What is Oxcarbazepine?
Oxcarbazepine is an active ingredient used for the treatment of epileptic seizures.
The brand names of Oxcarbazepine in the United States are: Trileptal and Oxtellar XR.
Mechanism of Action (MOA) of Oxcarbazepine
Stabilizes hyperexcited neuronal membranes by blocking voltage-dependent sodium channels.
It acts mainly through its metabolite MHD.
Therapeutic Indications, Uses and Benefits of Oxcarbazepine
Partial epileptic seizures with or without secondary generalization with tonic-clonic seizures, in monotherapy or combined, in adults and children ≥ 6 years.
Dosage of Oxcarbazepine
Oral.
Adults:
Monotherapy or combined: initial 600 mg/day in 2 doses; increase, if indicated, at a rate of 600 mg/day max. at weekly intervals; maintenance: 600-2,400 mg/day in 2 doses.
Children ≥ 6 years:
Initial, monotherapy or combined, 8-10 mg/kg/day in 2 doses; increase, if indicated, at a rate of 10 mg/kg/day max. at weekly intervals up to a maximum dose of 46 mg/kg/day in 2 doses.
Maintenance in combined therapy, 30 mg/kg/day in 2 doses.
Renal insufficiency (Clcr < 30 ml/min): initial dose 300 mg/day and minimum weekly increments.
Mode of administration of Oxcarbazepine
It can be taken with or without food.
The tablets are slotted and can be divided into two halves, allowing the patient to swallow the tablet more easily. However, the tablet cannot be divided into equal doses.
Oral suspension: Shake the bottle well and remove the prescribed amount of oral suspension with the included oral syringe, it can be taken directly or it can be mixed in a small glass of water just before administration.
Contraindications of Oxcarbazepine
Hypersensitivity.
Warnings and Precautions with Oxcarbazepine
- Cross hypersensitivity to carbamazepine.
- Risk of serious dermatological reactions.
- In patients with pre-existing renal disorder, concomitant treatment with medications that reduce Na levels, NSAID.
- It has been observed hyponatremia, measure serum Na levels before treatment, after 2 weeks and monthly for 3 months.
- In patients with heart failure and secondary heart failure control the weight in case it is caused by fluid retention.
- Severe liver failure.Kidney failure.
- Stop if there is evidence of bone marrow depression or liver disease.
- Risk of suicidal ideation and behavior.
- Cancels effectiveness of hormonal contraceptives.
- Alcohol consumption.
- Gradually stop treatment.
Liver failure
Caution in severe liver failure due to lack of data. Cases of hepatitis have been reported.
Suspend treatment if liver disease is suspected.
Kidney failure
Caution.
Decrease dose. If Clcr < 30 ml/min, initial dose 300 mg/day, and minimum weekly increments.
Interactions with Oxcarbazepine
- Increases plasma levels of: phenytoin (reduce dose), phenobarbital.
- Plasma levels reduced by: carbamazepine, phenytoin, phenobarbital, valproic acid.
- Cancels effectiveness of: hormonal contraceptives.
- Do not associate with: MAOI.
- Increases neurotoxicity with: lithium.
- Sedative synergistic effect with: alcohol.
Pregnancy and Oxcarbazepine
Insufficient clinical data. In animal studies were observed at levels toxic to the mother, increased embryo-mortality, growth retardation and malformations.
Plasma levels of the active metabolite oxcarbazepine (MHD) may decrease during pregnancy; monitor to ensure seizure control.
Supplement the mother with folic acid, and administer vitamin K1 to the mother (last weeks of pregnancy) and newborn to prevent haematological disorders.
Breastfeeding
In humans, oxcarbazepine and its active metabolite, MHD, are excreted in milk. A milk/plasma concentration ratio of 0.5 was found for both.
The effects on the child exposed to oxcarbazepine by this route are unknown. Thus, oxcarbazepine should not be used during lactation.
Effects on driving ability
Oxcarbazepine acts on the central nervous system and can produce: drowsiness, dizziness, visual alterations and decreased ability to react. These effects, as well as the disease itself, make it advisable to be cautious when driving vehicles or operating dangerous machinery, especially until each patient’s particular sensitivity to the medication has been established.
Adverse reactions and side effects of Oxcarbazepine
Hyponatremia, confusion, depression, apathy, agitation, affective lability, drowsiness, headache, dizziness, ataxia, tremor, nystagmus, altered attention, amnesia, diplopia, blurred vision, visual alterations, vertigo, nausea, vomiting, diarrhea, constipation, abdominal pain, rash, alopecia, acne, fatigue, asthenia.
⭐⭐⭐⭐⭐ VIDEO OF OXCARBAZEPINE/TRILEPTAL (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: VZI5B1W380
ChemIDplus
DrugPortal
PubChem CID: 34312
NCI Thesaurus: C47643