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P - Caution when used during pregnancy
L - Contraindicated in lactation
FI - Food *
Oxcarbazepine is an anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy. It is also used to treat anxiety and mood disorders, and benign motor tics.
Oxcarbazepine is a structural derivative of carbamazepine, with a ketone in place of the carbon-carbon double bond on the dibenzazepine ring. This difference helps reduce the impact on the liver of metabolizing the drug, and also prevents the serious forms of anemia or agranulocytosis occasionally associated with carbamazepine. Aside from this reduction in side effects, it is thought to have the same mechanism as carbamazepine - sodium channel inhibition (presumed to be the main mechanism of action) - and is generally used to treat the same conditions. Oxcarbazepine has recently been found to be associated with a greater enhancement in mood and reduction in anxiety symptoms than other drugs employed to treat epilepsy.
Oxcarbazepine and its active metabolite (MHD) exhibit anticonvulsant properties in animal seizure models. They protected rodents against electrically induced tonic extension seizures and, to a lesser degree, chemically induced clonic seizures, and abolished or reduced the frequency of chronically recurring focal seizures in Rhesus monkeys with aluminum implants. No development of tolerance (i.e., attenuation of anticonvulsive activity) was observed in the maximal electroshock test when mice and rats were treated daily for five days and four weeks, respectively, with Oxcarbazepine or MHD.
Oxcarbazepine blocks voltage-sensitive sodium channels, which inhibits repetitive firing, stabilises hyperexcited neuronal membranes and decreases release of synaptic impulses. These effects may prevent the spread of epileptic seizures.
Well absorbed from the GI tract.
Monohydroxy metabolite: Widely distributed; protein-binding: About 40%, mainly to albumin. Oxcarbazepine and metabolite: Cross the placental barrier and enter breast milk.
Metabolised in the liver to 10,11-dihydro-10-hydroxy-carbamazepine (principal metabolite; possesses antiepileptic activity).
Via urine (mainly as metabolites). Half-life: 2 hours (oxcarbazepine); 9 hours (monohydroxy metabolite).
Information Not Available
The adverse reactions include dizziness, somnolence, headache, ataxia, fatigue, vertigo, nervousness, amnesia, abnormal thinking, insomnia, speech disorder, agitation, confusion; vomiting, nausea, abdominal pain, diarrhoea, dyspepsia, constipation, gastritis, weight gain; abnormal gait, tremor, weakness, back pain, abnormal coordination, dysmetria, sprains/strains, muscle weakness; diplopia, nystagmus, abnormal vision and accommodation; hypotension, leg oedema; rash, acne; hyponatraemia; rhinitis, chest infection, epistaxis, sinusitis.
Potentially Fatal: Stevens-Johnson syndrome, toxic epidermal necrolysis. Anaphylaxis and angioedema.
Information Not Available
Cross-sensitivity to carbamazepine may occur. Do not discontinue abruptly. Renal and hepatic impairment. Patients at risk of hyponatraemia. May impair ability to drive or operate machinery. Pregnancy.
Reduced serum levels with carbamazepine, phenobarbitone, phenytoin, valproic acid. May reduce levels/effects of CYP3A4 substrates (e.g. benzodiazepines, calcium channel blockers, clarithromycin, ciclosporin, erythromycin, oestrogens, mirtazapine, nateglinide, nefazodone, nevirapine, protease inhibitors, tacrolimus, venlafaxine). May reduce efficacy of oral contraceptives. May reduce levels/effects of maraviroc. May increase levels of phenobarbitone, phenytoin.
Levels may be reduced with St John's wort. Evening primrose may reduce seizure threshold and reduce the effects of oxcarbazepine.
Monotherapy or adjunctive therapy in the treatment of partial seizures with or without secondary generalised tonic-clonic seizures
Adult: Initially, 600 mg daily in 2 divided doses; increase at a max increments of 600 mg daily at weekly intervals depending on response. Maintenance: 600-1,200 mg daily. Adjunctive therapy/refractory patients switched from other anticonvulsants: Up to 2,400 mg daily.
Child: >6 years: 8-10 mg/kg daily in 2 divided doses; increase as necessary to max increments of 10 mg/kg daily at about wkly intervals to a max of 46 mg/kg daily. Maintenance in adjunctive therapy: 30 mg/kg daily.
CrCl (ml/min) Dosage Recommendation
<30 Initially, 300 mg daily or 50% of usual dose. Increase at weekly intervals or longer.
May be taken with or without food
Caution when used during pregnancy
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindicated in lactation
Safety and efficacy not established in children younger than 2 years of age (adjunctive therapy). Safety and efficacy not established in children younger than 4 years of age (monotherapy).
Because of age-related reductions in CrCl, C max and AUC may be elevated.
Store at 25°C (77°F).
Store at 25°C (77°F).