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retigabine

N03AX21

Forms & Strengths

Oral tablets: 50 mg
Oral tablets: 100 mg
Oral tablets: 200 mg
Oral tablets: 300 mg
Oral tablets: 400 mg

Adult Dosing

Initial dose: 100 mg orally three times daily
Maintenance dose: 200 mg to 400 mg orally three times daily
Titration: Increase by no more than 150 mg/day every week
Maximum daily dose: 1200 mg/day (400 mg three times daily)

Pediatric Dosing

Safety and efficacy in pediatric patients (under 18 years) have not been established
Not recommended for use in children and adolescents

Indications

Adjunctive treatment of partial-onset seizures with or without secondary generalization in adult patients with epilepsy who have had an inadequate response to several other alternative antiepileptic drugs

Mechanism of Action

Potassium channel opener (specifically KCNQ2-Q5 / Kv7.2-7.5 channels)
Stabilizes the neuronal resting membrane potential
Reduces neuronal excitability and suppresses burst firing

Contraindications

Hypersensitivity to retigabine or any of its components
Patients with known QT prolongation or history of cardiac arrhythmias
Concomitant use with other drugs known to prolong the QT interval

Adverse Reactions

Dizziness and somnolence
Fatigue and confusion
Vertigo and tremor
Chromaturia (abnormal urine discoloration)
Skin pigmentation changes (blue/gray discoloration)
Retinal pigmentation and visual field constriction
Urinary retention and dysuria
Psychiatric disorders including hallucinations and psychosis

Drug Interactions

UGT inducers (e.g., carbamazepine, phenytoin) may increase clearance of retigabine
Potential for additive CNS depression with alcohol and other CNS depressants
Drugs associated with QT prolongation (theoretical additive risk)
Does not significantly inhibit or induce major CYP450 enzymes at clinical concentrations

Curated Content: Needs Vetting Before Put to Clinical Use