Revista de neurologia · 2006
[Oxcarbazepine in the treatment of epilepsy. A review and update].
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Horga de la Parte J F, Horga A
Аннотация
AIM: To review and update the most important information concerning the mechanism of action, efficacy, safety and clinical use of oxcarbazepine (OXC), one of the new antiepileptic drugs (AED).
DEVELOPMENT: In humans, OXC is rapid and extensively metabolized to its pharmacologically active 10-monohydroxy metabolite (MHD). OXC is a molecule derived from carbamazepine (CBZ), but these two drugs showed differences in their mechanism of action. OXC pharmacokinetics presents advantage over CBZ: in contrast with CBZ, OXC does not show autoinduction, the OXC dose-MHD serum concentration relationship displays a linear kinetics over the therapeutic dose range, and the frequency of drug-drug interactions is lower. So, we can establish standardized dose regimen and titration schedules in monotherapy and polytherapy. OXC shows better tolerability and safety than CBZ, in part at consequence of absence of 10-11-epoxi metabolites from CBZ. The better safety profile of OXC is reflected in less adverse drug reactions incidence, lower patient risk in overdosing, absence of reported cases of agranulocytosis or aplastic anemia, scarce cases founded of cardiotoxicity and lower risk of neurotoxicity. Common side effects of OXC are nausea, dizziness, vomiting, fatigue, diplopia and somnolence. During treatment with OXC must pay attention to development of hyponatremia, neurotoxicity or cutaneous hypersensitivity reactions. OXC is approved for use in infants. OXC is indicated for use as monotherapy or adjunctive therapy in the treatment of partial seizures with or without secondarily generalized seizures in adults and in children age 6 and over.
CONCLUSIONS: OXC showed important advances on safety and pharmacological properties for administration to adults and infants. OXC has similar clinical antiepileptic efficacy than older AED in the treatment of partial seizures, and it is recommended as a treatment of choice for partial seizures by several international guidelines.
DEVELOPMENT: In humans, OXC is rapid and extensively metabolized to its pharmacologically active 10-monohydroxy metabolite (MHD). OXC is a molecule derived from carbamazepine (CBZ), but these two drugs showed differences in their mechanism of action. OXC pharmacokinetics presents advantage over CBZ: in contrast with CBZ, OXC does not show autoinduction, the OXC dose-MHD serum concentration relationship displays a linear kinetics over the therapeutic dose range, and the frequency of drug-drug interactions is lower. So, we can establish standardized dose regimen and titration schedules in monotherapy and polytherapy. OXC shows better tolerability and safety than CBZ, in part at consequence of absence of 10-11-epoxi metabolites from CBZ. The better safety profile of OXC is reflected in less adverse drug reactions incidence, lower patient risk in overdosing, absence of reported cases of agranulocytosis or aplastic anemia, scarce cases founded of cardiotoxicity and lower risk of neurotoxicity. Common side effects of OXC are nausea, dizziness, vomiting, fatigue, diplopia and somnolence. During treatment with OXC must pay attention to development of hyponatremia, neurotoxicity or cutaneous hypersensitivity reactions. OXC is approved for use in infants. OXC is indicated for use as monotherapy or adjunctive therapy in the treatment of partial seizures with or without secondarily generalized seizures in adults and in children age 6 and over.
CONCLUSIONS: OXC showed important advances on safety and pharmacological properties for administration to adults and infants. OXC has similar clinical antiepileptic efficacy than older AED in the treatment of partial seizures, and it is recommended as a treatment of choice for partial seizures by several international guidelines.