TRILEPTAL film-coated tablets 600 mg No. 50

Trileptal®

Trileptal® can be used both as monotherapy and in combination with other antiepileptic drugs. In both cases, the course of treatment begins with a clinically effective dose, the frequency of administration is 2 times a day. The dose may be increased depending on the response to therapy. When replacing another antiepileptic drug with Trileptal, at the beginning of taking Trileptal, the dose of the drug being replaced should be gradually reduced. When using Trileptal as adjunctive therapy as part of polytherapy, a dose reduction of concomitant antiepileptic drugs and/or a slower increase in the dose of Trileptal may be required.

Trileptal can be taken regardless of meals (during, after meals or between meals).

The recommendations below apply to patients with normal renal function. For this category of patients, there is no need to monitor plasma concentrations of the active substance in order to optimize Trileptal therapy.

The tablets are marked and can be broken into two pieces to make them easier to swallow.

When used in children under 3 years of age

who cannot swallow tablets, as well as in cases where it is impossible to measure the required dose when using the drug in tablet form, Trileptal® is prescribed in the form of an oral suspension.

Adults and elderly patients

Monotherapy:

The initial dose is 600 mg/day (8-10 mg/kg body weight/day), divided into 2 doses. A good therapeutic response was observed in the dose range of 600-2400 mg/day. If necessary, a gradual increase in dose is possible. The dose is increased by no more than 600 mg/day at intervals of approximately 1 week until the desired therapeutic response is achieved. In hospital settings, there is experience with rapidly increasing the dose to 2400 mg/day over 48 hours.

Combination therapy:

The initial dose is 600 mg/day (8-10 mg/kg body weight/day), divided into 2 doses. A good therapeutic response was observed in the dose range of 600-2400 mg/day. If necessary, a gradual increase in dose is possible. The dose is increased by no more than 600 mg/day at intervals of approximately 1 week until the desired therapeutic response is achieved.

Use of the drug Trileptal® in a daily dose above 2400 mg. There is limited experience with the use of the drug in daily doses of up to 4200 mg.

No special adjustment of the dosage regimen is required for elderly patients, since the therapeutic dose of the drug is set individually.

Special dosage adjustments for elderly patients

is not required, since the therapeutic dose of the drug is determined individually.

Children

In monotherapy and when using the drug as part of combination therapy:

The recommended initial dose is 8-10 mg/kg body weight/day, divided into 2 doses.

If necessary, a gradual increase in dose is possible to achieve the desired therapeutic effect. At intervals of approximately 1 week, the dose is increased by a maximum of 10 mg/kg/day, to a maximum daily dose of 60 mg/kg.

When using the drug Trileptal® as monotherapy and as part of combination therapy, when adjusted for body weight, the apparent clearance in children decreases significantly with increasing age. Children aged 1 month to 4 years

a dose of the drug 2 times higher than the dose for adults may be required when adjusted for body weight;
Children aged 4 to 12 years
may require a dose 50% higher than the adult dose when adjusted for body weight.

In children aged 1 month to 4 years, the effect of antiepileptic drugs - inducers of liver enzymes on their apparent clearance is more pronounced than in children of older age groups (when adjusted for body weight). When using the drug Trileptal® in children aged 1 month to 4 years in combination with antiepileptic drugs - inducers of liver enzymes, a dose of oxcarbazepine may be required 60% higher (when adjusted for body weight) than with monotherapy with the drug Trileptal® or when using it in combination with antiepileptic drugs that do not induce enzymes. For children of older age groups, when conducting combination therapy with Trileptal® with liver enzyme inducers, a slight increase in the dose of the drug may be required compared to monotherapy.

In children under 3 years of age

the drug should be used in the form of an oral suspension due to the difficulties of using solid dosage forms in this age group.

No dosage adjustment is required in patients with mild to moderate liver dysfunction

.

For patients with impaired renal function (creatinine clearance less than 30 ml/min)

The recommended starting dose is 300 mg/day and should be increased slowly until the desired therapeutic response is achieved.

Instructions for use of oral suspension

Trileptal dose conversion table from mg to ml.

Before taking the oral suspension, the bottle should be shaken thoroughly and the required amount of suspension should be immediately measured. The required dose (ml) is drawn from the bottle using the supplied syringe. When using a 10 ml syringe (supplied with a 250 ml bottle - for adults and older children), the amount of suspension should be rounded to 0.5 ml. When using a 1 ml syringe (supplied with a 100 ml bottle - for young children), the amount of suspension should be rounded to 0.1 ml. After each use, close the bottle tightly and wipe the syringe with a clean, dry cloth. The suspension can be taken directly from the syringe or diluted with a small amount of water before use. Store an open bottle for no more than 7 weeks.

Oral suspension and film-coated tablets are interchangeable in equivalent doses.

TRILEPTAL film-coated tablets 600 mg No. 50

There are reports of a risk of worsening the course of epileptic seizures when using the drug Trileptal®. An increased risk of worsening seizures has been observed, mainly in children, but can also occur in adults. If, while using the drug Trileptal®, there is a worsening of the course of epileptic seizures, the use of the drug should be discontinued. Hypersensitivity reactions When using the drug Trileptal® in clinical practice, in isolated cases (post-marketing reports), the development of immediate type hypersensitivity reactions (type I), including rash, itching, urticaria, angioedema and anaphylactic reactions, was observed. Hypersensitivity reactions can cause the development of disorders of the skin, liver, blood and lymphatic system and other organs, both individually and as part of a systemic reaction. Angioedema and anaphylactic reactions affecting the larynx, vocal folds (glottis area), tongue, lips, and eyelids developed both during the first and repeated doses of the drug Trileptal®. If immediate hypersensitivity develops, Trileptal® should be discontinued immediately and alternative therapy should be prescribed. The drug should be used with caution in patients with known hypersensitivity to carbamazepine, because in this group of patients, in approximately 25-30% of cases, hypersensitivity reactions to oxcarbazepine may develop. In patients who do not have a history of hypersensitivity to carbamazepine, it is also possible to develop hypersensitivity reactions to the drug, including multiple organ disorders. If signs and symptoms of hypersensitivity reactions occur, Trileptal® should be discontinued immediately. Hyponatremia Hyponatremia (serum sodium less than 125 mmol/l) was observed in 2.7% of patients receiving Trileptal®, which was usually not accompanied by clinical manifestations and did not require adjustment of therapy. The sodium content is normalized upon discontinuation (dose reduction) of the drug Trileptal® or conservative treatment (restriction of fluid intake). In patients with a history of impaired renal function and low serum sodium levels (for example, in patients with syndrome of inappropriate antidiuretic hormone secretion), or in patients receiving concomitant treatment with drugs that promote sodium excretion from the body (diuretics, drugs that affect secretion of antidiuretic hormone), before starting therapy with Trileptal®, the sodium content in the blood serum should be determined. In the future, serum sodium levels should be monitored 2 weeks after the start of therapy and then monthly for 3 months or as needed. Particular attention should be paid to these risk factors in elderly patients. If it is necessary to use diuretics and other drugs that reduce serum sodium levels in patients receiving therapy with Trileptal®, the same recommendations should be followed. If clinical symptoms of hyponatremia appear, the sodium content in the blood serum should be determined. For other patients, serum sodium levels can be determined during routine blood tests. It is necessary to monitor body weight in all patients with heart failure to promptly diagnose fluid retention. If fluid retention occurs or as symptoms of heart failure progress, serum sodium levels should be determined. If hyponatremia occurs, the amount of fluid consumed should be limited. Because When using oxcarbazepine, cardiac conduction disturbances may occur in very rare cases; careful monitoring of patients with previous conduction disturbances (atrioventricular block, arrhythmia) receiving Trileptal® is necessary. Hematological changes According to post-marketing reports, when treated with Trileptal®, patients in very rare cases experienced the development of agranulocytosis, aplastic anemia and pancytopenia. Given the low incidence of agranulocytosis, aplastic anemia and pancytopenia, as well as associated factors (for example, concomitant use of other medications, the presence of concomitant diseases), a cause-and-effect relationship between the development of these adverse events and the use of the drug cannot be established. If symptoms of severe suppression of bone marrow hematopoiesis develop, it is necessary to consider discontinuing the drug. Suicidal thoughts and behavior Episodes of suicidal behavior and suicidal ideation have been reported in patients receiving anticonvulsants. The results of a meta-analysis of randomized placebo-controlled trials showed a small increase in the risk of developing suicidal behavior in patients receiving anticonvulsants. The mechanism for increasing the risk of suicide in this category of patients has not been established. Therefore, at all stages of treatment, careful monitoring of patients receiving treatment with the drug is necessary. Patients and medical personnel should be warned about the risk of suicidal thoughts and episodes in patients receiving therapy with Trileptal®. Dermatological reactions When using the drug Trileptal®, the development of serious dermatological reactions, such as Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), exudative erythema multiforme, has been very rarely reported. Patients with the above dermatological reactions may require hospitalization due to the development of life-threatening conditions; very rarely lethal outcomes are possible. When using the drug Trileptal®, dermatological reactions were observed in both children and adults, and developed on average 19 days after starting the drug. There are isolated reports of cases of recurrence of serious skin reactions when taking Trileptal® is resumed. If skin reactions develop while using the drug Trileptal®, you should consider discontinuing the drug and using another antiepileptic drug. Correlation with HLA-B*1502 There is considerable evidence to support the role of human leukocyte antigen (HLA) alleles in the development of serious skin reactions in patients with a predisposition to such conditions. Due to the similarity in the chemical structure of oxcarbamazepine and carbamazepine, there is a possibility of developing Stevens-Johnson syndrome and Lyell's syndrome in patients with the HLA-B*1502 allele in the genome taking oxcarbazepine. In patients of Chinese and Thai nationality, there was a clear connection between the development of Stevens-Johnson syndrome and Lyell's syndrome when using carbamazepine and the presence of the human leukocyte antigen HLA-B*1502 allele in their genome. The frequency of occurrence of this allele in patients of Chinese nationality is 2-12%, in Thai patients - about 8%, among some groups of the Malaysian population - more than 15%. The prevalence of the HLA-B*1502 allele in Korea and India is 2% and 6%, respectively. The prevalence of this allele in Caucasians, Blacks, Hispanics, Indians and Japanese is negligible ( Allele frequencies represent the percentage of chromosomes in certain populations that carry the allele. This means that the percentage of patients carrying a copy of the allele in at least one of the of their two chromosomes is almost twice the allele frequency. Thus, the percentage of patients who may be at risk is almost twice the allele frequency. When using the drug Trileptal® in possible carriers of the HLA-B*1502 allele, it is recommended to carry out genotyping according to this allele. The drug should be used in carriers of this allele only if the expected benefit from therapy outweighs the possible risk. The presence of this allele in people of Chinese nationality taking other antiepileptic drugs increases the risk of developing severe dermatological reactions. In patients with the HLA- allele B*1502 It is necessary to avoid the use of drugs leading to the development of Stevens-Johnson syndrome or Lyell's syndrome, with possible replacement with alternative drugs. Genotyping for the HLA-B*1502 allele before using Trileptal® is not necessary in patients belonging to populations with a low frequency of occurrence of this allele, as well as in patients already receiving therapy with this drug, since severe skin reactions were observed in most cases in the first months of treatment (regardless of the presence of HLA-B*1502). Correlation with HLA-B*3101 The presence of the HLA-A*3101 allele may be a risk factor for the development of severe skin lesions (Stevens-Johnson syndrome, Lyell's syndrome, drug rash with eosinophilia and systemic manifestations, acute generalized exanthematous pustulosis and macular nodular rash) in use of carbamazepine. The frequency of occurrence of the HLA-A*3101 allele of the human leukocyte antigen (HLA) gene may differ among different ethnic groups: about 2-5% in the European population, about 10% in the Japanese, about 6.7% in the Western European population, depending on geographical region. The allele frequency is less than 5% in the populations of Australia, Asia, Africa and North America, with exceptions ranging from 5% to 12%. A frequency of more than 15% has been found in some ethnic groups of South America (Argentina and Brazil), indigenous people of North America (Navajo and Sioux tribes, in Mexico - Sanora Seri), South India (Tamil Nadu), and 10-15% among other indigenous people these regions. These allele frequencies represent the percentage of chromosomes in specific populations that carry the allele. This means that the percentage of patients carrying a copy of the allele on at least one of their two chromosomes is almost twice the frequency of the allele. Thus, the percentage of patients who may be at risk is almost twice the allele frequency. There is no sufficient basis to recommend genotyping for this allele in patients before starting oxcarbazepine therapy. For patients already receiving therapy with Trileptal®, genotyping for this allele is not recommended, since skin reactions in most cases were observed in the first months of drug use (regardless of the presence of HLA-A*3101). However, the results of genotyping should not affect the degree of control of the patient's condition and the doctor's alertness regarding severe skin reactions. The development of severe skin lesions is possible in patients negative for these alleles. Also, in many cases, in patients positive for the HLA-B*1502 or HLA-A*3101 alleles, the development of severe skin syndromes was not observed when using the drug Trilertal®. When genotyping for the HLA-B*1502 allele, preference should be given to methods with high resolution. The test is considered positive if at least one of the alleles is detected, negative if no allele is detected. The same recommendations should be followed when genotyping for the HLA-A*3101 allele. The influence of other factors, such as the dose of anticonvulsants, patient compliance, concomitant therapy with other drugs, concomitant diseases, or the level of control of dermatological reactions, on the incidence and prevalence of severe skin reactions has not been established. Impaired liver function There are reports of very rare cases of hepatitis, which in most cases resolved safely. If hepatitis is suspected, discontinuation of the drug should be considered. Hypothyroidism Hypothyroidism is an extremely rare adverse event with oxcabazepine. Considering the influence of thyroid hormones on the development of children, in this category of patients, especially under the age of two, it is recommended to determine the concentration of thyroid hormones before starting drug therapy, and also to monitor this indicator during the use of the drug Trileptal®. Concomitant use of oral contraceptives Women of childbearing age taking oral contraceptives concomitantly with Trileptal should be warned about the possible decrease in the effectiveness of oral contraceptives. For this category of patients receiving Trileptal®, additional use of non-hormonal methods of contraception is recommended. Withdrawal syndrome As with other antiepileptic drugs, abrupt cessation of therapy with Trilertal should be avoided due to the risk of an increase in the frequency of convulsive seizures. Persons taking alcohol during therapy with Trileptal® should be warned of a possible increase in sedative effect. The drug Trileptal® in the form of an oral suspension contains ethanol in an amount of less than 100 mg per dose. The suspension also contains parabens, which may cause allergic reactions (possibly delayed). The oral suspension contains sorbitol, therefore Trileptal® in suspension form should not be used in patients with hereditary impaired fructose tolerance. Impact on the performance of potentially hazardous activities that require special attention and quick reactions Due to the possibility of development of such adverse effects as dizziness, drowsiness, ataxia, diplopia, blurred vision, visual impairment, hyponatremia, and depression of consciousness or other disorders of the central nervous system, especially at the beginning of treatment or during dose selection, patients should be careful when driving or operating machinery while using the drug. If the described adverse events occur, you should refrain from performing these activities.

Trileptal tablet film 150 mg pack contact cell/pack card x50

Trade name: Trileptal International name: Oxcarbazepine Pharmacological group: antiepileptic drug Pharmacological group according to ATC: N03AF02. Oxcarbazepine Pharmacological action: analgesic, antiepileptic, tranquilizing Pharmacodynamics: Antiepileptic drug, the exact mechanism of action and its active metabolite 10-monohydroxy derivative (MHD) is unknown. Oxcarbazepine and MGP block voltage-dependent Na+ channels, which leads to stabilization of the membranes of overexcited neurons, inhibition of the occurrence of serial neuronal discharges and a decrease in synaptic conduction of impulses. Increased K+ conductance and modulation of Ca2+ channels activated by high membrane potential are also involved in the antiepileptic effect of the drug. Pharmacokinetics: Completely absorbed after oral administration. Rapidly metabolized to form a pharmacologically active metabolite - MGP. Food intake does not affect the speed and completeness of absorption. Communication with MHD proteins is 40% (mainly with albumin). In the therapeutic dose range, the degree of binding does not depend on the concentration of the drug in the blood serum. Oxcarbazepine and MGP do not bind to alpha1-acid glycoprotein. The distribution volume of MGP is 49 liters. Cmax of the active metabolite is 34 µmol/l, TCmax is 4.5 hours (3-13 hours) after a single dose of 600 mg. Only 2% of oxcarbazepine, 70% of MGP are determined in the blood plasma, and the rest are secondary metabolites that are quickly eliminated from the blood plasma. Css MGP in blood plasma is achieved within 2-3 days when taking oxcarbazepine 2 times a day. The pharmacokinetic parameters of the steady state are linear and dose-dependent in the range of daily doses of 300-2400 mg. Oxcarbazepine is rapidly metabolized by cytosolic liver enzymes to the pharmacologically active metabolite MGP, which undergoes further glucuronidation. About 4% of the dose is hydroxylated to form an inactive metabolite, the 10,11-dihydroxy derivative (DHP). T1/2 - 1.3-2.3 hours. T1/2 MGP - 9.3±1.8 hours. Excreted mainly by the kidneys (95%) in the form of metabolites, 1% is excreted unchanged. About 80% of excreted metabolites are MGP, of which 49% are glucuronides and 27% are unchanged MGP. DHP is excreted unchanged (about 3%), oxcarbazepine conjugates account for 13%. About 4% of the dose is excreted through the intestines. Mild and moderate liver failure does not affect the pharmacokinetic parameters of oxcarbazepine and MHD. Pharmacokinetics in severe hepatic impairment have not been studied. There is a linear relationship between the renal clearance of MHD and CC. When CC is less than 30 ml/min after a single dose of 300 mg of oxcarbazepine, T1/2 MLP increases to 19 hours, AUC - 2 times. Following a single dose of 5 to 15 mg/kg body weight, dose-adjusted AUC for MHD is 30% lower in children 2 to 5 years of age compared to children 6 to 12 years of age. In children with normal renal function, the renal clearance of MHD is higher than in adults, and T1/2 decreases by 10-50% (up to 5-9 hours) compared to adults. After taking a single (300 mg) or multiple (600 mg/day) dose in patients aged 60-82 years, Cmax and AUC for MHD are 30-60% higher, which is associated with an age-related decrease in CC. There were no differences in pharmacokinetic parameters depending on gender in childhood, adulthood or the elderly. Indications for use: Monotherapy (as a drug of first choice), as well as as part of combination therapy: simple and complex partial epileptic seizures (with or without loss of consciousness), incl. with secondary generalization, generalized tonic-clonic epileptic seizures. Contraindications: Hypersensitivity, lactation period. Dosage regimen: Orally, regardless of food intake, with a small amount of liquid. The suspension can be taken undiluted directly from the syringe or diluted with a small amount of water. In the case of monotherapy or in combination with other antiepileptic drugs, the course of treatment begins with a clinically effective dose, divided into 2 doses. The dose may be increased depending on the response to therapy. When replacing another antiepileptic drug with oxcarbazepine, at the beginning of taking oxcarbazepine, the dose of the drug being replaced should be gradually reduced. When using oxcarbazepine as an additional therapy in combination therapy, a dose reduction of concomitant antiepileptic drugs and/or a slower increase in the dose of oxcarbazepine may be required.

Monotherapy: initial dose for adults - 600 mg/day (8-10 mg/kg/day), divided into 2 doses. An adequate therapeutic response is observed in the dose range of 600-2400 mg per day. The dose may be gradually increased at weekly intervals by no more than 600 mg/day until the desired therapeutic response is achieved. In hospital settings, a rapid dose increase to 2400 mg per day over 48 hours is possible.

As part of combination therapy: initial dose for adults - 600 mg per day (8-10 mg/kg body weight per day), divided into 2 doses. An adequate therapeutic response is observed in the dose range of 600-2400 mg per day. If clinically indicated, the dose may be gradually increased by no more than 600 mg/day at weekly intervals until the desired therapeutic response is achieved. There is limited experience with daily doses up to 4200 mg. The recommended initial dose for children over 2 years of age is 8-10 mg/kg body weight per day, divided into 2 doses, both as monotherapy and as part of combination therapy. In combination with other antiepileptic drugs, an adequate therapeutic effect is observed at a maintenance dose of 30 mg/kg body weight per day. To achieve the desired therapeutic response, it is possible to gradually increase the dose by 10 mg/kg/day per week up to a maximum daily dose of 46 mg/kg body weight. No dosage adjustment is required in patients with mild to moderate hepatic impairment. For renal failure (creatinine clearance less than 30 ml/min), the recommended initial dose is 300 mg/day, which is slowly increased until the desired therapeutic response is achieved. Side effects: Very often - more than 10%, often - 1-10%, sometimes - 0.1-1%, rarely - 0.01-0.1%, very rarely - less than 0.01%. Most often: in adults - drowsiness, headache, dizziness, diplopia, nausea, vomiting, fatigue (more than 10%), in children (from 1 month to 4 years) - drowsiness (11%), often - ataxia, irritability, vomiting, lethargy, fatigue, nystagmus, tremor, decreased appetite, hyperuricemia. From the nervous system: very often - dizziness, headache, drowsiness, often - asthenia, increased fatigue, agitation, amnesia, agitation, apathy, ataxia, impaired concentration, disorientation, depression, emotional lability, nystagmus, tremor. From the cardiovascular system: very rarely - arrhythmia, AV block. From the digestive system: very often - nausea, vomiting, often - constipation, abdominal pain, diarrhea, sometimes - increased activity of liver transaminases and/or alkaline phosphatase, very rarely - pancreatitis and/or increased activity of lipase and/or amylase. From the hematopoietic organs: sometimes - leukopenia, very rarely - thrombocytopenia, suppression of bone marrow hematopoiesis, agranulocytosis, aplastic anemia, neutropenia, pancytopenia. From the side of water and electrolyte metabolism: often - asymptomatic hyponatremia, very rarely - clinically manifested hyponatremia (convulsions, confusion, encephalopathy, blurred vision, nausea, vomiting). From the skin: often - acne, alopecia, rash, sometimes - urticaria, very rarely - erythema multiforme (including Stevens-Johnson syndrome), Lyell's syndrome, SLE. From the senses: very often - diplopia, often - blurred vision, dizziness. Allergic reactions: very rarely - multiple organ disorders, incl. with fever and rash: damage to the circulatory and lymphatic systems (eosinophilia, thrombocytopenia, lymphadenopathy, splenomegaly), muscles and joints (myalgia, swelling in the joints, arthralgia), nervous system (encephalopathy), kidneys (proteinuria, interstitial nephritis, renal failure) , lungs (shortness of breath, pulmonary edema, bronchospasm, interstitial inflammation), changes in the activity of liver enzymes, angioedema. Other: very rarely - clinically significant hyponatremia (Na+ - more than 125 mmol/l), usually during the first 3 months of therapy (in some patients - more than 1 year).

Overdose Symptoms: drowsiness, dizziness, nausea, vomiting, hypokinesia, hyponatremia, ataxia, nystagmus. Treatment: symptomatic and supportive. Gastric lavage and taking activated charcoal to reduce absorption (if you have recently taken the drug). There is no specific antidote. Interaction: Oxcarbazepine and MGP are inhibitors of cytochrome CYP2C19. The simultaneous administration of high doses of oxcarbazepine and drugs metabolized by CYP2C19 (phenobarbital, phenytoin) may lead to interaction. Some patients may require a dose reduction of drugs that are CYP2C19 substrates. Oxcarbazepine and MGP have little or no interaction with CYP1A2, CYP2A6, CYP2C9, CYP2D9, CYP2E1, CYP4A4 and CYP4C11. Oxcarbazepine and MGP are inducers of cytochromes CYP3A4 and CYP3A5, which are involved in the metabolism of dihydropyridine derivatives of BMCC, oral contraceptives and antiepileptic drugs (including carbamazepine). Co-administration of oxcarbazepine and CYP3A4 and CYP3A5 substrates may reduce the concentration of the latter in the blood plasma. In vitro, MGP is a weak inducer of UDP-glucuronyltransferase and, therefore, is unlikely to influence the metabolism of drugs excreted in the form of conjugates (including valproic acid and lamotrigine) in vivo; however, an increase in the doses of concomitantly used drugs may be required. metabolized by the CYP3A4 or UDP-glucuronyltransferase system. If it is necessary to discontinue oxcarbazepine, the doses of these drugs should be adequately reduced. In vivo, the concentration of phenytoin in blood plasma increases up to 40% when oxcarbazepine is administered at a dose of 1200 mg/day or higher, so a reduction in the dose of phenytoin may be required. At the same time, phenytoin can reduce the concentration of oxcarbazepine by 29-35%. Oxcarbazepine increases phenobarbital concentrations by 15% when administered concomitantly. In turn, phenobarbital can reduce the concentration of oxcarbazepine by 30-31%. Oxcarbazepine can reduce carbamazepine concentrations by 22%, while carbamazepine can reduce oxcarbazepine concentrations by 40%. Clobazam and felbamate do not affect oxcarbazepine concentrations. The effect of oxcarbazepine on the concentrations of these drugs has not been studied. Valproic acid can reduce oxcarbazepine concentrations by 18%. The simultaneous administration of powerful P450 inducers (including carbamazepine, phenytoin and phenobarbital) reduces the concentration of MHD in the blood plasma (by 29-40%). No autoinduction phenomena were detected. Reduces the AUC of ethinyl estradiol and levonorgestrel by 48-52 and 35-52%, respectively. There are no data for other oral or implantable contraceptives. However, simultaneous administration of oxcarbazepine and hormonal contraceptives may lead to a decrease in the effectiveness of the latter. Reduces the AUC of felodipine by 28%, however, plasma concentrations remain within the therapeutic range. Strengthens the sedative effect of ethanol. Verapamil can reduce the concentration of MHD by 20% (clinically insignificant). Cimetidine, erythromycin, dextropropoxyphene do not affect the pharmacokinetic parameters of MGP. No interactions with warfarin were observed with single or course administration of oxcarbazepine. Special instructions: Allergic reactions may develop in patients without a history of hypersensitivity to carbamazepine. If allergic reactions develop, the drug should be discontinued immediately. Hyponatremia (serum Na+ concentration below 125 mmol/l) is usually not clinically manifested and does not require dosage adjustment; it is observed in 2.7% of patients. The Na+ concentration is normalized when oxcarbazepine is discontinued (dose reduced) or fluid intake is limited. In patients with impaired renal function associated with hyponatremia, or during simultaneous therapy with diuretics, drugs that affect the secretion of ADH, before starting therapy with oxcarbazepine, the concentration of Na+ in the blood plasma should be determined, and 2 weeks after the start of therapy, and then monthly or accordingly. as necessary. If it is necessary to simultaneously prescribe saluretics and other drugs that cause hyponatremia, the same recommendations should be followed. If clinical symptoms of hyponatremia appear, serum Na+ concentration should be determined. During the treatment period, it is necessary to monitor body weight in patients with CHF for timely detection of fluid retention. In case of fluid retention or progression of symptoms of CHF, serum Na+ concentration should be determined. In case of hyponatremia, the amount of fluid consumed should be limited. During the treatment period, careful monitoring of patients with a history of rhythm and conduction disturbances is necessary. If the development of hepatitis is suspected during the treatment period, the drug should be discontinued. Women of childbearing age taking oral contraceptives should be warned that simultaneous administration of the drug may reduce their effectiveness, therefore additional use of non-hormonal methods of contraception is recommended. Experience with the drug during pregnancy is limited. There are isolated reports of a possible connection between taking the drug and congenital deformities (including cleft palate). It is necessary to carefully compare the expected benefits of therapy and its possible complications, especially in the first pregnancy if it is necessary to prescribe during pregnancy. The minimum effective dose should be used. In women of childbearing age, the drug is recommended to be used as monotherapy. The patient should be warned about possible developmental disorders of the fetus and the need for antenatal diagnosis. Antiepileptic drugs can increase folic acid deficiency during pregnancy (one of the possible causes of fetal development disorders), therefore additional folic acid intake is recommended during the treatment period. The use of antiepileptic drugs during pregnancy can lead to increased bleeding in newborns, so it is recommended to prescribe vitamin K in the last weeks of pregnancy and to the newborn. Oxcarbazepine and MGP cross the placental barrier and are excreted into breast milk. During treatment it is necessary to stop breastfeeding. The drug should be discontinued gradually (risk of increased frequency of epileptic seizures). During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

With caution: history of hypersensitivity to carbamazepine (in 25-30%, cross-allergic reactions to oxcarbazepine may develop), pregnancy. The use of the drug in children under 2 years of age has not been studied.

Update date 06/24/2010

Manufacturer: Novartis Farma SpA, Italy Registration certificate holder: Novartis Pharma AG, Switzerland Release form: film-coated tablets 150, 300, 600 mg (blisters) Composition: oxcarbazepine 150/300/600 mg Belongs to VED Shelf life: 3 years Data on registration: P No. 015199/01 dated June 18, 2009 Status of the registration certificate: valid HS codes: 3004 90 190 9

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.
  150 mg 50 pcs Novartis Pharma S.р.A RUR 325 order

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%.

Efficacy and tolerability of Trileptal (oxcarbazepine) in epilepsy

The main requirements for modern AEDs are maximum therapeutic effectiveness and a wide spectrum of action with a minimum of side effects (AE) [2]. Currently, old AEDs are used less and less: phenobarbital due to severe adverse events, and domestic diphenin due to low effectiveness. Valproates, while remaining the basic drugs in pediatric epileptology, often lead to a number of serious adverse events [8,14] and have a pronounced teratogenic effect [10]. Carbamazepine drugs have proven themselves well in the treatment of epilepsy in children and adults. Prolonged forms are especially convenient. At the same time, the carbamazepine metabolite (epoxide) is a fairly active and toxic chemical compound that predetermines some side effects in case of drug overdose [3]. A new drug synthesized on the basis of carbamazepine, oxcarbazepine (Trileptal, Novartis), largely lacks the adverse effects of its predecessor. The mechanism of action of oxcarbazepine is associated with the blockade of voltage-dependent sodium and calcium channels, which leads to the stabilization of neuronal membranes, inhibition of neuronal discharges and has a powerful anticonvulsant effect [1,11,20]. Peak drug concentrations are achieved on average 4.5 hours after a single oral dose. The half-life is 8–10 hours, binding to blood plasma proteins is about 40%. The therapeutic level of the drug in blood plasma is 10–35 mcg/ml. The drug is excreted primarily by the kidneys. Recommended doses for adults are 1200–2400 mg/day, for children 20–40 mg/kg/day. twice, less often in 3 doses [4]. Slow titration of the dose is recommended, reaching the minimum maintenance dose in at least 14 days. The purpose of our study was to study the effectiveness of oxcarbazepine (Trileptal, Novartis) in the treatment of epilepsy, as well as to analyze the frequency and nature of side effects. We observed 30 patients with epilepsy (16 men and 14 women) who received Trileptal for 6 months. and more. The age of the patients was from 5 months. up to 25 years (average – 12.5 years). The study was dominated by children under 18 years of age – 87%. Symptomatic and presumably symptomatic forms of epilepsy made up the main group - 29 patients, and 1 patient was diagnosed with idiopathic epilepsy with isolated generalized convulsive seizures. Trileptal was prescribed in combination therapy when previous AEDs were insufficiently effective (28 patients) or as monotherapy (2 patients). Clinical effectiveness was assessed by the effect of the drug on the frequency of attacks: complete remission; reduction in attacks by more than 50%; insufficient effectiveness (less than 50%) or lack of effect; increased frequency of attacks (aggravation). The frequency and nature of PE were analyzed. At the end of the study, the “retention on therapy” parameter was determined: the number of patients who continued to take Trileptal after 6 months. therapy and the number of patients who stopped taking it for various reasons. Study results Symptomatic (17 patients) and presumably symptomatic (12 patients) forms of epilepsy dominated the study. Only 1 patient was diagnosed with idiopathic epilepsy with generalized seizures. Patients with frequent polymorphic seizures resistant to basic AEDs also predominated. The main types of attacks in the examined patients were asymmetrical tonic axial, dialeptic and secondary generalized paroxysms. Trileptal doses ranged from 225 to 2100 mg/day, which was 15–44 mg/kg/day. In 28 cases, the drug was prescribed in combination therapy when added mainly to valproate or topiramate. All patients underwent slow dose titration with gradual increases over 4–7 weeks. The effectiveness and tolerability of Trileptal therapy were assessed after 6 months. or more from the start of taking the drug. The maximum follow-up period was 1.5 years. The following results were obtained during the study: clinical remission - 4 patients (13.3%); significant reduction in the frequency of attacks – 21 (70%); no effect or insignificant effectiveness – 3 (10%); aggravation of attacks – 2 (6.7%). The greatest effectiveness of Trileptal was found in dialeptic and automotor seizures as part of temporal lobe epilepsy, as well as in focal motor and secondary generalized convulsive seizures. To a lesser extent, Trileptal was effective in hypermotor and tonic axial seizures. In 1 patient with idiopathic generalized epilepsy, the drug completely stopped generalized seizures (follow-up 1.5 years). In this case, Trileptal was prescribed as monotherapy at a dose of 1200 mg/day. (15 mg/kg/day) instead of sodium valproate, which caused severe obesity and opsomenorrhea. Of particular note is the effectiveness of Trileptal in 7 patients aged 5 to 14 months. with attacks in the form of asymmetric infantile spasms (West syndrome, mimicking symptomatic focal epilepsy). In all patients of this group, the addition of Trileptal led to a significant reduction in spasms, converting them from serial to single and abortive. In 1 case, complete clinical (but not electrical) remission was observed for 8 months. Drug dosages varied from 18 to 44 mg/kg/day. The smallest effect of Trileptal was obtained in patients with pseudogeneralized seizures: focal epileptic myoclonus, negative myoclonus, atypical absence seizures. This type of seizures was observed mainly in frontal lobe epilepsy with the presence of the phenomenon of secondary bilateral synchronization on the EEG. It was in this group of patients that 2 cases of seizure aggravation were identified: negative myoclonus and atypical absence seizures, which required discontinuation of the drug. The study showed good tolerability of Trileptal in most patients. Side effects highly likely associated with the drug were observed in 6 patients (20%). The following AEs were noted: drowsiness (2), double vision (2), irritability (1), insomnia (1). It should be noted that in 5 of 6 cases, AEs occurred during the dose titration period and disappeared within 3–8 weeks. Diplopia in two patients occurred during the gradual replacement of carbamazepine with Trileptal, when the patients took these drugs simultaneously for some time. Only in 1 case (3.3% of the total group) severe irritability in combination with the low effectiveness of the drug served as a reason to discontinue Trileptal. As a result of the analysis of the “retention on therapy” parameter, the following results were obtained: after 6 months. 24 patients (80%) continued taking Trileptal, and 6 (20%) stopped taking the drug. The reasons for refusal to take the drug (by the patient, his family or the attending physician) were: increased frequency of attacks (2), low efficiency (2), side effects (1), financial difficulties (1). Discussion As a result of the study, the positive effect of Trileptal in the treatment of epilepsy was noted in 83% of cases. Side effects were observed in 20% of patients, but drug discontinuation was required in only 1 case. The “retention in therapy” parameter was 80%. Currently, a large number of serious studies around the world have proven the high clinical effectiveness and relative safety of Trileptal in the treatment of epilepsy [1,3–7,11–13]. In a review article, Schmidt & Elger [16] reported 21 publications on the use of Trileptal in 2191 patients with epilepsy. Trileptal has been shown to be highly effective and well tolerated in doses of 600–2400 mg/day. (30–46 mg/kg/day), as a basic drug for epilepsy in children, adolescents and adults. The drug is recommended as a basic drug (including as initial monotherapy) for symptomatic focal forms of epilepsy with simple partial, complex partial and secondary generalized seizures. Our study showed high effectiveness (reduction of seizures in all cases) for infantile spasms as part of symptomatic focal epilepsy in children of the first year of life. Northam et al. [13] also demonstrated the promise of using Trileptal for focal epileptic seizures in young children (average - 20.4 months) and noted good tolerability of the drug in this age category. Glauser et al. [9] conducted a double-blind, placebo-controlled study on the effectiveness of oxcarbazepine as an adjunctive therapy for epilepsy in children. This multicenter study included 267 children aged 3 to 17 years with refractory partial epileptic seizures (138 received oxcarbazepine and 129 placebo). The dose of the drug varied from 6 to 51 mg/kg/day. (average – 31.4 mg/kg/day). Oxcarbazepine was shown to be significantly more effective in the treatment of focal epilepsy compared to placebo. The addition of oxcarbazepine led to complete remission in 4% of patients (placebo in 1%) and a reduction in the frequency of attacks by more than 50% in 41% (placebo in 22%). The effectiveness of the drug was noted both in simple and complex partial seizures, and in secondary generalized convulsive seizures and did not depend on the gender and age of the patients. After 28 days from the start of oxcarbazepine therapy, the overall frequency of attacks in patients decreased by 35% (placebo - by 9%). Even more encouraging results are presented in the publication of Serdaroglu et al. [17]. The authors analyzed the effectiveness of oxcarbazepine as monotherapy in 42 children (mean age 11.9 years) with symptomatic focal epilepsy and epilepsy with isolated generalized seizures. The drug was prescribed in a dose of 10 to 45 mg/kg/day. (with slow titration). After 6 months from the start of therapy, complete remission of seizures was found in 87.5% of patients: 91.7% with generalized epilepsy and 81.2% with focal epilepsy. In our study, Trileptal was prescribed to only 1 patient with idiopathic generalized epilepsy; At the same time, complete remission of attacks was achieved. It is obvious that the use of Trileptal may be promising for epilepsy with isolated generalized convulsive seizures in cases where valproate or topiramate are not effective enough or lead to the development of PE. One of the first studies on the results of Trileptal use in various forms of epilepsy in adolescents and adults was performed by Van Parys & Meinardi [19] on a Dutch cohort of patients. The vast majority of patients received carbamazepine with unsatisfactory results before oxcarbazepine was prescribed. Among 253 patients treated with Trileptal, clinical remission was observed in 8% of cases and a significant reduction in seizures in 33%. Aggravation of attacks was observed in 6 patients (2%); in the remaining 57% of patients, no significant changes were noted during therapy. According to the authors, oxcarbazepine can be successfully used in cases where carbamazepine drugs are not effective enough. In this regard, the study of Albani et al. is of interest. [3], who showed the possibility of simultaneously switching patients from carbamazepine to oxcarbazepine without gradual replacement and without dose titration. Moreover, according to the authors, the replacement of carbamazepine with oxcarbazepine should be carried out at a dose rate of 1:1.5 (for example, 800 mg of carbamazepine is simultaneously replaced by 1200 mg of oxcarbazepine). In a study by Beydoun et al. [5] compared the effectiveness of oxcarbazepine in monotherapy and as part of combination therapy for refractory focal epilepsy in adults at a dose of 600–2400 mg/day. Among 42 patients receiving monotherapy with oxcarbazepine and 34 patients receiving combination treatment, the results were distributed as follows: with monotherapy, remission of attacks was achieved in 9.5% of cases, and a reduction in the frequency of attacks by 50% or more - in 57.1%, general reduction in the frequency of attacks - 59.7%; with combination therapy, remission was achieved in 2.9% of cases, a reduction in the frequency of attacks by 50% or more - in 32.4%, a general reduction in the frequency of attacks - in 28%. Thus, the greater effectiveness of oxcarbazepine when used as monotherapy was convincingly demonstrated. Christe et al. [7] studied the comparative effectiveness of oxcarbazepine and sodium valproate in 249 adolescents and adults with newly diagnosed focal epilepsy (focal and secondary generalized seizures). Equal effectiveness was found for oxcarbazepine (remission 56.6%) and valproate (remission 53.8%) in the treatment of newly diagnosed focal epilepsy. There was also no significant difference in the incidence of PE. This study allows us to position oxcarbazepine as a basic drug in the treatment of focal epilepsy. Along with effectiveness, of course, the most important characteristic of the drug is its tolerability - one of the main components of the concept of “quality of life” for patients. The tolerability of oxcarbazepine, the frequency and nature of AEs have been analyzed in a large number of publications. Our study demonstrated good tolerability of the drug, the absence of serious AEs, and the discontinuation of Trileptal due to AEs in only 1 patient (3.3%). Beydoun et al. [5] analyzed the frequency and nature of PE when oxcarbazepine was prescribed to 76 adolescents and adults at a dose of 600–2400 mg/day. The drug was discontinued due to PE in 13% of cases. Most PEs were mild and moderate in nature. The following AEs were noted: fatigue, drowsiness, irritability, headache, diplopia, nausea, skin rash. In several cases, a transient increase in the level of liver enzymes in the blood occurred without any clinical manifestations. All AEs were observed significantly more often during polytherapy. Only in 2 cases (2.6%) were serious adverse events observed: acute psychosis (1) and hyponatremia (1). According to our observations, diplopia occurs only in cases where carbamazepine is gradually withdrawn with a slow titration of the dose of oxcarbazepine and patients receive both drugs simultaneously for some time. To prevent this adverse event, it is recommended to immediately switch patients from carbamazepine to Trileptal [3]. Hyponatremia (a decrease in plasma sodium levels below 125 mmol/ml) is a serious potential adverse event when taking oxcarbazepine. However, the incidence of this PE is low, and in pediatric practice it occurs rarely [6]. However, you should monitor your blood sodium levels while taking oxcarbazepine. Also, unlike carbamazepine, there are rare cases of skin rash when prescribing Trileptal - 2.7% in the study by Bourgeois & D'Souza [6]. Of note is the original study by Van Parys & Meinardi [19] on the analysis of AEs experienced by patients taking carbamazepine after switching to oxcarbazepine. It turned out that out of 164 patients who had PE on carbamazepine, in 129 (79%) they gradually disappeared when switching to Trileptal. Skin manifestations were leveled out in 72.5% of patients when carbamazepine was replaced with Trileptal. Thus, the significantly better tolerability of oxcarbazepine compared with carbamazepine was convincingly demonstrated. To date, there is the only serious publication by Montouris [12] devoted to studying the safety of oxcarbazepine during pregnancy. Using available databases and global registries, the author analyzed pregnancy outcomes in women taking Trileptal. Data were obtained on 248 women who received Trileptal as monotherapy, and on 61 women who received Trileptal in combination with other AEDs. Congenital malformations were detected in 6 cases out of 248 (2.4%) and in 4 out of 61 (6.6%). The risk of congenital malformations in the general population, according to the author, is 2–4%. Thus, the safety of using Trileptal during pregnancy in monotherapy and a slight increase in the risk of malformations in combination with other AEDs has been shown. However, most authors recommend refraining from prescribing oxcarbazepine to pregnant women, since the number of observations in the world is still limited. The most important characteristic of the drug is the “retention on therapy” indicator, which reflects the number of patients who continued to take the drug after a certain period of time after the start of treatment and the number of patients who stopped taking it for various reasons. Our study found a high retention rate on therapy: 80% of patients continued to take Trileptal continuously after 6 months. from the start of treatment. The reasons for refusing to take the drug were: increased frequency of attacks (2), low effectiveness (2), side effects (1), financial difficulties (1). Retention on Trileptal monotherapy after 1 year was analyzed in the study by Rainesalo et al. [15] in 175 adult patients with epilepsy. Patients were divided into 2 groups: 1 – starting monotherapy with Trileptal (97 people) and 2 – monotherapy with Trileptal in case of ineffectiveness of other previously prescribed AEDs (78). The percentage of deduction in therapy in the 1st group was 91%, and in 2 - 77%. The abolition of therapy due to side effects was stated in 1 group only in 3%of cases, in 2 - in 14%, and due to loss of efficiency - in the 1st group - in 2%, in 2 - in 8%. Thus, a high indicator of deduction on therapy with trileptal and a low percentage of treatment for treatment due to PE or loss of efficiency over time was demonstrated. The best effect was observed when prescribing a trileptal as starting monotherapy. Thus, we conducted the study and analysis of existing publications indicate the high efficiency and good tolerance of Okskarbazepine (trileptala) in the treatment of epilepsy in children and young adults. The high efficiency of the drug has been proved with symptomatic and presumably symptomatic focal forms of epilepsy with focal motor, automotor and secondary generated attacks. In this category of patients, trileptal can be prescribed as starting monotherapy. In focal forms of epilepsy with pseudo -generated attacks and the phenomenon of secondary bilateral synchronization on EEG, trileptal can lead to an aggravation of seizures and epileptiform changes to the EEG. At the same time, in these cases, the addition of average doses of trileptal to valproates can be quite safe and effective. The question of the use of trileptal in the treatment of idiopathic epilepsy with isolated generalized convulsive attacks is the subject of discussion. Trilepal, of course, is highly effective with isolated generalized convulsive attacks, but it can, like carbamazepine, lead to the connection of absans and myoclonus. In this regard, in our opinion, the drug may be prescribed for this syndrome in case of insufficient effectiveness or poor tolerance of topiramate and valPaters. All studies show the best tolerance of Okskarbazepine, including when compared with carbamazepine. Heavy PEs arose extremely rarely. In the first months of therapy, it is recommended to control the level of sodium in the blood, especially in adult patients. To reduce the risk of developing PE, slow title of the dose of trileptal within 4-6 weeks is recommended. However, when replacing carbamazepine with trileptal, it is advisable to do it at once. Preliminary studies showed the safety of monotherapy with trileptal during pregnancy.

Literature 1. Zenkov L.R. The role of oxcarbazepine in the treatment of epilepsy.// Consilium medicum, 2005, volume 7 No. 8, pp. 710–714 2. Mukhin K.Yu., Petrukhin A.S. Epileptic syndromes. Diagnostics and standards of therapy, // Moscow, 2005, 143 C 3. Albani F., Grassi B., Ferrara R., Turrini R., Baruzi A. Immediate (overnight) switching from carbamazepine monotherapy is equivalent to a progressive switch./ /Seizure, 2004; 13:254–263 4. Beydoun A, Kutluay E. Oxcarbazepine. Expert Opin Pharmacother, 2002; 3:59–71 5. Beydoun A., Sachdeo RC, Kutluay E., McCague K., DSouza J. Sustained efficacy and long-term safety of oxcarbazepine: one-year open-label extension of a study in refractory partial epilepsy. // Epilepsia, 2003, 44(9): 1160–1165 6. Bourgeois B., DSouza J. Long-term safety and tolerance of oxcarbazepine in children: a review of clinical experience.// Epilepsy& Behavior, 7 ((2005) , pp 375–382 7. Christe W., Kramer G., Vigonius U., Pohlmann H., Steinhoff B., Brodie M., Moore A. A double–blind controlled clinical trial: oxcarbazepine versus sodium valproate in newlywed adults diagnosed epilepsy. // Epilepsy research 26 (1997), pp 451–460 8. Demir E.; Aysun S. Weight gain associated with valproate in childhood // Pediatr Neurol. – 2000. – 22(5) – P. 361– 4. 9. Glauser TA, Nigro M., Sachdeo R., Pasteris LA, Weinstein S., Abou–Khalil B., Frank LM, Grinspan A., Guarino T., Bettis D. Adjunctive therapy with oxcarbazepine in children with partial seizures // Neurology 2000; 54:2237–2244 10. Morrow JJ Craig Antiepileptic drugs in pregnancy: current safety and other issues // Expert Opin Pharmacother. – 2003. – V. 4(4). – P. 445–446 11 McLean MJ Oxcarbazepine: mechanisms of action In: Levy RH, Mattson RH, Meldrum BS, et al., eds. Antiepileptic drugs. 5th ed. Philadelphia: Lipincott Williams & Wilkins, 2001:451–8 12. Montouris G. Safety of the new antiepileptic drug oxcarbazepine during pregnancy.// Current medical research and opinion, vol.21, 5 2005, pp. 693–701 13. Northam RS, Hernandez AW, Litzinger MJ, Minecan DN, Glauser TA, Mangat S., Zheng C., Souppart C., Sturm Y. Oxcarbazepine in infants and young children with partial seizures. // Pediatr Neurol 2005 ; 33:337–344 14. Novak GP; Maytal J; Alshansky A; Eviatar L; Sy Kho R; Siddique Q. Risk of excessive weight gain in epileptic children treated with valproate // J Child Neurol. – 1999. – V. 14(8). – P. 490–5. 15. Rainesalo S., Peltola J., Auvinen A., Keranen T. Retention rate of oxcarbazepine monotherapy in an unselected population of adult epileptics.// Seizure, 2005 (14), pp. 72–74 16. Schmidt D., Elger CE What is the evidence that oxcarbazepine and carbamazepine are distinctly different antiepileptic drugs? Epilepsy & Behavior, 5 2004, pp. 627–635 17. Serdaroglu G., Kurul S., Tutuncuoglu S., Dirik E., Sarioglu B. Oxcarbazepine in the treatment of childhood epilepsy. // Pediatr Neurol 2003; 28:37–41 18. Vainionpaa LK; Rattya J.; Knip M.; Tapanainen JS; Pakarinen AJ; Lanning P.; Tekay A.; Myllyla VV; Isojarvi JI Valproate induced hyperandrogenism during pubertal maturation in girls with epilepsy // Ann Neurol. – 1999 – V 45(4) – P. 444–50. 19. Van Parys JA, Meinardi H. Survey of 260 epileptic patients treated with oxcarbazepine (Trileptal) on a named–patient basis. // Epilepsy Research 19 (1994) 79–85 20. White HS Pediatric epilepsy: diagnosis and therapy. – 2001. – P.301–316. 21. Wolf P. Determinants of outcome in childhood epilepsy.// Acta neurol scand, 2005: 112 (Suppl. 182): 5–8

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.

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.

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.

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 .