Carbamazepine

Carbamazepine is an inhibitor of sodium channels.¹ It preferentially inhibits inactivated voltage-gated sodium channel Na_v1.7 and Na_v1.3 (IC₅₀s = 406 and 900 µM, respectively) over resting (closed) Na_v1.7 and Na_v1.3 channels in whole-cell patch-clamp assays using HEK293 cells (IC₅₀s = 1,584 and 2,464 µM, respectively). Carbamazepine (100 µM) inhibits sodium currents in a rat sciatic nerve patch-clamp assay ex vivo.² It reduces levels of the endogenous catecholamine dopamine in the striatum and hippocampus, as well as the levels of the dopamine precursor L-DOPA (Item No. 13248) in the striatum, in rats when administered at a dose of 100 mg/kg.³ Dietary administration of carbamazepine (0.5% w/w) reduces amphetamine-induced hyperactivity in mice.⁴ It decreases immobility time in the forced swim test in mice when administered in the diet at 0.75% w/w. Formulations containing carbamazepine have been used in the treatment of seizures, trigeminal neuralgia, and bipolar disorder.

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1. Sheets, P.L., Heers, C., Stoehr, T., et al. Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepine. J. Pharmacol. Exp. Ther. 326(1), 89-99 (2008).

2. Schwarz, J.R., and Grigat, G. Phenytoin and carbamazepine: Potential- and frequency-dependent block of Na currents in mammalian myelinated nerve fibers. Epilepsia 30(3), 286-294 (1989).

3. Okada, M., Hirano, T., Mizuno, K., et al. Biphasic effects of carbamazepine on the dopaminergic system in rat striatum and hippocampus. Epilepsy Res. 28(2), 143-153 (1997).

4. Kara, N.Z., Karpel, O., Toker, L., et al. Chronic oral carbamazepine treatment elicits mood-stabilising effects in mice. Acta Neuropsychiatr. 26(1), 29-34 (2014).