Convulex - instructions for use, reviews, analogs and formulations (tablets and capsules 150 mg, 300 mg and 500 mg retard, drops, syrup, injections for injections) for the treatment of epilepsy, seizures in adults, children and pregnancy

In this article, you can read the instructions for using the drug Convoolex. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Convulex 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 Convulex in the presence of existing structural analogues.Use for the treatment of epilepsy, seizures, seizures in adults, children, as well as during pregnancy and lactation.

Convoolex antiepileptic drug. It also has a central muscle relaxant and sedative effect.

The mechanism of action is mainly due to an increase in the GABA content in the CNS due to inhibition of the GABA-transferase enzyme. GABA reduces the excitability and convulsive readiness of the motor zones of the brain. In addition, the action of valproic acid on the GABAA receptors (activation of GABA-ergic transfer), as well as the effect on the voltage-dependent sodium channels, play an important role in the mechanism of action of the drug. According to another hypothesis, it acts on the sites of postsynaptic receptors, imitating or enhancing the inhibitory effect of GABA. A possible direct effect on membrane activity is associated with changes in conductivity for potassium ions. It improves the mental state and mood of patients, has antiarrhythmic activity.

Composition

Valproic acid + auxiliary substances (capsules, solution for intravenous administration).

Valproate sodium + excipients (tablets, drops, syrup).

Pharmacokinetics

Valproic acid is almost completely absorbed from the digestive tract, the bioavailability when ingested is 100%. Eating does not reduce the absorption rate. Values ​​of concentration in the cerebrospinal fluid correlate with the value of the fraction of the active substance not associated with proteins. Valproic acid penetrates the placental barrier, excreted in breast milk. Concentration in breast milk is 1-10% concentration in the blood plasma of the mother. Valproic acid is subjected to glucuronidation and oxidation in the liver. Valproic acid (1-3% of the dose) and its metabolites are excreted by the kidneys, small amounts - with feces and exhaled air.

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 convulsions in children, children's teak;
• treatment and prevention of bipolar affective disorders.

Forms of release

Capsules 150 mg, 300 mg and 500 mg.

Tablets of prolonged retard action of 300 mg and 500 mg.

Drops for oral administration.

Syrup for children.

Solution for intravenous administration (injections in ampoules for injection).

Instructions for use and dosage

Capsules

Capsules are taken orally, without chewing, 2-3 times a day, during or immediately after a meal, with a small amount of water.

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

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

The recommended daily dose is about 1-2 g, i.е. 20-25 mg / kg. If necessary, the dose may be increased to a maximum dose of 2.5 g per day (30 mg / kg).

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

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

Children with a body weight of more than 25 kg are prescribed in an initial dose of 300 mg per day (5-15 mg / kg per day), with a gradual increase of 5-10 mg / kg per week to achieve a clinical effect (disappearance of seizures), with a dose , as a rule, is 1-1.5 g per day (20-30 mg / kg per day).

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

For children weighing 7.5-25 kg with monotherapy, the average dose is 15-45 mg / kg per day, the maximum - 50 mg / kg per day. With combined therapy, 30-100 mg / kg per day.

Retard tablets

Tablets of prolonged action are taken orally, without chewing, 1-2 times a day, during or immediately after a meal, with a small amount of water.

Adults are given an initial dose of 600 mg per day with a gradual increase every 3 days until the clinical effect (disappearance of seizures) is reached.

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

The recommended daily dose is about 1-2 g, i.е. 20-30 mg / kg. If necessary, the dose can be increased to 2.5 g per day (30 mg / kg per day).

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

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

Children with a body weight of more than 25 kg are prescribed in an initial dose of 300 mg per day (5-15 mg / kg per day), with a gradual increase of 5-10 mg / kg per week to achieve a clinical effect (disappearance of seizures), with a dose , as a rule, is 1-1.5 g per day (20-30 mg / kg per day).

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

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

Although the pharmacokinetics of valproic acid in the elderly may have its own peculiarities, this is of limited clinical importance, and the dose should be determined by the clinical effect. Due to a decrease in binding to serum albumin, the proportion of unbound preparation in plasma increases. This causes the expediency of a more careful selection of the dose of the drug in the elderly, with the possible use of smaller doses of the drug.

Syrup

Children with a body weight of more than 25 kg are prescribed in an initial dose of 300 mg per day with a gradual increase to the clinical effect (disappearance of seizures), with the dose, as a rule, 20-30 mg / kg per day.

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

The maximum dose is 30 mg / kg per day (can be increased to 60 mg / kg per day under the control of the concentration of valproic acid in blood plasma).

For children weighing 7.5-25 kg with monotherapy, the average dose is 15-45 mg / kg per day, the maximum - 50 mg / kg per day. With combined therapy, 30-100 mg / kg per day.

Ampoules

The drug is administered intravenously (slowly) or infuzionno.

The recommended daily dose for intravenous administration is 5-10 mg of sodium valproate / kg body weight.

With IV infusion introduction, the recommended dose is 0.5-1 mg of sodium valproate / kg body weight / h.

When switching from oral to intravenous administration, the dose does not change, the first IV administration is recommended 12 hours after the last oral ingestion. The injection solution for injection should be replaced by taking the drug inside, as soon as the patient's condition allows it. The first intake is also recommended 12 hours after the last injection.

If you need to quickly achieve and maintain a high concentration in the plasma, the following dosing regimen is recommended: intravenous administration at a dose of 15 mg / kg for 5 minutes, after 30 minutes to begin infusion at a rate of 1 mg / kg / h with constant monitoring of concentration to a level in plasma of about 75 μg / ml.

The maximum daily dose of the drug should not exceed 2500 mg.

The average daily doses are 20 mg / kg in adults (including elderly patients), 25 mg / kg in adolescents, and 30 mg / kg in children.

As an infusion solution for Convulex, isotonic sodium chloride solution, 5% glucose solution, Ringer's solution can be used.The prepared infusion solution can be used for 24 hours, the unused volume of the solution is destroyed. If IV drugs are used, Convulex should be administered on a separate infusion system.

Side effect

• nausea, vomiting;
• gastralgia;
• decreased or increased appetite;
• diarrhea, constipation;
• pancreatitis;
• tremor;
• diplopia;
• nystagmus;
• flickering flies before your eyes;
• behavior changes;
• mood or mental state (depression, fatigue, hallucinations, aggressiveness, hyperactive state, psychoses, unusual arousal, motor anxiety or irritability);
• ataxia;
• dizziness;
• drowsiness;
• headache;
• encephalopathy;
• dysarthria;
• enuresis;
• stupor;
• impaired consciousness;
• coma;
• anemia, leukopenia, thrombocytopenia;
• decrease in fibrinogen content and platelet aggregation, leading to the development of hypocoagulation (accompanied by prolonged bleeding time, petechial hemorrhages, bruising, bruising, bleeding);
• decrease or increase in body weight;
• dysmenorrhea;
• secondary amenorrhea;
• increased mammary glands;
• galactorrhea;
• hyperbilirubinemia;
• skin rash;
• hives;
• angioedema;
• photosensitization;
• malignant exudative erythema (Stevens-Johnson syndrome);
• peripheral edema;
• loss of hair (usually restored after the drug is discontinued).

Contraindications

• liver failure;
• acute and chronic hepatitis;
• impaired pancreatic function;
• porphyria;
• hemorrhagic diathesis;
• severe thrombocytopenia;
• disorders of urea metabolism (including in family history);
• combination with mefloquine, St. John's wort, perforated, lamotrigine;
• 1 trimester of pregnancy (for syrup);
• lactation period;
• children's age up to 3 years (for capsules, tablets);
• increased sensitivity to valproic acid and its salts or components of the drug.

Application in pregnancy and lactation

During treatment with the drug, Convulex should be protected from pregnancy.

In the first trimester of pregnancy, do not start treatment with Conlevix. If the pregnant woman is already receiving the drug, then due to the risk of more seizures, treatment should not be interrupted. The drug should be used at the lowest effective dose, avoiding the combination with other anticonvulsants and, if possible, regularly monitoring the level of the drug in the plasma.

In experimental animal studies, the teratogenic effect of valproic acid has been revealed.

The frequency of neural tube defects in children born to women taking valproate in the first trimester of pregnancy is 1-2%. It is advisable in this regard, the use of folic acid preparations.

During the lactation period, the use of the preparation of Convulex is contraindicated. At the same time, breastfeeding is possible, because the concentration in breast milk does not exceed 1-10% of the level of the drug in the blood plasma of the mother.

Use in children

Contraindicated in children under 3 years (for tablets with prolonged action and capsules).

special instructions

In connection with the available reports of severe and lethal cases of hepatic insufficiency and pancreatitis with the use of valproic acid preparations, it is necessary to bear in mind the following:

• High-risk groups are infants and children under 3 years of age, with severe epilepsy, often associated with brain damage and congenital metabolic or degenerative diseases;
• in most cases, liver function abnormalities developed in the first 6 months (usually between 2 and 12 weeks) of treatment, more often with combined antiepileptic treatment;
• cases of pancreatitis were observed irrespective of the patient's age and duration of treatment, although the risk of developing pancreatitis decreased with the age of the patient;
• Lack of liver function in pancreatitis increases the risk of death;
• early diagnosis (before the icteric stage) is based mainly on clinical observation - the detection of early symptoms such as asthenia, anorexia, extreme fatigue, drowsiness, sometimes accompanied by vomiting and abdominal pain; with the recurrence of epileptic seizures against a background of unchanged antiepileptic therapy.

In such cases, you should immediately consult a doctor for clinical examination and liver function analysis.

During treatment, especially in the first 6 months, it is necessary to periodically check the liver function - the activity of hepatic transaminases, the level of prothrombin, fibrinogen, coagulation factors, bilirubin concentration, and amylase activity (every 3 months, especially when combined with other antiepileptic drugs) and a picture of peripheral blood, in particular, blood platelets.

Patients who receive other antiepileptic drugs, transfer to admission valproic acid should be carried out gradually, reaching a clinically effective dose after 2 weeks, after which a gradual cancellation of other antiepileptic drugs is possible. In patients who were not treated with other antiepileptic drugs, a clinically effective dose should be achieved after 1 week.

The risk of developing side effects from the liver is increased when combined anticonvulsant therapy, as well as in children. Do not drink drinks containing ethanol (alcohol).

Before the surgical intervention, a general blood test (including platelet numbers), bleeding time, coagulogram indices is required.

If there is a "acute abdomen" symptom complex before treatment, it is recommended to determine the activity of amylase in the blood to exclude acute pancreatitis.

During treatment it is necessary to take into account the possible distortion of the results of urinalysis in diabetes mellitus (due to an increase in the content of ketone bodies), thyroid function indices.

With the development of any acute serious side effects, it is necessary to immediately discuss with the doctor the advisability of continuing or discontinuing treatment.

To reduce the risk of developing dyspeptic disorders, it is possible to take antispasmodics and enveloping agents.

A sharp discontinuation of the use of Convulex can lead to an increase in epileptic seizures.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Drug Interactions

Contraindications

Meflohin. The risk of epileptic seizures is due to the increased metabolism of valproic acid and a decrease in its plasma concentration and, on the other hand, the convulsant effect of mefloquine.

Saint John's wort. The risk of a decrease in the concentration of valproic acid in the blood plasma.

Unrecommended combinations

Lamotrigine. Increased risk of severe skin reactions (toxic epidermal necrolysis).Valproic acid inhibits microsomal liver enzymes that provide lamotrigine metabolism, which slows its T1 / 2 to 70 hours in adults and up to 45-55 hours in children and increases plasma concentration. If a combination is necessary, careful clinical and laboratory testing is required.

Combinations that require special precautions

Carbamazepine. Convulex increases the concentration of the active metabolite of Carbamazepine in plasma to signs of overdose. In addition, carbamazepine increases the hepatic metabolism of valproic acid and reduces its concentration. These circumstances require the attention of the doctor and the determination of the concentrations of drugs in the plasma and the possible revision of their doses.

Phenobarbital, primidon. Valproic acid increases the concentration of Phenobarbital or primidone in plasma to signs of overdose, more often in children. In turn, phenobarbital or primidone increases the hepatic metabolism of valproic acid and reduces its concentration. Clinical observation is recommended during the first 2 weeks of combined treatment with an immediate reduction in the dose of phenobarbital or primidon when signs of sedative action appear, and the level of anticonvulsants in the blood is determined.

Phenytoin. Variations in the concentration of phenytoin in the plasma are possible, phenytoin increases the hepatic metabolism of valproic acid and reduces its concentration. Clinical observation is recommended, the level of anticonvulsants in the blood is determined, and the dosage is changed if necessary.

Clonazepam. Addition of valproic acid to Clonazepam in single cases can lead to an increase in the expression of absent status.

Ethosuximide. Convulex can both increase and decrease the concentration of ethosuximide in the blood serum due to a change in its metabolism. Clinical observation is recommended, the level of anticonvulsants in the blood is determined, and the dosage is changed if necessary.

Topiramate. The risk of hyperammonemia and encephalopathy increases.

Felbamat. An increase in the concentration of valproic acid in plasma by 35-50%, with the risk of overdose. Clinical observation, valproate acid level in the blood, change in the dosage of valproic acid when combined with felbamate and after its cancellation is recommended.

Neuroleptics, MAO inhibitors, antidepressants, benzodiazepines.Neuroleptics, tricyclic antidepressants, MAO inhibitors that reduce the threshold of convulsive readiness, reduce the effectiveness of the drug. In turn, valproic acid potentiates the effect of these psychotropic drugs, as well as benzodiazepines.

Cimetidine, erythromycin. Suppress the hepatic metabolism of valproic acid and increase its concentration in the plasma.

Zidovudine. Valproic acid increases the concentration of zidovudine in the plasma, which leads to an increase in its toxicity.

Carbapenems, monobactams. Meropenem, panipenem, as well as aztreonam and imipenem reduce the concentration of valproic acid in the plasma, which can lead to a decrease in the anticonvulsant effect.

Combinations that should be taken into account

Acetylsalicylic acid. Strengthening the effects of valproic acid due to its displacement from the bond with plasma proteins. Valproic acid enhances the effect of acetylsalicylic acid.

Indirect anticoagulants. Valproic acid increases the effect of indirect anticoagulants, careful monitoring of the prothrombin index is required when co-administered with vitamin K-dependent anticoagulants.

Nimodipine.Strengthening the hypotensive effect of nimodipine due to an increase in its concentration in the plasma due to the suppression of its metabolism with valproic acid.

Myelotoxic drugs. Increased risk of oppression of bone marrow hematopoiesis.

Ethanol (alcohol) and hepatotoxic drugs. Increase the likelihood of liver damage.

Other combinations

Oral contraceptives. Valproic acid does not induce the induction of microsomal liver enzymes and does not reduce the effectiveness of hormonal oral contraceptives.

Analogues of the drug Konvuleks

Structural analogs for the active substance:

• Valparin;
• Valproate sodium;
• Valproic Acid Sandoz;
• Depakin;
• Depakin chrono;
• Depakin Chronosphere;
• Depakin enteric;
• Dipromal;
• Convulsofin;
• Enkorat;
• Enkorat is chrono.

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