After oral administration, oxcarbazepine is completely absorbed and largely metabolized with the formation of the pharmacologically active metabolite. After a single in the form of a suspension for oral administration at a dose of 600 mg in healthy volunteers fasted maximum plasma deca durabolin concentration, the average time to achieve it – about 6 hours. After a single dose Trileptal in the form of tablets, coated tablets, 600 mg dose in healthy volunteers fasted , the median time to achieve – about 4.5 hours. The pharmacokinetic studies demonstrated that the plasma is determined of oxcarbazepine ; the rest comes from secondary metabolites rapidly eliminated from the blood plasma. Food intake does not affect the rate and extent of absorption. The connection to plasma proteins and the distribution of apparent volume of distribution 49 liters.Approximately binds to plasma proteins, mainly albumin. The therapeutic range of the degree of binding is not dependent on the concentration of oxcarbazepine in serum. Oxcarbazepine and do not bind to alpha-1-acid glycoprotein.
Metabolism Oxcarbazepine is rapidly metabolized by the liver cytosolic enzymes to the active metabolite , which causes a pharmacological effect is further conjugated with glkzhuronovoy acid. Minor quantities (about 4% of the dose) are oxidized with formation of inactive metabolites . Derivation ofoxcarbazepine is excreted mainly as metabolites, mainly by the kidneys. More than 95% of the dose excreted by the kidneys as metabolites, less than 1% – unchanged. Approximately 80% of the dose is excreted , in the form of glucuronides (49%) and as unchanged IHP (27%); inactive is about 3%, conjugates of oxcarbazepine – about 13% of the dose. About 4% of the dose is excreted in the feces. Oxcarbazepine is rapidly eliminated from the blood plasma, the apparent half-life is 1.3 – 2.3 hours. In contrast to oxcarbazepine, the apparent half-life is an average of 9,3 ± 1,8 hours. The equilibrium concentration of IHL in plasma are reached 2-3 hours while taking Trileptal 2 times a day. In the equilibrium state pharmacokinetic parameters are dose-dependent and linear in the range of daily .
Patients with hepatic impairment pharmacokinetic parameters and metabolism of oxcarbazepine and IHL after a single oral administration of the drug at a dose of 900 mg were evaluated in healthy volunteers and in patients with impaired hepatic function. Human liver mild to moderate degrees do not affect the pharmacokinetic parameters of oxcarbazepine . Pharmacokinetics with severe deca durabolin hepatic impairment has not been studied. Patients with impaired renal function. There is a linear dependence of the renal clearance of creatinine clearance . In patients with impaired renal function (creatinine clearance less than 30 ml / min) after a single dose of 300 mg oxcarbazepine during IHP-life increases to 19 hours, and the area under the curve “concentration – time” increased by 2 times. Children Clearancadjusted for body mass, in children decreases with increasing age and body weight, approaching a clearance adults. Clearance adjusted for body mass, in children aged 1 to 4 months of age by an average of 93% higher than in adults. Thus it is assumed that among children in this age group is expected to be 2 times smaller than that of adults when using the same dosage (when adjusting for body weight). Clearance adjusted for body weight in children aged 4 to 12 years old on average 43% higher than in adults. Alleged in children of this age group is 2/3 of that of adults when using the same dosage (when adjusting for body weight). It is assumed that children aged 13 years and over due to the increase in body weight clearance corrected for body weight, corresponds to the clearance in adults. Pregnant patients in pregnant women is a series of physiological changes that can lead to a gradual reduction level in plasma during pregnancy. elderly patients after receiving once and again (at a dose of 600 mg / day) in the elderly volunteers aged 60-82 years30-60% higher compared to the same parameters in young volunteers (18-32 years), which is associated with age-related reduction in creatinine clearance. Gender is not observed any differences in pharmacokinetic parameters according to sex in childhood, adulthood or old age.
- Simple, complex partial seizures with secondary generalization and without adults and children aged 1 month and over.
- Generalized tonic-clonic seizures in deca durabolin adults and children aged 2 years and older.
Trileptap is the drug of first-line monotherapy or in combination therapy.
Trileptap can be used to replace other antiepileptic drugs in cases where the application of the latter is not achieved a satisfactory therapeutic response.Contraindications
- Hypersensitivity to oxcarbazepine or any other components of the drug,
- For tablets, film-coated: children up to 3 years.
- For suspension for the reception inside: children up to 1 month