Chemistry:Rufinamide
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| Trade names | Banzel, Inovelon |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a609001 |
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| Routes of administration | By mouth |
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| Bioavailability | 85% (under fed conditions); tmax = 4–6 hours |
| Protein binding | 34% |
| Metabolism | Carboxylesterase-mediated hydrolysis (CYP not involved) |
| Metabolites | Inactive |
| Elimination half-life | 6–10 hours |
| Excretion | Urine (85%)[1] |
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| Formula | C10H8F2N4O |
| Molar mass | 238.198 g·mol−1 |
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Rufinamide is an anticonvulsant medication. It is used in combination with other medication and therapy to treat Lennox–Gastaut syndrome[2] and various other seizure disorders. Rufinamide, a triazole derivative, was developed in 2004 by Novartis Pharma, AG, and is manufactured by Eisai.
Rufinamide was approved by the US Food and Drug Administration (FDA) in November 2008, as adjunctive treatment of seizures associated with Lennox-Gastaut syndrome in children four years and older and adults. Its official FDA-approved labeling does not mention use in the treatment of partial seizures inasmuch as clinical trials submitted to the FDA were marginal. However, several recent clinical trials suggest that the drug has efficacy for partial seizures [3] It is marketed under the brand name Banzel.[4] It is also marketed in the European Union under the brand name Inovelon.[5] It is available as a generic medication.[6]
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,[7][8] a common target for antiepileptic drugs.[9] 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.[10] However, this action cannot explain the unique spectrum of activity of rufinamide.
References
- ↑ 1.0 1.1 "Banzel- rufinamide tablet, film coated Banzel- rufinamide suspension". 15 April 2020. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0a3fa925-1abd-458a-bd57-4ae780a1ef2d.
- ↑ "Rufinamide: a new anti-epileptic medication". Expert Opinion on Pharmacotherapy 8 (12): 1931–1940. August 2007. doi:10.1517/14656566.8.12.1931. PMID 17696794.
- ↑ "Rufinamide for the adjunctive treatment of partial seizures in adults and adolescents: a randomized placebo-controlled trial". Epilepsia 50 (8): 1899–1909. August 2009. doi:10.1111/j.1528-1167.2009.02160.x. PMID 19490053.
- ↑ FDA press release - FDA Approves New Drug to Treat Severe Form of Epilepsy
- ↑ "European Public Assessment Report for rufinamide (INOVELON)". http://www.emea.europa.eu/humandocs/Humans/EPAR/inovelon/inovelon.htm.
- ↑ "2022 First Generic Drug Approvals". 3 March 2023. https://www.fda.gov/drugs/drug-and-biologic-approval-and-ind-activity-reports/2022-first-generic-drug-approvals.
- ↑ "Diverse mechanisms of antiepileptic drugs in the development pipeline". Epilepsy Research 69 (3): 273–294. June 2006. doi:10.1016/j.eplepsyres.2006.02.004. PMID 16621450.
- ↑ "Rufinamide for the treatment of Lennox-Gastaut syndrome: evidence from clinical trials and clinical practice". Epileptic Disorders 20 (1): 13–29. February 2018. doi:10.1684/epd.2017.0950. PMID 29313492.
- ↑ "The neurobiology of antiepileptic drugs". Nature Reviews. Neuroscience 5 (7): 553–564. July 2004. doi:10.1038/nrn1430. PMID 15208697. https://zenodo.org/record/1233562.
- ↑ "Nav1.1 modulation by a novel triazole compound attenuates epileptic seizures in rodents". ACS Chemical Biology 9 (5): 1204–1212. May 2014. doi:10.1021/cb500108p. PMID 24635129.
External links
- "Rufinamide". Drug Information Portal. U.S. National Library of Medicine. https://druginfo.nlm.nih.gov/drugportal/name/rufinamide.
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