APTIOM

Clinical safety rating: caution

Comprehensive clinical and safety monograph for APTIOM (APTIOM).

How it works

Selective enhancement of slow inactivation of voltage-gated sodium channels, stabilizing neuronal membranes and inhibiting excitatory neurotransmitter release.

What the body does with it

Metabolism	Primarily glucuronidation via UGT2B7; also metabolized by CYP3A4, CYP2C19, and CYP1A2 to a lesser extent.
Excretion	Primarily eliminated by hepatic metabolism, with approximately 95% excreted as metabolites in urine and <2% as unchanged drug. Fecal excretion accounts for about 5%.
Half-life	Terminal elimination half-life ranges from 20 to 48 hours (mean ~32 hours). Steady-state achieved within 5-7 days.
Protein binding	Approximately 90% bound to human plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Volume of distribution is approximately 1.3 L/kg, suggesting extensive distribution into tissues.
Bioavailability	Oral bioavailability is approximately 60% (range 53-68%).
Onset of Action	Not applicable for acute effect; steady-state concentrations achieved after ~5-7 days of once-daily dosing.
Duration of Action	Once-daily dosing provides sustained therapeutic effect over 24 hours, with trough concentrations maintaining efficacy.

Classification & Brands

Dosing & administration

Initial: 50 mg orally once daily; titrate at weekly intervals by 50 mg twice daily increments to maintenance dose of 200 mg twice daily (400 mg/day). Maximum: 400 mg twice daily (800 mg/day).

Dosage form	TABLET
Renal impairment	Estimated creatinine clearance (CrCl) >50 mL/min: no adjustment. CrCl 30-50 mL/min: reduce maintenance dose by 50%; CrCl <30 mL/min and not on hemodialysis: not recommended. Hemodialysis: 50 mg once daily with supplement of 25 mg after dialysis.
Liver impairment	Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce maintenance dose by 50%; initiate at 50 mg once daily, titrate slowly. Child-Pugh Class C: contraindicated.
Pediatric use	Children (≥4 years): Initial 1.5 mg/kg/day orally divided twice daily; titrate weekly by increments of 1.5 mg/kg/day to a maintenance of 3-6 mg/kg/day twice daily. Maximum: 400 mg twice daily.
Geriatric use	No specific dose adjustment based on age alone. Dose selection should be cautious, reflecting higher frequency of decreased renal/hepatic function and concomitant disease or drug therapy. Consider creatinine clearance and titrate slowly.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for APTIOM (APTIOM).

Breastfeeding	Excreted in human milk. Milk-to-plasma ratio not established. Potential for serious adverse reactions in nursing infants (sedation, poor suckling). Use only if benefit outweighs risk; consider alternative anticonvulsants.
Teratogenic Risk	Pregnancy Category D. First trimester: Increased risk of major congenital malformations, including neural tube defects, craniofacial defects, and cardiac anomalies. Second and third trimesters: Risk of fetal antiepileptic drug syndrome (facial dysmorphism, growth retardation, neurodevelopmental delay). Neonatal hemorrhage due to vitamin K deficiency may occur.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to eslicarbazepine acetate or any oxcarbazepine derivative"]

Clinical Precautions

Precautions	["Suicidal behavior and ideation","Angioedema","Anaphylaxis","Dermatological reactions including Stevens-Johnson syndrome","Decreased serum sodium","Dizziness and gait disturbance","Hepatic injury"]
Food/Dietary	Take with or without food. No specific food interactions reported.

Clinical Tips & Counseling

Clinical Pearls

APTIOM (eslicarbazepine acetate) is a once-daily antiepileptic drug for partial-onset seizures. Monitor serum sodium, especially in elderly or those on concomitant hyponatremia-inducing drugs. Titrate to maintenance dose over 2 weeks. Avoid abrupt discontinuation. Contraindicated in second- or third-degree AV block.

Drug interactions

Loading safety data…

APTIOM

Clinical safety rating: caution

Comprehensive clinical and safety monograph for APTIOM (APTIOM).

How it works

Selective enhancement of slow inactivation of voltage-gated sodium channels, stabilizing neuronal membranes and inhibiting excitatory neurotransmitter release.

What the body does with it

Metabolism	Primarily glucuronidation via UGT2B7; also metabolized by CYP3A4, CYP2C19, and CYP1A2 to a lesser extent.
Excretion	Primarily eliminated by hepatic metabolism, with approximately 95% excreted as metabolites in urine and <2% as unchanged drug. Fecal excretion accounts for about 5%.
Half-life	Terminal elimination half-life ranges from 20 to 48 hours (mean ~32 hours). Steady-state achieved within 5-7 days.
Protein binding	Approximately 90% bound to human plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Volume of distribution is approximately 1.3 L/kg, suggesting extensive distribution into tissues.
Bioavailability	Oral bioavailability is approximately 60% (range 53-68%).
Onset of Action	Not applicable for acute effect; steady-state concentrations achieved after ~5-7 days of once-daily dosing.
Duration of Action	Once-daily dosing provides sustained therapeutic effect over 24 hours, with trough concentrations maintaining efficacy.

Classification & Brands

Dosing & administration

Initial: 50 mg orally once daily; titrate at weekly intervals by 50 mg twice daily increments to maintenance dose of 200 mg twice daily (400 mg/day). Maximum: 400 mg twice daily (800 mg/day).

Dosage form	TABLET
Renal impairment	Estimated creatinine clearance (CrCl) >50 mL/min: no adjustment. CrCl 30-50 mL/min: reduce maintenance dose by 50%; CrCl <30 mL/min and not on hemodialysis: not recommended. Hemodialysis: 50 mg once daily with supplement of 25 mg after dialysis.
Liver impairment	Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce maintenance dose by 50%; initiate at 50 mg once daily, titrate slowly. Child-Pugh Class C: contraindicated.
Pediatric use	Children (≥4 years): Initial 1.5 mg/kg/day orally divided twice daily; titrate weekly by increments of 1.5 mg/kg/day to a maintenance of 3-6 mg/kg/day twice daily. Maximum: 400 mg twice daily.
Geriatric use	No specific dose adjustment based on age alone. Dose selection should be cautious, reflecting higher frequency of decreased renal/hepatic function and concomitant disease or drug therapy. Consider creatinine clearance and titrate slowly.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for APTIOM (APTIOM).

Breastfeeding	Excreted in human milk. Milk-to-plasma ratio not established. Potential for serious adverse reactions in nursing infants (sedation, poor suckling). Use only if benefit outweighs risk; consider alternative anticonvulsants.
Teratogenic Risk	Pregnancy Category D. First trimester: Increased risk of major congenital malformations, including neural tube defects, craniofacial defects, and cardiac anomalies. Second and third trimesters: Risk of fetal antiepileptic drug syndrome (facial dysmorphism, growth retardation, neurodevelopmental delay). Neonatal hemorrhage due to vitamin K deficiency may occur.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to eslicarbazepine acetate or any oxcarbazepine derivative"]

Clinical Precautions

Precautions	["Suicidal behavior and ideation","Angioedema","Anaphylaxis","Dermatological reactions including Stevens-Johnson syndrome","Decreased serum sodium","Dizziness and gait disturbance","Hepatic injury"]
Food/Dietary	Take with or without food. No specific food interactions reported.

Clinical Tips & Counseling

Clinical Pearls

Drug interactions

Loading safety data…