Sulthiame

Sulthiame is a pan-inhibitor of carbonic anhydrases (CA; K_is = 6-1,540 nM for CAI, -II, and IV-XIV) and an anticonvulsant.¹ It is selective for these CAs over CAIII (K_i = 630 µM). Sulthiame (10 µg/ml) also inhibits voltage-gated sodium currents in isolated guinea pig hippocampal CA1 neurons.² It reduces epileptiform activity induced by 4-aminopyridine (Item No. 18511) in guinea pig hippocampal slices when used at a concentration of 2.5 mM.³ Sulthiame (100-300 mg/kg, i.p.) induces neuronal cell death in neonatal rats.⁴ It decreases forelimb clonus duration in a rat model of partial epilepsy induced by amygdaloid kindling when administered at doses ranging from 25 to 200 mg/kg.⁵ Formulations containing sulthiame have been used in the treatment of epilepsy.

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1. De Simone, G., Scozzafava, A., and Supuran, C.T. Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates? Chem. Biol. Drug Des. 74(3), 317-321 (2009).

2. Madeja, M., Wolf, C., and Speckmann, E.J. Reduction of voltage-operated sodium currents by the anticonvulsant drug sulthiame. Brain Res. 900(1), 88-94 (2001).

3. Leniger, T., Wiemann, M., Bingmann, D., et al. Carbonic anhydrase inhibitor sulthiame reduces intracellular pH and epileptiform activity of hippocampal CA3 neurons. Epilepsia 43(5), 469-474 (2002).

4. Manthey, D., Asimiadou, S., Stefovska, V., et al. Sulthiame but not levetiracetam exerts neurotoxic effect in the developing rat brain. Exp. Neurol. 193(2), 497-503 (2005).

5. Song, H.K., Hamada, K., Yagi, K., et al. Effects of single and repeated administration of sulthiame on amygdaloid kindled seizures in rats. Epilepsy Res. 27(2), 81-87 (1997).