Details

Konvulex tablets p / o prolonged action 300mg, No. 50

epilepsy of various etiologies (idiopathic, cryptogenic and symptomatic);

generalized epileptic seizures in adults and children (clonic, tonic, tonic-clonic, absences, myoclonic, atonic);

partial epileptic seizures in adults and children (with or without secondary generalization);

specific syndromes (Vesta, Lennox-Gastaut);

behavioral disorders due to epilepsy;

febrile seizures in children;

children's teak;

treatment and prevention of bipolar disorder, resistant to treatment with lithium or other drugs.

The drug is taken orally, without chewing, 1-2 times / day, during or immediately after a meal, with a small amount of water.

Adults are prescribed at an initial dose of 600 mg / day with a gradual increase in the dose by 150-250 mg every 3 days until a clinical effect is achieved (the disappearance of seizures).

The initial dose for monotherapy is 5-15 mg / kg / day, then the dose is gradually increased by 5-10 mg / kg per week.

The recommended daily dose is about 1000-2000 mg, i.e. 20-25 mg / kg. If necessary, the dose can be increased to a maximum dose of 2500 mg / day (30 mg / kg / day).

The maximum dose is 30 mg / kg / day (in patients with accelerated metabolism of valproic acid, the maximum dose can be increased to 60 mg / kg / day under the control of the concentration of the drug in the blood plasma).

When carrying out combination therapy, the dose is 10-30 mg / kg / day, followed by an increase of 5-10 mg / kg per week.

For children weighing more than 25 kg, the drug is prescribed at an initial dose of 300 mg / day (5-15 mg / kg / day) with a gradual increase by 5-10 mg / kg per week until a clinical effect (disappearance of seizures) is achieved, while the dose , as a rule, is 1000-1500 mg / day (20-30 mg / kg / day).

The maximum dose is 30 mg / kg / day (in patients with accelerated metabolism of valproic acid, the maximum dose can be increased to 60 mg / kg / day under the control of the concentration of the drug in the blood plasma).

For children weighing 20-25 kg with monotherapy, the average dose is 15-45 mg / kg / day, the maximum dose is 50 mg / kg / day. With combination therapy - 30-100 mg / kg / day. It should be borne in mind that children weighing less than 20 kg are not recommended to use the drug in the form of prolonged-release tablets, they should be prescribed other forms of the drug.

Although the pharmacokinetics of valproic acid in the elderly may have their own characteristics, this is of limited clinical significance, and the dose should be determined by the clinical effect. Due to a decrease in binding to serum albumin, the proportion of unbound drug in plasma increases. This makes it advisable to carefully select the dose of the drug in the elderly, with the possible use of smaller doses of the drug.

In patients with renal impairment, it may be necessary to reduce the dose of the drug. The dose should be selected according to the monitoring of the clinical condition, since the plasma concentration indicators may be insufficiently informative.

Active ingredient: sodium valproate - 300 mg

Excipients: citric acid - 39 mg, ethyl cellulose - 60 mg, copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2: 0.1) (eudragit RS30D) - 20.1 mg, talc - 8.1 mg, colloidal silicon dioxide - 6 mg, magnesium stearate - 6 mg.

Shell composition: copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2: 0.2) (eudragit RL30D type A) - 2.25 mg, copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2: 0.130) (eudragitol 530) (eudragitol530) (eudragitol) - 0.9 mg, sodium carmellose - 1.27 mg, titanium dioxide - 1.06 mg, talc - 2.02 mg, vanillin - 0.11 mg.

liver failure;

acute and chronic hepatitis;

dysfunction of the pancreas;

porphyria;

hemorrhagic diathesis;

severe thrombocytopenia;

disorders of urea metabolism (including family history);

lactation period;

children weighing less than 20 kg;

children under 3 years old;

hypersensitivity to valproic acid and its salts or drug components.

Care should be taken to prescribe the drug to the following categories of patients:

with anamnestic data on diseases of the liver and pancreas;

with inhibition of bone marrow hematopoiesis (leukopenia, thrombocytopenia, anemia);

with renal failure;

with congenital fermentopathies;

with organic diseases of the brain;

with hypoproteinemia;

during pregnancy (especially the first trimester);

children with mental retardation.

Description:

Sustained-release tablets, film-coated white, oval, biconvex, with a break line and engraved 'CC3' on one side, with a vanillin smell; at the break - white or almost white.

Composition:

Active ingredient: sodium valproate - 300 mg

Excipients: citric acid - 39 mg, ethyl cellulose - 60 mg, copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2: 0.1) (eudragit RS30D) - 20.1 mg, talc - 8.1 mg, colloidal silicon dioxide - 6 mg, magnesium stearate - 6 mg.

Shell composition: copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2: 0.2) (eudragit RL30D type A) - 2.25 mg, copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2: 0.130) (eudragitol 530) (eudragitol530) (eudragitol) - 0.9 mg, sodium carmellose - 1.27 mg, titanium dioxide - 1.06 mg, talc - 2.02 mg, vanillin - 0.11 mg.

Clinical and pharmacological group: Anticonvulsant drug

Pharmaco-therapeutic group: Antiepileptic drug

pharmachologic effect

Antiepileptic drug. It has a central muscle relaxant and sedative effect.

The mechanism of action is mainly due to an increase in the content of gamma-aminobutyric acid (GABA) in the central nervous system due to inhibition of the enzyme GABA-transferase. GABA reduces the excitability and seizure readiness of the motor areas of the brain. In addition, the effect of valproic acid on GABAA receptors (activation of GABA-ergic transmission), as well as the effect on voltage-dependent sodium channels, plays a significant role in the mechanism of action of the drug. According to another hypothesis, it acts on the sites of postsynaptic receptors, mimicking or enhancing the inhibitory effect of GABA. A possible direct effect on membrane activity is associated with changes in the conductivity of potassium ions.

Improves the mental state and mood of patients, has antiarrhythmic activity.

Pharmacokinetics

Suction

Valproic acid is almost completely absorbed from the gastrointestinal tract, oral bioavailability is 100%. Food intake does not decrease the rate of absorption. Cmax in blood plasma is reached after 4 hours. The therapeutic concentration of valproic acid in blood plasma is 50-150 mg / l.

The prolonged form is characterized by slow absorption, lower (by 25%), but more stable plasma concentration between 4 and 14 hours.

Distribution

Css is achieved on days 2-4 of treatment, depending on the intervals between doses.

At a plasma concentration of up to 50 mg / l, the binding of valproic acid to plasma proteins is 90-95%, at a concentration of 50-100 mg / l - 80-85%.

Penetrates the BBB. The values ??of the concentration in the cerebrospinal fluid correlate with the value of the non-protein-bound fraction of the active substance. Valproic acid crosses the placental barrier and is excreted in breast milk. The concentration in breast milk is 1-10% of the concentration in the mother's blood plasma.

Metabolism

Valproic acid undergoes glucuronidation and oxidation in the liver.

Withdrawal

Valproic acid (1-3% of the dose) and its metabolites are excreted by the kidneys, small amounts - with feces and exhaled air. T1 / 2 of valproic acid in monotherapy and in healthy volunteers is 8-20 hours.

Pharmacokinetics in special clinical situations

With uremia, hypoproteinemia and cirrhosis, the binding of valproic acid to plasma proteins decreases.

When combined with other drugs, T1 / 2 can be 6-8 hours due to the induction of metabolic enzymes.

In patients with impaired liver function, elderly patients and children under the age of 18 months, a significant increase in T1 / 2 is possible.

Indications

epilepsy of various etiologies (idiopathic, cryptogenic and symptomatic);

generalized epileptic seizures in adults and children (clonic, tonic, tonic-clonic, absences, myoclonic, atonic);

partial epileptic seizures in adults and children (with or without secondary generalization);

specific syndromes (Vesta, Lennox-Gastaut);

behavioral disorders due to epilepsy;

febrile seizures in children;

children's teak;

treatment and prevention of bipolar disorder, resistant to treatment with lithium or other drugs.

Dosage regimen