| Indication |
For use as monotherapy or adjunctive therapy in the treatment of
partial seizures in adults with epilepsy and as adjunctive therapy in
the treatment of partial seizures in children ages 4-16 with epilepsy. |
| Pharmacodynamics |
Oxcarbazepine is structurally a derivative of carbamazepine,
adding an extra oxygen atom to the benzylcarboxamide group. This
difference helps reduce the impact on the liver of metabolizing the
drug, and also prevents the serious forms of anemia occasionally
associated with carbamazepine. Aside from this reduction in side
effects, it is thought to have the same mechanism as carbamazepine -
sodium channel inhibition - and is generally used to treat the same
conditions. |
| Mechanism of action |
The exact mechanism by which oxcarbazepine exerts its
anticonvulsant effect is unknown. It is known that the pharmacological
activity of oxcarbazepine occurs primarily through its 10-monohydroxy
metabolite (MHD). In vitro studies indicate an MHD-induced blockade of
voltage-sensitive sodium channels, resulting in stabilization of
hyperexcited neuronal membranes, inhibition of repetitive neuronal
discharges, and diminution of propagation of synaptic impulses. |
| Absorption |
Completely absorbed following oral administration. Food has no effect on the rate and extent of absorption of oxcarbazepine. |
| Volume of distribution |
|
| Protein binding |
Approximately 40% of the active 10-monohydroxy metabolite (MHD) is
bound to serum proteins, predominantly to albumin. Neither
oxcarbazepine nor its MHD binds with alpha-1–acid blycoprotein. |
| Metabolism |
Oxcarbazepine is completely absorbed and extensively metabolized
to its pharmacologically active 10-monohydroxy metabolite (MHD). MHD is
metabolized further by conjugation with glucuronic acid. |
| Route of elimination |
Oxcarbazepine is cleared from the body mostly in the form of
metabolites which are predominantly excreted by the kidneys. Fecal
excretion accounts for less than 4% of the administered dose. |
| Half life |
The half-life of the parent is about 2 hours, while the half-life
of MHD is about 9 hours, so that MHD is responsible for most
anti-epileptic activity. |
| Clearance |
Not Available |
| Toxicity |
Isolated cases of overdose with oxcarbazepine have been reported.
The maximum dose taken was approximately 24,000 mg. All patients
recovered with symptomatic treatment. |
