Version May 2024
Seizures, partial (focal) onset:
Note: For patients already on a single antiseizure medication and converting to lacosamide monotherapy, maintain the maintenance dose for 3 days before beginning withdrawal of the concomitant antiseizure drug. Gradually taper the concomitant antiseizure drug over ≥6 weeks. When switching from oral to IV formulations in patients weighing ≥6 kg, the total daily dose and frequency should be the same; IV therapy should only be used temporarily. Clinical study experience of IV lacosamide is limited to 5 days of consecutive treatment.
Infants, Children, and Adolescents <17 years:
Monotherapy and adjunctive therapy:
<6 kg: In patients <6 kg, oral and intravenous dosing is different; use caution.
IV:
Initial: IV: 0.66 mg/kg/dose 3 times daily; may be increased at weekly intervals by 0.66 mg/kg/dose 3 times daily based on response and tolerability.
Maintenance: IV: 2.5 to 5 mg/kg/dose 3 times daily.
Oral:
Initial: Oral (immediate release): 1 mg/kg/dose twice daily; may be increased at weekly intervals by 1 mg/kg/dose twice daily based on response and tolerability.
Maintenance: Oral (immediate release): 3.75 to 7.5 mg/kg/dose twice daily.
6 to <30 kg:
Initial: Oral (immediate release), IV: 1 mg/kg/dose twice daily; may be increased at weekly intervals by 1 mg/kg/dose twice daily based on response and tolerability.
Maintenance: Oral (immediate release), IV: 3 to 6 mg/kg/dose twice daily.
30 to <50 kg:
Initial: Oral (immediate release), IV: 1 mg/kg/dose twice daily; may be increased at weekly intervals by 1 mg/kg/dose twice daily based on response and tolerability.
Maintenance: Oral (immediate release), IV: 2 to 4 mg/kg/dose twice daily.
≥50 kg:
Immediate-release preparations:
Initial (monotherapy and adjunctive therapy): Oral (immediate release), IV: 50 mg twice daily; may be increased at weekly intervals of 50 mg twice daily based on response and tolerability.
Maintenance:
Monotherapy maintenance: Oral (immediate release), IV: 150 to 200 mg twice daily.
Adjunctive therapy maintenance: Oral (immediate release), IV: 100 to 200 mg twice daily.
Extended-release preparations:
Initial (monotherapy and adjunctive therapy): Oral (extended release [eg, Motpoly XR]): 100 mg once daily; may be increased at weekly intervals in 100 mg/day increments based on response and tolerability.
Maintenance:
Monotherapy maintenance: Oral (extended release [eg, Motpoly XR]): 300 to 400 mg once daily.
Adjunctive therapy maintenance: Oral (extended release [eg, Motpoly XR]): 200 to 400 mg once daily.
Adolescents ≥17 years:
Immediate-release preparations:
Monotherapy:
Initial: Oral (immediate release), IV: 100 mg twice daily; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability.
Alternate initial dosage: Oral (immediate release), IV: Loading dose: 200 mg followed approximately 12 hours later by 100 mg twice daily for 1 week; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability. Note: Administer loading doses under medical supervision because of the increased incidence of CNS adverse reactions.
Maintenance: Oral (immediate release), IV: 150 to 200 mg twice daily. Note: Doses up to 300 mg twice daily may provide additional benefit in some patients (Ref).
Adjunctive therapy:
Initial: Oral (immediate release), IV: 50 mg twice daily; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability.
Alternative initial dosage: Oral (immediate release), IV: Loading dose of 200 mg followed approximately 12 hours later by 100 mg twice daily for 1 week; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability. Note: Administer loading doses under medical supervision because of the increased incidence of CNS adverse reactions.
Maintenance dose: Oral (immediate release), IV: 100 to 200 mg twice daily. Note: Doses up to 300 mg twice daily may provide additional benefit in some patients; however, risk of adverse effects may be greater when higher doses of lacosamide are used in combination with other agents (Ref).
Extended-release preparations :
Monotherapy:
Initial: Oral (extended release [Motpoly XR]): 200 mg once daily; may be increased at weekly intervals in 100 mg/day increments based on response and tolerability.
Maintenance: Oral (extended release [Motpoly XR]): 300 to 400 mg once daily.
Adjunctive therapy:
Initial: Oral (extended release [Motpoly XR]): 100 mg once daily; may be increased at weekly intervals in 100 mg/day increments based on response and tolerability.
Maintenance: Oral (extended release [Motpoly XR]): 200 to 400 mg once daily.
Seizures, primary generalized tonic-clonic; adjunctive therapy:
Note: When switching from oral to IV formulations, the total daily dose and frequency should be the same; IV therapy should only be used temporarily. Clinical study experience of IV lacosamide is limited to 5 days of consecutive treatment.
Children ≥4 years and Adolescents <17 years:
Immediate-release preparations:
11 to <30 kg:
Initial: Oral (immediate release), IV: 1 mg/kg/dose twice daily; may be increased at weekly intervals by 1 mg/kg/dose twice daily based on response and tolerability.
Maintenance: Oral (immediate release), IV: 3 to 6 mg/kg/dose twice daily.
30 to <50 kg:
Initial: Oral (immediate release), IV: 1 mg/kg/dose twice daily; may be increased at weekly intervals by 1 mg/kg/dose twice daily based on response and tolerability.
Maintenance: Oral (immediate release), IV: 2 to 4 mg/kg/dose twice daily.
≥50 kg:
Initial: Oral (immediate release), IV: 50 mg twice daily; may be increased at weekly intervals of 50 mg twice daily based on response and tolerability.
Maintenance: Oral (immediate release), IV: 100 to 200 mg twice daily. Note: In clinical trials of adjunctive therapy in adults, doses higher than 400 mg/day were not more effective and were associated with more adverse reactions.
Adolescents ≥17 years:
Immediate-release preparations:
Initial: Oral (immediate release), IV: 50 mg twice daily; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability.
Alternative initial dosage: Oral (immediate release), IV: Loading dose of 200 mg followed approximately 12 hours later by 100 mg twice daily for 1 week; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability. Note: Administer loading doses under medical supervision because of the increased incidence of CNS adverse reactions.
Maintenance dose: Oral (immediate release), IV: 100 to 200 mg twice daily. Note: In clinical trials of adjunctive therapy in adults, doses higher than 400 mg/day were not more effective and were associated with more adverse reactions.
Seizures, refractory: Limited data available: Infants ≥6 months, Children, and Adolescents: Oral (immediate release), IV: Initial: 0.5 to 1 mg/kg/dose twice daily (usual maximum initial dose: 50 mg/dose); may titrate by 0.5 to 1 mg/kg/dose weekly based on response and tolerability. Mean maintenance dose: 3.6 mg/kg/dose; reported range: 0.5 to 10 mg/kg/dose twice daily (Ref). Note: Lacosamide may be more effective in refractory focal seizures as compared to generalized seizures, and efficacy may decrease after initial response (Ref).
Status epilepticus, refractory: Limited data available: Note: Optimal place in therapy not defined; variable regimens reported; use is typically reported after failure of ≥2 to 3 agents; dosing based on retrospective case series (Ref).
Infants, Children, and Adolescents:
Loading dose: IV: 5 to 10 mg/kg/dose as a single dose, infused over 15 to 30 minutes; reported range for loading dose: 2 to 11 mg/kg/dose (Ref). Usual maximum loading dose in adults: 400 mg/dose; doses up to 600 mg/dose have been reported (Ref).
Maintenance dose: IV: 6.5 mg/kg/dose twice daily; range of reported maintenance doses: 0.5 to 7 mg/kg/dose twice daily; usual adult maximum dose: 200 mg/dose (Ref).
Discontinuation of therapy: There is currently no standard method for the withdrawal of antiseizure medications in pediatric patients. Successful discontinuation of an antiseizure medication is dependent on several factors including but not limited to: Time of seizure freedom, underlying reason for the seizures, neuroimaging abnormalities, underlying neurodevelopmental status, and medication to be withdrawn (including dose, duration of therapy, and other pharmacokinetic/dynamic considerations) (Ref). Avoid abrupt discontinuation; gradually withdraw over ≥1 week (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Infants, Children, and Adolescents: Immediate release, extended release:
Note: Titrate dose with caution; use the Schwartz equation for calculation in pediatric patients.
Mild to moderate renal impairment (CrCl ≥30 mL/minute/1.73 m2): No dose adjustment necessary.
Severe renal impairment (CrCl <30 mL/minute/1.73 m2): Maximum daily dose: Reduce dose to 75% of maximum dose, not to exceed 300 mg/day.
End-stage renal disease (ESRD) requiring hemodialysis: Maximum daily dose: Reduce dose to 75% of maximum dose. Removed by hemodialysis; after 4-hour hemodialysis treatment, a supplemental dose of up to 50% should be considered.
Infants, Children, and Adolescents: Titrate dose with caution.
Mild to moderate hepatic impairment: Maximum daily dose: Reduce dose to 75% of maximum dose.
Severe hepatic impairment: Use is not recommended.
(For additional information see "Lacosamide: Drug information")
Focal (partial) onset seizures:
Monotherapy:
Oral:
Immediate release (tablets, oral solution): Initial: 50 to 100 mg twice daily; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability to a maintenance dose of 150 to 200 mg twice daily. Doses up to 600 mg/day may provide additional benefit in some patients (Ref). Alternatively, may give 200 mg loading dose followed 12 hours later by 100 mg twice daily with same titration schedule. Administer loading doses under medical supervision due to increased incidence of CNS adverse reactions (Ref).
Extended release (capsules): Initial: 200 mg once daily; may be increased at weekly intervals by 100 mg once daily based on response and tolerability to a maintenance dose of 300 to 400 mg once daily.
IV: Initial: 50 to 100 mg twice daily; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability to a maintenance dose of 150 to 200 mg twice daily (Ref). Doses up to 600 mg/day may provide additional benefit in some patients based on data with the oral formulation (Ref). Alternatively, may give 200 mg loading dose followed 12 hours later by 100 mg twice daily with same titration schedule. Administer loading doses under medical supervision due to increased incidence of CNS adverse reactions (Ref).
Adjunctive therapy:
Oral:
Immediate release (tablets, oral solution): Initial: 50 mg twice daily; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability to a maintenance dose of 100 to 200 mg twice daily (Ref). Alternatively, may give 200 mg loading dose followed 12 hours later by 100 mg twice daily with same titration schedule. Doses up to 600 mg/day may provide additional benefit in some patients; however, risk of adverse effects may be greater when higher doses of lacosamide are used in combination with other agents (Ref). Administer loading doses under medical supervision due to increased incidence of CNS adverse reactions (Ref).
Extended release (capsules): Initial: 100 mg once daily; may be increased at weekly intervals by 100 mg once daily up to a maintenance dose of 200 to 400 mg once daily.
IV: Initial: 50 mg twice daily; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability to a maintenance dose of 100 to 200 mg twice daily (Ref). Alternatively, may give 200 mg loading dose followed 12 hours later by 100 mg twice daily with same titration schedule. Doses up to 600 mg/day may provide additional benefit in some patients based on data with the oral formulation; however, risk of adverse effects may be greater when higher doses of lacosamide are used in combination with other agents (Ref). Administer loading doses under medical supervision due to increased incidence of CNS adverse reactions (Ref).
Primary generalized tonic-clonic seizures:
Adjunctive therapy:
Oral (immediate release tablets, oral solution), IV: Initial: 50 mg twice daily; may be increased at weekly intervals by 50 mg twice daily based on response and tolerability to a maintenance dose of 100 to 200 mg twice daily. Alternatively, may give 200 mg loading dose followed 12 hours later by 100 mg twice daily with same titration schedule. Administer loading doses under medical supervision due to increased incidence of CNS adverse reactions.
Status epilepticus (alternative agent) (off-label use):
IV: Initial: 200 to 400 mg as a single dose followed by a maintenance dose of 200 to 400 mg/day in 2 divided doses (Ref); some patients may require up to 600 mg/day (Ref).
Note: The Neurocritical Care Society recommends an administration rate of 200 mg over 15 minutes; however, some experts administer doses up to 400 mg at a rate of ≤80 mg/minute (eg, 400 mg over 5 minutes) (Ref).
Discontinuation of therapy: Avoid abrupt discontinuation.
Immediate release (tablets, oral solution), IV: Withdraw gradually in weekly intervals by 200 mg/day (Ref).
Extended release (capsules): Withdraw gradually over ≥1 week.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
IV, oral (IR tablets, oral solution; ER capsules) :
Altered kidney function: Note: Renal function may be estimated using the Cockcroft-Gault formula.
CrCl ≥30 mL/minute: Initial and maintenance: No dosage adjustment necessary (Ref).
CrCl <30 mL/minute:
Initial: No dosage adjustment necessary; base initiation and titration schedule on clinical response and tolerability (Ref).
Maintenance: Administer up to 75% of the indication-specific maximum dose (Ref).
Hemodialysis, intermittent (thrice weekly): Dialyzable (50% after a 4-hour hemodialysis session) (Ref):
Initial: No dosage adjustment necessary; administer a supplemental dose (up to 50%) after each hemodialysis session (Ref).
Maintenance: Administer up to 75% of the indication-specific maximum dose; administer a supplemental dose (up to 50%) after each hemodialysis session (Ref).
Peritoneal dialysis:
Initial: No dosage adjustment necessary (Ref).
Maintenance: Administer up to 75% of the indication-specific maximum dose (Ref).
CRRT: Drug clearance is dependent on the effluent flow rate, filter type, and method of renal replacement (Ref). Recommendations are based on high-flux dialyzers and effluent flow rates of 20 to 25 mL/kg/hour (or ~1,500 to 3,000 mL/hour) unless otherwise noted. Appropriate dosing requires consideration of adequate drug concentrations (eg, seizure control) and consideration of initial loading doses, if applicable. Close monitoring of response and adverse reactions (eg, CNS effects) due to drug accumulation is important.
Initial and maintenance: No dosage adjustment is likely necessary (Ref) since lacosamide is significantly removed by CRRT (Ref). However, at higher effluent flow rates (eg, >4,000 mL/hour), some patients may require higher than normal doses (Ref); may consider therapeutic drug monitoring.
PIRRT (eg, sustained, low-efficiency diafiltration): Drug clearance is dependent on the effluent flow rate, filter type, and method of renal replacement. Appropriate dosing requires consideration of adequate drug concentrations (eg, seizure control) and consideration of initial loading doses, if applicable. Close monitoring of response and adverse reactions (eg, CNS effects) due to drug accumulation is important.
Initial: No dosage adjustment necessary; administer a supplemental dose (up to 50%) after each PIRRT session (Ref).
Maintenance: Administer up to 75% of the indication-specific maximum dose; administer a supplemental dose (up to 50%) after each PIRRT session (Ref).
IV, oral ( IR tablets, oral solution; ER capsules):
Mild to moderate hepatic impairment: Administer up to 75% of the indication-specific maximum dose; base initiation and titration schedule on clinical response and tolerability.
Severe hepatic impairment: Use is not recommended.
Lacosamide may cause cardiac arrhythmias including, but not limited to bradycardia, atrioventricular block, and tachyarrhythmias such as atrial fibrillation, atrial flutter, and ventricular tachycardia (Ref). Cardiovascular (CV) adverse reactions are rare but potentially life-threatening (Ref). Restoration of normal cardiac rhythm has occurred following discontinuation (Ref).
Mechanism: Dose-related; acts predominantly by enhancing the slow inactivation of voltage-dependent sodium channels (Ref). Sodium channel-blocking drugs such as lacosamide cause slowing of conduction velocity in cardiac tissues, predominantly in non-nodal tissues (Ref). Specifically, lacosamide appears to disrupt the SCN5A channel for which mutations have been previously linked to Brugada syndrome (Ref).
Onset: Exact onset is unknown. Some literature suggests onset may occur during IV administration (Ref), but some cases reported abnormal ECG after chronic oral use as well (Ref).
Risk factors:
• Higher doses (Ref)
• CV comorbidities (eg, CV disease, cardiac conduction abnormalities) (Ref)
• Older age (Ref)
• Concurrent use of other proarrhythmic medications (eg, antiarrhythmics, other antiseizure medications) (Ref)
CNS effects, such as dizziness, drowsiness, headache, and ataxia are common and expected adverse reactions that may occur with lacosamide (Ref). Other CNS-related adverse reactions may include confusion, cognitive dysfunction, memory impairment, paresthesia, and sleep disturbance (Ref). CNS effects may be minimized by gradual dose titration, and some may regress spontaneously during continuation of therapy (Ref).
Mechanism: Dose-related; related to the pharmacologic action (Ref).
Onset: Varied; more likely to occur in the early stages of treatment (~3 months). One report showed incidence of dizziness to be 3 to 4 times higher in the titration period than in the maintenance period (Ref).
Risk factors:
• Higher doses (Ref)
• Rapid titration (Ref)
• Older age (Ref)
• Concurrent antiseizure medications or medications that cause sedation (Ref)
A variety of delayed hypersensitivity reactions, ranging from mild with skin rash (Ref) to severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome/toxic epidermal necrolysis and drug reaction with eosinophilia and systemic symptoms (DRESS) have been reported (Ref).
Mechanism: Non–dose-related; immunologic. Delayed hypersensitivity reactions, including rashes (often maculopapular) and SCARs, are T-cell-mediated (Ref).
Onset: Delayed hypersensitivity reactions: Varied; a diffuse skin rash developed in 1 patient after 8 days of treatment with lacosamide (Ref). SCARs usually occur 1 to 8 weeks after initiation (Ref); reexposure to the same or similar drug may lead to more rapid onset (usually with 1 to 4 days) (Ref).
Risk factors:
• Cross-reactivity: Cross-reactivity has not been well defined. In one report, DRESS developed rapidly after initiation of lacosamide following a previous reaction with phenobarbital. Cross-reactivity with phenobarbital was hypothesized based on the common aromatic ring in phenobarbital and lacosamide (Ref).
Antiseizure medications have been associated with suicidal ideation and suicidal tendencies. However, the FDA meta-analysis has been criticized due to several important limitations (Ref). The risk of suicide is increased in epilepsy (Ref), but the occurrence of suicidal ideation/tendencies in epilepsy is multifactorial. While some antiseizure medications (but not all) have been associated with treatment-emergent psychiatric effects such as anxiety and depression, other factors such as postictal suicidal behavior and pertinent patient history must also be evaluated to provide an accurate assessment of risk for any individual drug (Ref). Suicidal ideation and suicidal tendencies have been reported in association with lacosamide (Ref).
Onset: Varied; peak incidence of suicidality across antiseizure medications (not specific to individual agents) has been noted to occur between 1 and 12 weeks of therapy (Ref). A review of clinical trials noted that risk extended from 1 week to 24 weeks of therapy, corresponding to the duration of most trials.
Risk factors:
• History of depression (Ref)
• Use in conditions other than epilepsy or bipolar disorder (Ref)
• In patients with bipolar disorder, risk for repeat suicide attempt was increased in patients with alcohol/substance abuse disorder, rapid cycling, and earlier age at onset of first manic episode (Ref)
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. As reported with immediate-release oral formulations, unless otherwise noted.
>10%:
Gastrointestinal: Nausea (7% to 11%)
Nervous system: Dizziness (16% to 30%) (table 1), drowsiness (5% to 17%) (table 2), headache (11% to 14%) (table 3)
|
Drug (Lacosamide) |
Placebo |
Population |
Dose |
Dosage Form |
Indication |
Number of Patients (Lacosamide) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|---|
|
23% |
7% |
Children and adolescents |
N/A |
Oral solution |
Tonic-clonic seizures |
N/A |
N/A |
|
30% |
8% |
Adults |
400 mg/day |
Oral solution and tablet |
Partial-onset seizures |
471 |
364 |
|
16% |
8% |
Adults |
200 mg/day |
Oral solution and tablet |
Partial-onset seizures |
270 |
364 |
|
Drug (Lacosamide) |
Placebo |
Population |
Dose |
Dosage Form |
Indication |
Number of Patients (Lacosamide) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|---|
|
17% |
14% |
Children and adolescents |
N/A |
Oral solution |
Tonic-clonic seizures |
N/A |
N/A |
|
8% |
5% |
Adults |
400 mg/day |
Oral solution and tablet |
Partial-onset seizures |
471 |
364 |
|
5% |
5% |
Adults |
200 mg/day |
Oral solution and tablet |
Partial-onset seizures |
270 |
364 |
|
Drug (Lacosamide) |
Placebo |
Population |
Dose |
Dosage Form |
Indication |
Number of Patients (Lacosamide) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|---|
|
14% |
10% |
Children and adolescents |
N/A |
Oral solution |
Tonic-clonic seizures |
N/A |
N/A |
|
14% |
9% |
Adults |
400 mg/day |
Oral solution and tablet |
Partial-onset seizures |
471 |
364 |
|
11% |
9% |
Adults |
200 mg/day |
Oral solution and tablet |
Partial-onset seizures |
270 |
364 |
1% to 10%:
Dermatologic: Pruritus (2% to 3%)
Gastrointestinal: Diarrhea (5%), vomiting (6% to 9%)
Hematologic & oncologic: Bruise (4%)
Local: Irritation at injection site (IV: 1%), pain at injection site (IV: 3%)
Nervous system: Abnormal gait (2%), asthenia (2%), ataxia (4% to 7%) (table 4), balance impairment (1% to 5%), depression (2%), fatigue (7%), tremor (6%), vertigo (3% to 5%)
|
Drug (Lacosamide) |
Placebo |
Population |
Dose |
Dosage Form |
Indication |
Number of Patients (Lacosamide) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|---|
|
7% |
2% |
Adults |
400 mg/day |
Oral solution and tablet |
Partial-onset seizures |
471 |
364 |
|
4% |
2% |
Adults |
200 mg/day |
Oral solution and tablet |
Partial-onset seizures |
270 |
364 |
Ophthalmic: Blurred vision (9%), diplopia (6% to 10%), nystagmus disorder (5%)
Miscellaneous: Laceration (3%)
<1%:
Cardiovascular: Bradycardia, first-degree atrioventricular block
Hepatic: Abnormal hepatic function tests, hepatitis
Local: Erythema at injection site (IV)
Renal: Nephritis
Frequency not defined:
Gastrointestinal: Constipation, oral hypoesthesia, xerostomia
Hematologic & oncologic: Anemia
Nervous system: Cerebellar syndrome, dysarthria, euphoria, falling, hypoesthesia, intoxicated feeling
Neuromuscular & skeletal: Muscle spasm
Otic: Tinnitus
Miscellaneous: Fever
Postmarketing:
Cardiovascular: Angina pectoris (Steinhoff 2016), atrial fibrillation (Steinhoff 2016), atrial flutter (Steinhoff 2016), atrioventricular block (Steinhoff 2016), cardiac arrhythmia (Steinhoff 2016), complete atrioventricular block (Steinhoff 2016), palpitations (Steinhoff 2016), prolongation P-R interval on ECG (Steinhoff 2016), prolonged QT interval on ECG (Steinhoff 2016), syncope (Steinhoff 2016), ventricular tachycardia (Steinhoff 2016)
Dermatologic: Skin rash (Kim 2020), Stevens-Johnson syndrome (Kardaun 2016), toxic epidermal necrolysis (Kardaun 2016), urticaria
Endocrine & metabolic: Hyponatremia (Steinhoff 2016)
Gastrointestinal: Dyspepsia (Verrotti 2013)
Hematologic & oncologic: Agranulocytosis (Shibata 2021), neutropenia (Rao 2018)
Hypersensitivity: Angioedema (Goodwin 2011), drug reaction with eosinophilia and systemic symptoms (Fong 2017)
Nervous system: Aggressive behavior (Flores 2012), agitation, amnesia (Steinhoff 2016), cognitive dysfunction (Steinhoff 2016), confusion (Steinhoff 2016), depressed mood (Steinhoff 2016), disturbance in attention (Steinhoff 2016), hallucination (Flores 2012), irritability (Verrotti 2013), memory impairment (Steinhoff 2016), mood changes (Flores 2012), paresthesia (Verrotti 2013), psychosis, sleep disturbance (Flores 2012), suicidal ideation (Steinhoff 2016), suicidal tendencies (Steinhoff 2016)
Neuromuscular & skeletal: Dyskinesia (Madani 2020), panniculitis (Zhao 2022)
There are no contraindications listed in the US manufacturer's labeling.
Canadian labeling: Hypersensitivity to lacosamide or any component of the formulation; second- or third-degree atrioventricular (AV) block (current or history of).
Disease-related concerns:
• Hepatic impairment: Not recommended for use in patients with severe hepatic impairment; dosage adjustment required for mild to moderate hepatic impairment.
• Ocular conditions: Blurred vision and diplopia may occur during therapy. Patients with persistent visual disturbances may need further assessment. Consider increased monitoring in patients with preexisting ocular conditions or vision-related issues.
• Renal impairment: Use caution in patients with renal impairment; dosage adjustment required for severe renal impairment (CrCl ≤30 mL/minute) and supplementation may be necessary in hemodialysis.
Dosage form specific issues:
• Phenylalanine: Some products may contain phenylalanine.
• Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated hyperosmolality, lactic acidosis, seizures and respiratory depression; use caution (AAP 1997; Zar 2007).
Other warnings/precautions:
• Withdrawal: Antiseizure medications should not be discontinued abruptly because of the possibility of increasing seizure frequency; therapy should be withdrawn gradually (≥1 week) to minimize the potential of increased seizure frequency, unless safety concerns require a more rapid withdrawal.
In vitro data has shown lacosamide interferes with collapsing response mediator protein-2 (CRMP-2), a protein involved with neuronal differentiation and control of axonal outgrowth; potential effect on CNS development cannot be excluded. Lacosamide administered to neonatal and juvenile rats resulted in decreased brain weights and long-term neurobehavioral changes including learning and memory deficits. Studies of the effects of lacosamide on human CNS development are needed before this medication can be recommended for routine use in pediatric patients <4 years of age.
Some dosage forms may contain propylene glycol; in neonates, large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule Extended Release 24 Hour, Oral:
Motpoly XR: 100 mg, 150 mg
Motpoly XR: 200 mg [contains fd&c blue #1 (brilliant blue)]
Solution, Intravenous:
Generic: 200 mg/20 mL (20 mL)
Solution, Intravenous [preservative free]:
Vimpat: 200 mg/20 mL (20 mL)
Generic: 200 mg/20 mL (20 mL)
Solution, Oral:
Vimpat: 10 mg/mL (200 mL, 465 mL [DSC]) [contains aspartame, methylparaben, polyethylene glycol (macrogol), propylene glycol]
Generic: 10 mg/mL (5 mL, 10 mL, 15 mL, 20 mL, 200 mL, 465 mL)
Tablet, Oral:
Vimpat: 50 mg [contains fd&c blue #2 (indigo carm) aluminum lake]
Vimpat: 100 mg, 150 mg
Vimpat: 200 mg [contains fd&c blue #2 (indigo carm) aluminum lake]
Generic: 50 mg, 100 mg, 150 mg, 200 mg
May be product dependent
Capsule ER 24 Hour Therapy Pack (Motpoly XR Oral)
100 mg (per each): $25.00
150 mg (per each): $25.00
200 mg (per each): $25.00
Solution (Lacosamide Intravenous)
200 mg/20 mL (per mL): $2.40 - $4.72
Solution (Lacosamide Oral)
10 mg/mL (per mL): $0.44 - $2.23
Solution (Vimpat Intravenous)
200 mg/20 mL (per mL): $5.80
Solution (Vimpat Oral)
10 mg/mL (per mL): $2.74
Tablets (Lacosamide Oral)
50 mg (per each): $1.48 - $12.63
100 mg (per each): $2.46 - $19.75
150 mg (per each): $2.95 - $20.91
200 mg (per each): $2.95 - $20.92
Tablets (Vimpat Oral)
50 mg (per each): $14.13
100 mg (per each): $22.10
150 mg (per each): $23.40
200 mg (per each): $23.41
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravenous:
Vimpat: 200 mg/20 mL (20 mL)
Tablet, Oral:
Vimpat: 50 mg [contains fd&c blue #2 (indigo carm) aluminum lake]
Vimpat: 100 mg, 150 mg
Vimpat: 200 mg [contains fd&c blue #2 (indigo carm) aluminum lake]
Generic: 50 mg, 100 mg, 150 mg, 200 mg
C-V
Oral: May be administered with or without food.
Immediate release:
Solution: Should be administered with a calibrated measuring device (not a household teaspoon or tablespoon). May be administered via a nasogastric or gastrostomy tube. Discard any remaining product in bottle after 6 months from first opening.
Tablets: Swallow tablets whole; do not divide.
Extended release: Motpoly XR: Capsules: Swallow capsules whole; do not open, chew, or crush.
Parenteral: IV: Administer over 30 to 60 minutes to minimize adverse effects; may be administered undiluted or diluted in compatible diluent. Infusion times <30 minutes are generally not recommended in pediatric patients; in adults, infusions of 15 minutes may be used if necessary. IV infusion may cause bradycardia, AV blocks, and ventricular tachyarrhythmias; monitor closely. Rapid administration has been associated with higher CNS adverse effects (eg, dizziness, somnolence, paresthesia); monitor closely.
IV:
Infusion: According to the manufacturer, administer over 30 to 60 minutes to minimize adverse effects; infusions of 15 minutes may be used if needed. IV administration has been used for up to 5 days. Administer loading doses under medical supervision due to increased risk of adverse reactions, including cardiovascular and CNS. Can be administered without further dilution or may be mixed with compatible diluents (NS, LR, D5W).
Bolus (off label): Doses up to 400 mg may be administered undiluted at ≤80 mg/minute (eg, 400 mg over 5 minutes) (Ref).
Oral:
Capsules, oral solution, tablets: May be administered with or without food. Oral solution should be administered with a calibrated measuring device (not a household teaspoon or tablespoon). Oral solution may also be administered via a nasogastric or gastrostomy tube. Swallow tablets whole; do not divide. Swallow capsules whole; do not open, chew, or crush.
Injection: Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F). Do not freeze. Stable when mixed with compatible diluents (NS, LR, D5W) for up to 4 hours at room temperature; extended storage information for prepared solution at room temperature may be available; contact product manufacturer to obtain current recommendations. Discard any unused portion.
Oral solution, tablets, capsule: Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F). Do not freeze oral solution. Discard any unused portion of oral solution after 6 months.
An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:
Motpoly XR: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/216185s000lbl.pdf#page=22
Oral:
Immediate release (eg, Vimpat): Treatment (monotherapy or adjunctive) of partial-onset seizures (FDA approved in ages ≥1 month and adults); adjunctive treatment of primary generalized tonic-clonic seizures (All indications: FDA approved in ages ≥4 years and adults); has also been used for treatment of refractory seizures.
Extended release (eg, Motpoly XR): Treatment of partial-onset seizures (FDA approved in pediatric patients weighing ≥50 kg and adults).
Parenteral: Injection (eg, Vimpat): Treatment (monotherapy or adjunctive) of partial-onset seizures (FDA approved in ages ≥1 month and adults); adjunctive treatment of primary generalized tonic-clonic seizures (All indications: FDA approved in ages ≥4 years and adults); has also been used for treatment of refractory seizures and refractory status epilepticus.
Lacosamide may be confused with zonisamide
Vimpat may be confused with Venofer, Vfend, Vimovo
Substrate of CYP2C19 (minor), CYP2C9 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Antiarrhythmic Agents (Class III): May enhance the adverse/toxic effect of Lacosamide. Specifically the risk for bradycardia, ventricular tachyarrhythmias, or a prolonged PR interval may be increased. Risk C: Monitor therapy
Antiseizure Agents (Sodium Channel Blockers): May enhance the adverse/toxic effect of Lacosamide. Specifically the risk for bradycardia, ventricular tachyarrhythmias, or a prolonged PR interval may be increased. Risk C: Monitor therapy
Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification
Bradycardia-Causing Agents: May enhance the AV-blocking effect of Lacosamide. Risk C: Monitor therapy
Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider therapy modification
Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy
Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider therapy modification
Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification
Desmopressin: Hyponatremia-Associated Agents may enhance the hyponatremic effect of Desmopressin. Risk C: Monitor therapy
DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification
Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Doxylamine: CNS Depressants may enhance the CNS depressant effect of Doxylamine. Risk C: Monitor therapy
DroPERidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination
Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification
Ixabepilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification
Lidocaine (Systemic): May enhance the adverse/toxic effect of Lacosamide. Specifically the risk for bradycardia, ventricular tachyarrhythmias, or a prolonged PR interval may be increased. Risk C: Monitor therapy
Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Mefloquine: May diminish the therapeutic effect of Antiseizure Agents. Mefloquine may decrease the serum concentration of Antiseizure Agents. Management: Mefloquine is contraindicated for malaria prophylaxis in persons with a history of seizures. If antiseizure drugs are being used for another indication, monitor antiseizure drug concentrations and treatment response closely with concurrent use. Risk D: Consider therapy modification
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification
Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
MetyraPONE: Antiseizure Agents may diminish the diagnostic effect of MetyraPONE. Management: Consider alternatives to the use of the metyrapone test in patients taking antiseizure agents. Risk D: Consider therapy modification
MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy
Mexiletine: May enhance the adverse/toxic effect of Lacosamide. Specifically the risk for bradycardia, ventricular tachyarrhythmias, or a prolonged PR interval may be increased. Risk C: Monitor therapy
Mianserin: May diminish the therapeutic effect of Antiseizure Agents. Risk C: Monitor therapy
Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification
Orlistat: May decrease the serum concentration of Antiseizure Agents. Risk C: Monitor therapy
Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination
Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D: Consider therapy modification
OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification
Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination
Perampanel: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy
Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy
Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
QT-prolonging Class IA Antiarrhythmics (Highest Risk): May enhance the adverse/toxic effect of Lacosamide. Specifically the risk for bradycardia, ventricular tachyarrhythmias, or a prolonged PR interval may be increased. Risk C: Monitor therapy
QT-prolonging Class IC Antiarrhythmics (Moderate Risk): May enhance the adverse/toxic effect of Lacosamide. Specifically the risk for bradycardia, ventricular tachyarrhythmias, or a prolonged PR interval may be increased. Risk C: Monitor therapy
Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification
ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy
Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy
Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy
Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification
Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination
Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy modification
Zuranolone: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider therapy modification
Some products may contain phenylalanine.
Lacosamide crosses the placenta (Ylikotila 2015; Zárubová 2016) and can be detected in the newborn serum at delivery (Landmark 2021).
Outcome data following maternal use of lacosamide during pregnancy are limited (Golembesky 2017; Hoeltzenbein 2011; Lattanzi 2017; Zárubová 2016; Zutshi 2021). In general, maternal polytherapy with antiseizure drugs may increase the risk of congenital malformations; monotherapy with the lowest effective dose is recommended. Newborns of patients taking antiseizure medications during pregnancy may be at an increased risk of adverse events (Harden 2009).
Due to pregnancy-induced physiologic changes, some pharmacokinetic properties of lacosamide may be altered (Fukushima 2021; Pennell 2022; Zárubová 2016; Zutshi 2021).
Data collection to monitor pregnancy and infant outcomes following exposure to lacosamide is ongoing. Patients exposed to lacosamide during pregnancy are encouraged to enroll themselves into the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling 1-888-233-2334. Additional information is available at http://www.aedpregnancyregistry.org.
Seizure frequency, duration, and severity; patients with conduction problems, sodium channelopathies, severe cardiac disease, or concomitant medications that affect cardiac conduction or prolong the PR interval should have ECG tracing prior to start of therapy and when at steady-state; monitor heart rate and blood pressure during IV administration (bradycardia, atrioventricular block, or ventricular tachyarrhythmias may occur during infusions); monitor hepatic and renal function; suicidality (eg, suicidal thoughts, depression, behavioral changes).
Therapeutic reference range: Note: There is no clear correlation with therapeutic concentrations and efficacy or tolerability and suggested therapeutic ranges vary depending on source; base dosing on therapeutic response as opposed to serum concentrations (AGNP [Hiemke 2018]; Patsalos 2018). However, therapeutic drug monitoring may be useful in pediatric patients, females, and patients receiving drugs that may interact with lacosamide (Contin 2013; Larsen Burns 2019; May 2018).
Seizures: 1 to 10 mcg/mL (SI: 2.66 to 26.6 micromole/L) (AGNP [Hiemke 2018]) or 10 to 20 mcg/mL (SI: 40 to 80 micromole/L) (Patsalos 2018).
Timing of serum samples: Draw trough at steady-state, at the end of the scheduled dosing interval (just before the next dose).
In vitro studies have shown that lacosamide stabilizes hyperexcitable neuronal membranes and inhibits repetitive neuronal firing by enhancing the slow inactivation of sodium channels.
Absorption: Oral: Complete.
Distribution: Vd: ~0.6 to 0.67 L/kg.
Protein binding: <15%.
Metabolism: Hepatic via CYP3A4, CYP2C9, and CYP2C19; forms metabolite, O-desmethyl-lacosamide (inactive).
Bioavailability: ~100%.
Half-life elimination:
Children ≥4 years and Adolescents:
Mean weight 11 kg: 7.4 hours.
Mean weight 28.9 kg: 10.6 hours.
Mean weight 70 kg: 14.8 hours.
Adults: ~13 hours.
Time to peak, plasma: Oral: Immediate release (tablets, oral solution): 1 to 4 hours; extended release (capsules): 7 hours.
Excretion: Urine (95%; 40% as unchanged drug, 30% as inactive metabolite, 20% as uncharacterized metabolite); feces (<0.5%).
Altered kidney function: AUC is increased ~25% in patients with mild or moderate renal impairment (CrCl >30 to 80 mL/minute) and 60% in patients with severe renal impairment (CrCl ≤30 mL/minute). Following a 4-hour hemodialysis treatment, AUC is reduced by ~50%.
Hepatic function impairment: AUC is increased by ~50% to 60% in patients with moderate hepatic impairment (Child-Pugh class B).
Older adult: In patients >65 years of age, AUC and Cmax are increased ~20% compared with younger subjects.
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