Oxcarbazepine

Oxcarbazepine. A Use Dependent Anti Epileptic Na_v Channel Blocker.

Epilepsy is one of the most common neurological disorders and it is estimated that the majority of epileptic patients are treated with only four drugs: phenobarbital, phenytoin, carbamazepine (CBZ) and valproic acid. It is widely accepted that the majority of antiepileptic drugs (AEDs) act by more than one mechanism.
Oxcarbazepine (OCBZ) is an anticonvulsant drug and its main mechanism of action is the inhibition of voltage-dependent sodium channels.
OCBZ is a keto homologue of CBZ with a completely different metabolic profile. OCBZ and CBZ have a comparable anticonvulsant efficacy, but OCBZ has the advantage of a low incidence of allergic reactions, enzyme induction and side effects.
Clinical trials, with OCBZ treated patients with epilepsy, confirmed the efficacy, tolerability, and safety of OCBZ at a daily dose of 30пїЅ46пїЅmg/kg (600пїЅ2400пїЅmg/day) as first-line treatment for children, adolescents, and adults with partial seizures including simple partial seizures, complex partial seizures, and secondarily generalized seizures.
In humans, the keto group of OCBZ is rapidly and quantitatively reduced to form a monohydroxy derivative (MHD), which is the main active agent during OCBZ therapy. OCBZ (IC₅₀ - 500 μM) and MHD (IC₅₀ - 200 μM) inhibit sustained, high frequency, repetitive firing of cultured spinal cord neurons due to an inhibitory effect on voltage-dependent sodium channels. This effect was found to be voltage- and frequency-dependent.
Neurochemical studies also showed that OCBZ binds to sodium channels and modulates sodium entry in cortical synaptosomes. An additional mechanism of action such as an effect on potassium channels, might be also clinically important.

Ion Channel Modulators; Voltage-Gated Na⁺ Channel Blockers

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