Rufinamide

Products

Rufinamide is commercially available as film-coated tablets and as an oral suspension (Inovelon). It was approved in the EU in 2007 and in many countries in 2009. The suspension was registered in many countries in 2012.

Structure and properties

Rufinamide (C10H8F2N4O, Mr = 238.2 g/mol) is a methyl triazole carboxamide. It exists as a white, crystalline, odorless, and slightly bitter-tasting powder that is practically insoluble in water.

Effects

Rufinamide (ATC N03AF03) has antiepileptic properties. The effects are due to modulation of sodium channels. Rufinamide prolongs their inactivated state.

Indications

As adjunctive therapy for the treatment of seizures associated with Lennox-Gastaut syndrome in patients aged four years and older. This is a rare and severe form of epilepsy that generally affects children but may continue into adulthood.

Dosage

According to the SmPC. The drug is taken in the morning and evening with meals. Discontinuation must be gradual.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Rufinamide is metabolized by hydrolysis and interacts little with CYP450, but it is an inducer of CYP3A4 and thus may cause drug-drug interactions. Interactions are possible with other antiepileptic drugs and oral contraceptives, among others.

Adverse effects

The most common potential adverse effects include fatigue, drowsiness, headache, dizziness, nausea, and vomiting. Rufinamide may shorten (not lengthen) the QT interval.