Lacosamide

Mechanism :

It is proposed that lacosamide's inhibition of sodium channels is responsible for analgesia. Lacosamide may be selective for inhibiting depolarized neurons rather than neurons with normal resting potentials. Pain and nociceptor hyperexcitability are associated with neural membrane depolarization. Lacosamide binds to collapsin response mediator protein-2 (CRMP-2), a phosphoprotein which is expressed primarily in the nervous system and is involved in neuronal differentiation and control of axonal outgrowth. The role CRMP-2 of binding in seizure control is hasn't been elucidated.

Indication :

Adjunct therapy in partial seizures in older children

Contraindications :

Hypersensitivity to drug/class/component; Avoid abrupt withdrawal

Caution if hepatic or renal impairment, severe cardiac disease, cardiac conduction defects, diabetic neuropathy, depression or history of similar mental disorders.

Dosing :

Under 4 years:

Safety and efficacy not established.

4-17 years:

1 mg/kg orally twice a day after which increase dose at weekly intervals by 1 mg/kg/day to a recommended 3-6 mg/kg orally twice a day in children weighing 11 to 29 kg and 2-4 mg/kg orally twice a day in children weighing 30 to 49 kg.

≥50 kg:

50 mg orally twice a day, after which increase dose at weekly intervals by 50 mg orally twice a day up to a recommended 150-200 mg orally twice a day (300-400 mg/day).

Adverse Effect :

Common Reactions: Dizziness, headache, somnolence, tremor, nystagmus, diplopia, nausea, vomiting, pruritus, injection site pain fatigue, ataxia, blurred vision, vertigo, diarrhea, contusion, asthenia, abnormal gait, depression, impaired memory.

Serious Reactions: Stevens-Johnson syndrome, PR prolongation, AV block, atrial fibrillation, atrial flutter, syncope, suicidality, drug rash with eosinophilia and systemic symptoms, neutropenia, agranulocytosis, toxic epidermal necrolysis.

Interaction :

Avoid/Use Alternative:
Dolasetron, Saquinavir.
Monitor/Modify Treatment:
Lopinavir/Ritonavir, Ritonavir.
Caution Advised:
Acebutolol, Atazanavir, Atenolol, Betaxolol, Bisoprolol, Boceprevir, Carvedilol, Chloramphenicol, Clarithromycin, Cobicistat, Conivaptan, Cyclosporine, Darunavir, Delavirdine, Digoxin, Diltiazem, Esmolol, Fluorouracil, Fosamprenavir, Gemfibrozil, Itraconazole, Ketoconazole, Labetalol, Metoprolol, Nadolol, Nebivolol, Nefazodone, Nelfinavir, Penbutolol, Pindolol, Posaconazole, Propranolol, Quinine, Telaprevir, Telithromycin, Timolol, Tipranavir, Verapamil, Voriconazole.

Hepatic Dose :

Mild and moderate hepatic impairment: Reduce dose by 25% of the maximum dose.
Severe hepatic impairment: Use is contraindicated
Patients with hepatic impairment who are taking strong inhibitors of CYP3A4 and CYP2C9 may need dosage reduction of lacosamide.