Rufinamide

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Rufinamide
Rufinamide.svg
Names
Trade namesBanzel, Inovelon
  • 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]
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
US NLMRufinamide
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)
  • O=C(c1nnn(c1)Cc2c(F)cccc2F)N
  • 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
 ☒NcheckY (what is this?)  (verify)

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. 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 "Rufinamide Monograph for Professionals". Drugs.com. Retrieved 19 October 2021.
  2. 2.0 2.1 2.2 2.3 2.4 2.5 "Inovelon". Retrieved 19 October 2021.
  3. 3.0 3.1 "Banzel- rufinamide tablet, film coated Banzel- rufinamide suspension". DailyMed. 15 April 2020. Retrieved 21 October 2020.
  4. "Rufinamide (Banzel) Use During Pregnancy". Drugs.com. Retrieved 19 October 2021.
  5. 5.0 5.1 "Rufinamide Prices, Coupons & Savings Tips - GoodRx". GoodRx. 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.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.
  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.
  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.

External links

External sites:
Identifiers: