Valparin XP, 500 mg 30 pcs

Sodium valproate has anticonvulsant activity in various types of epilepsy in humans. The drug does not have pronounced hypnotic and sedative effects and has no depressant effect on the respiratory center. Valproate sodium has no adverse effect on BP, HR, renal function and body temperature.

Sodium valproate increases gamma-aminobutyric acid (GABA) levels in the brain, which consequently increases GABA levels in postsynaptic neurons. In addition, sodium valproate affects the transport of potassium ions across neuronal membranes. The result is the suppression of development as well as the spread of epileptic excitation through neurons.

Pharmacokinetics

Intake

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

Therapeutic efficacy is seen at plasma concentrations of valproic acid 40-100 mg/l. The pharmacological and therapeutic effects of this controlled-release drug are not always dependent on its plasma concentration.

Distribution

The binding to plasma proteins is 80-90%.

Vd is 0.2 l/kg.

Metabolism and excretion

Metabolized in the liver and excreted in the urine. No presystemic metabolism is noted. T1/2 is approximately 8-20 h.

Pharmacokinetics in special clinical cases

The T1/2 is decreased in children.

Indications

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

Partial epilepsy:

Specific syndromes (West, Lennox-Gasto).

Active ingredient

Composition

1 tabletcalproate 333 mg

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

Excipients:

colloidal silicon dioxide,

hydroxypropyl methylcellulose,

How to take, the dosage

The dosing regimen is adjusted individually depending on the patient’s age and body weight.

In adults, the initial dose is 600 mg/day with subsequent dose increases by 200 mg every 3 days until optimal effect is achieved. The frequency of administration is 1-2 times a day. The maximum recommended dose is 1-2 g/day.

The tablets should be swallowed whole with a small amount of water.

In elderly patients the dosing regimen of Valparin XP is similar to that of adults and is individualized.

In children with a body weight of 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.

In children weighing less than 20 kg, Valparin XP should not be used.

Interaction

Sodium valproate increases the effect of antipsychotic drugs, anticonvulsants and antidepressants. Unlike other anticonvulsants, sodium valproate does not cause induction of hepatic enzymes, so it does not reduce the effectiveness of oral contraceptives.

When co-administration of sodium valproate and warfarin the percentage of binding to plasma proteins of the latter decreases.

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

Special Instructions

Transaminases, bilirubin, blood platelets, and amylase should be monitored regularly (every 3 months).

Valproic acid inhibits platelet aggregation, which increases the risk of increased clotting time in bleeding. The possibility of complications associated with bleeding in the postoperative period in patients receiving sodium valproate should be considered. When prolonged administration of sodium valproate, spontaneous hematomas and bleeding may develop. In this case, the drug should be stopped immediately.

Sodium valproate may cause drug-induced pancreatitis and impaired liver function (usually in the first 6 months of use). In this regard, during the first 23 months of treatment it is necessary to monitor the condition of the pancreas, conduct hepatic tests, monitor prothrombin levels. Hepatic dysfunction, liver failure during therapy with sodium valproate are sometimes observed in children with epilepsy and combined metabolic and degenerative diseases, organic pathology of brain tissue and delayed mental development. If symptoms such as marked weakness, lethargy, edema, vomiting and jaundice occur, the drug should be stopped immediately.

Impact on driving and operating machinery

The patient should use caution when operating machinery because the drug reduces the ability to concentrate.

Contraindications

Side effects

The digestive system: rarely – nausea, vomiting, diarrhea and/or constipation, hepatitis, pancreatitis.

Allergic reactions: rare – skin rash, itching, photosensitization, erythema multiforme, Stevens-Johnson syndrome.

CNS disorders: rarely – ataxia, tremor, impaired consciousness, coma.

Perior genital system disorders: rarely – menstrual cycle disorders, secondary amenorrhea.

Hematopoietic system: rarely – anemia, thrombocytopenia, neutropenia, leukopenia, decreased fibrinogen, inhibition of platelet aggregation.

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

Overdose

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

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

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

Pregnancy use

Prescription of the drug during pregnancy is possible only when the expected benefits to the mother exceed the potential risk to the fetus. If the drug is administered during pregnancy, specialized prenatal monitoring of the fetus is mandatory.

The use of the drug during breastfeeding is not recommended.

Perinent use in children

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

In children with a body weight of 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.

In children weighing less than 20 kg, Valparin XP should not be used.

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