatologic reactions (e.g., DRESS, Stevens-Johnson syndrome)"]
Food/Dietary	Avoid high-fiber foods within 1 hour of taking ASPRUZYO as they may impair enzyme activity. Do not mix with milk, ice cream, or other alkaline foods/drinks. Take with acidic foods like applesauce, pears, or fruit juice (pH < 5.5). Enteral tube feeding: do not mix with tube feed formulas; administration via tube is not recommended due to microsphere size.

Clinical Tips & Counseling

Drug interactions

Loading safety data…