Compound
1 tablet of oxcarbazepine 150 mg, 300 mg or 600 mg.
Silicon dioxide, crospovidone, hypromellose, magnesium stearate, MCC - as excipients.
1 ml of oxcarbazepine 60 mg. Sodium saccharinate, sorbic acid, propyl parahydroxybenzoate, macrogol stearate, sorbitol , methyl parahydroxybenzoate, ascorbic acid, propylene glycol, cellulose, plum-lemon flavor, purified water - as excipients.
Pharmacodynamics and pharmacokinetics
Pharmacodynamics
The mechanism of antiepileptic action is associated with the blockade of sodium channels, which respond to changes in membrane potential. This entails the stabilization of overexcited neurons, a decrease in the conduction of impulses in synapses and the suppression of serial discharges. In the antiepileptic effect of the drug, an increase in K+ conductivity and modulation of calcium channels, which are activated by high neuronal membrane potential, are also important. There are no interactions of the active substance with brain neurotransmitters.
Effective against epileptic seizures in monotherapy and combination therapy in adults and children. In addition, Trileptal has a normothimic effect - it eliminates circular mental disorders (mood fluctuations) and prevents the development of depression.
Pharmacokinetics
When taken orally it is well absorbed. Food intake does not affect the degree of absorption. Metabolized to form the active metabolite MHP (monohydroxy derivative). 40% of MGP is bound to blood proteins. After taking a suspension at a dose of 600 mg, Cmax MGP is achieved after 6 hours, and when taking the same dose in tablet form - after 4.5 hours. In the form of metabolites, 95% is excreted by the kidneys, 4% with feces.
Analogs
Trileptal analogues are presented on the pharmacological market, which are similar to it in composition or in therapeutic direction. The choice of analogue should be made by the attending physician. Popular analogues of the drug:
Finlepsin is a drug similar to tricyclic antidepressants. By blocking sodium channels, it reduces the paroxysmal activity of the sodium ion pacemaker. In addition to its antiepileptic effects, the medication has antipsychotic properties and is an antidepressant that improves mood and produces an analgesic effect.- Konvulex is a highly effective antiepileptic drug that is used for all types of epilepsy of various etiologies. The drug blocks GABA and reduces the excitability of brain cells (neurons). For children, the medicine is prescribed in syrup. Intravenous administration is used only for rapid relief of epistatus.
- Topamax is a latest generation anticonvulsant drug and has a neuroprotective effect on brain cells. The medication belongs to the pharmacological group of sulfate-substituted monosaccharides. The medication is used in the treatment of partial tonic-clonic seizures, as well as Lennox-Gastaut syndrome and for preventive purposes for migraines.
Side effects of Trileptal
Side effects that occur very often (more than 10%): dizziness , drowsiness, diplopia , headache, nausea, vomiting .
Commonly encountered (up to 10%): asthenia , fatigue, amnesia , apathy , impaired concentration , depression , emotional instability, nystagmus , blurred vision, tremor , , abdominal pain , diarrhea , hyponatremia , acne , alopecia , rash .
Rarely observed: leukopenia , increased transaminase activity , urticaria , angioedema .
Features of using the drug in old age
Dose adjustment of Trileptal may also be required for patients over 65 years of age. At this age, kidney function is often impaired. Therefore, when taking Trileptal, a sharp decrease in sodium in the blood is possible. Such patients require strict medical supervision with regular monitoring of sodium levels. Therefore, combination therapy is rarely used to avoid overdose and side effects. But in general, Trileptal is well tolerated and, when used correctly, significantly improves the patient’s condition at any age. In addition to relieving seizures, it can reduce headaches resulting from vascular spasms, prevent blood clotting, improve performance, relieve stress and increase the efficiency of mental activity.
Instructions for use of Trileptal (Method and dosage)
Inside, regardless of the time of food.
For monotherapy, adults are prescribed 600 mg/day in 2 divided doses. The therapeutic effect is usually observed at doses of 600–2400 mg, so the dose is gradually increased once a week to no more than 600 mg. In a hospital setting, the dose is increased more quickly. At these dosages, it is more advisable to take Trileptal 600 mg tablets.
In combination therapy, the drug is prescribed at 600 mg per day in 2 divided doses. According to indications, the dose is increased by 600 mg/day per week. Use in combination therapy at a dose of 2400 mg without reducing the dose of another drug is accompanied by poor tolerability. The use of the drug at a dose higher than 2400 mg has not been studied.
The initial dose for children over 2 years of age is 8–10 mg/kg body weight in 2 divided doses (with combination therapy and monotherapy). The therapeutic effect is most often observed at a dosage of 30 mg/kg per day, so the dose is increased by 10 mg/kg per day once a week to 46 mg/kg body weight.
The drug in the form of a suspension is used in children from 1 month. Before taking the suspension, the bottle must be shaken well and the required amount of the drug must be measured. The dose in ml is drawn from the bottle using a syringe. The package includes a 10 ml syringe for adults and a 1 ml syringe for small children. The suspension is taken directly from the syringe or diluted with water. An opened bottle can be stored for up to 7 weeks. Suspension and tablets are interchangeable, therefore the instructions for use of Trileptal contain a table for converting the dose from mg to ml.
special instructions
Before starting to use the medicine, it is important to pay attention to several special instructions:
- The medicine is prescribed only by a doctor if there are appropriate medical indications.
- The dosage is titrated by a doctor, and a conclusion about the achievement of the required therapeutic effect is made on the basis of certain neurological criteria.
- The appearance of the first signs of the development of undesirable reactions is a reason to stop taking the medication and consult a doctor for advice.
- Alcohol intake is avoided during drug therapy, as the sedative effect is significantly enhanced.
- After taking the medication, it is not recommended to perform potentially dangerous work that requires sufficient speed of psychomotor reactions and concentration.
Interaction
It should be borne in mind that the active substance is an inhibitor of cytochrome CYP2C19, therefore the administration of large doses of this drug and Phenobarbital , Phenytoin leads to interaction.
The concentration of Phenytoin increases by 40% when Trileptal is co-administered above 1200 mg/day, and therefore the dose of Phenytoin can be reduced. The drug increases the concentration of Phenobarbital, at the same time Phenobarbital reduces its concentration by 30-31%.
Felbamate and Clobazam do not affect the concentration of this drug.
Valproic acid reduces concentration by 18%.
Prescription along with hormonal contraceptives leads to a decrease in the effectiveness of contraceptives.
Strengthens the sedative effect of ethanol .
Cimetidine , Erythromycin , Warfarin , Dextropropoxyphene do not affect MGP parameters.
Verapamil reduces the concentration of active metabolites by 20%.
For whom the drug is contraindicated
This remedy is prescribed to children from 1 month. But up to 3 years, only Trileptal suspension is used. The instructions note good tolerability and high efficiency in cases where other drugs did not help. But not all patients with epilepsy can take Trileptal. This treatment is contraindicated during pregnancy and breastfeeding. Oxcarbazepine has already been shown to cause severe malformations in infants in this setting.
People with severely impaired liver and kidney function should take Trileptal with caution. The drug is also not prescribed to patients with individual intolerance to this substance. Therefore, if allergic reactions occur, you must stop taking Trileptal. In this case, a doctor should help you choose its analogues.
Reviews about Trileptal
Reviews of Trileptal on forums indicate the effectiveness of this drug both in focal epileptic seizures and in generalized tonic-clonic ones . Many patients have successfully replaced Carbamazepine , Gabapentin , Phenytoin or Valproate with Trileptal alone on the recommendation of a physician.
Its effectiveness was no lower, and tolerability was much better, which made it possible to take this drug for a long time without complications. Thus, it is noted that within 12 months. treatment with this drug alone, a complete disappearance of seizures was observed in patients with a generalized form of epilepsy . All those who have taken the drug note that it, compared to Finlepsin and Carbamazepine , has fewer side effects.
“I finally switched from Finlepsin to Trileptal, after taking it the headache does not hurt, and the night attacks have passed. Among the side effects, I can complain about drowsiness.”
“Very good drug. I switched to Trileptal 300 and everything changed - minimal drowsiness, appetite as usual. Only positive reviews."
“I take 1800 mg (3 times 600), transferred a year ago. Compared to Finlepsin, I feel very cheerful, I walked around like a somnambulist on Finlepsin.”
“My daughter has been taking Trileptal for six years, she has no seizures, before that she took Finlepsin and had seizures at night.”
The most common adverse reactions are drowsiness, increased appetite, tearfulness, dizziness and double vision 40 minutes after taking the tablet.
Pharmacological group
The main active compound of the drug has an anticonvulsant effect, so it is classified as an antiepileptic drug. The implementation of the therapeutic effect occurs due to the blockade of potential-dependent sodium channels of cells of the nervous system (neurocytes), which is carried out by oxcarbazepine and its active metabolite. Blockade of the channels leads to stabilization of overexcited cell membranes of neurocytes with subsequent suppression of the formation of serial neuronal discharges, which are the pathophysiological basis for the development of skeletal muscle spasms in epilepsy.
The antiepileptic therapeutic effects of the drug are sufficiently pronounced during monotherapy or in combination with other anticonvulsants. It is allowed to replace Trileptal with other drugs if their therapeutic effectiveness is insufficient.
After taking a tablet or suspension orally, oxcarbazepine is quickly and almost completely absorbed into the blood. It penetrates the blood-brain barrier into the brain structures, where it has a therapeutic effect. The active compound is metabolized in the liver, the breakdown products are excreted primarily in the urine.
Trileptal price, where to buy
You can buy it in many pharmacies in Moscow. The price of Trileptal depends on the dose. Tablets of 150 mg No. 50 can be purchased for 402–515 rubles, and tablets of 600 mg No. 50 for 1444–1638 rubles.
- Online pharmacies in RussiaRussia
ZdravCity
- Trileptal tablets p.p.o.
600 mg 50 pcs Novartis Pharma S.р.A RUB 1,372 order - Trileptal Susp. internal 60mg/ml 100ml n1Novartis Pharma/Delpharm Young
RUB 419 order
Possible drug overdose
Trileptal is considered safe in recommended therapeutic doses. Reviews note that cases of overdose are very rare. To do this, you need to take a lot of pills at once. But a total overdose of antiepileptic drugs is possible with complex therapy and taking Trileptal in the maximum possible dose. What could happen?
- The water-electrolyte balance is disturbed, which is expressed in a lack of sodium salts.
- The organ of vision suffers: double vision, blurred vision, and nystagmus are observed.
- The functioning of the digestive system is disrupted, the patient feels nausea, and may vomit.
- Often there is weakness, fatigue, sleep disturbances, dizziness, and decreased blood pressure.
- Possible confusion, loss of coordination of movement, appearance of aggressiveness and irritability.
- In the most severe cases, there is disruption of the respiratory system, convulsions, loss of consciousness and even coma.
If an overdose of the drug occurs, it is necessary to perform gastric lavage. Adsorbents, for example, activated carbon, are also prescribed. To prevent this, it is necessary to study the instructions before using the drug "Trileptal".
