Summary
Rufinamide is a triazole derivative structurally unrelated to currently marketed antiepileptic drugs. Rufinamide was profiled for anticonvulsant activity at the National Institutes of Health and showed broad-spectrum anticonvulsant properties at nontoxic doses in animal models. The principal mechanism of action of rufinamide is considered to be the modulation of the activity of sodium channels and, in particular, prolongation of the inactive state of the channel. Rufinamide provides an efficacious and well-tolerated treatment option for use as adjunctive therapy in patients with partial seizures and with Lennox-Gastaut syndrome (LGS). In LGS, rufinamide is effective in controlling multiple seizure types and in reducing the severity of the seizures. The most commonly observed (≥10%) adverse experiences seen in association with rufinamide are headache, dizziness, fatigue, somnolence and nausea. Rufinamide is generally well tolerated, and its safety profile is well-established.
Key Words: Rufinamide, epilepsy, partial seizures, Lennox-Gastaut syndrome
References
- 1.Anonymous. Rufinamide: CGP 33101, E 2080, RUF 331, Xilep. Drugs R D 2005:6:249–252. [DOI] [PubMed]
- 2.McLean MJ, Schmutz M, Pozza MF, Wamil AW. Effects of rufinamide on sodium-dependent action potential firing and sodium currents of rodent central neurons. Epilepsia. 2005;46(suppl 6):375–375. [Google Scholar]
- 3.White S, Schmutz M, Pozza MF, et al. Rufinamide (CGP 33101): a broad-spectrum anticonvulsant with excellent tolerability profile in rodents. Epilepsia. 2005;46(suppl 6):373–373. [Google Scholar]
- 4.Brunner LA, Harrigan EP, John VA, Powell ML. Pharmacokinetics of a new anticonvulsant (CGP 33101) in epileptic male patients and healthy male subjects after single ascending oral doses of 400–1200 mg. Am J Ther. 1994;1:215–220. doi: 10.1097/00045391-199410000-00008. [DOI] [PubMed] [Google Scholar]
- 5.Cardot JM, Lecaillon JB, Czendlik C, et al. The influence of food on the disposition of the antiepileptic rufinamide in healthy volunteers. Biopharm Drug Dispos. 1998;19:259–262. doi: 10.1002/(SICI)1099-081X(199805)19:4<259::AID-BDD98>3.0.CO;2-V. [DOI] [PubMed] [Google Scholar]
- 6.Arroyo S, Sachdeo R, Rosenfeld W, Critchley D, Perdomo C. Pharmacokinetics and safety of ascending doses of adjunctive rufinamide in pediatric patients with inadequately controlled seizures. Epilepsia. 2005;46(suppl 8):193–193. [Google Scholar]
- 7.Chang SW, Choi L, Karoplchyk MA. A pharmacokinetic evaluation of rufinamide in elderly and younger subjects. Epilepsia. 1998;39(suppl 6):59–59. [Google Scholar]
- 8.Fuseau E, Critchley D, Perdomo C, Arroyo S. Population pharmacokinetic drug-drug interaction analyses of rufinamide studies in patients with epilepsy. Epilepsia. 2005;46(suppl 8):210–211. [Google Scholar]
- 9.Brodie MJ, Rosenfeld W, Vazquez B, Ko D, Perdomo C, Arroyo S. Efficacy and safety of rufinamide as adjunctive therapy in adult patients with inadequately controlled partial seizures. Neurology. 2006;66(suppl 2):A35–A36. [Google Scholar]
- 10.Elger C, Stefan H, Perdomo C, Arroyo S. Dose-response relationships of rufinamide in patients with inadequately controlled partial seizures. Neurology. 2006;66(suppl 2):A37–A38. [Google Scholar]
- 11.Todorov A, Biton V, Krauss GL, Perdomo C, Arroyo S. Efficacy and safety of high-versus low-dose rufinamide monotherapy in patients with inadequately controlled partial seizures. Epilepsia. 2005;46(suppl 8):218–219. [Google Scholar]
- 12.Glauser T, Kluger G, Sachdeo R, Krauss G, Perdomo C, Arroyo S. Efficacy and safety of rufinamide adjunctive therapy in patients with Lennox-Gastaut Syndrome (LGS): a multicenter, randomized, double-blind, placebo-controlled, parallel trial. Neurology. 2005;64(suppl 1):1826–1826. [Google Scholar]
- 13.Glauser T, Kluger G, Sachdeo R, Krauss G, Perdomo C, Arroyo S. Open-label extension study of the efficacy and safety of rufinamide adjunctive therapy in patients with Lennox-Gastaut syndrome. Epilepsia. 2005;46(suppl 6):408–408. [Google Scholar]
- 14.Krauss GL, Perdomo CA, Arroyo S. Short and long-term safety of rufinamide in patients with epilepsy. Epilepsia. 2005;46(suppl 8):213–213. [Google Scholar]