Valparin XP prolonged-release tablets, p / o 500mg, No. 100

Treatment of generalized or partial epilepsy, especially for the following types of seizures:

• absences;

• myoclonic;

• tonic-clonic;

• atonic.

Partial epilepsy:

• simple or combined seizures;

• secondary generalized seizures.

Specific syndromes (Vesta, Lennox-Gastaut).

The dosage regimen is selected individually, depending on the age and body weight of the patient.

For adults, the initial dose is 600 mg / day, followed by an increase of 200 mg every 3 days until the optimal effect is achieved. Frequency rate of admission - 1-2 times / day. The maximum recommended dose is 1-2 g / day.

The tablets should be swallowed whole with a little water.

In elderly patients, the dosage regimen of Valparin XP is similar to the dosage regimen in adults and is selected individually.

For children weighing more than 20 kg, the initial dose is 400 mg / day. The dose should be increased gradually until optimal values ??are reached - usually 20-30 mg / kg / day in 1 or 2 doses.

Valparin XP should not be used in children weighing up to 20 kg .

Active substance:

sodium valproate - 333 mg

valproic acid - 145 mg, which corresponds to the total sodium content of valproate - 500 mg

Excipients: colloidal silicon dioxide, hydroxypropyl methylcellulose, ethyl cellulose, silicon dioxide hydrate, sodium saccharin, glycerin, titanium dioxide, eudragit E-100, eudragit NE-30D, polyethylene glycol 1500, talc.

• severe dysfunction of the pancreas;

• acute or chronic hepatitis, cases of active hepatitis in a family history (primarily of drug origin);

• porphyria;

• thrombocytopenia;

• pregnancy;

• lactation (breastfeeding);

• children under 3 years old;

• hypersensitivity to valproic acid and other components of the drug.

Clinical and pharmacological group: Anticonvulsant drug

Pharmaco-therapeutic group: Anticonvulsant

pharmachologic effect

Anticonvulsant drug. Sodium valproate increases the content of gamma-aminobutyric acid (GABA) in the brain, which accordingly increases the content of GABA in postsynaptic neurons. In addition, sodium valproate affects the transport of potassium ions across neuronal membranes. As a result, the development is suppressed, as well as the spread of epileptic excitation through the neurons.

Sodium valproate has anticonvulsant activity in various types of epilepsy in humans. The drug does not have pronounced hypnotic and sedative effects, and also does not have a depressing effect on the respiratory center. Sodium valproate has no negative effect on blood pressure, heart rate, renal function and body temperature.

Pharmacokinetics

Suction

After oral administration of controlled-release tablets, Cmax in plasma is achieved within 2-8 hours. The bioavailability of the drug is about 100%.

Therapeutic efficacy is manifested at a concentration of valproic acid in blood plasma of 40-100 mg / l. At the same time, the pharmacological and therapeutic effects of this controlled release drug do not always depend on its plasma concentration.

Distribution

Plasma protein binding is 80-90%.

Vd is 0.2 l / kg.

Metabolism and excretion

It is metabolized in the liver and excreted in the urine. Pre-systemic metabolism is not observed. T1 / 2 is approximately 8-20 hours.

Pharmacokinetics in special clinical situations

In children, T1 / 2 decreases.

Indications

Treatment of generalized or partial epilepsy, especially for the following types of seizures:

• absences;

• myoclonic;

• tonic-clonic;

• atonic.

Partial epilepsy:

• simple or combined seizures;

• secondary generalized seizures.

Specific syndromes (Vesta, Lennox-Gastaut).

Dosage regimen

The dosage regimen is selected individually, depending on the age and body weight of the patient.

For adults, the initial dose is 600 mg / day, followed by an increase of 200 mg every 3 days until the optimal effect is achieved. Frequency rate of admission - 1-2 times / day. The maximum recommended dose is 1-2 g / day.

The tablets should be swallowed whole with a little water.

In elderly patients, the dosage regimen of Valparin XP is similar to the dosage regimen in adults and is selected individually.

For children weighing more than 20 kg, the initial dose is 400 mg / day. The dose should be increased gradually until optimal values ??are reached - usually 20-30 mg / kg / day in 1 or 2 doses.

Valparin XP should not be used in children weighing up to 20 kg .

Side effect

From the digestive system: rarely - nausea, vomiting, diarrhea and / or constipation, hepatitis, pancreatitis.

Allergic reactions: rarely - skin rash, itching, photosensitivity, erythema multiforme, Stevens-Johnson syndrome.

From the side of the central nervous system: rarely - ataxia, tremor, impaired consciousness, coma.

From the reproductive system: rarely - menstrual irregularities, secondary amenorrhea.

From the hematopoietic system: rarely - anemia, thrombocytopenia, neutropenia, leukopenia, decreased fibrinogen content, inhibition of platelet aggregation.

Others: 2-12% - hair loss; rarely - weight gain, hyperammonemia, creatininemia.

Contraindications for use

• severe dysfunction of the pancreas;

• acute or chronic hepatitis, cases of active hepatitis in a family history (primarily of drug origin);

• porphyria;

• thrombocytopenia;

• pregnancy;

• lactation (breastfeeding);

• children under 3 years old;

• hypersensitivity to valproic acid and other components of the drug.

Application during pregnancy and lactation

Prescribing the drug during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. In the case of taking the drug during pregnancy, it is imperative to carry out specialized prenatal monitoring of the fetus.

The use of the drug during breastfeeding is not recommended.

Application for violations of liver function

Contraindicated in acute or chronic hepatitis, cases of active hepatitis in a family history (primarily of drug origin

Application in children

The drug is contraindicated in children under 3 years of age.

For children weighing more than 20 kg, the initial dose is 400 mg / day. The dose should be increased gradually until optimal values ??are reached - usually 20-30 mg / kg / day in 1 or 2 doses.

Valparin XP should not be used in children weighing up to 20 kg .

Use in elderly patients

In elderly patients, the dosage regimen of Valparin XP is similar to the dosage regimen in adults and is selected individually.

special instructions

It is necessary to regularly monitor the activity of transaminases, the content of bilirubin, blood platelets, amylase (every 3 months).

Valproic acid inhibits platelet aggregation, which increases the risk of increased blood clotting time during bleeding. Consideration should be given to the possibility of complications associated with bleeding in the postoperative period in patients receiving sodium valproate. With prolonged intake of sodium valproate, spontaneous hematomas and bleeding may develop. In this case, you should immediately stop taking the drug.

Sodium valproate can cause drug-induced pancreatitis and liver dysfunction (usually in the first 6 months of use). In this regard, it is necessary during the first 23 months of treatment to monitor the state of the pancreas, conduct liver tests, and monitor the level of prothrombin. Dysfunction of the liver, liver failure during therapy with sodium valproate is sometimes observed in children with epilepsy and combined metabolic and degenerative diseases, organic pathology of brain tissue and retarded mental development. If symptoms such as severe weakness, lethargy, edema, vomiting and jaundice occur, the drug should be discontinued immediately.

Influence on the ability to drive vehicles and use mechanisms

The patient should be careful when working with mechanisms, because the drug reduces the ability to concentrate.

Overdose

Rare cases of accidental or intentional drug overdose have been reported.

Symptoms: nausea, vomiting, dizziness, diarrhea, respiratory depression, hyporeflexia, coma.

Treatment: gastric lavage, intake of activated charcoal. If necessary, inpatient treatment with symptomatic therapy, hemodialysis.

Drug interactions

Sodium valproate enhances the effect of antipsychotic drugs, anticonvulsants, and antidepressants. Unlike other anticonvulsants, sodium valproate does not induce hepatic enzymes and therefore does not reduce the effectiveness of oral contraceptives.

With the combined use of sodium valproate and warfarin, the percentage of binding to blood plasma proteins of the latter decreases.

Sodium valproate alters the plasma concentrations of phenytoin and lamotrigine. In combination with anticoagulants and derivatives of acetylsalicylic acid, the antiplatelet effect is enhanced.

Storage conditions

The drug should be stored at temperatures below 30 ? C, protected from moisture, out of reach of children.

Shelf life

Shelf life is 3 years.

Conditions of dispensing from pharmacies

The drug is available with a prescription.