Rufinamide

Not to be confused with ralfinamide.
Rufinamide
Names
Trade namesBanzel, Inovelon
IUPAC name
  • 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide
Clinical data
Main usesLennox–Gastaut syndrome, partial seizures[1]
Side effectsSleepiness, headache, dizziness, vomiting[2]
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Pregnancy
category
  • AU: B3
  • US: N (Not classified yet)
    Routes of
    use    		By mouth (tablets)
    Typical dose200 to 400 mg (10mg/kg)
    External links
    AHFS/Drugs.comMonograph
    MedlinePlusa609001
    Legal
    License data
    Legal status
    • UK: POM (Prescription only)
    • US: ℞-only [3]
    • In general: ℞ (Prescription only)
    Pharmacokinetics
    Bioavailability85% (under fed conditions); tmax = 4–6 hours
    Protein binding34%
    MetabolismCarboxylesterase-mediated hydrolysis (CYP not involved)
    MetabolitesInactive
    Elimination half-life6–10 hours
    ExcretionUrine (85%)[3]
    Chemical and physical data
    FormulaC10H8F2N4O
    Molar mass238.198 g·mol−1
    3D model (JSmol)
    SMILES
    • O=C(c1nnn(c1)Cc2c(F)cccc2F)N
    InChI
    • InChI=1S/C10H8F2N4O/c11-7-2-1-3-8(12)6(7)4-16-5-9(10(13)17)14-15-16/h1-3,5H,4H2,(H2,13,17) checkY
    • Key:POGQSBRIGCQNEG-UHFFFAOYSA-N checkY

    Rufinamide, sold under the brand name Banzel among others, is a medication used to treat Lennox–Gastaut syndrome and partial seizures not controlled by other measures.[1] It is taken by mouth.[1]

    Common side effects include sleepiness, headache, dizziness, and vomiting.[2] Other symptoms may include drug reaction with eosinophilia and systemic symptoms, suicide, and poor coordination.[1] Safety in pregnancy is unclear.[4] It is a triazole derivative that is believed to work by attaching to sodium channels in the brain.[2][1]

    Rufinamide was approved for medical use in Europe in 2007 and the United States in 2008.[2][1] It is available as a generic medication.[5] In the United Kingdom a dose of 800 mg per day costs the NHS costs about £100.[6] In the United States this amount costs about 425 USD per month.[5]

    Medical use

    Several recent clinical trials suggest that the drug has efficacy for partial seizures [7]

    Dosage

    In children it is started at a dose of 10 mg/kg.[2] This may be increased to 45 mg/kg.[1] In older people 200 to 800 mg per day is used and increased up to 3,200 mg.[2][1]

    Mechanism of action

    The mechanism of action of rufinamide is not fully understood. There is some evidence that rufinamide can modulate the gating of voltage-gated sodium channels,[8][9] a common target for antiepileptic drugs.[10] A recent study indicates subtle effects on the voltage-dependence of gating and the time course of inactivation in some sodium channel isoforms that could reduce neuronal excitability.[11] However, this action cannot explain the unique spectrum of activity of rufinamide.

    References

    1. 1 2 3 4 5 6 7 8 "Rufinamide Monograph for Professionals". Drugs.com. Archived from the original on 30 September 2021. Retrieved 19 October 2021.
    2. 1 2 3 4 5 6 "Inovelon". Archived from the original on 20 May 2021. Retrieved 19 October 2021.
    3. 1 2 "Banzel- rufinamide tablet, film coated Banzel- rufinamide suspension". DailyMed. 15 April 2020. Archived from the original on 26 October 2020. Retrieved 21 October 2020.
    4. ↑ "Rufinamide (Banzel) Use During Pregnancy". Drugs.com. Archived from the original on 4 October 2021. Retrieved 19 October 2021.
    5. 1 2 "Rufinamide Prices, Coupons & Savings Tips - GoodRx". GoodRx. Archived from the original on 19 October 2021. Retrieved 19 October 2021.
    6. ↑ BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 343. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
    7. ↑ Brodie MJ, Rosenfeld WE, Vazquez B, Sachdeo R, Perdomo C, Mann A, Arroyo S (August 2009). "Rufinamide for the adjunctive treatment of partial seizures in adults and adolescents: a randomized placebo-controlled trial". Epilepsia. 50 (8): 1899–909. doi:10.1111/j.1528-1167.2009.02160.x. PMID 19490053. S2CID 38485532.
    8. ↑ Rogawski, M. A. (2006). "Diverse mechanisms of antiepileptic drugs in the development pipeline". Epilepsy Research. 69 (3): 273–94. doi:10.1016/j.eplepsyres.2006.02.004. PMC 1562526. PMID 16621450.
    9. ↑ Striano, P.; McMurray, R.; Santamarina, E.; Falip, M. (2018). "Rufinamide for the treatment of Lennox-Gastaut syndrome: Evidence from clinical trials and clinical practice". Epileptic Disorders. 20 (1): 13–29. doi:10.1684/epd.2017.0950. PMID 29313492. Archived from the original on 2021-08-29. Retrieved 2021-06-08.
    10. ↑ Rogawski, A.; Löscher, W. (Jul 2004). "The neurobiology of antiepileptic drugs". Nature Reviews. Neuroscience. 5 (7): 553–564. doi:10.1038/nrn1430. ISSN 1471-003X. PMID 15208697. S2CID 2201038. Archived from the original on 2020-12-16. Retrieved 2021-06-08.
    11. ↑ Gilchrist, J; Dutton, S; Diaz-Bustamante, M; McPherson, A; Olivares, N; Kalia, J; Escayg, A; Bosmans, F (2014). "Nav1.1 modulation by a novel triazole compound attenuates epileptic seizures in rodents". ACS Chemical Biology. 9 (5): 1204–12. doi:10.1021/cb500108p. PMC 4027953. PMID 24635129.
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