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Additional information about the drug Oxcarbazepine


Oxcarbazepine is an anticonvulsant medication primarily used in the treatment of epilepsy.
Common side effects include nausea, vomiting, dizziness, drowsiness, headache, double vision and trouble with walking.
Oxcarbazepine is marketed as Trileptal by Novartis and available in some countries as a generic drug.
Contents
1 Medical uses
1.1 Pregnancy
1.2 Nursing mothers
2 Adverse effects
3 Interactions
4 Pharmacology
4.1 Pharmacokinetics
4.2 Pharmacodynamics
4.3 Pharmacogenetics
4.4 Structure
5 History
6 See also
7 References
8 External links
Medical uses
Oxcarbazepine is an anticonvulsant used to reduce the occurrence of epileptic episodes, and is not intended to cure epilepsy.
In addition, oxcarbazepine has been used in the treatment of bipolar disorder, with limited high-quality evidence regarding efficacy.
Oxcarbazepine may also be beneficial in trigeminal neuralgia..
Pregnancy
Oxcarbazepine is listed as Pregnancy Category C.
Currently, there is limited data analyzing the impact of oxcarbazepine on a human fetus.
Pregnant persons on oxcarbazepine should be closely monitored, as plasma levels of the active metabolite (MHD) has been shown to potentially decrease during pregnancy.
Nursing mothers
Oxcarbazepine and MHD are both present in human breast milk and thus, some of the active drug can be transferred to a nursing infant.
Adverse effects
Adverse effects are dose dependent. The most common include dizziness, blurred or double vision, nystagmus, ataxia, fatigue, headaches, nausea, vomiting, sleepiness, and difficulty in concentration and mental sluggishness.
Other rare side effects of oxcarbazepine include severe low blood sodium (hyponatremia), anaphylaxis / angioedema, hypersensitivity (especially if experienced with carbamazepine, toxic epidermal necrolysis, Stevens–Johnson syndrome, and thoughts of suicide.
Measurement of serum sodium levels should be considered in maintenance treatment or if symptoms of hyponatremia develop.
Interactions
Oxcarbazepine and its active metabolite (monohydroxy derivative; MHD) have been shown to exhibit drug interactions when indicated with medications that are metabolized via CYP2C19, CYP3A4 and CYP3A5.
In addition, oxcarbazepine and MHD are CYP3A4 and CYP3A5 inducers and thus, have the potential to decrease the plasma concentration and therapeutic efficacy of medications that are CYP3A substrates.
Furthermore, oxcarbazepine has been shown to interact with other anticonvulsant medications when used in combination.
Pharmacology
Oxcarbazepine and MHD exert their action by blocking voltage-sensitive sodium channels, thus leading to the stabilization of hyper excited neural membranes, suppression of repetitive neuronal firing and diminishment propagation of synaptic impulses.
Pharmacokinetics
Oxcarbazepine has high bioavailability once it is administrated orally as tablets.
Pharmacodynamics
Both oxcarbazepine and its MHD the active metabolite were found to show anticonvulsant properties in seizure models done on animals.
Pharmacogenetics
Trileptal (oxcarbazepine), oral suspension 100 mg/ml
Since the structure of oxcarbazepine is similar to carbamazepine, there is a consideration for genetic testing in patients who are of Asian descent (mainly populations of Han Chinese (2–12%), Thai (8%), Philippines (15%), Malaysia) due to the higher frequency of the HLA-B*1502 allele.
Structure
Oxcarbazepine is a structural derivative of carbamazepine, with a ketone in place of the carbon–carbon double bond on the dibenzazepine ring at the 10 position (10-keto). 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 is a prodrug which is activated to licarbazepine in the liver.
History
300mg Trileptal tablets
First made in 1965,
See also
Carbamazepine
Eslicarbazepine acetate

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