Depakin - instructions for use, reviews, analogs and formulations (syrup, granules 100 mg, 250 mg, 500 mg, 750 mg and 1000 mg Chronosphere, 300 mg tablets Enteric and Chrono, injections) drugs for the treatment of epilepsy in adults, children and during pregnancy

In this article, you can read the instructions for using the drug Depakin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Depakin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Depakin in the presence of existing structural analogues. Use for the treatment of epilepsy, tic and manic-depressive psychosis in adults, children, as well as during pregnancy and lactation.

Depakin antiepileptic agent. It is believed that the mechanism of action is associated with an increase in GABA in the central nervous system, which is due to inhibition of GABA transaminase, as well as a decrease in GABA reuptake in the brain tissues. This, apparently, leads to a decrease in excitability and convulsive readiness of the motor zones of the brain. Promotes improvement of mental state and mood of patients.

Composition

Valproate sodium + excipients.

Sodium valproate + Valproic acid + auxiliary substances (Chronospher granules and Chrono tablets).

Pharmacokinetics

The bioavailability of valproate for oral administration is close to 100%. Eating does not affect the pharmacokinetic profile. Binding to plasma proteins is high, dose-dependent and saturable. Valproate penetrates into the cerebrospinal fluid and into the brain. Valproate is mainly excreted in the urine in the form of glucuronide.

Indications

In adults (as a monotherapy or in combination with other antiepileptic drugs):

• for the treatment of generalized epileptic seizures: clonic, tonic, tonic-clonic, absences, myoclonic, atonic; the Lennox-Gastaut syndrome;
• for the treatment of partial epileptic seizures: partial seizures with or without secondary generalization;
• manic-depressive psychosis with a bipolar course, not amenable to treatment with lithium drugs or other drugs;
• the Lennox-Gastaut syndrome.

In infants (starting at 6 months of age) and children (as monotherapy or in combination with other antiepileptic drugs):

• for the treatment of generalized epileptic seizures: clonic, tonic, tonic-clonic, absences, myoclonic, atonic; the Lennox-Gastaut syndrome;
• for the treatment of partial epileptic seizures: partial seizures with or without secondary generalization;
• prevention of seizures at high temperature, when such prophylaxis is necessary;
• the Lennox-Gastaut syndrome;
• children's teak.

Forms of release

Granules of prolonged action of 100 mg, 250 mg, 500 mg, 750 mg and 1000 mg (Depakin Chronosphere).

Tablets of prolonged action, coated with 300 mg and 500 mg (Chrono).

Syrup (the ideal children's form of the drug).

Tablets coated with 300 mg (Enteric).

Lyophilizate for the preparation of a solution for intravenous administration (injections in ampoules for injections).

Instructions for use and how to use them

Individual. For oral administration in adults and children with a body weight of more than 25 kg, the initial dose is 10-15 mg / kg per day. Then the dose is gradually increased by 200 mg per day with an interval of 3-4 days until the clinical effect is achieved. The average daily dose is 20-30 mg / kg. For children weighing less than 25 kg and newborns, the average daily dose is 20-30 mg / kg.

The frequency of reception - 2-3 times a day during meals.

Intravenously (in the form of sodium valproate) is administered at a dose of 400-800 mg or drip at a rate of 25 mg / kg for 24, 36 and 48 hours. If it is necessary to use concomitantly intravenously and intravenously, the first administration is carried out by iv infusion in a dose 0.5-1 mg / kg / h 4-6 hours after the last oral administration.

Maximum doses: when ingested for adults and children weighing more than 25 kg - 50 mg / kg per day. Use in a dose of more than 50 mg / kg per day is possible under the condition of monitoring the concentration of valproate in the blood plasma. At a plasma concentration of more than 200 mg / l, the dose of valproic acid should be reduced.

Syrup

Inside (1 double-sided dosing spoon of syrup contains sodium valproate 100 or 200 mg). The initial daily dose is 10-15 mg / kg, then the doses are gradually increased to optimal concentrations.

Usually the optimal dose is 20-30 mg / kg.However, if the seizures do not stop, the dose can be adequately increased; It requires careful monitoring of patients receiving doses above 50 mg / kg.

Children the usual dose is approximately 30 mg / kg per day.

Adults - 20-30 mg / kg per day.

Depakin syrup can be administered twice a day.

Chronosphere granules

Depakine Chronosphere is a dosage form that is especially suitable for treating children (if they are able to swallow soft food) or adults with difficulty swallowing.

The drug is prescribed inside. The daily dose is determined depending on the age and body weight of the patient, and a wide range of individual sensitivity to valproate should also be taken into account.

The initial daily dose is 10-15 mg / kg of body weight, then it is increased by 5-10 mg / kg per week until the optimal dose is reached.

The average daily dose is 20-30 mg / kg. It is possible to increase the dose of the drug with careful monitoring of the patient's condition, if epilepsy can not be controlled with the use of daily average doses.

The average daily intake for adults is 20 mg / kg; for adolescents - 25 mg / kg; for children, incl. thoracic (starting from the 6th month of life) - 30 mg / kg.

Application rules

Depakin Chronosphere in sachets of 100 mg is used only in children and infants. Depakin Chronosphere in bags of 1 g is used only in adults.

The daily dose should be taken in 1 or 2 doses, preferably during meals. Use in 1 reception is possible with well-controlled epilepsy.

The contents of the sachet should be poured on the surface of soft food or drinks cold or at room temperature (including yogurt, orange juice, fruit puree, etc.). If Depakin Chronosphere is taken with a liquid, it is recommended to rinse the glass with a little water and drink this water. The granules can stick to the glass. The mixture should always be swallowed immediately, without chewing. It should not be stored for later use.

The drug Depakin Chronosphere can not be used with hot food or drinks (such as soups, coffee, tea, etc.). Preparation Depakin Chronosphere can not be poured into a bottle with a pacifier, tk. The granules can clog the nipple opening.

Considering the duration of the process of releasing the active substance and the nature of the auxiliary substances, the inert matrix of the granule is not absorbed from the digestive tract; it is excreted with feces after complete release of the active substance.

Chrono tablets

Depakin Chrono is a sustained-release dosage form that provides more uniform concentrations during the day compared to conventional Depakin dosage forms.

The drug is taken orally. The daily dose should be taken in 1 or 2 doses, preferably during meals.

The dose should be set according to the age and body weight of the patient, and also taking into account individual sensitivity to the drug.

A good correlation between the daily dose, the concentration of the drug in the serum and the therapeutic effect is established, so the optimal dose should be determined depending on the clinical response. Determining the concentration of valproic acid in plasma can be considered as an adjunct to clinical monitoring when epilepsy is not amenable to control or there is a suspicion of side effects. The concentration range at which the clinical effect is observed is usually 40-100 mg / l (300-700 μmol / l).

For adults and children weighing more than 17 kg, the initial daily dose is usually 10-15 mg / kg of body weight, then the dose is increased to the optimum. The average dose is 20-30 mg / kg per day.If there is no therapeutic effect (if the seizures do not stop), the dose can be increased; careful monitoring of the patient's condition is necessary.

For children aged 6 years and older, the average daily dose is 30 mg / kg.

In elderly patients, the dose should be adjusted according to their clinical condition.

Tablets are taken without crushing or chewing them.

Use in 1 reception is possible with well-controlled epilepsy.

When switching from immediate release valproate tablets, which provided the necessary control over the disease, a sustained release form (Depakin Chrono) should be maintained at a daily dose.

The replacement of other antiepileptic drugs by Depakin Chrono should be carried out gradually, reaching the optimal dose of valproate for about 2 weeks. Depending on the patient's condition, the dose of the previous drug is reduced.

For patients who do not take other antiepileptic drugs, the dose should be increased after 2-3 days in order to reach the optimal dose within about a week.

If necessary, the combination with other anticonvulsants against the background of the use of Depakin Chrono, such drugs should be administered gradually.

Side effect

• trembling of hands or hands;
• changes in behavior, mood or mental state;
• nystagmus;
• spots before the eyes;
• violations of coordination of movements;
• dizziness;
• drowsiness;
• headache;
• unusual agitation;
• motor anxiety;
• irritability;
• weak cramping in the abdomen or in the stomach;
• loss of appetite;
• diarrhea;
• digestive disorders;
• nausea, vomiting;
• constipation;
• thrombocytopenia, prolonged bleeding time;
• unusual decrease or increase in body weight;
• menstrual cycle disorders;
• alopecia;
• skin rash.

Contraindications

• violations of the liver and pancreas;
• hemorrhagic diathesis;
• acute and chronic hepatitis;
• porphyria;
• children's age up to 6 months (granules); Children under 6 years of age for tablets (risk of getting into the respiratory tract when swallowing);
• increased sensitivity to valproic acid.

Application in pregnancy and lactation

Application in pregnancy is not recommended. It should be borne in mind that valproic acid can cause various congenital anomalies, especially spina bifida.

Valproic acid is excreted in breast milk. There are reports that the concentrations of valproate in breast milk were 1-10% of the concentration in the blood plasma of the mother. During lactation, the application is possible in cases of extreme necessity.

Women of childbearing age during the period of treatment are recommended to use reliable methods of contraception.

Use in children

Children are at increased risk for developing severe or life-threatening hepatotoxic effects. In patients under 2 years of age and in children receiving combination therapy, the risk is even higher, but with increasing age, it decreases

special instructions

They are used with caution in patients with pathological changes in blood, with organic brain diseases, liver diseases in history, hypoproteinemia, renal dysfunction.

Patients who receive other anticonvulsants, treatment with valproic acid should be started gradually, reaching a clinically effective dose in 2 weeks. Then, a gradual cancellation of other anticonvulsants is carried out.In patients who have not been treated with other anticonvulsants, a clinically effective dose should be achieved after 1 week.

It should be borne in mind that the risk of side effects from the liver is elevated when combined anticonvulsant therapy is performed.

During the treatment it is necessary to regularly monitor liver function, the picture of peripheral blood, the state of the blood coagulation system (especially during the first 6 months of treatment).

Children are at increased risk for developing severe or life-threatening hepatotoxic effects. In patients under 2 years of age and in children receiving combination therapy, the risk is even higher, but with increasing age, it decreases.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, care should be taken when driving vehicles and other activities requiring high concentration of attention and rapid psychomotor reactions.

Drug Interactions

With the simultaneous use of neuroleptics, antidepressants, MAO inhibitors, benzodiazepine derivatives, ethanol (alcohol), the oppressive effect on the central nervous system increases.

At simultaneous application of the means possessing hepatotoxic action, strengthening of a hepatotoxic action is possible.

With simultaneous use, the effects of antiplatelet agents (including acetylsalicylic acid) and anticoagulants are enhanced.

With simultaneous use, the concentration of zidovudine in the blood plasma increases, which leads to an increase in its toxicity.

With simultaneous use with carbamazepine, the concentration of valproic acid in the blood plasma decreases due to an increase in the rate of its metabolism, caused by the induction of microsomal enzymes of the liver under the influence of carbamazepine. Valproic acid potentiates the toxic effect of carbamazepine.

With simultaneous use, metabolism of lamotrigine is slowed down.

With simultaneous use with mefloquine, the metabolism of valproic acid in the blood plasma increases and the risk of seizures increases.

With simultaneous use with meropenem, a decrease in the concentration of valproic acid in the blood plasma is possible; with primidon - an increase in the concentration of primidone in blood plasma; with salicylates - it is possible to enhance the effects of valproic acid due to its displacement by salicylates from the connection with plasma proteins.

With simultaneous application with felbamate, the concentration of valproic acid in the blood plasma increases, which is accompanied by manifestations of toxic effects (nausea, drowsiness, headache, decrease in the number of platelets, cognitive impairment).

With the simultaneous use of Depakin with phenytoin for the first few weeks, the total concentration of phenytoin in the blood plasma may decrease due to its displacement from the sites of binding to plasma proteins by sodium valproate, induction of microsomal enzymes of the liver and acceleration of the metabolism of phenytoin. Then there is an inhibition of the metabolism of phenytoin by valproate and, as a result, an increase in the concentration of phenytoin in the blood plasma. Phenytoin reduces the concentration of valproate in the blood plasma, probably due to an increase in its metabolism in the liver. It is believed that phenytoin as an inducer of hepatic enzymes may also increase the formation of a secondary but hepatotoxic metabolite of valproic acid.

With the simultaneous use of valproic acid displaces Phenobarbital from the connection with plasma proteins, as a result, its concentration in the blood plasma increases.Phenobarbital increases the metabolic rate of valproic acid, which leads to a decrease in its concentration in the blood plasma.

There have been reports of increased effects of fluvoxamine and Fluoxetine when used concomitantly with valproic acid. With simultaneous use with fluoxetine, some patients experienced an increase or decrease in the concentration of valproic acid in the blood plasma.

With the simultaneous use of cimetidine, erythromycin, it is possible to increase the concentration of valproic acid in the plasma by reducing its metabolism in the liver.

Analogues of the drug Depakin

Structural analogs for the active substance:

• Valparin;
• Valproate sodium;
• Depakin chrono;
• Depakin Chronosphere;
• Depakin enteric 300;
• Dipromal;
• Convulex;
• Convulsofin;
• Enkorat;
• Enkorat is chrono.

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