Overview
11 DESCRIPTION BANZEL (rufinamide) is a triazole derivative structurally unrelated to currently marketed antiepileptic drugs (AEDs). Rufinamide has the chemical name 1-[(2,6-difluorophenyl)methyl]-1 H -1,2,3-triazole-4 carboxamide. It has an empirical formula of C 10 H 8 F 2 N 4 O and a molecular weight of 238.2.
Mechanism of Action
12 C LINICAL P HARMACOLOGY 12.1 Mechanism of Action The precise mechanism(s) by which rufinamide exerts its antiepileptic effect is unknown. The results of in vitro studies suggest that the principal mechanism of action of rufinamide is modulation of the activity of sodium channels and, in particular, prolongation of the inactive state of the channel. Rufinamide (≥ 1 μM) significantly slowed sodium channel recovery from inactivation after a prolonged prepulse in cultured cortical neurons, and limited sustained repetitive firing of sodium-dependent action potentials (EC 50 of 3.8 μM). 12.3 Pharmacokinetics Overview BANZEL oral suspension is bioequivalent on a mg per mg basis to BANZEL tablets. BANZEL is well absorbed after oral administration.
Indications
- 1 I NDICATIONS AND USAGE BANZEL is indicated for adjunctive treatment of seizures associated with Lennox-Gastaut Syndrome in pediatric patients 1 year of age and older and in adults. BANZEL is indicated for adjunctive treatment of seizures associated with Lennox-Gastaut Syndrome (LGS) in pediatric patients 1 year of age and older, and in adults ( 1 )
Common Doses
- 10 mg
- 45 mg
- 3200 mg
- 800 mg
Dosage
2 DOSAGE AND ADMINISTRATION BANZEL should be given with food. Tablets can be administered whole, as half tablets, or crushed ( 2.2 ) Measure oral suspension using provided adapter and dosing syringe ( 2.2 ) Pediatric patients 1 year and older: Starting daily dose: 10 mg/kg per day in two equally divided doses ( 2.1 ) Increase by 10 mg/kg increments every other day to maximum dose of 45 mg/kg per day, not to exceed 3200 mg per day, in two divided doses ( 2.1 ) Adults: Starting daily dose: 400-800 mg per day in two equally divided doses ( 2.
Contraindications
- 4 CONTRAINDICATIONS BANZEL is contraindicated in patients with Familial Short QT syndrome [ see Warnings and Precautions ( 5.3 ) ] . BANZEL is contraindicated in patients with Familial Short QT syndrome ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following serious adverse reactions are described below and elsewhere in the labeling: Suicidal Behavior and Ideation [see Warnings and Precautions ( 5.1 )] Central Nervous System Reactions [see Warnings and Precautions ( 5.2 )] QT Shortening [see Warnings and Precautions ( 5.3 )] Multi-Organ Hypersensitivity/Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) [see Warnings and Precautions ( 5.4 )] Leukopenia [see Warnings and Precautions ( 5.
Interactions
- 7 D RUG INTERACTION S Patients on valproate should begin at a BANZEL dose lower than 10 mg/kg per day (pediatric patients) or 400 mg per day (adults) ( 7.2 ) Hormonal contraceptives may be less effective with BANZEL; use additional non-hormonal forms of contraception ( 7.3 ) 7.1 Effects of BANZEL on other AEDs Population pharmacokinetic analysis of average concentration at steady state of carbamazepine, lamotrigine, phenobarbital, phenytoin, topiramate, and valproate showed that typical rufinamide C avss levels had little effect on the pharmacokinetics of other AEDs.