Rufinamide
Rufinamide is an anticonvulsant medication primarily used for the treatment of certain seizure disorders, especially in patients with Lennox-Gastaut syndrome, a severe form of childhood epilepsy. Rufinamide works by modulating sodium channels in the brain, helping to stabilize the electrical activity and prevent seizures.
Trade Names
Rufinamide is marketed under the trade name Banzel in the United States and Inovelon in Europe.
Chemical Properties
Chemical Structure: Rufinamide is a triazole derivative with anticonvulsant properties.
Molecular Formula: C₁₀H₈F₂N₄O
Molecular Weight: 238.2 g/mol
Solubility: Rufinamide is sparingly soluble in water and is available in tablet and oral suspension forms.
Biochemical Properties
Mechanism of Action: Rufinamide works by prolonging the inactive state of sodium channels, which decreases the rapid firing of neurons associated with seizure activity. This action helps to stabilize neuronal excitability and reduce seizure frequency.
Pharmacology
Administration: Rufinamide is taken orally, with absorption enhanced when taken with food. Bioavailability: Its bioavailability improves with food intake, and peak plasma concentrations are generally reached within 4-6 hours.
Metabolism: Rufinamide undergoes minimal metabolism in the liver and is primarily excreted unchanged in urine.
Half-Life: The half-life of rufinamide ranges from 6 to 10 hours, so it is typically taken twice daily.
Clinical Indications
Lennox-Gastaut Syndrome: Rufinamide is approved for adjunctive therapy in Lennox-Gastaut syndrome, especially for controlling drop attacks (sudden loss of muscle strength).
Other Seizure Disorders: In some cases, it may be used off-label for other types of difficult-to-control seizures, though its main use is for Lennox-Gastaut syndrome.
Side Effects
Drowsiness and Fatigue: Sedation is common, particularly at the beginning of treatment or during dose adjustments.
Headache and Dizziness: Frequently reported and often dose-related.
Nausea and Vomiting: Gastrointestinal upset, including nausea, is common, especially if taken on an empty stomach.
Coordination Problems: Some patients may experience problems with balance or coordination.
Mood Changes: In rare cases, rufinamide can cause mood changes, irritability, or aggressive behavior.
Monitoring and Precautions
Liver Function: Although rufinamide undergoes minimal liver metabolism, liver function should still be monitored in patients with pre-existing liver conditions.
Suicidal Thoughts: Like many antiepileptics, rufinamide carries a small risk of causing or worsening depression or suicidal ideation.
Withdrawal and Discontinuation: Abrupt discontinuation may increase seizure risk. Gradual dose reduction is recommended when stopping therapy.
Pregnancy and Breastfeeding: Rufinamide should be used in pregnancy only if absolutely necessary, and breastfeeding is generally not recommended.
Rufinamide is a valuable medication for managing seizures in Lennox-Gastaut syndrome, offering a unique mechanism that supports seizure control. However, careful monitoring is required to manage potential side effects and ensure therapeutic effectiveness.
