Topiramate is a sugar sulfamate that exhibits potent anticonvulsant activity. It completely blocks seizures (ED50 = 39 mg/kg when given orally) in mice in the maximal electroshock seizure test.1,2 This effect is sustained for over eight hours.1,2 In the rotoreel test of neurotoxicity, topiramate has a peak neurotoxic dose ED50 value of 407 mg/kg in mice at one hour.1 It is virtually inactive against seizures caused by pentylenetetrazol, bicuculline, picrotoxin, and strychnine. It does not bind to norepinephrine, serotonin, γ-amino butyric acid, muscarinic, or dopamine receptors.1,2 The drug form of Topiramate, Topamax®, is used alone or with other medications to treat seizures associated with epilepsy and to prevent migraine headaches.3,4
1
Maryanoff, B.E., Nortey, S.O., Gardocki, J.F., et al. Anticonvulsant O-alkyl sulfamates. 2,3:4,5-bis-O-(1-methylethylidene)-β-D-fructopyranose sulfamate and related compounds. J Med Chem30880-887(1987).
2
Shank, R.P., Gardocki, J.F., Vaught, J.L., et al. Topiramate: Preclinical evaluation of a structurally novel anticonvulsant. Epilepsia35(2)450-460(1994).
3
Ben-Menachem, E., Sander, J.W., Stefan, H., et al. Topiramate monotherapy in the treatment of newly or recently diagnosed epilepsy. Clin Ther30(7)1180-1195(2008).
4
Ruiz, L., and Ferrandi, D. Topiramate in migraine progression. J Headache Pain10419-422(2009).
Maryanoff, B.E., Nortey, S.O., Gardocki, J.F., et al. Anticonvulsant O-alkyl sulfamates. 2,3:4,5-bis-O-(1-methylethylidene)-β-D-fructopyranose sulfamate and related compounds. J Med Chem30880-887(1987).
Shank, R.P., Gardocki, J.F., Vaught, J.L., et al. Topiramate: Preclinical evaluation of a structurally novel anticonvulsant. Epilepsia35(2)450-460(1994).
Ruiz, L., and Ferrandi, D. Topiramate in migraine progression. J Headache Pain10419-422(2009).
Ben-Menachem, E., Sander, J.W., Stefan, H., et al. Topiramate monotherapy in the treatment of newly or recently diagnosed epilepsy. Clin Ther30(7)1180-1195(2008).