Rufinamide
- Atc Codes:N03AF03
- CAS Codes:106308-44-5
- PHARMGKB ID:106308-44-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Inovelon; Czech Republic: Inovelon; Denmark: Inovelon; Estonia: Inovelon; Finland: Inovelon; France: Inovelon; Germany: Inovelon; Greece: Inovelon; Hungary: Inovelon; Ireland: Inovelon; Italy: Inovelon; Latvia: Inovelon; Lithuania: Inovelon; Luxembourg: Inovelon; Malta: Inovelon; Netherlands: Inovelon; Poland: Inovelon; Portugal: Inovelon; Romania: Inovelon; Slovakia: Inovelon; Slovenia: Inovelon; Spain: Inovelon; Sweden: Inovelon; UK: Inovelon.
North America
USA: Banzel.
Drug combinations
Chemistry
Rufinamide: C~10~H~8~F~2~N~4~O. Mw: 238.2. 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4 carboxamide. CAS-106308-44-5.
Pharmacologic Category
Anticonvulsants, Miscellaneous; Triazole Derivative. (ATC-Code: N03AF03).
Mechanism of action
The precise mechanism(s) by which rufinamide exerts its antiepileptic effect are 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).
Therapeutic use
Anti-epileptic drug indicated for adjunctive treatment of seizures associated with Lennox-Gastaut syndrome (LGS) in children of 4 years and older and adults.
Pregnancy and lactiation implications
Rufinamide produced developmental toxicity when administered orally to pregnant animals at clinically relevant doses. There are no adequate and well-controlled studies in pregnant women. Should be used during pregnancy only if potential benefit justifies potential risk to fetus. There is an Antiepileptic Drug Pregnancy Registry to enroll pregnant patients taking rufinamide. The effect on labor and delivery in humans is not known. Not recommended during lactation (likely to be excreted in human milk).
Unlabeled use
Contraindications
Contraindicated in patients with familial short QT syndrome.
Warnings and precautions
Antiepileptic drugs (AEDs), including rufinamide, increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication (should be monitored closely). Has been associated with central nervous system-related adverse reactions (somnolence or fatigue, coordination abnormalities, dizziness, gait disturbances, and ataxia). Formal cardiac ECG studies demonstrated shortening of the QT interval (mean=20 ms, for doses ≥2400 mg twice daily) with this treatment (caution should be used when administering rufinamide with other drugs that shorten the QT interval). Multi-organ hypersensitivity reactions have occurred in association with rufinamide (if this reaction is suspected, it should be discontinued and alternative treatment started). As with all AEDs, should be withdrawn gradually to minimize the risk of precipitating seizures, seizure exacerbation, or status epilepticus. Rufinamide-treated patients have had episodes that could be described as status epilepticus. Leucopenia (white cell count <3 10^9^ L) has been reported.