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
Therapeutic class
Atypical Antidepressant & Antiepileptic
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.
Side effects
Common Adverse Reactions:
- Dizziness
- Headache
- Somnolence
- Ataxia
- Tremor
- Nausea
- Vomiting
- Fatigue
- Diplopia
- Blurred vision
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
Contraindications
- Hypersensitivity to Lacosamide or any of its excipients
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.
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.
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.
Storage conditions
Do not store above 30°C; keep away from light and out of reach of children.
Chemical structure
Lacosamide