VIMPAT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VIMPAT (VIMPAT).

How it works

Selective enhancement of slow inactivation of voltage-gated sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing.

What the body does with it

Metabolism	Primarily via glucuronidation by UGT2B7, UGT1A8, UGT1A9, and UGT1A1; minor oxidation via CYP2C19 to O-desmethyl metabolite.
Excretion	Renal: ~95% (40% as parent drug, 39% as O-desmethyl metabolite, and ~15% as other minor metabolites); minimal biliary/fecal elimination (less than 1%).
Half-life	Terminal half-life: 13-16 hours (mean ~13 h at steady state); prolonged with renal impairment (CrCl <30 mL/min: ~22 h) and in patients with hepatic impairment (Child-Pugh B: ~17 h; Child-Pugh C: ~22 h).
Protein binding	<15% bound to serum proteins; binding is to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.45 L/kg (mean); distributes into total body water; higher Vd in children (0.6-0.7 L/kg).
Bioavailability	Oral immediate-release: ~100% (nearly complete absorption). Intravenous: 100% (bioequivalent to oral). Oral extended-release: ~100% (slightly lower Cmax but bioequivalent in AUC).
Onset of Action	Oral: Peak plasma concentration (Tmax) 1-4 hours; initial clinical effect may be seen within a week of starting titration. Intravenous: similar to oral, with Tmax at the end of infusion (30-60 min).
Duration of Action	Steady state achieved within 3-4 days; dosing interval is 12 hours for immediate-release; extended-release (XR) formulation allows once-daily dosing. Duration of antiepileptic effect requires consistent dosing; immediate effects for breakthrough seizures are not applicable.

Classification & Brands

Dosing & administration

Adults: 200 mg oral or IV as a loading dose, followed by 100 mg twice daily (200 mg/day) starting the day after loading. May increase by 50 mg twice daily every week up to 200 mg twice daily (400 mg/day).

Dosage form	SOLUTION
Renal impairment	CrCl ≥50 mL/min: usual dose. CrCl 30-49 mL/min: maximum 250 mg/day. CrCl 15-29 mL/min: maximum 200 mg/day. CrCl <15 mL/min: not recommended. Hemodialysis: maximum 250 mg/day; consider supplement after dialysis.
Liver impairment	Child-Pugh A: maximum 300 mg/day. Child-Pugh B: maximum 200 mg/day. Child-Pugh C: not recommended.
Pediatric use	1 month to <17 years: loading dose optional 3.5 mg/kg IV, then 1 mg/kg twice daily (2 mg/kg/day); may increase by 0.5 mg/kg twice daily every week to maintenance 3 mg/kg twice daily (6 mg/kg/day, max 200 mg twice daily).
Geriatric use	Consider dose adjustment based on renal function; start at lower dose (e.g., 100 mg/day) if CrCl <50 mL/min. Monitor for adverse effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for VIMPAT (VIMPAT).

Breastfeeding

Lacosamide is excreted in human milk. The milk-to-plasma ratio (M/P) is 0.4-0.6. Infant exposure is estimated at 2-3% of maternal weight-adjusted dose. Monitor infant for somnolence, poor feeding, and growth. Caution recommended.

Teratogenic Risk

VIMPAT (lacosamide) is classified as Pregnancy Category C. Animal studies have shown fetal harm at doses comparable to human therapeutic levels. In first trimester, there is a potential risk of major congenital malformations, though human data are limited. During second and third trimesters, there is risk of adverse neurodevelopmental outcomes and growth restriction. Use only if benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to lacosamide or any ingredient in the formulation"]

Clinical Precautions

Precautions

["Suicidal behavior and ideation","Dizziness and ataxia","Syncope and hypotension","Cardiac conduction abnormalities (PR prolongation, atrial fibrillation, atrial flutter)","Withdrawal seizures"]

Clinical Tips & Counseling

Drug interactions

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VIMPAT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VIMPAT (VIMPAT).

How it works

Selective enhancement of slow inactivation of voltage-gated sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing.

What the body does with it

Metabolism	Primarily via glucuronidation by UGT2B7, UGT1A8, UGT1A9, and UGT1A1; minor oxidation via CYP2C19 to O-desmethyl metabolite.
Excretion	Renal: ~95% (40% as parent drug, 39% as O-desmethyl metabolite, and ~15% as other minor metabolites); minimal biliary/fecal elimination (less than 1%).
Half-life	Terminal half-life: 13-16 hours (mean ~13 h at steady state); prolonged with renal impairment (CrCl <30 mL/min: ~22 h) and in patients with hepatic impairment (Child-Pugh B: ~17 h; Child-Pugh C: ~22 h).
Protein binding	<15% bound to serum proteins; binding is to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.45 L/kg (mean); distributes into total body water; higher Vd in children (0.6-0.7 L/kg).
Bioavailability	Oral immediate-release: ~100% (nearly complete absorption). Intravenous: 100% (bioequivalent to oral). Oral extended-release: ~100% (slightly lower Cmax but bioequivalent in AUC).
Onset of Action	Oral: Peak plasma concentration (Tmax) 1-4 hours; initial clinical effect may be seen within a week of starting titration. Intravenous: similar to oral, with Tmax at the end of infusion (30-60 min).
Duration of Action	Steady state achieved within 3-4 days; dosing interval is 12 hours for immediate-release; extended-release (XR) formulation allows once-daily dosing. Duration of antiepileptic effect requires consistent dosing; immediate effects for breakthrough seizures are not applicable.

Classification & Brands

Dosing & administration

Dosage form	SOLUTION
Renal impairment	CrCl ≥50 mL/min: usual dose. CrCl 30-49 mL/min: maximum 250 mg/day. CrCl 15-29 mL/min: maximum 200 mg/day. CrCl <15 mL/min: not recommended. Hemodialysis: maximum 250 mg/day; consider supplement after dialysis.
Liver impairment	Child-Pugh A: maximum 300 mg/day. Child-Pugh B: maximum 200 mg/day. Child-Pugh C: not recommended.
Pediatric use	1 month to <17 years: loading dose optional 3.5 mg/kg IV, then 1 mg/kg twice daily (2 mg/kg/day); may increase by 0.5 mg/kg twice daily every week to maintenance 3 mg/kg twice daily (6 mg/kg/day, max 200 mg twice daily).
Geriatric use	Consider dose adjustment based on renal function; start at lower dose (e.g., 100 mg/day) if CrCl <50 mL/min. Monitor for adverse effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for VIMPAT (VIMPAT).

Breastfeeding

Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to lacosamide or any ingredient in the formulation"]

Clinical Precautions

Precautions

["Suicidal behavior and ideation","Dizziness and ataxia","Syncope and hypotension","Cardiac conduction abnormalities (PR prolongation, atrial fibrillation, atrial flutter)","Withdrawal seizures"]

Clinical Tips & Counseling

Drug interactions

Loading safety data…