Oxcarbazepine

BRAND NAMES

Oxtellar – It contains the active ingredients of oxcarbazepine. It is available in the form of tablets used to treat partial seizures.

Trileptal- It contains the active ingredient of Oxcarbazepine. It is available in the form of capsules and oral suspensions used to treat partial seizures.

MECHANISM OF ACTION

Oxcarbazepine binds to sodium channels and suppresses high-frequency, repeated neuronal activity. It prevents the release of glutamate. The liver metabolizes this medicine, and the kidneys eliminate it. It quickly transforms into licarbazepine, its active metabolite. Licarbazepine is responsible for oxcarbazepine's anti-seizure action. The half-life of oxcarbazepine is 1 to 3.7 hours, but that of licarbazepine is 8 to 10 hours. Oxcarbazepine, unlike carbamazepine, has not been found to produce metabolic auto-induction.

PHARMACOKINETICS

Absorption

Oxcarbazepine is completely absorbed after oral administration. The rate and extent of absorption of carbazepine is not affected by food intake. 

Distribution

The apparent volume of distribution for (S)- and (R)- was determined to be 23.6 L and 31.7 L, respectively. The apparent volume of distribution for oxcarbazepine is 49 L.

Metabolism

This medication gets metabolized by the liver. Oxacarbazepine rapidly coverts to licarbazepine, its active metabolite. Licarbazepine is responsible for the anti-seizure activity of oxcarbazepine.

Excretion

After oral treatment, more than 95% of the administered dosage of oxcarbazepine is detected in urine. Fecal elimination accounted for just 4% of the given dosage.

PHARMACODYNAMICS

Oxcarbazepine is an anticonvulsant medication that lowers the frequency of seizures in people with epilepsy by blocking aberrant brain activity. There have been occasional instances of oxcarbazepine causing hematologic problems such as agranulocytosis and aplastic anemia. It has also been linked to the development of dermatologic responses, which can range from a minor rash to potentially lethal reactions like toxic epidermal necrolysis. 

DOSAGE AND ADMINISTRATION

Oxcarbazepine is available as an oral tablet, an extended-release tablet, and an oral suspension. Every twelve hours, the pill and suspension are typically taken with or without meals. Typically, the extended-release pill is taken once daily, either one hour before or two hours after a meal, on an empty stomach. Take oxcarbazepine daily at around the same time. 

DRUG INTERACTIONS

Drug interactions of Oxcarbazepine may include

• Anti-psychotic – aripiprazole, lurasidone and quetiapine
• Sedative – Zolpidem
• Anti-depressant – duloxetine, escitalopram, pregabalin, fluoxetine, trazodone and sertraline
• Antibiotics – erythromycin
• Pain-killers – hydrocodone and methadone
• Anti-convulsant – lamotrigine and topiramate
• Antacid – esomeprazole
• Anti-anxiety – alprazolam
• Anti-histamine - cetirizine

CONTRAINDICATIONS

Avoid rapid discontinuation of Oxcarbazepine. Prescribers should use caution when prescribing carbamazepine to children, the elderly, pregnant women, and patients with renal impairment. 

SIDE EFFECTS

The common side effects of Oxcarbazepine

• Diarrhea
• Constipation
• Heartburn
• Stomach pain
• Nausea
• Vomiting
• Loss of appetite
• Dry mouth
• Thirst
• Weight gain
• Headache
• Back, arm, or leg pain

OVERDOSE

Symptoms of overdose may include

• Hyperkinesia
• Ataxia
• Vomiting
• Nausea
• Drowsiness

TOXICITY

Oxcarbazepine investigations in rats and dogs over 3 and 6 months revealed reversible dose-dependent liver weight increases, which were attributed to centrilobular megalocytosis. Oxcarbazepine metabolism varies significantly between people and rates, hence its toxicity cannot be applied to human patients.