Oxcarbazepine (Trileptal) is an analog of carbamazepine that has better tolerability when taken orally and fewer drug-drug interactions. It is used in the management of patients with seizures.

Oxcarbazepine Uses:

Focal (partial) onset seizures:

• Immediate-release:
  • Used in the treatment of focal (partial) onset seizures in adults as monotherapy or adjunctive therapy, in the treatment of focal (partial) onset seizures in children under the age of four who have epilepsy, and in the treatment of focal (partial) onset seizures in children under the age of two who have epilepsy.
• Extended-release:
  • Treatment for adults and children under the age of six who have focal (partial) onset seizures

Off Label Use Oxcarbazepine in Adults:

• Neuropathic pain.

Oxcarbazepine Dose in Adults

Oxcarbazepine Dose in the treatment of Adjunctive therapy, focal (partial) onset seizures (epilepsy): Oral:

Immediate release:

• 600 mg first, divided into 2 doses.
• At weekly intervals, the dose may be raised by as much as 600 mg per day.
• The maximum amount suggested is 1,200 mg divided into 2 doses each day.
• Most patients were unable to tolerate doses of 2,400 mg per day, despite the fact that doses >1,200 mg per day were marginally more effective (due to CNS effects).

Extended-release:

• 600 mg once daily at first.
• At weekly intervals, the dosage can be raised by 600 mg/day increments.
• It is advised to take 1,200 to 2,400 mg once daily.
• Although higher daily doses were marginally more effective, most patients could not handle doses of 2,400 mg per day (due to CNS effects).

Conversion to monotherapy, focal (partial) onset seizures (epilepsy): Patients receiving concomitant antiepileptic drugs (AEDs):

Oral: Immediate release:

• Initial: 600 mg twice daily, split, while also lowering the dosage of ancillary AEDs.
• Concomitant AEDs should be entirely stopped using over the course of 3 to 6 weeks, while the oxcarbazepine dosage should be increased by 600 mg every week in order to achieve the maximum dose (2,400 mg/day) in around 2 to 4 weeks (lower doses have been effective in patients in whom monotherapy has been initiated).

Oxcarbazepine Dose in the treatment of Initiation of monotherapy, focal (partial) onset seizures (epilepsy): Oral:

Immediate-release:

• 600 mg first, divided into 2 doses.
• Every third day, increase the dosage by 300 mg, bringing it to 1,200 mg per day.
• Patients switching from various AEDs to monotherapy have been proven to respond well to higher doses (2,400 mg daily).

Extended-release:

• 600 mg initially, once daily.
• At weekly intervals, the dosage can be raised in increments of 600 mg per day.
• It is advised to take 1,200 to 2,400 mg once daily.
• Although daily doses greater than 1,200 mg per day might be a little more effective, bigger doses are linked to more side effects.

Conversion from immediate-release to extended-release:

• It might be essential to use higher doses of the extended-release formulation.

Dosage adjustment with concomitant strong CYP3A4 inducers or UGT inducers (eg, carbamazepine, phenobarbital, phenytoin, rifampin): Extended-release:

• Think about starting with 900 mg once daily.

Oxcarbazepine Dose in the treatment of Neuropathic pain (off-label):

Oral:

• 300 mg every day at first.
• After three days, increase the dosage to 300 mg twice daily. From there, you can increase the dose by 300 mg every five days, up to a maximum of 900 mg twice a day, depending on your response and tolerance.
• During the clinical trial's maintenance phase, the mean dose was 1,445 mg per day.

Oxcarbazepine Dose in Children

Note:

• On a mg-for-mg basis, oral suspension and tablets that are for immediate release are interchangeable.
• Extended-release and immediate-release medications cannot be substituted for one another on a mg-for-mg basis since they are not bioequivalent.

Oxcarbazepine Dose in the treatment of Partial-onset seizures, monotherapy: Oral:

Immediate-release (Trileptal):

Children ≥4 years and Adolescents ≤16 years:

• Initiation of monotherapy: Patients not receiving concomitant anti-epileptic drugs (AEDs):

Initial: The suggested monotherapy maintenance dose by weight is 8 to 10 mg/kg/day in two divided doses; the typical starting daily dose in adults is 600 mg/day; the dose is increased every third day by 5 mg/kg/day to reach this level.

Maintenance dose:

• 20 to <25 kg: 600 to 900 mg/day in 2 divided doses.
• 25 to <35 kg: 900 to 1,200 mg/day in 2 divided doses.
• 35 to <45 kg: 900 to 1,500 mg/day in 2 divided doses.
• 45 to <50 kg: 1,200 to 1,500 mg/day in 2 divided doses.
• 50 to <60 kg: 1,200 to 1,800 mg/day in 2 divided doses.
• 60 to <70 kg: 1,200 to 2,100 mg/day in 2 divided doses.
• ≥70 kg: 1,500 to 2,100 mg/day in 2 divided doses.

Conversion to monotherapy:

• Patients taking AEDs concurrently: Initial: 8 to 10 mg/kg/day in 2 split doses (the typical adult initial dose is 600 mg/day), with a concurrent initial dose reduction of accompanying AEDs.
• Concomitant AEDs should be entirely tapered off over the course of 3 to 6 weeks, with the dosage of oxcarbazepine being increased as necessary by no more than 10 mg/kg/day at intervals of about a week.
• To reach the suggested monotherapy maintenance dose, increase the oxcarbazepine dosage.

Adolescents ≥17 years: Initiation of monotherapy: Patients not receiving prior AEDs:

• At first, take 300 mg twice daily.
• Every third day, increase the dosage by 300 mg, reaching a maintenance dose of 1,200 mg divided into 2 doses.

Conversion to monotherapy: Patients receiving concomitant AEDs:

• Initial: 300 mg twice daily while also lowering the dosage of any coadministered AEDs.
• Concomitant AEDs should be totally stopped using over the course of 3 to 6 weeks, while the oxcarbazepine dosage should be increased by 600 mg every week in order to reach the goal maintenance dose of 2,400 mg per day split into 2 doses within 2 to 4 weeks.

Oxcarbazepine Dose in the treatment of Partial-onset seizures, adjunctive therapy: Oral:

Immediate-release (Trileptal):

Children 2 to <4 years:

Patient weight <20 kg: Initial:

• 8 to 10 mg per kg, divided into two dosages, every day.
• Due to enhanced clearance at this age, starting at a higher dose of 16 to 20 mg per kg per day may be an option.
• dose gradually over the course of two to four weeks.
• The maximum daily dose is 60 milligrammes per kilogramme.

Patient weight ≥20 kg:

• Initial: 2 split dosages of 8 to 10 mg per kilogramme per day (usual maximum initial daily dose: 600 mg per day).
• dose gradually over the course of two to four weeks.
• The maximum daily dose is 60 milligrammes per kilogramme.

Note:

• With a target dose of 60 mg per kg per day, 50% of patients who were 2 to 4 years old had their dose titrated to at least 55 mg per kg per day.
• Children 2 to 4 years old may need up to twice the dose per unit of body weight compared to adults due to a higher medication clearance rate.

Children ≥4 years and Adolescents ≤16 years:

• Initial: 2 split dosages of 8 to 10 mg per kg per day.
• The typical beginning daily dose maximum is 600 mg.

Maintenance dose:

• 20 to 29 kg: 900 mg per day split into two doses.
• 1,200 mg/day in two divided doses for 1 to 39 kg.
• >39 kg: 1,800 mg divided into 2 doses per day.

Note:

• Pediatric patients aged 4 to 16 received doses ranging from 6 to 51 mg per kg per day (median dose: 31 mg per kg per day) in one clinical trial that used these paediatric target maintenance dosages.
• Children 4 to 12 years of age may need a 50% greater dose per body weight than adults due to a higher drug clearance.

Adolescents ≥17 years:

• At first, take 300 mg twice daily.
• Up to a goal maintenance dose of 1,200 mg per day in 2 split doses, the dose may be increased by 600 mg per day increments at weekly intervals.
• Most patients were unable to tolerate doses of 2,400 mg per day, despite the fact that doses >1,200 mg per day were marginally more effective (due to CNS effects).

Extended-release (Oxtellar XR):

Children and Adolescents 6 to ≤16 years:

• Initial dosage: 8 to 10 mg per kilogramme once daily.
• 600 mg per day is the maximum initial dose during the first week of treatment.
• To reach the appropriate maintenance dose based on weight, increase the dose every week in increments of 8 to 10 mg per kg per day (maximum dosage incremental increase: 600 mg per dose) as follows:

Maintenance dose:

• 20 to 29 kg: 900 mg once a day.
• 1 to 39 kg: 1,200 mg once a day.
• >39 kg: 1,800 mg once a day.

Adolescents ≥17 years:

• 600 mg initially, once daily.
• At weekly intervals, the dosage can be raised in increments of 600 mg per day.
• It is advised to take 1,200 to 2,400 mg once daily.
• Most patients were unable to tolerate 2,400 mg per day, despite daily doses >1,200 mg being slightly more effective (due to CNS effects).

Conversion from immediate-release (Trileptal) to extended-release (Oxtellar XR):

• Children ≥6 years and Adolescents:
  • Higher doses of Oxtellar XR may be necessary; on an mg per mg basis dosage forms are not bioequivalent.

Dosage adjustment with concomitant drugs:

• Strong inducers of CYP3A4 and/or UGT (eg, rifampin, carbamazepine, phenytoin, phenobarbital):
• Immediate-release:
  • Children ≥2 years and Adolescents:
    • During oxcarbazepine titration, monitor serum concentrations of 10-monohydroxy (MHD) metabolite (active).
    • Additional oxcarbazepine dose adjustments may be necessary if inducer initiated, dose modified, or discontinued.

• Extended-release:
  • Children ≥6 years and Adolescents:
    • Initial: Consider higher initial doses of oxcarbazepine:
    • 6 to ≤16 years:
      • Oral: 12 to 15 mg per kg per day once a day (maximum daily dose: 900 mg per day).
    • ≥17 years:
      • Oral: 900 mg per day.
      • Additional oxcarbazepine dose adjustments may be necessary if inducer initiated, dose modified, or discontinued.

Oxcarbazepine Pregnancy Category: C

• Oxcarbazepine is the active metabolite MHD and inactive metabolite DHD. They cross the placenta and are detectable in newborns.
• According to the manufacturer data from a small number of pregnancies from pregnancy registries suggests congenital malformations related to oxcarbazepine monotherapy.
• This includes craniofacial defects as well as cardiac malformations.
• AED monotherapy is more likely to produce teratogenic effects than AED polytherapy.
• Due to the physiologic changes during pregnancy, plasma concentrations of MHD slowly decrease; patients should be closely monitored during and after delivery.
• Oxcarbazepine could lower plasma levels of hormonal contraceptives.
• Continuous data collection is underway to monitor the outcomes of oxcarbazepine-exposed infants and pregnant women.
• Patients who were exposed to oxcarbazepine in pregnancy should call 1-888-233-3233 to register for the NAAED Pregnancy Registry.
• Additional information can be found at aedpregnancyregistry.org.

Use of oxycarbazepine while breastfeeding

• Breast milk contains oxycarbazepine as well as the active 10-hydroxy metabolite MHD.
• According to the manufacturer breastfeeding during therapy is a decision that should be made after considering the risks to infants and the benefits to mothers.

Oxcarbazepine Dose in Kidney Disease:

Mild-to-moderate impairment:

• The manufacturer's labelling does not provide any dosage modifications.

Severe impairment (CrCl <30 mL/minute):

• Immediate release, Extended-release: To obtain the desired clinical response, therapy should be started at half the typical starting dose (300 mg daily), then raised gradually (eg, 300 to 450 mg daily at weekly intervals).

ESRD (on dialysis):

• Use immediate-release formulations rather than the extended-release ones.

Oxcarbazepine dose in Liver Disease:

Mild-to-moderate impairment:

• No dose changes are required.

Severe impairment:

• Immediate release:
  • The manufacturer's labelling does not disclose dosage modifications; proceed with caution (has not been studied).
• Extended-release:
  • The manufacturer's labelling does not disclose dosage changes, and usage is not advised (has not been studied).

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• The incidence of adverse effects is from monotherapy and adjunctive AED studies.
• The incidence in children was similar.

Common Side Effects of Oxcarbazepine:

• Central Nervous System:

  • Dizziness
  • Drowsiness
  • Headache
  • Ataxia
  • Fatigue
  • Abnormal Gait
  • Vertigo

• Gastrointestinal:

  • Vomiting
  • Nausea
  • Abdominal Pain

• Neuromuscular & Skeletal:

  • Tremor

• Ophthalmic:

  • Diplopia
  • Nystagmus
  • Visual Disturbance

Less Common Side Effects Of Oxcarbazepine:

• Cardiovascular:

  • Chest Pain
  • Edema
  • Lower Extremity Edema
  • Hypotension

• Central Nervous System:

  • Emotional Lability
  • Anxiety
  • Equilibrium Disturbance
  • Confusion
  • Nervousness
  • Amnesia
  • Seizure
  • Falling
  • Abnormality In Thinking
  • Insomnia
  • Hypoesthesia
  • Dysmetria
  • Speech Disorder
  • Abnormal Electroencephalogram
  • Agitation
  • Lack Of Concentration
  • Feeling Abnormal
  • Myasthenia

• Dermatologic:

  • Skin Rash
  • Diaphoresis
  • Acne Vulgaris

• Endocrine & Metabolic:

  • Hyponatremia
  • Hot Flash
  • Increased Thirst
  • Weight Gain

• Gastrointestinal:

  • Diarrhea
  • Constipation
  • Dyspepsia
  • Anorexia
  • Dysgeusia
  • Upper Abdominal Pain
  • Xerostomia
  • Gastritis
  • Toothache

• Genitourinary:

  • Urinary Tract Infection
  • Urinary Frequency
  • Vaginitis

• Hematologic & Oncologic:

  • Bruise
  • Lymphadenopathy
  • Purpuric Rash
  • Rectal Hemorrhage

• Hypersensitivity:

  • Hypersensitivity Reaction

• Infection:

  • Viral Infection
  • Infection

• Neuromuscular & Skeletal:

  • Asthenia
  • Back Pain
  • Muscle Spasm
  • Sprain

• Ophthalmic:

  • Blurred Vision
  • Accommodation Disturbance

• Otic:

  • Otalgia
  • Otic Infection

• Respiratory:

  • Upper Respiratory Tract Infection
  • Rhinitis
  • Cough
  • Epistaxis
  • Pulmonary Infection
  • Sinusitis
  • Bronchitis
  • Nasopharyngitis
  • Pharyngitis
  • Pneumonia

• Miscellaneous:

  • Fever
  • Head Trauma

Frequency of Side effects Not Defined:

• Cardiovascular:

  • Bradycardia
  • Cardiac Failure
  • Flushing
  • Hypertension
  • Orthostatic Hypotension
  • Palpitations
  • Syncope
  • Tachycardia

• Central Nervous System:

  • Aggressive Behavior
  • Apathy
  • Aphasia
  • Aura
  • Cerebral Hemorrhage
  • Delirium
  • Delusions
  • Dystonia
  • Euphoria Extrapyramidal Reaction
  • Hemiplegia
  • Hyperkinesia
  • Hyperreflexia
  • Hypertonia
  • Hypokinesia
  • Hyporeflexia
  • Hypotonia
  • Hysteria
  • Impaired Consciousness
  • Intoxicated Feeling
  • Malaise
  • Manic Behavior
  • Migraine
  • Neuralgia
  • Nightmares
  • Oculogyric Crisis
  • Panic Disorder
  • Paralysis
  • Paranoia
  • Personality Disorder
  • Precordial Pain
  • Psychomotor Retardation
  • Psychosis
  • Rigors
  • Speech Disturbance
  • Stupor
  • Voice Disorder

• Dermatologic:

  • Alopecia
  • Contact Dermatitis
  • Eczema
  • Erythematosus Rash
  • Facial Rash
  • Folliculitis
  • Genital Pruritus
  • Maculopapular Rash
  • Miliaria
  • Psoriasis
  • Skin Photosensitivity
  • Urticaria
  • Vitiligo

• Endocrine & Metabolic:

  • Change In Libido
  • Decreased T4
  • Heavy Menstrual Bleeding
  • Hyperglycemia
  • Hypocalcemia
  • Hypoglycemia
  • Hypokalemia
  • Increased Gamma-Glutamyl Transferase
  • Intermenstrual Bleeding
  • Weight Loss

• Gastrointestinal:

  • Aphthous Stomatitis
  • Biliary Colic
  • Bloody Stools
  • Cholelithiasis
  • Colitis
  • Duodenal Ulcer
  • Dysphagia
  • Enteritis
  • Eructation
  • Esophagitis
  • Flatulence
  • Gastric Ulcer
  • Gingival Hemorrhage
  • Gingival Hyperplasia
  • Hematemesis
  • Hemorrhoids
  • Hiccups
  • Increased Appetite
  • Retching
  • Sialadenitis
  • Stomatitis

• Genitourinary:

  • Dysuria
  • Hematuria
  • Leukorrhea
  • Priapism
  • Urinary Tract Pain

• Hematologic & Oncologic:

  • Thrombocytopenia

• Hepatic:

  • Increased Liver Enzymes

• Hypersensitivity:

  • Angioedema

• Neuromuscular & Skeletal:

  • Right Hypochondrium Pain
  • Systemic Lupus Erythematosus
  • Tetany

• Ophthalmic:

  • Blepharoptosis
  • Cataract
  • Conjunctival Hemorrhage
  • Hemianopia
  • Mydriasis
  • Ocular Edema
  • Photophobia
  • Scotoma
  • Xerophthalmia

• Otic:

  • Otitis Externa
  • Tinnitus

• Renal:

  • Nephrolithiasis
  • Polyuria
  • Renal Pain

• Respiratory:

  • Asthma
  • Dyspnea
  • Laryngismus
  • Pleurisy

Contraindications to Oxcarbazepine:

• Hypersensitivity to eslicarbazepine-acetate, oxcarbazepine, or any other formulation ingredient.
• Limited documentation exists on the existence of allergenic cross-reactivity between carbamazepine analogs and carbamazepine.
• Cross-sensitivity can be possible due to similarities in chemical structure or pharmacologic effects.

Warnings and precautions

• Blood dyscrasias

  • Rarely, reports of agranulocytosis and leukopenia have been made about the use of this medication.
  • It may be necessary to discontinue treatment and convert to an alternate form of therapy.

• Bone disorders

  • The long-term effects of prolonged use have been linked to decreased bone mineral density and osteopenia.

• CNS effects

  • There have been reports of adverse effects in the CNS, including cognitive symptoms such as psychomotor slowing, difficulty concentrating, speech or language problems, somnolence, fatigue, coordination abnormalities and ataxia.
  • Patients should be cautious when performing tasks that require mental alertness, such as operating machinery or driving.

• Dermatologic reactions

  • There have been reports of potentially fatal and sometimes deadly dermatologic reactions in children and adults (eg, Stevens Johnson, toxic epidermal necrolysis).
  • The median time for onset was 19 days after treatment began.
  • Be aware of signs and symptoms that could indicate skin reactions. Alternate therapy may be necessary.
  • Oxcarbazepine has been associated with serious skin reactions that recurred.

• Hepatic dysfunction

  • Rarely has hepatitis been reported.
  • Stop the medication at away if you experience any symptoms of hepatic dysfunction, including anorexia, nausea/vomiting, pain in the right upper quadrant, pruritus, or other symptoms.

• Hypersensitivity reactions

  • Even after the initial dose, there have been a few uncommon reports of anaphylaxis or gioedema. If symptoms persists, stop using the medication forever.
  • Patients who have a history of carbamazepine hypersensitivity should exercise caution. Between 25 and 30 percent of patients may experience cross-sensitivity.
  • Oxcarbazepine-related drug reactions with eosinophilia (DRESS), also known as multiorgan hypersensitivity responses, have also been recorded in close proximity to the start of the treatment.
  • You should monitor for possible manifestations of lymphatic, hepatic and renal dysfunctions. Alternate therapy may be necessary.

• Hyponatremia

  • Treatment-related side effects include syndrome of incorrect antidiuretic hormone secretion and clinically severe hyponatremia (serum salt 125 mmol/L).
  • It usually occurs within the first three months of treatment, but it can occur up to one year later.
  • If hyponatremia symptoms occur (eg, nausea and malaise, headaches, lethargy or confusion, seizures), you should measure your serum sodium concentration.
  • Patients at high risk of hyponatremia should be monitored for serum sodium, particularly if they are elderly or taking medications that lower their sodium levels.
  • Hyponatremia patients may need to be given fluid restriction, dosage reduction or discontinuation of therapy.

• Hypothyroidism

  • Hypothyroidism has been documented; it is worth monitoring thyroid function, especially in children.
  • The return to normal thyroxine levels has been linked with discontinuing therapy.

• Suicidal thoughts:

  • A pooled analysis of antiepileptics trials (regardless if they were indicated) revealed an increase in suicidal thoughts/behavior. The incidence rate was 0.43% for patients treated, compared to 0.2% for patients who received placebo.
  • Risk can be observed as soon as one week after initiation, and continues throughout the trial (most trials last less than 24 weeks).
  • For any changes in behavior that could indicate depression or suicidal thoughts, monitor all patients.
  • If symptoms develop, patients should immediately notify their healthcare provider.

• Cardiovascular disease

  • Patients with severe cardiovascular disease or ECG abnormalities were not included in clinical trials.
  • Patients with HF should be monitored for body weight and fluid retention.
  • Assess serum sodium for signs of worsening cardiac function and fluid retention.

• Renal impairment

  • Single-dose studies have shown that patients with CrCl >30 mL/minute have a longer half-life.
  • These patients may require dose adjustment.

• Seizure disorder

  • Children have been known to experience exacerbation or new-onset primary generalized seizure, especially in the case of children.
  • Stop using oxcarbazepine in the event of seizure aggravation.

Oxcarbazepine: Drug Interaction

Risk Factor C (Monitor therapy)
Alcohol (Ethyl)	May enhance the CNS depressant effect of OXcarbazepine.
CloZAPine	CYP3A4 Inducers (Weak) may lower the level of CloZAPine in the serum.
CYP3A4 Inducers (Strong)	OXcarbazepine's serum concentration can drop. Particularly, oxcarbazepine's active metabolite, 10-monohydroxy, may have lower amounts.
Lacosamide	Antiepileptic drugs (Sodium Channel Blockers) may make lacosamide more harmful or poisonous. Particularly, there may be an increased risk for bradycardia, ventricular tachyarrhythmias, or a longer PR interval.
LevETIRAcetam	LevETIRAcetam's serum levels may be reduced by oxcarbazepine.
Mianserin	May reduce an anticonvulsant's therapeutic impact.
NiMODipine	CYP3A4 Inducers (Weak) may decrease the serum concentration of NiMODipine.
Orlistat	May decrease the serum concentration of Anticonvulsants.
RifAMPin	May lower serum levels of the active OXcarbazepine metabolite(s). Particularly, levels of the main active 10-monohydroxy metabolite may drop.
Rivaroxaban	Rivaroxaban's serum levels may drop if you use oxcarbazepine.
Thiazide and Thiazide-Like Diuretics	May enhance the adverse/toxic effect of OXcarbazepine. Specifically, there may be an increased risk for hyponatremia.
Valproate Products	OXcarbazepine's serum concentration can drop.
Risk Factor D (Consider therapy modification)
Bictegravir	Bictegravir's serum concentration may drop if you take oxcarbazepine. Management: When combining bictegravir, emtricitabine, and tenofovir alafenamide, consider using a different anticonvulsant. If the combination must be taken, keep a cautious eye out for signs of diminished antiviral efficacy.
CarBAMazepine	May lower serum levels of the active OXcarbazepine metabolite(s). Particularly, levels of the main active 10-monohydroxy metabolite may drop. Management: Take into account raising the starting dose of Oxtellar XR (oxcarbazepine extended release tablet) for adults to 900 mg per day. For additional oxcarbazepine formulations, there are no particular guidelines available.
Cobicistat	The serum concentration of Cobicistat may drop when OXcarbazepine is used. Management: When a different antiepileptic is an option, do so.
Estrogen Derivatives (Contraceptive)	Estrogen derivatives' serum levels may be reduced by oxycarbazepine (Contraceptive). Failure with contraception is possible. Management: It is advised to use a complementary, nonhormonal method of birth control.
Fosphenytoin-Phenytoin	May lower serum levels of the active OXcarbazepine metabolite(s). Particularly, levels of the main active 10-monohydroxy metabolite may drop. The serum concentration of fosphenytoin-phenytoin may rise when using oxcarbazepine. Management: Take into account raising the starting dose of Oxtellar XR (oxcarbazepine extended release tablet) for adults to 900 mg per day. For additional oxcarbazepine formulations, there are no particular guidelines available.
Mefloquine	May reduce an anticonvulsant's therapeutic impact. Anticonvulsant serum concentrations may be reduced by mefloquine. Treatment: Mefloquine should not be used to prevent malaria in those who have a history of convulsions. keep an eye on anticonvulsant levels.
Perampanel	OXcarbazepine serum concentration might rise. The serum concentration of Perampanel may drop when using oxycarbazepine. Management: When using perampanel along with oxcarbazepine, increase the initial dose to 4 mg/day. Patients using this combination should be continuously monitored for responsiveness, particularly if their oxcarbazepine medication is altered.
PHENobarbital	May lower serum levels of the active OXcarbazepine metabolite(s). Particularly, levels of the main active 10-monohydroxy metabolite may drop. PHENobarbital's serum levels may rise in response to oxcarbazepine. Management: Take into account raising the starting dose of Oxtellar XR (oxcarbazepine extended release tablet) for adults to 900 mg per day. For additional oxcarbazepine formulations, there are no particular guidelines available.
Progestins (Contraceptive)	OXcarbazepine could lower the level of progestins in the serum (Contraceptive). Management: It is possible for contraceptives to fail. Utilization of a second or additional hormonal-free form of contraception.
Risk Factor X (Avoid combination)
Dolutegravir	Dolutegravir's serum concentration may drop if you take oxcarbazepine.
Doravirine	The serum levels of doravirine may drop when using oxycarbazepine.
Elvitegravir	Elvitegravir's serum concentration may drop if you take oxcarbazepine.Oxcarbazepine should not be used in combination products containing elvitegravir, cobicistat, emtricitabine, and tenofovir; instead, consider using a different antiepileptic drug wherever practical.
Eslicarbazepine	May intensify OXcarbazepine's negative or harmful effects.
Ledipasvir	Ledipasvir's serum concentration may drop if you use oxcarbazepine.
Rilpivirine	Rilpivirine's serum concentration could drop if you take oxcarbazepine.
Selegiline	OXcarbazepine might make Selegiline's serotonergic effects stronger.
Simeprevir	Simeprevir's serum levels may drop when OXcarbazepine is used.
Sofosbuvir	It's possible that oxcarbazepine will lower sofosbuvir's serum levels.
Tenofovir Alafenamide	Tenofovir Alafenamide's serum concentration may drop if you take oxcarbazepine.
Ulipristal	Ulipristal's serum concentration may drop if you take oxcarbazepine.

Monitoring Parameters:

• Seizure frequency.
• As needed (especially during the first three months of therapy), serum sodium.
• CNS depression symptoms (dizziness headaches somnolence)
• Hypersensitivity reactions.
• Patients who are taking other medications that lower sodium levels should have additional serum sodium monitoring.
• This is especially true for patients with hyponatremia signs and symptoms, as well as patients experiencing an increase in the severity or frequency of seizures.
• Periodic thyroid function testing (especially for children) and CBC.
• Suicidality monitoring (e.g. suicidal thoughts and depression, behavioral changes)
• As needed, serum levels of concomitant antiepileptic medications during titration.

How to administer Oxcarbazepine?

Immediate release:

• Administer twice a day without regard to meals.

Suspension:

• Prior to using it for the first time, firmly insert the plastic adapter provided with the bottle.
• Cover adapter with the child-resistant cap when not in use.
• Shake bottle for at least 10 seconds, remove the child-resistant cap and insert the oral dosing syringe provided to withdraw the appropriate dose.
• The dose may be taken directly from an oral syringe or may be mixed in a small glass of water immediately prior to swallowing.
• Rinse the syringe with warm water after use and allow to dry thoroughly.
• Discard any unused portion after 7 weeks of first opening the bottle.

Extended-release:

• On an empty stomach, at least one hour before or two hours after eating, administer once daily.
• Swallow whole; do not cut, crush, or chew the tablets.

Mechanism of action of Oxcarbazepine (Trileptal):

• The drug oxcarbazepine and its monohydroxy metabolite, MHD, both have pharmacological effects.
• It is not known what the mechanism behind this anticonvulsant effect is.
• MHD and Oxcarbazepine block voltage-sensitive sodium channel voltage. They stabilize hyperexcited neuronal membranes and inhibit repetitive firing.
• This is thought to prevent seizures from spreading.
• The conductance of potassium is likewise increased by MHD and oxcarbazepine, and the activity of high-voltage activated calcium channels is modulated.

Absorption:

• Complete

Protein binding:

• Oxcarbazepine: 67%; MHD: 40%, primarily to albumin; parent drug and metabolite do not bind to alpha-1 acid glycoprotein.

Metabolism:

• Oxcarbazepine is extensively metabolized in the liver to its active 10-monohydroxy metabolite (MHD).
• MHD undergoes further metabolism via glucuronide conjugation.
• 4% of the dose is oxidized to the 10,11-dihydroxy metabolite (DHD) (inactive); 70% of serum concentration appears as MHD, 2% as unchanged oxcarbazepine, and the rest as minor metabolites

Note: Unlike carbamazepine, autoinduction of metabolism has not been observed and biotransformation of oxcarbazepine does not result in an epoxide metabolite

Bioavailability:

• Immediate-release tablets and suspension have similar bioavailability (based on MDH serum concentrations).
• Extended-release tablets and immediate-release products are not bioequivalent.
• Immediate release: Decreased in children <8 years; increased in elderly >60 years

Half-life elimination:

• Children (Rey 2004): 2 to 5 years: MHD: Single dose: Mean range: 4.8 to 6.7 hours; 6 to 12 years: MHD: Single dose: Mean range: 7.2 to 9.3 hours
• Adults: Immediate release: Parent drug: 2 hours; MHD: 9 hours; renal impairment (CrCl 30 mL/minute): MHD: 19 hours.
• Extended-release: Parent drug: 7 to 11 hours; MHD: 9 to 11 hours

Time to peak serum concentration:

• Children 2 to 12 years: Immediate release: Oxcarbazepine: 1 hour; MHD: 3 to 4 hours (Rey 2004).
• Adults: Immediate release: MHD: Tablets: Median: 4.5 hours (range: 3 to 13 hours); Suspension: Median 6 hours.
• Extended-release: MHD: 7 hours

Excretion:

• Urine (95%, <1% as unchanged oxcarbazepine, 27% as unchanged MHD, 49% as MHD glucuronides, 3% as DHD (inactive), and 13% as a conjugate of oxcarbazepine and MHD);
• feces (<4%)
• Clearance (per body weight):
  • Children 2 to <4 years: Increased by ∼80% compared to adults
  • Children 4 to 12 years: Increased by ∼40% compared to adults
  • Children ≥13 years: Values approach adult clearance.

International Brand Names of Oxcarbazepine:

• Oxtellar XR
• Trileptal
• APO-OXcarbazepine
• JAMP-OXcarbazepine
• Trileptal
• Actinium
• Carbox
• Deprectal
• Leptal
• Lonazet
• Neurtrol
• Ocnobel
• Oleptal
• Oxalepsy
• Oxalept
• Oxazep
• Oxcar
• Oxetol
• Oxpin
• Oxrate
• Oxypine
• Prolepsi
• Sytoclon
• Timox
• Trileptal
• Trileptin

Oxcarbazepine Brand Names in Pakistan:

Oxcarbazepine Suspension 300 mg in Pakistan
Oxep	Macter International (Pvt) Ltd.

Oxcarbazepine Suspension 300 mg/5ml in Pakistan
Oxaze	Shrooq Pharmaceuticals

Oxcarbazepine 150 mg Tablets in Pakistan
Oxalepsy	S.J. & G. Fazul Ellahie (Pvt) Ltd.
Oxaze	Shrooq Pharmaceuticals
Oxep	Macter International (Pvt) Ltd.
Oxzepin	Nabiqasim Industries (Pvt) Ltd.
Telox	Platinum Pharmaceuticals (Pvt.) Ltd.

Oxcarbazepine 300 mg Tablets in Pakistan
Oxalepsy	S.J. & G. Fazul Ellahie (Pvt) Ltd.
Oxatep	Pakistan Pharmaceutical Products (Pvt) Ltd.
Oxaze	Shrooq Pharmaceuticals
Oxep	Macter International (Pvt) Ltd.
Oxzepin	Nabiqasim Industries (Pvt) Ltd.
Telox	Platinum Pharmaceuticals (Pvt.) Ltd.
Trioptal	Novartis Pharma (Pak) Ltd

Oxcarbazepine 600 mg Tablets in Pakistan
Oxalepsy	S.J. & G. Fazul Ellahie (Pvt) Ltd.
Oxatep	Pakistan Pharmaceutical Products (Pvt) Ltd.
Oxaze	Shrooq Pharmaceuticals
Oxep	Macter International (Pvt) Ltd.
Oxzepin	Nabiqasim Industries (Pvt) Ltd.
Telox	Platinum Pharmaceuticals (Pvt.) Ltd.
Trioptal	Novartis Pharma (Pak) Ltd