Oxcarbazepine (oxcarbazepine)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Oxcarbazepine is an anticonvulsant agent.
Oxcarbazepine is an anticonvulsant agent that is structurally and chemically related to carbamazepine. Although the exact mechanism of action of oxcarbazepine is unknown, in vitro electrophysiologic studies indicate that the drug may stabilize excitatory neuronal membranes, inhibit repetitive neuronal firing, and decrease propagation of synaptic impulses by blocking voltage-sensitive sodium channels, actions that may prevent spread of epileptic seizures. Increased potassium conductance and modulation of high-voltage activated calcium channels also may contribute to the anticonvulsant activity of oxcarbazepine.
No substantial interactions between the drug and neurotransmitter receptors in the brain have been observed to date.
Oxcarbazepine and its active 10-monohydroxy metabolite (MHD (10,11-dihydro-10-hydroxy-5H-dibenz(b, f)azepine-5-carboxamide)) exhibit anticonvulsant activity in several animal seizure models. Oxcarbazepine protects against electrically induced tonic extension seizures and, to a lesser degree, chemically induced clonic seizures and may abolish or reduce frequency of chronically recurring focal seizures.
Following oral administration, oxcarbazepine is completely absorbed and extensively metabolized in the liver by cytosolic enzymes to MHD, which is believed to be responsible for the pharmacologic activity of oxcarbazepine. Food does not affect the rate or extent of absorption of the immediate-release tablets; although not specifically studied, food is also not expected to alter bioavailability of the oral suspension. Administration of oxcarbazepine extended-release tablets with a high-fat meal increased peak plasma concentrations of MHD by about 60%.
The oral bioavailabilities of oxcarbazepine immediate-release tablets and oral suspension appear to be similar; however, the extended-release tablets (administered once daily) are not bioequivalent to the same total daily dose of the immediate-release formulation (administered twice daily). More than 95% of an oral dose of oxcarbazepine is excreted in urine, mainly as metabolites with less than 1% as unchanged drug; less than 4% is excreted in feces.
USES: Oxcarbazepine is used to treat seizures.
Generic name: oxcarbazepine
Pronunciation: (ox-kar-BAY-zih-peen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Oxcarbazepine
Indications
The following indications are listed for Oxcarbazepine:
- Complex-Partial Epilepsy
- Focal Epilepsy
- Partial Epilepsy Treatment Adjunct
- Simple-Partial Epilepsy
Also known as: Automatic Epilepsy, Complex Focal Epilepsy, Complex Focal Seizures, Complex Local Seizures, Complex Partial Epilepsy, Complex Partial Seizures, Complex Psychomotor Epilepsy, Complex Psychomotor Seizure, Complex Temporal Lobe Epilepsy, Complex Temporal Lobe Seizures, Cortical Epilepsy, Elementary Focal Seizures, Elementary Partial Seizures, Focal Seizures, Local Epilepsy, Partial Epilepsy, Partial Onset Seizures, Partial Onset Seizures Treatment Adjunct, Partial Seizures, Partial Seizures Treatment Adjunct, Psychic Epilepsy, Psychomotor Epilepsy, Psychomotor Seizure, Simple Focal Epilepsy, Simple Focal Seizures, Simple Local Seizures, Simple Partial Epilepsy, Simple Psychomotor Epilepsy, Simple Psychomotor Seizures, Simple Temporal Lobe Epilepsy, Simple Temporal Lobe Seizures, Temporal Lobe Epilepsy, Temporal Lobe Seizure.
Dosing
No dosing information is available for this tab.
Oxcarbazepine is administered orally as conventional (immediate-release) tablets, oral suspension, or extended-release tablets.
Oxcarbazepine conventional tablets and oral suspension are administered twice daily without regard to meals. Oxcarbazepine extended-release tablets are administered once daily on an empty stomach (i.e., at least 1 hour before or 2 hours after a meal). (See Description.) The extended-release tablet should be swallowed whole with water or other liquid, and should not be cut, chewed, or crushed; because of these limitations, the extended-release tablet formulation is not recommended for use in children younger than 6 years of age.
Oxcarbazepine oral suspension should be shaken well immediately prior to administration. The appropriate dose should be administered using the oral dosing syringe supplied by the manufacturer. The oral suspension may be added to a small glass of water or swallowed directly from the syringe. After each use, the oral syringe should be rinsed with warm water and allowed to dry thoroughly.
The oral bioavailability of oxcarbazepine immediate-release tablets appears to be similar to that of the oral suspension and, therefore, these preparations can be used interchangeably on a mg-for-mg basis. At steady state, the extended-release tablets administered once daily are not bioequivalent to the immediate-release tablets administered twice daily; when converting from immediate-release preparations of oxcarbazepine to the extended-release tablets, a higher daily dosage may be required.
Patients currently receiving or beginning therapy with oxcarbazepine and/or any other anticonvulsant for any indication should be closely monitored for the emergence or worsening of depression, suicidal thoughts or behavior (suicidality), and/or any unusual changes in mood or behavior. (See Suicidality Risk under Cautions: Warnings/Precautions.)
Oxcarbazepine therapy should be withdrawn gradually to minimize the potential for increased seizure frequency and status epilepticus.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to oxcarbazepine or any ingredient in the formulation, or to eslicarbazepine acetate.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in 10% or more of patients receiving conventional oxcarbazepine include dizziness, somnolence, diplopia, fatigue, nausea, vomiting, ataxia, abnormal vision, abdominal pain, nystagmus, tremor, dyspepsia, and abnormal gait.
Adverse effects occurring in 5% or more of patients receiving oxcarbazepine extended-release tablets include dizziness, somnolence, headache, balance disorder, tremor, vomiting, diplopia, asthenia, and fatigue.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of oxcarbazepine conventional preparations as monotherapy of partial seizures have not been established in children younger than 4 years of age.
Safety and efficacy of oxcarbazepine conventional preparations as adjunctive therapy of partial seizures have not been established in children younger than 2 years of age.
Oxcarbazepine extended-release tablets are not recommended for use in children younger than 6 years of age because of administration difficulties and lack of studies in children younger than 4 years of age. (See Dosage and Administration: Administration.)
Clearance of the active MHD metabolite of oxcarbazepine decreases as age and weight increase. In children 2 to younger than 4 years of age, mean weight-adjusted clearance is approximately 80% higher than that of adults. In children 4-12 years of age, mean weight-adjusted clearance is approximately 40% higher than that of adults. In children 13 years of age or older, weight-adjusted MHD clearance is expected to be similar to that of adults.
Oxcarbazepine has been studied as adjunctive therapy and monotherapy for partial seizures in children 1 month to 17 years of age in controlled clinical trials.
As in adults, severe dermatologic and other sensitivity reactions have been reported in pediatric patients.
Category C. (See Users Guide.)
There are no adequate and well-controlled studies of oxcarbazepine in pregnant women; however, the drug is closely related to carbamazepine, which has been associated with teratogenic effects in humans. Limited data from pregnancy registries suggest that use of oxcarbazepine during pregnancy may be associated with congenital malformations. The drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Because of physiologic changes that occur during pregnancy, plasma concentrations of the active metabolite of oxcarbazepine (MHD) may gradually decrease during pregnancy; patients should be monitored during pregnancy and throughout the postpartum period.
Women who are pregnant while receiving oxcarbazepine should be encouraged to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry at 888-233-2334 (for patients); registry information also can be found on the website http://www.aedpregnancyregistry.org.
Both oxcarbazepine and its active MHD metabolite are distributed into milk in humans. Because of the potential for serious adverse reactions to oxcarbazepine in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Peak plasma concentrations of MHD and the area under the plasma concentration-time curve (AUC) may be 30-60% higher in geriatric patients 60 years of age or older than in younger adults (possibly related to decreases in renal function with age).
Close monitoring of serum sodium concentrations is recommended in geriatric patients at risk for hyponatremia.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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