Rufinamide

Uses

Rufinamide is an antiepileptic drug used as adjunctive therapy to treat seizures associated with Lennox-Gastaut Syndrome (LGS).

Adjunct therapy for treatment of seizures associated with Lennox-Gastaut syndrome.

Rufinamide is also used to associated treatment for these conditions: Lennox-Gastaut Syndrome (LGS)

How Rufinamide works

Rufinamide is a triazole derivative antiepileptic that prolongs the inactive state of voltage gated sodium channels thus stabilizing membranes, ultimately blocking the spread of partial seizure activity.

Toxicity

The most commonly observed adverse reactions (≥10% and greater than placebo) were headache, dizziness, fatigue, somnolence, and nausea.

Food Interaction

• Take with food. Food can increase the absorption of rufinamide.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of rufinamide.

Use in combination may result in additive central nervous system depression and
ADJUST DOSING INTERVAL: Food enhances the oral absorption and bioavailability of rufinamide.

In healthy volunteers, administration of a single 400 mg dose of rufinamide with food resulted in an approximately 56% increase in mean peak plasma concentration (Cmax) and a 34% increase in systemic exposure (AUC) compared to administration during a fasting state.

MANAGEMENT: To ensure maximal oral absorption, it is preferable to administer rufinamide with food.

Patients receiving rufinamide should be advised to avoid consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how rufinamide affects them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Rufinamide Drug Interaction

Moderate: lorazepam, diphenhydramine, cannabidiol, perampanel, levetiracetam, lamotrigine, clobazam, topiramate, cholecalciferolUnknown: emollients topical, ocular lubricant ophthalmic, ipratropium, multivitamin, miconazole topical, glycopyrrolate, fluticasone nasal, fluticasone, polyethylene glycol 3350, glycerin, acetaminophen

Rufinamide Disease Interaction

Major: depression, liver disease, renal dysfunction, short QT syndrome

Volume of Distribution

Rufinamide was evenly distributed between erythrocytes and plasma. The apparent volume of distribution is dependent upon dose and varies with body surface area. The apparent volume of distribution was about 50 L at 3200 mg/day. Volume of distribution is similar between adults and children and is non-linear.

Elimination Route

The oral suspension and tablet are bioequivalent on a mg per mg basis. Rufinamide is well absorbed but the rate is slow and the extent of absorption decreases as dose is increases. Based on urinary excretion, the extent of absorption was at least 85% following oral administration of a single dose of 600 mg rufinamide tablet under fed conditions. Bioavailability= 70%-85% (decreases with increasing doses); Tmax, fed and fasted states= 4-6 hours; Cmax, 10 mg/kg/day= 4.01 µL/mL; Cmax, 30mg/kg/day= 8.68 µL/mL; AUC (0h-12h), 10mg/kg/day= 37.8±47 µg·h/mL; AUC (0h-12h), 30mg/kg/day= 89.3±59 µg·h/mL.

Half Life

Elimination half-life, healthy subjects and patients with epilepsy = 6-10 hours.

Elimination Route

Renally (91%; 66% as CGP 47292, 2% as unchanged drug) and fecally (9%) eliminated.

Innovators Monograph

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