Trade Names:Vimpat- Tablets, oral 50 mg- Tablets, oral 100 mg- Tablets, oral 150 mg- Tablets, oral 200 mg- Injection, solution 10 mg/mL
Precise mechanism of action is unknown; however, lacosamide selectively enhances slow inactivation of voltage-gated sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing.
Completely absorbed following oral administration with negligible first-pass effect and an absolute bioavailability of approximately 100%. Food does not affect the rate or extent of absorption. Following IV administration, the C max is reached at the end of the infusion.
Vd is approximately 0.6 L/kg. Less than 15% is bound to plasma proteins.
Primarily cleared from the systemic circulation by renal excretion and biotransformation. Lacosamide is a CYP2C19 substrate.
Approximately 95% is eliminated in the urine and less than 0.5% in the feces, mainly as unchanged drug (40%), 30% as the O-desmethyl metabolite, and about 20% as a structurally unknown inactive polar metabolite. Elimination half-life is approximately 13 h.
AUC is increased approximately 25% in patients with mild or moderate renal function impairment and 60% in patients with severe renal function impairment. No dosage adjustment is needed in patients with mild or moderate renal function impairment.Hepatic Function Impairment
AUC is increased by approximately 50% to 60% in patients with moderate hepatic function impairment.Elderly
In patients older than 65 yr of age, AUC and C max are increased about 20% compared with younger subjects.Children
Pharmacokinetics have not been studied.Gender
Pharmacokinetics not affected by gender.Race
No differences in pharmacokinetics among Asian, black, and white subjects.
Adjunctive treatment of partial-onset seizures.Parenteral
Adjunctive treatment of partial-onset seizures when oral route is not feasible.
PO/IV Start with 50 mg twice daily. The dosage may be increased by 50 mg twice daily at weekly intervals up to the recommended maintenance dosage of 200 to 400 mg/day, based on response and tolerability.Hepatic Function ImpairmentAdults and Children 17 yr of age and older
PO/IV Titrate the dose with caution. Max dosage of 300 mg/day is recommended in patients with mild or moderate hepatic function impairment. Not recommended in patients with severe hepatic function impairment.Renal Function ImpairmentAdults and Children 17 yr of age and older
PO/IVMild or moderate renal function impairment
No dosage adjustment is needed.Severe renal function impairment (CrCl less than 30 mL/min) and end-stage renal disease
Max dosage is 300 mg/day. Following a 4-hour hemodialysis treatment, supplementation with up to 50% of the dose should be considered.
Store at 59° to 86°F. Store IV form following dilution for up to 24 h at 59° to 86°F. Store in glass or polyvinyl chloride bags. Discard any unused portion.
None well documented.
None well documented.
Dizziness (53%); ataxia, fatigue (15%); headache (14%); tremor (12%); nystagmus (10%); somnolence (8%); balance disorder, memory impairment (6%); vertigo (5%); asthenia, gait disturbance (4%); depression (2%).
Contusion (4%); pruritus, skin laceration (3%).
Blurred vision, diplopia (16%).
Nausea (17%); vomiting (16%); diarrhea (5%).
Injection-site pain or discomfort (3%); irritation (1%).
In patients with known conduction problems or severe cardiac disease, obtain ECG before starting treatment and after titrating to steady state. Monitor patients for emergence or worsening of depression, suicidal thoughts or behavior, or any unusual changes in mood or behavior.
Category C .
Safety and efficacy not established in children younger than 17 yr of age.
Titrate dose with caution.
A max dosage of 300 mg/day is recommended for patients with severe renal function impairment or end-stage renal disease.
Titrate dose with caution in patients with mild or moderate hepatic function impairment. A max dosage of 300 mg/day is recommended for patients with mild or moderate hepatic function impairment. Not recommended in patients with severe hepatic function impairment.
May occur. Patients should not drive or operate complex machinery until they are familiar with the drug's effects on their ability to perform.
Has been reported in patients with diabetic neuropathy who received treatment with lacosamide.
Dose-related PR interval prolongation may occur. Use with caution in patients with known conduction problems (eg, marked first-degree AV block, second-degree or higher AV block, sick sinus syndrome without a pacemaker), or with severe cardiac disease (eg, myocardial ischemia, heart failure).
Gradually withdraw treatment over a minimum of 1 wk to minimize the potential of increased seizure frequency.
Has been reported rarely.
The risk of suicidal thoughts and behavior is increased.
Has been reported in patients with diabetic neuropathy who were treated with lacosamide.
Limited experience available. Adverse reactions in patients receiving supratherapeutic doses were not different from those of patients receiving recommended doses.
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