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Trileptal is an anticonvulsant used to control certain types of seizures. It is also used as a mood stabilizing drug.

Brand: Oxcarbazepine

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: May 2024
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Trileptal 600 mg
180 pills - 600 mg
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$383.79 $2.13 $199.11 Add to cart
120 pills - 600 mg
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$273.53 $2.28 $115.07 Add to cart
90 pills - 600 mg
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$217.75 $2.42 $73.70 Add to cart
60 pills - 600 mg
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$161.91 $2.70 $32.39 Add to cart
30 pills - 600 mg $97.15 $3.24 No Add to cart
Trileptal 300 mg
360 pills - 300 mg
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$461.99 $1.28 $113.41 Add to cart
270 pills - 300 mg
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$349.75 $1.30 $81.80 Add to cart
180 pills - 300 mg
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$239.93 $1.33 $47.77 Add to cart
120 pills - 300 mg
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$162.93 $1.36 $28.87 Add to cart
90 pills - 300 mg
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$127.99 $1.42 $15.86 Add to cart
60 pills - 300 mg $89.95 $1.50 $5.95 Add to cart
30 pills - 300 mg $47.95 $1.60 No Add to cart
Trileptal 150 mg
360 pills - 150 mg
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$251.93 $0.70 $159.07 Add to cart
270 pills - 150 mg
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$195.95 $0.73 $112.30 Add to cart
180 pills - 150 mg
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$136.75 $0.76 $68.75 Add to cart
120 pills - 150 mg $97.93 $0.82 $39.07 Add to cart
90 pills - 150 mg $77.99 $0.87 $24.76 Add to cart
60 pills - 150 mg $55.95 $0.93 $12.55 Add to cart
30 pills - 150 mg $34.25 $1.14 No Add to cart

Product description


Trileptal (Oxcarbazepine)

Pharmacological action

Antiepileptic agent. Pharmacological activity is due primarily to the action of metabolite - oxcarbazepine monohydroxy derivative (MGD). Mechanism of action of oxcarbazepine and its metabolite is associated mainly with blockade of potential-dependent sodium channels, which leads to stabilization of overexcited neuronal membranes, inhibition of serial neuronal discharges and reduction of synaptic impulse conduction.

Increase of potassium ions conductance and modulation of calcium channels activated by high membrane potential contribute to realization of anticonvulsant action. No significant interaction with brain neuromediators or binding to receptors was observed. Oxcarbazepine and its metabolite have been shown in experimental studies to have pronounced anticonvulsant effects.

The effectiveness of oxcarbazepine in epileptic seizures has been demonstrated both in monotherapy and in the use of oxcarbazepine as part of combination therapy in children and adults.

Pharmacokinetics .

After oral administration oxcarbazepine is completely absorbed and largely metabolized to form pharmacologically active metabolite - 10-monohydroxy derivative. After a single administration of oxcarbazepine, depending on the dosage form used, Cmax of metabolite in blood plasma is 24.9-34 μmol/l, average time of its achievement - about 4.5-6 hours. Pharmacokinetic studies have shown that 2% of oxcarbazepine and 70% of MGP are determined in plasma; the remainder is due to secondary metabolites that are rapidly eliminated from the blood plasma.

Binding of the metabolite to plasma proteins, mainly to albumin, is about 40%. In the therapeutic range the degree of binding is independent of the drug concentration in blood serum. Oxcarbazepine and MNP do not bind to α1-acid glycoprotein. Apparent Vd is 49 l. Plasma concentrations of MND are reached on 2-3 days when oxcarbazepine is taken 2 times per day. In equilibrium pharmacokinetic parameters of MND are linear and dose-dependent within a range of daily doses of 300 mg-2400 mg.

Oxcarbazepine is rapidly metabolized by hepatic cytosolic enzymes to pharmacologically active metabolite MND, which undergoes further glucuronization. Small amounts of MND (about 4% of the dose) are oxidized to form an inactive metabolite - 10, 11-dihydroxy derivative (DHD).

Oxcarbazepine is excreted as metabolites mainly by the kidneys (95%), less than 1% is excreted unchanged. About 80% of excreted metabolites are MND, including 49% are glucuronides and 27% are unchanged MND. DHP is excreted unchanged (about 3%), oxcarbazepine conjugates are 13%. About 4% of the dose is excreted with the feces.

Oxcarbazepine is rapidly excreted from the blood plasma, the apparent T1/2 is 1.3 - 2.3 h. The apparent T1/2 of MND averages 9.3±1.8 h.

There is a linear dependence of renal clearance of MND on creatinine clearance. In AC less than 30 ml/min after a single dose of 300 mg of oxcarbazepine T1/2 of MND is increased up to 19 hours, and AUC is doubled.

Weight-adjusted clearance of MND in children decreases with increasing age and body weight, approaching clearance in adults. Weight-adjusted clearance in children aged 1 month to 4 years is 93% higher than in adults. Due to this it is assumed that AUC of MND in children of this age group will be half as much as in adults when using the same doses (when adjusted by body weight). Weight-adjusted clearance in children aged 4 to 12 years is 43% higher than in adults. Estimated AUC of MND in children of this age group is 2/3 of that in adults when using the same doses (when adjusted by body weight). It is supposed that in children aged 13 years and older due to weight gain MND clearance, corrected by body weight, corresponds to MND clearance in adults.

After oxcarbazepine administration in single dose of 300 mg or repeatedly in dose 600 mg/day in healthy volunteers aged 60-82 years old Cmax in plasma and AUC values for MND were 30-60% higher in comparison with the same data in young volunteers (18-32 years old) that was connected with age decreasing of CC.

A number of physiological changes occur in pregnant women that may lead to a gradual decrease in plasma levels of MND during pregnancy.

Contraindications to use

Children under 3 years of age; hypersensitivity to oxcarbazepine.

Administration during pregnancy and lactation

The experience of use in pregnancy is limited. There are reports about possible connection of oxcarbazepine usage during pregnancy with development of congenital defects (for example, wolf's mouth).

In experimental studies, when oxcarbazepine was used in toxic doses, an increase in fetal death, delayed and impaired fetal development and growth were noted. If a patient plans to become pregnant or became pregnant during oxcarbazepine use as well as if the question of oxcarbazepine use during pregnancy arises it is necessary to carefully compare the expected benefits of therapy and the possible risk to the fetus, especially in the first trimester of pregnancy.

Oxcarbazepine should be used in pregnancy at the lowest effective dose.

If there is sufficient clinical efficacy in women of childbearing age, oxcarbazepine should be used as monotherapy.

In pregnancy, effective antiepileptic treatment should not be interrupted, since the progression of the disease may have a negative effect on the mother and the fetus.

Folic acid deficiency is known to develop in pregnancy. Antiepileptic drugs can exacerbate this deficiency, which is one of the possible causes of fetal development disorders, so it is recommended to take additional folic acid preparations.

When using during pregnancy, it should be taken into account that physiological changes occurring in the body of a pregnant woman may lead to a gradual decrease in the concentration of the active metabolite in blood plasma. In order to achieve maximum control of the disease symptoms, it is necessary to regularly assess the clinical effect of oxcarbazepine and determine the plasma concentration of the metabolite. Determination of plasma concentrations of MND is also recommended in the postpartum period, especially if the dose of oxcarbazepine was increased during pregnancy.

There are reports that the use of antiepileptic drugs in pregnancy may lead to increased bleeding in the newborn. As a precautionary measure, vitamin K1 administration in the last few weeks of pregnancy is recommended, as well as in newborns whose mothers have received oxcarbazepine.

Oxcarbazepine and MND penetrate the placental barrier and are excreted with breast milk. The ratio of concentrations in milk to plasma was 0.5 for both substances. Since the effect of oxcarbazepine and MND excreted with mother's milk on neonates is unknown, oxcarbazepine should not be used during breastfeeding.

Special indications

Use with caution in patients with known hypersensitivity to carbamazepine, since this group of patients may develop hypersensitivity reactions to oxcarbazepine in about 25-30% of cases. Patients with no history of hypersensitivity to carbamazepine may also develop hypersensitivity reactions to oxcarbazepine, including multi-organ disorders. In the case of development of immediate hypersensitivity reactions oxcarbazepine should be immediately discontinued and alternative therapy should be prescribed.

Use with caution in patients with severe hepatic dysfunction.

In patients with impaired renal function and having low sodium concentration in serum, or in patients receiving concomitant treatment with drugs that promote sodium excretion from the body (diuretics, drugs that affect ADH secretion), sodium concentration in serum should be determined before starting oxcarbazepine therapy. Thereafter sodium concentration in serum should be controlled in 2 weeks after the therapy start and further monthly during 3 months or as it is necessary. Elderly patients should be treated with particular attention to these risk factors. If it is necessary to prescribe diuretics and other drugs that reduce sodium concentration in serum, patients receiving oxcarbazepine should follow the same recommendations. In case of clinical symptoms, which allow suspecting hyponatremia, sodium concentration in serum should be measured. For other patients sodium concentration in serum may be measured during routine blood tests.

If symptoms of marked suppression of medullary hematopoiesis develop, it is necessary to consider cancelling oxcarbazepine.

Patients receiving anticonvulsants have rarely had episodes of suicidal behavior and thinking. The mechanism of increased risk of suicide in this patient population has not been established. Therefore, close monitoring of patients receiving oxcarbazepine is necessary at all stages of treatment.

It is necessary to monitor body weight in all patients with heart failure for timely determination of fluid retention. In case of fluid retention or during progression of symptoms of heart failure serum sodium concentration should be determined. In case of hyponatremia the amount of fluid intake should be limited. When using oxcarbazepine in very rare cases cardiac conduction disorders are possible, therefore during the treatment it is necessary to monitor closely patients with previous conduction disorders (AV-blockade, arrhythmia).

When using oxcarbazepine, dermatological reactions have been observed in both children and adults, and developed an average of 19 days after the start of treatment. There have been some reports about cases of relapse of skin reactions when resuming oxcarbazepine administration. If skin reactions develop against the background of oxcarbazepine use, it should be considered to cancel it and prescribe another antiepileptic drug.

If hepatitis is suspected, oxcarbazepine should be considered for discontinuation.

As any other antiepileptic drugs, oxcarbazepine should be withdrawn gradually due to the risk of increased frequency of seizures.

Effect on the ability to drive vehicles and mechanisms

Patients who experience dizziness, somnolence or other CNS disorders during oxcarbazepine use should not drive motor transport or work with mechanisms during treatment.

Indications of active ingredients of Trileptal

Simple and complex partial seizures with or without secondary generalization in adults and children aged 1 month and over.

Generalized tonic-clonic epileptic seizures in adults and children 2 years of age and older.

Dosing regimen

The optimal dosing regimen is determined by the doctor. Should strictly follow the compliance of the dosage form used by a particular drug indications for use and the dosing regimen.

It is taken orally.

The initial dose is 8-10 mg/kg body weight/day. Further, the dose is adjusted depending on the treatment regimen, patient's age, treatment efficacy and renal function.

For patients with impaired renal function (CKD less than 30 ml/min) the initial dose and dosing regimen should be adjusted.