Valparin HR

General characteristics. Structure:

Active ingredient: tablets on 300 mg: 200 mg of Valproatum of sodium, 87 mg of valproic acid (together there correspond 300 mg of Valproatum of sodium); tablets on 500 mg: 333 mg of Valproatum of sodium, 145 mg of valproic acid (together there correspond 500 mg of Valproatum of sodium).

Excipients: colloid silicon dioxide, hydroxypropyl, methyl cellulose, ethyl cellulose, hydrate of silicon dioxide, sodium saccharin.

Pharmacological properties:

Sodium Valproatum increases the maintenance of GABA (gamma аминобутировой acids) in a brain that respectively increases the maintenance of GABA in postsynaptic neurons. Besides, sodium Valproatum influences transfer of potassium ions through membranes of neurons. The cart of action is result of similar emergence suppression, and also distribution of epileptic excitement on neurons.

Pharmacodynamics. Valproatum has anticonvulsant activity at various types of epilepsy at people. Drug does not possess expressed somnolent and sedative by effects, and also does not depress a respiratory center. Valparin of HR has no negative effect on the arterial pressure, heart rate, function of kidneys and body temperature.

Firmakokinetika. Bioavailability of drug - about 100%. Peak concentration in plasma are reached within 2-8 hours after oral administration of tablets with controlled release. 80-90% of drug contact proteins of a blood plasma, time of semi-removal makes about 8-20 hours (at children well). The therapeutic effectiveness is shown at concentration of valproic acid in a blood plasma of 40-100 mg/l. At the same time pharmacological and therapeutic effects of drug with controlled release not always depends on its concentration in plasma. Distribution volume – 0,2 liters/kg of body weight. Drug is metabolized in a liver and removed with urine. For this drug presistemny metabolism is noted.

Indications to use:

Treatment of generalized or partial epilepsy, especially at the following types of attacks:

• absentias epileptica;
• myoclonic;
• toniko-clonic;
• atonic.

Partial epilepsy:
• the simple or combined attacks;
• secondary generalized attacks.

Specific syndromes (Vest, Lennox-Gasto).

Route of administration and doses:

The mode of dosing is selected individually depending on age and the body weight of the patient.

Adults: an initial dose – 600 mg/day. To increase a dosage by 200 mg each three days before achievement of optimum effect.

Tablets should be swallowed entirely, washing down with a small amount of water. To accept 1-2 times a day. Most recommended dose of 1-2 g.

To children with body weight over 20 kg: an initial dose – 400 mg/day. To raise a dosage gradually to achievement optimum, usually 20-30 mg/kg once a day or in two separate doses.

To children with body weight to 20 kg: it is not necessary to apply Valparin HR to children of this category.

Elderly patients: The dosing mode Valparin is similar HR to the dosing mode at adults and is selected individually.

Features of use:

It is necessary to be careful during the work with mechanisms since drug weakens attention. Regular monitoring procedure of level of transaminases, bilirubin, thrombocytes of blood, amylase (each 3 months) is necessary.

Valproic acid inhibits aggregation of thrombocytes that increases risk of increase in a blood coagulation at bleedings. It is necessary to consider a possibility of development of the complications connected with bleeding at the operated patients receiving HR Valproatum. At patients, it is long accepting drug, development of spontaneous hematomas and bleedings is possible. In that case it is necessary to stop administration of drug immediately.

Valproatum can cause medicinal pancreatitis and an abnormal liver function (usually in the first 6 months of use). In this regard it is necessary to control a condition of a pancreas within the first 6 months of treatment, to carry out hepatic tests, to watch prothrombin level. The abnormal liver function, a liver failure during therapy by Valproatum is sometimes observed at children with epilepsy and the combined metabolic and degenerative diseases, organic pathology of brain fabric and the slowed-down intellectual development. At emergence of such symptoms as the expressed weakness, a lethargic state, puffiness, vomiting and jaundice, it is necessary to stop drug use immediately.

Use at pregnancy and a lactation. Purpose of drug to pregnant women is possible only in case the estimated advantage for mother exceeds potential risk for a fruit. In case of administration of drug at pregnancy carrying out specialized prenatal observation of a fruit is obligatory. Use of drug during breastfeeding is not recommended.

Side effects:

It was in rare instances reported about emergence of the following side effects: nausea, vomiting, diarrhea and/or lock; hepatitis; pancreatitis; increase in body weight, skin rash, itch, photosensitization, multiformny erythema, Stephen-Johnson's syndrome; a hair loss (at 2-12% of patients); ataxy, tremor, disturbance of consciousness, lump; disturbances of a menstrual cycle, secondary amenorrhea; anemia, hypercreatinemia, thrombocytopenia, neutropenia, leukopenia, decrease in content of fibrinogen, braking of aggregation of thrombocytes.

Interaction with other medicines:

Valproatum strengthens effect of antipsychotic drugs, anticonvulsant drugs and antidepressants.

Unlike other anticonvulsant drugs Valproatum does not cause induction of liver enzymes therefore does not reduce efficiency of oral contraceptives.

At combined use of Valproatum and warfarin the percent of linkng with proteins of a blood plasma of the last decreases.

Valproatum changes plasma concentration of Phenytoinum and lamotridzhin.

In combination with anticoagulants and derivatives of acetylsalicylic acid braking of aggregation of thrombocytes increases.

Contraindications:

Individual intolerance drug, the expressed dysfunctions of a pancreas, acute or chronic hepatitis, cases of active hepatitis in the family anamnesis, first of all medicinal genesis, pregnancy, a lactation, a porphyria, thrombocytopenia, children's age up to 3 years.

Overdose:

It was reported about exceptional cases of accidental or deliberate overdose of drug. At the same time nausea, vomiting, dizziness, diarrhea, respiratory depression, a hyporeflexia, coma was observed.

First aid: gastric lavage, reception of absorbent carbon. If necessary – hospitalization with use of symptomatic therapy, a hemodialysis.

Storage conditions:

To store at a temperature below 30 °C in the place protected from moisture. To store in the place, unavailable to children. A period of validity - 3 years. Not to use after the term specified on packaging.

Issue conditions:

According to the recipe

Packaging:

10 tablets in a strip from aluminum foil. 3 strips or 10 strips with the application instruction are packed into a cardboard pack. A sample not for sale: 4 or 10 tablets in a strip from aluminum foil; 1 strip with the application instruction is packed into a cardboard pack.