Antiepileptic Drugs Carbamazepine and oxcarbazepine

Carbamazepine and oxcarbazepine, the 10-keto analog of carbamazepine, have relatively similar pharmacological profiles. Both have been shown to block tetrodotoxin-resistant Na1 channels in brain tissue.1 Neuronal hyper-excitability, linked to accumulation of sodium channels in injured peripheral axons and cell bodies, is reduced by carbamazepine, as is similar excitability in dorsal horn neurons2, 3 and possibly elsewhere in the central nervous system (CNS) where sodium channel may be up-regulated.4 The selectivity of Na1 channel blockade remains to be determined, but interaction with a low activation state of Nav1.8 channels may be one of the key mechanisms of carbamazepine.5 In addition, both car-bamazepine and oxcarbazepine appear to antagonize the A1 adenosine receptor, increase dopaminergic transmission, and potentiate voltage-gated potassium channels, all potentially useful properties in chronic pain.1 Both drugs inhibit L-type voltage-gated calcium channels and presyn-aptic glutamate release, although it is uncertain whether this happens in sufficient concentrations in clinical conditions.1 Oxcarbazepine and its metabolites are also thought to modulate other calcium channels.6 Both car-bamazepine and oxcarbazepine have been shown to possess some antihyperalgesic effects in experimental models of inflammatory pain, probably mediated by indirect activation of adrenergic a2 receptors.7

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