pronounced as (ox car baz' e peen)
Oxcarbazepine (Trileptal) is used alone or in combination with other medications to control certain types of seizures in adults and children. Oxcarbazepine extended-release tablets (Oxtellar XR) are used in combination with other medications to control certain types of seizures in adults and children 6 years of age and older. Oxcarbazepine is in a class of medications called anticonvulsants. It works by decreasing abnormal electrical activity in the brain.
Oxcarbazepine comes as a tablet, an extended-release tablet, and a suspension (liquid) to take by mouth. The tablet and suspension are usually taken every 12 hours (twice a day) with or without food. The extended-release tablet is usually taken once a day on an empty stomach, 1 hour before or 2 hours after a meal. Take oxcarbazepine at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take oxcarbazepine exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Shake the suspension well right before each use to mix the medication evenly. Use the oral dosing syringe that came with the medication to withdraw the right amount of suspension from the bottle. You can swallow the suspension straight from the syringe or you can mix it with a small glass of water and swallow the mixture. Wash the syringe with warm water and allow it to dry thoroughly after use.
Swallow the extended-release tablets whole with water or another liquid; do not split, chew, or crush them.
Your doctor will probably start you on a low dose of oxcarbazepine and gradually increase your dose, not more often than once every 3 days. If you were taking another medication to treat your seizures and are switching to oxcarbazepine, your doctor may gradually decrease your dose of the other medication while increasing your dose of oxcarbazepine. Follow these directions carefully and ask your doctor if you are not sure how much medication you should take.
Oxcarbazepine may help control your seizures but will not cure your condition. Continue to take oxcarbazepine even if you feel well. Do not stop taking oxcarbazepine without talking to your doctor, even if you experience side effects such as unusual changes in behavior or mood. If you suddenly stop taking oxcarbazepine, your seizures may get worse. Your doctor will probably decrease your dose gradually.
Your doctor or pharmacist will give you the manufacturer's patient information sheet (Medication Guide) when you begin treatment with oxcarbazepine and each time you refill your prescription. Read the information carefully and ask your doctor or pharmacist if you have any questions. You can also visit the Food and Drug Administration (FDA) website (http://www.fda.gov/Drugs) or the manufacturer's website to obtain the Medication Guide.
Oxcarbazepine is also sometimes used to treat bipolar disorder (manic-depressive disorder; a disease that causes episodes of depression, episodes of frenzied abnormal excitement, and other abnormal moods). Talk to your doctor about the possible risks of using this medication for your condition.
This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.
Before taking oxcarbazepine:
- tell your doctor and pharmacist if you are allergic to oxcarbazepine, carbamazepine (Carbatrol, Epitol, Equetro, Tegretol), any other medications, or any of the inactive ingredients in oxcarbazepine tablets, extended release tablets, or suspension. Ask your pharmacist for a list of the inactive ingredients in oxcarbazepine tablets or suspension.
- tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Other medications may interact with oxcarbazepine, so be sure to tell your doctor and pharmacist about all the medications you are taking, even those that do not appear on this list. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
- tell your doctor if you have or have ever had kidney or liver disease.
- tell your doctor if you are of Chinese, Thai, Malaysian, Korean, Indian, or Filipino descent. The risk of life-threatening allergic reactions called Stevens-Johnson syndrome (SJS) or toxic epidermal necrolysis (TEN) is increased in people of Asian ancestry who have a genetic (inherited) risk factor. If you are Asian, your doctor may order a test to see if you have the genetic risk factor before prescribing oxcarbazepine.
- tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you are using hormonal contraceptives, you should know that this type of birth control may not work well when used with oxcarbazepine. Hormonal contraceptives should not be used as your only method of birth control while you are taking this medication. Talk to your doctor about birth control methods that will work for you. Call your doctor if you miss a period or think you may be pregnant while you are taking oxcarbazepine.
- you should know that this medication may make you drowsy or dizzy, affect the way you move, or may cause double vision or other vision changes. Do not drive a car or operate machinery until you know how this medication affects you.
- remember that alcohol can add to the drowsiness caused by this medication.
- you should know that your mental health may change in unexpected ways and you may become suicidal (thinking about harming or killing yourself or planning or trying to do so) while you are taking oxcarbazepine for the treatment of epilepsy, mental illness, or other conditions. A small number of adults and children 5 years of age and older (about 1 in 500 people) who took anticonvulsants such as oxcarbazepine to treat various conditions during clinical studies became suicidal during their treatment. Some of these people developed suicidal thoughts and behavior as early as 1 week after they started taking the medication. There is a risk that you may experience changes in your mental health if you take an anticonvulsant medication such as oxcarbazepine, but there may also be a risk that you will experience changes in your mental health if your condition is not treated. You and your doctor will decide whether the risks of taking an anticonvulsant medication are greater than the risks of not taking the medication. You, your family, or your caregiver should call your doctor right away if you experience any of the following symptoms: panic attacks; agitation or restlessness; new or worsening irritability, anxiety, or depression; acting on dangerous impulses; difficulty falling or staying asleep; aggressive, angry, or violent behavior; mania (frenzied, abnormally excited mood); talking or thinking about wanting to hurt yourself or end your life; withdrawing from friends and family; preoccupation with death and dying; giving away prized possessions; or any other unusual changes in behavior or mood. Be sure that your family or caregiver knows which symptoms may be serious so they can call the doctor if you are unable to seek treatment on your own.
Unless your doctor tells you otherwise, continue your normal diet.
Before you begin your treatment, talk to your doctor about what you should do if you accidentally miss a dose. Be sure to ask your doctor how long you should wait between taking a missed dose and taking your next scheduled dose of oxcarbazepine. Do not take a double dose to make up for a missed one.
Keep this medication in the container it came in, tightly closed, and out of reach and sight of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Store the extended-release tablets away from light. Dispose of any unused suspension 7 weeks after the bottle is first opened.
Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA's Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.
It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org
In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services at 911.
Keep all appointments with your doctor and the laboratory. Your doctor may order certain lab tests to check your response to oxcarbazepine.
Before having any laboratory test, tell your doctor and the laboratory personnel that you are taking oxcarbazepine.
Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.
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Continuing Education Activity
Oxcarbazepine is a medication used in the treatment of partial seizures. It is in the anticonvulsant drug classification. This activity reviews the indications, action, and contraindications for oxcarbazepine as a valuable agent in treating partial seizures. This activity will highlight the mechanism of action, adverse event profile, pharmacokinetics, and drug interactions pertinent for interprofessional team members in the treatment of patients with partial seizures.
Describe the mechanism of action of oxcarbazepine.
Review the therapeutic uses of oxcarbazepine.
Explain the potential side effects of oxcarbazepine.
Outline the importance of collaboration and coordination among the interprofessional team to enhance patient care when dosing and monitoring oxcarbazepine therapy.
Oxcarbazepine is a 10-keto derivative of carbamazepine, which came to the market in 2000. However, the minor structural differences between oxcarbazepine and carbamazepine have led to significant differences in the induction of metabolic pathways and the metabolism of the two medications.
Oxcarbazepine is also available as an extended-release (XR) dosage form. It is a member of a class of medications known as anticonvulsants and voltage-sensitive sodium channel antagonists. Oxcarbazepine is FDA-approved for partial seizures in adults with epilepsy or partial seizures in children with epilepsy ages 4 to 16. This medication is useful as monotherapy or adjunctive to another medication for the management of seizures. Oxcarbazepine is also an option for bipolar disorder; however, this medication is not yet FDA-approved for bipolar disorder.
Mechanism of Action
Oxcarbazepine binds to sodium channels and inhibits the high-frequency repetitive neuronal firing. Oxcarbazepine also inhibits the release of glutamate. This medication gets metabolized by the liver and excreted by the kidneys. Oxcarbazepine very rapidly converts to licarbazepine, which is its active metabolite (monohydroxy metabolite, MHD). Licarbazepine is responsible for the antiseizure activity of oxcarbazepine. The half-life of oxcarbazepine is 1 to 3.7 hours, while the half-life of licarbazepine is 8 to 10 hours. Oxcarbazepine has not been shown to cause the autoinduction of its metabolism, such as carbamazepine.
Oxcarbazepine is known to be a weak inducer of the CYP3A4, which plays a role in estrogen metabolism. Thus oxcarbazepine can reduce the efficacy of oral contraceptives when used in high doses. Oxcarbazepine is also a weak inhibitor of CYP2C19 and can cause an increase in phenytoin concentrations when used in very high doses. Oxcarbazepine itself is not affected by CYP3A4 inhibitors like carbamazepine is.
Oxcarbazepine is only available in the oral dosage form at this time; both tablets and liquid formulations are available. Oxcarbazepine shows rapid and nearly complete absorption after oral administration, about 95% absorption. The usual doses range for oxcarbazepine is 1200 to 2400 mg per day.
Partial seizures: 600 mg by mouth twice daily, starting at 300 mg twice daily; max 2400 mg daily. Recommendations include screening for HLA-B*1502 allele prior to starting therapy for at-risk populations.
Initial monotherapy: 600 mg orally twice daily, starting with 300 mg twice daily and increasing by 300 mg per day every 3 days to a maximum of 2400 mg daily.
- Conversion to monotherapy: 1200 mg by mouth twice daily, starting with 300 mg and increasing by 600 mg daily each week to a max of 2400 mg daily.
Discontinue other anticonvulsants over a 3 to 6-week timeframe
When using oxcarbazepine with other sedating medications, the physician should slowly titrate the medication for the patient to best tolerate the sedating side effects of the medications.
The immediate-release dosage form should be taken two times a day with or without food. The patient may mix the liquid formulation with water for better tolerability.
The extended-release dosage form should be taken once a day. It is important to take the extended-release oxcarbazepine on an empty stomach and not cut or crush the medication before ingesting it.
It is essential to taper off oxcarbazepine slowly. If the patient discontinues oxcarbazepine suddenly, it may cause the epilepsy patient to seize or may cause a relapse of a bipolar patient.
Oxcarbazepine can lead to central nervous system (CNS) side effects due to its blockade of voltage-sensitive sodium channels. Some common side effects that patients experience when taking oxcarbazepine are sedation, dizziness, abnormal gait, headache, ataxia, fatigue, confusion, nausea, vomiting, abdominal pain, or rash. Hyponatremia and increased suicidal ideation are two of the most dangerous and life-threatening side effects patients may experience while taking oxcarbazepine. Weight gain and sedation can occur as well in a minority of patients. If patients have experienced hypersensitivity with carbamazepine, they are more likely to experience hypersensitivity with oxcarbazepine.
Oxcarbazepine is structurally similar to carbamazepine and thus an increased risk of Stevens-Johnson syndrome or toxic epidermal necrolysis in Asian patients with the HLA-B*1502 allele. When experiencing a side effect, the recommendation is to wait and continue medication if the side effect is not disruptive to life or dangerous. With time, most side effects do cease. If side effects continue, physicians should consider switching to another agent, and augmenting oxcarbazepine with another agent is usually not successful. It is important to note that side effects may increase when increasing the dose of oxcarbazepine.
Avoid abrupt withdrawal of oxcarbazepine. Prescribers should exercise caution in pediatric, elderly, pregnant, and renal impairment patients who have had a hypersensitivity reaction to carbamazepine. It is also contraindicated in treatment-naive patients with the HLA-B*1502 allele.
It is essential to monitor serum sodium concentrations. Hyponatremia is a severe risk that can occur with the use of oxcarbazepine. The risk for hyponatremia is the highest in the first three months of medication use, and 2% to 3% of patients may experience hyponatremia. Hyponatremia is when sodium concentrations are below 125 mmol/L. It is essential to monitor the use of selective serotonin reuptake inhibitor (SSRI) with oxcarbazepine, as these medications can cause a decrease in sodium concentrations through the syndrome of inappropriate antidiuretic hormone (SIADH) production.
Approved for use in children four years and older as monotherapy or adjunctive therapy for partial seizures. The initial dose should be 8 to 10 mg/kg per day, separated into two divided doses.
Oxcarbazepine and licarbazepine (MHD) can cross the placenta, and research has found these drugs in the newborn. Data from a limited number of pregnancy registries suggest congenital malformations can occur, e.g., craniofacial, cardiac. Pregnant patients taking oxcarbazepine are encouraged to enroll in a pregnancy registry (www.aedpregnancyregistry.org).
May need to start a lower starting dose and titrate more slowly in patients with renal complications because the kidney excretes oxcarbazepine. In patients with creatinine clearance between 10 and 50, reduce the dose by 25%. If creatinine clearance is below 10, reduce the dose by 50%.
No adjustment in the oxcarbazepine dose is required.
No adjustment in the oxcarbazepine dose is required.
The geriatric population may have decreased renal clearance and thus should be started at lower doses and titrated more slowly as oxcarbazepine undergoes renal excretion.
Oxcarbazepine studies done in rats and dogs over a 3 and 6-month period have shown reversible dose-dependent liver weight increases, which is considered due to centrilobular megalocytosis. Oxcarbazepine metabolism differs significantly between humans and rats, and therefore this toxicity cannot be generalized to human patients.
Enhancing Healthcare Team Outcomes
Healthcare workers (including physicians, NPS, and PAs) who prescribe oxcarbazepine should be aware of its indications and adverse effect profile. The drug is known to cause many CNS adverse effects, including sedation, dizziness, abnormal gait, headache, ataxia, fatigue, confusion, nausea, vomiting, abdominal pain, or rash. Hyponatremia and increased suicidal ideation are two of the most dangerous and life-threatening side effects patients may experience while taking oxcarbazepine. Weight gain and sedation can occur as well in a minority of patients. If side effects continue, physicians should consider switching to another agent because augmenting oxcarbazepine with another agent is usually unsuccessful. It is important to note that side effects may increase with higher doses of oxcarbazepine.
Nurses should actively participate in this monitoring since they often have more frequent contact with the patient. They can also assess treatment effectiveness on follow-up visits, as well as monitoring for adverse drug effects. They will report any issues to the physician and/or pharmacist. Pharmacists need to verify dosing and in cases of drugs like oxcarbazepine, checking for potential drug-drug interactions is crucial since they can impair the therapeutic effectiveness of oxcarbazepine. If any interactions are present, the pharmacist must contact the prescriber immediately. If the patient is receiving cognitive therapy as well from a different provider, that individual also needs to know about the patient's regimen so that they can monitor for adverse effects as well.
All medications require interprofessional coordination, but it may even be more crucial for drugs such as oxcarbazepine; all healthcare team members need to participate, collaborate, and communicate to optimize results and minimize adverse effects. [Level 5]
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Jansen AC, Andermann E. Progressive Myoclonus Epilepsy, Lafora Type. In: Adam MP, Ardinger HH, Pagon RA, Wallace SE, Bean LJH, Mirzaa G, Amemiya A, editors. GeneReviews® [Internet]. University of Washington, Seattle; Seattle (WA): Dec 28, 2007. [PubMed: 20301563]
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Trileptal (oxcarbazepine) for Bipolar Disorder
What is Trileptal?
Trileptal is a medication known as an anticonvulsant that is used to treat seizures. It is also sometimes used as a mood stabilizer to treat the symptoms of bipolar disorder.
When did the U.S. Food and Drug Administration (FDA) approve the medication?
Trileptal was first approved by the FDA in 2001.
Is there a generic version of Trileptal?
Yes, the generic version is known as oxcarbazepine and is sold in the U.S.
Are there any major differences between Trileptal and other medications used to treat bipolar disorder?
Trileptal belongs to the class of medications known as anticonvulsants. Anticonvulsants are sometimes prescribed to treat manic episodes associated with bipolar disorder. Trileptal may be prescribed in combination with other medications to treat symptoms. Talk to your doctor about the potential risks and benefits of taking Trileptal.
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Can children take Trileptal?
Children are prescribed Trileptal for seizures, but the effectiveness and safety of use for bipolar disorder has not been established. Talk to your child’s doctor about the risks and benefits and potential side effects to monitor.
Are there potential interaction issues for people taking Trileptal and any other drugs?
There are hundreds of drugs which are known to interact with Trileptal in major, moderate, or mild ways, so let your doctor know what other medications you are taking before you begin taking the medication. Some of these might include amiodarone, amitriptyline, calcium channel blockers, chlorpromazine, clomipramine, cyclophosphamide, desmopressin, diazepam, diuretics, hormonal contraceptives, indapamide, seizure medications, proton-pump inhibitors, theophylline, and selective serotonin reuptake inhibitors. The medication can also decrease the effectiveness of hormonal contraceptives.
Are there any other medical conditions that would make someone ineligible for Trileptal therapy?
Talk to your doctor about other medical conditions before you take Trileptal, such as kidney or liver disease.
What is the typical dose that would be prescribed to someone taking Trileptal?
Dosage will vary depending on the age of the patient and the condition being treated.
What do I do if I miss a dose?
You should never take extra doses of the medication to make up for missed doses. Talk to your doctor about how long you should wait in between doses.
What side effects can Trileptal cause?
Common side effects can include:
• cold symptoms
• lack of balance
• changes in vision
• depressed mood
• spinning sensation
• uncontrolled eye movement
It also is recommended that you wait to drive or operate machinery until you know how the medication affects you. It is also recommended that people avoid alcohol and illegal drugs while on the medication, as they can worsen adverse effects. Report major side effects to your doctor immediately, which can include swelling, thirst, nausea, vomiting, headache, confusion, decreased alertness, rash, fever, blisters, irritated eyes, blotches on skin, yellowing of skin or eyes, bleeding or bruising, joint pain, chest pain, signs of infection, or changes in urination. You can also report side effects to the FDA at 1-800-FDA-1088 or online.
What are the potential psychological side effects of taking Trileptal?
Taking anticonvulsant medications can sometimes result in increased suicidal thoughts and behaviors in a small percentage of people. Seek medical help if you experience these thoughts or other changes in your behavior or mood.
Is it safe for a woman who is pregnant, about to become pregnant, or nursing to take Trileptal?
Trileptal may cause birth defects and fetal harm when taken during pregnancy. The drug can be transferred via breast milk and potentially harm a baby. Therefore, talk to your doctor if you are pregnant, planning to become pregnant, or are nursing before you take Trileptal. The medication can also impact the effectiveness of hormonal contraceptives.
Can symptoms occur if Trileptal is discontinued?
It’s important not to discontinue use of the drug before talking with your doctor. Withdrawal symptoms of Trileptal can include insomnia and return of seizures or bipolar symptoms (depending on the purpose of taking the medication).
What should I do if I overdose on Trileptal?
An overdose of Trileptal could be fatal, so seek immediate help or call the Poison Help Line at 1-800-222-1222 if you overdose. Overdose symptoms can include dizziness, sedation, decreased heart rate, low blood pressure, low sodium levels, seizures, and coma.
Is Trileptal habit-forming?
Trileptal is not habit-forming, but it is not recommended that you discontinue use of the drug before talking with your doctor, as withdrawal symptoms can occur.
How much does Trileptal cost?
According to goodrx.com, 60 tables of 300 mg generic oxcarbazepine cost approximately $150. 60 tablets of 300 mg Trileptal cost approximately $500.
Are there any disadvantages to Trileptal?
The biggest disadvantages of Trileptal are potential side effects. Pregnant women are also typically advised not to take the medication due to the risks.
DISCLAIMER: The information contained herein should NOT be used as a substitute for the advice of an appropriately qualified and licensed physician or other healthcare providers. This article mentions drugs that were FDA-approved and available at the time of publication and may not include all possible drug interactions or all FDA warnings or alerts. The author of this page explicitly does not endorse this drug or any specific treatment method. If you have health questions or concerns about interactions, please check with your physician or go to the FDA site for a comprehensive list of warnings.
Oxcarbazepine, sold under the brand name Trileptal among others, is a medication used to treat epilepsy and bipolar disorder. For epilepsy it is used for both focal seizures and generalized seizures. It has been used both alone and as add-on therapy in people with bipolar who have had no success with other treatments. It is taken by mouth.
Common side effects include nausea, vomiting, dizziness, drowsiness, double vision and trouble with walking. Serious side effects may include anaphylaxis, liver problems, pancreatitis, suicide ideation, and an abnormal heart beat. While use during pregnancy may harm the baby, use may be less risky than having a seizure. Use is not recommended during breastfeeding. In those with an allergy to carbamazepine there is a 25% risk of problems with oxcarbazepine. How it works is not entirely clear.
Oxcarbazepine was patented in 1969 and came into medical use in 1990. It is available as a generic medication. In 2018, it was the 158th most commonly prescribed medication in the United States, with more than 3 million prescriptions.
Oxcarbazepine is an anticonvulsant used to reduce the occurrence of epileptic episodes, and is not intended to cure epilepsy. Oxcarbazepine is used alone or in combination with other medications for the treatment of focal (partial) seizures in adults. In pediatric populations, it can be used by itself for the treatment of partial seizures for children 4 years and older, or in combination with other medications for children 2 years and older. A 2020 Cochrane review found that it was effective in reducing seizure frequency when used as an add-on therapy for drug-resistant focal epilepsy but there were concerns over tolerability.
Research has investigated the use of oxcarbazepine as a mood stabilizer in bipolar disorder, with further evidence needed to fully assess its suitability. It may be beneficial in trigeminal neuralgia.
Oxcarbazepine is listed as pregnancy category C.
There is limited data analyzing the impact of oxcarbazepine on a human fetus. Animal studies have shown increased fetal abnormalities in pregnant rats and rabbits exposed to oxcarbazepine during pregnancy. In addition, oxcarbazepine is structurally similar to carbamazepine, which is considered to be teratogenic in humans (pregnancy category D). Oxcarbazepine should only be used during pregnancy if the benefits justify the risks.
Pregnant women on oxcarbazepine should be closely monitored, as plasma levels of the active metabolite licarbazepine have been shown to potentially decrease during pregnancy.
Oxcarbazepine and its metabolite licarbazepine are both present in human breast milk and thus, some of the active drug can be transferred to a nursing infant. When considering whether to continue this medication in nursing mothers, the impact of the drug's side effect profile on the infant, should be weighed against its anti-epileptic benefit for the mother.
Side effects are dose-dependent. The most common include dizziness, blurred or double vision, nystagmus, ataxia, fatigue, headaches, nausea, vomiting, sleepiness, 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. Low blood sodium is seen in 20-30% of people taking oxcarbazepine and 8-12% of those experience severe hyponatremia. Some side effects, such as headaches, are more pronounced shortly after a dose is taken and tend to fade with time (60 to 90 minutes). Other side effects include stomach pain, tremor, rash, diarrhea, constipation, decreased appetite and dry mouth. Photosensitivity is a potential side-effect and people could experience severe sunburns as a result of sun exposure.
Oxcarbazepine, licarbazepine and many other common drugs influence each other through interaction with the Cytochrome P450 family of enzymes. This leads to a cluster of dozens of common drugs interacting with one another to varying degrees, some of which are especially noteworthy:
Oxcarbazepine and licarbazepine are potent inhibitors of CYP2C19 and thus have the potential to increase plasma concentration of drugs, which are metabolized through this pathway. Other antiepileptics, which are CYP2C19 substrates and thus may be metabolised at a reduced rate when combined with oxcarbazepine include diazepam,hexobarbital,mephenytoin,methylphenobarbital,nordazepam,phenobarbital,phenytoin,primidone. However, many classes of drugs are ligands to CYP2C19.
In addition, oxcarbazepine and licarbazepine are CYP3A4 and CYP3A5 inducers and thus have the potential to decrease the plasma concentration of CYP3A4 and CYP3A5 substrates. Drugs which are CYP3A4 or CYP3A5 substrates and therefore may have reduced efficacy include calcium channel antagonists against high blood pressure and oral contraceptives. However, whether the extent of CYP3A4/5 induction at therapeutic doses reaches clinical significance is unclear. Furthermore, for example phenytoin and phenobarbital are known to reduce plasma levels of licarbazepine through induction of Cytochrome P450 enzymes.
Oxcarbazepine is a prodrug, which is largely metabolised to its pharmacologically active 10-monohydroxy derivative licarbazepine (sometimes abbreviated MHD). 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. Furthermore, anticonvulsant effects of these compounds could be attributed to enhanced potassium conductance and modulation of high-voltage activated calcium channels.
Oxcarbazepine has high bioavailability upon oral administration. In a study in humans, only 2% of oxcarbazepine remained unchanged, 70% were reduced to licarbazepine; the rest were minor metabolites. The half-life of oxcarbazepine is considered to be about 2 hours, whereas licarbazepine has a half-life of nine hours. Through its chemical difference to carbamazepine metabolic epoxidation is avoided, reducing hepatic risks. Licarbazepine is metabolised by conjugation with Glucuronic acid. Approximately 4% are oxidised to the inactive 10,11-dihydroxy derivative. Elimination is almost completely renal, with faeces accounting to less than 4%. 80% of the excreted substances are to be attributed to licarbazepine or its glucuronides.
Both oxcarbazepine and licarbazepine were found to show anticonvulsant properties in seizure models done on animals. These compounds had protective functions whenever tonic extension seizures were induced electrically, but such protection was less apparent whenever seizures were induced chemically. There was no observable tolerance during a four weeks course of treatment with daily administration of oxcarbazepine or licarbazepine in electroshock test on mice and rats. Most of the antiepileptic activity can be attributed to licarbazepine. Aside from its reduction in side effects, it is presumed to have the same main mechanism as carbamazepine, sodium channel inhibition, and is generally used to treat the same conditions.
The human leukocyte antigen (HLA) allele B*1502 has been associated with an increased incidence of Stevens–Johnson syndrome and toxic epidermal necrolysis in people treated with carbamazepine, and thus those treated with oxcarbazepine might have similar risks. People of Asian descent are more likely to carry this genetic variant, especially some Malaysian populations, Koreans (2%), Han Chinese (2–12%), Indians (6%), Thai (8%), and Philippines (15%). Therefore, it has been suggested to consider genetic testing in these people prior to initiation of treatment.
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.
First made in 1966, it was patent-protected by Geigy in 1969 through DE 2011087 . It was approved for use as an anticonvulsant in Denmark in 1990, Spain in 1993, Portugal in 1997, and eventually for all other EU countries in 1999. It was approved in the US in 2000. In September 2010, Novartis, of which Geigy are part of its corporate roots, pleaded guilty to marketing Trileptal for the unapproved uses of neuropathic pain and bipolar disorder.
There is also an extended-release formulation.
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Neuropathic pain and fibromyalgiapharmacotherapies
|Ion channel blockers|
Class oxcarbazepine drug
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