Generic
Lacosamide
3 brands available in the market
At a glance
Lacosamide is an antiepileptic medicine used for the treatment of partial-onset seizures and primary generalized tonic-clonic seizures. It selectively enhances slow inactivation of voltage-gated sodium channels, stabilizing hyperexcitable neuronal membranes and inhibiting repetitive neuronal firing.
Description
The precise mechanism by which Lacosamide exerts its anti-epileptic effects remains to be fully elucidated. In vitro electrophysiological studies have shown that Lacosamide selectively enhances slow inactivation of voltage-gated sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing. Lacosamide binds to collapsin response mediator protein-2 (CRMP-2), a phosphoprotein expressed primarily in the nervous system involved in neuronal differentiation and control of axonal outgrowth.
Indications
- Partial-onset seizures - monotherapy or adjunctive therapy in patients 1 month and older
- Primary generalized tonic-clonic seizures - adjunctive therapy in patients 4 years and older
Pharmacological class
Voltage-gated Sodium Channel Modulator
Pharmacology
Lacosamide selectively enhances slow inactivation of voltage-gated sodium channels, stabilizing hyperexcitable neuronal membranes and inhibiting repetitive neuronal firing. It also binds to CRMP-2, which is involved in neuronal differentiation and axonal outgrowth.
Mechanism of action
Stabilizes neuronal membranes and prevents seizures by enhancing slow inactivation of voltage-gated sodium channels.
Dosage
Adults (≥17 years):
- Monotherapy: Initial 100 mg twice daily; Maintenance 150-200 mg twice daily
- Adjunctive therapy: Initial 50 mg twice daily; Maintenance 100-200 mg twice daily
- Titrate by 50 mg twice daily every week
Pediatric (Weight-based):
- ≥50 kg: 50 mg twice daily; Maintenance 100-200 mg twice daily
- 30-50 kg: 1 mg/kg twice daily; Maintenance 2-4 mg/kg twice daily
- 6-30 kg: 3-6 mg/kg twice daily
- <6 kg: 3.75-7.5 mg/kg twice daily
Administration
- Tablets or oral solution may be taken with or without food
- Take at regular times as advised by your doctor
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose.
Drug interactions
- Dose reduction may be necessary in renal or hepatic impairment with strong CYP3A4 & CYP2C9 inhibitors
- Use with caution with medications affecting cardiac conduction (sodium channel blockers, beta-blockers, calcium channel blockers, potassium channel blockers)
Food interactions
No food interactions known.
Contraindications
- Hypersensitivity to Lacosamide or any of its excipients
Side effects
Common Adverse Reactions:
- Dizziness
- Headache
- Somnolence
- Ataxia
- Tremor
- Nausea
- Vomiting
- Fatigue
- Diplopia
- Blurred vision
Use in pregnancy
Use in Pregnancy: No adequate well-controlled studies; use only if potential benefit justifies potential risk to the fetus.
Use in lactation
Use in Lactation: Lacosamide is excreted in human breast milk. Weigh the known benefits of breastfeeding against the unknown risks of infant exposure.
Precautions & warnings
- Monitor patients for suicidal behavior
- Monitor for dizziness, ataxia, PR interval prolongation, AV block, ventricular tachyarrhythmia, atrial fibrillation, atrial flutter, syncope
- Monitor for multi-organ hypersensitivity
- Use during pregnancy only if potential benefit justifies risk
- Weigh benefits of breastfeeding against unknown risks to the infant
Pediatric use
Safety and efficacy not established in pediatric patients below 1 month for partial seizures and below 4 years for primary generalized tonic-clonic seizures.
Geriatric use
Start at the lower end of the dosing range.
Renal / hepatic impairment
Renal Impairment: Mild to moderate: no dose adjustment; Severe and ESRD: 25% reduction of maximum dosage recommended.
Hepatic Impairment: Mild to moderate: 25% reduction of maximum dosage recommended; Severe: not recommended.
Overdose effects
There is no specific antidote for overdose. General supportive and symptomatic measures should be employed.
Therapeutic class
Atypical Antidepressant & Antiepileptic
Storage conditions
Do not store above 30°C; keep away from light and out of reach of children.
Chemical structure
Lacosamide