ESLICARBAZINE
Eslicarbazepine
acetate (ESL) is a prodrug that has been approved in Europe as adjunctive
therapy in adults with partial-onset seizures, with or without secondary
generalization. ESL is more rapidly converted to S(+)-licarbazine (eslicarbazine) than is oxcar-bazepine; clearly
both prodrugs have the same metabolite as active product. The mechanism of
action of carbamazepine, oxcarba-zepine, and ESL appears to be the same, ie,
blocking of voltage-gated Na+ channels. The R(–) enantiomer has some activity, but much less than its
counterpart.Clinically, the drug is similar to carbamazepine and oxcarba-zepine
in its spectrum of action, but it is less well studied in other possible
indications. The possible advantage of ESL is its once-daily dosing regimen.
The measured half-life of the S(+)
enantiomer is 9–11 hours. The drug is administered at a dosage of 400– 1200
mg/d; titration is typically required for the higher doses.Minimal drug level
effects are observed with coadministration of carbamazepine, levetiracetam,
lamotrigine, topiramate, and valproate. Oral contraceptives may be less
effective with concomi-tant ESL administration.
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