Convulex pills 500mg №50

Coated Extended Release Tablets

Composition

1 tab. contains valproic acid 500 mg, excipients: citric acid monohydrate; ethyl cellulose; Eudragit RS30D; purified talc; colloidal anhydrous silicon; Magnesium stearate; Eudragit L30D; dibutyl phthalate; sodium carmellose; macrogol 6000; titanium dioxide; vanillin; simethicone

Packaging

50 pcs.

Mechanism of action

Convulex - antiepileptic drug. The mechanism of action is due to inhibition of the enzyme GABA-transferase and an increase in the content of GABA in the central nervous system. GABA prevents pre- and postsynaptic discharges and thus prevents the spread of seizure activity in the central nervous system. In addition, the effect of valproic acid on GABA A receptors, as well as the effect on voltage-dependent Na-channels, plays a significant role in the mechanism of the drug's action. According to another hypothesis, valproic acid acts on postsynaptic receptor sites, mimicking or enhancing the inhibitory effect of GABA. A possible direct effect on membrane activity is associated with changes in potassium permeability. Improves the mental state and mood of patients, has antiarrhythmic activity.

Indications and usage

• epilepsy of any genesis;
• epileptic seizures (including generalized and partial, as well as against the background of organic brain diseases);
• character and behavioral disorders associated with epilepsy;
• febrile seizures in children;
• manic-depressive syndrome with bipolar course, not amenable to treatment with lithium drugs or other drugs.

Contraindications

• hypersensitivity;
• severe disorders of the liver and / or pancreas;
• porphyria;
• severe thrombocytopenia;
• hemorrhagic diathesis;
• pregnancy (I term);
• breast-feeding.

Pregnancy and breastfeeding

During treatment should be protected from pregnancy. In animal experiments, the teratogenic effect of valproic acid was revealed. The incidence of neural tube defects in children born to women who took valproate in the first trimester of pregnancy is 1–2%. It is advisable in this regard, the use of drugs of folic acid. If the pregnant woman is already receiving the drug, then due to the risk of increased seizures, treatment should not be interrupted. The drug should be used in the lowest effective doses, avoiding combination with other anticonvulsants and, if possible, regularly controlling the level of the drug in the plasma. When lactation drug should be taken with caution. At the same time, breastfeeding is possible, because concentration in milk does not exceed 1-10% of the level of the drug in the blood plasma of the mother.

Dosage and Administration

The drug should be taken orally, regardless of the food, with a small amount of liquid, 2-3 times a day. For adults, the initial daily dose is 600 mg with a gradual increase in dose every 3 days until a clinical effect is achieved (the disappearance of seizures). With monotherapy, the initial dose is 5–15 mg / kg / day, then the dose is gradually increased by 5–10 mg / kg per week. The average daily dose is about 1000–2000 mg / day, i.e. 20–30 mg / kg. If necessary, increase the dose to 2500 mg / day. The maximum dose - 30 mg / kg / day (can be increased with the possibility of organizing control over plasma concentration up to 60 mg / kg / day). In combination therapy, 10–30 mg / kg / day, followed by an increase in dose of 5–10 mg / kg per week.

Adverse reactions

In general, Convulex well tolerated by patients. Side effects are possible mainly when the level of the drug in plasma is higher than 100 mg / l or in combination therapy.
On the part of the digestive tract: nausea, vomiting, gastralgia, anorexia or increased appetite, diarrhea, hepatitis; rarely - constipation, pancreatitis, up to severe lesions with a fatal outcome (in the first 6 months of treatment, usually for 2-12 weeks).
From the side of the central nervous system: tremor; rarely - changes in behavior, mood, or mental state (depression, fatigue, hallucinations, aggressiveness, hyperactive condition, psychosis, unusual agitation, restlessness or irritability), ataxia, dizziness, drowsiness, headache, encephalopathy, dysarthria, stupor, consciousness coma
Special senses: diplopia, nystagmus, flickering "fly" before his eyes.
From the side of blood-forming organs and hemostasis system: anemia, leukopenia, thrombocytopenia, a decrease in the content of fibrinogen, platelet aggregation and blood clotting, accompanied by prolonged bleeding time, petechial hemorrhages, hemorrhages, hematomas, hemorrhage, etc.
Metabolism: decrease or increase in body weight.
Allergic reactions: skin rash, urticaria, angioedema, photosensitivity, Stevens-Johnson syndrome.
Laboratory values: hypercreatininemia, hyperammonemia, hyperbilirubinemia, a slight increase in the activity of liver transaminases, LDH (dose-dependent).
On the part of the endocrine system: dysmenorrhea, secondary amenorrhea, breast enlargement, galactorrhea.
Other: peripheral edema, hair loss (usually stopped after drug withdrawal).

Special notes

During treatment, it is advisable to monitor the activity of “liver” transaminases, bilirubin level, peripheral blood pattern, blood platelets, the state of the blood coagulation system, amylase activity every 3 months (especially when combined with other antiepileptic drugs). Patients who receive other anti-epileptic drugs, transfer to the reception of valproic acid should be carried out gradually, reaching a clinically effective dose after 2 weeks, then the gradual cancellation of other anti-epileptic drugs is possible.In patients 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 anti-convulsant therapy is used in children. During the period of treatment, it is necessary to refrain from engaging in potentially hazardous activities that require high concentration of attention and quickness of psychomotor reactions. It is not allowed to accept beverages containing ethanol. Before surgery, a complete blood count is necessary (including platelet counts), bleeding time, and coagulogram values. If the symptoms of an acute abdomen occur during treatment, it is recommended to determine the level of amylase in the blood prior to the start of surgical intervention in order to rule out acute pancreatitis. During treatment, consideration should be given to the possible distortion of the results of urine tests for diabetes mellitus (due to an increase in ketoproducts), indicators of thyroid function. With the development of any acute serious side effects, you should immediately discuss with your doctor the appropriateness of continuing or stopping treatment. To reduce the risk of dyspeptic phenomena, it is possible to take antispasmodics and coating agents. Abrupt discontinuation of Konvuleks® can lead to an increase in epileptic seizures. During treatment, it is advisable to monitor the activity of liver transaminases, bilirubin level, peripheral blood pattern, blood platelets, the state of the blood coagulation system, amylase activity every 3 months (especially when combined with other antiepileptic drugs). Patients who receive other anti-epileptic drugs, transfer to the reception of valproic acid should be carried out gradually, reaching a clinically effective dose after 2 weeks, then the gradual cancellation of other anti-epileptic drugs is possible. In patients 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 anti-convulsant therapy is used in children. During the period of treatment, it is necessary to refrain from engaging in potentially hazardous activities that require high concentration of attention and quickness of psychomotor reactions. It is not allowed to accept beverages containing ethanol. Before surgery, a complete blood count is necessary (including platelet counts), bleeding time, and coagulogram values. If the symptoms of an acute abdomen occur during treatment, it is recommended to determine the level of amylase in the blood prior to the start of surgical intervention in order to rule out acute pancreatitis. During treatment, consideration should be given to the possible distortion of the results of urine tests for diabetes mellitus (due to an increase in ketoproducts), indicators of thyroid function.With the development of any acute serious side effects, you should immediately discuss with your doctor the appropriateness of continuing or stopping treatment. To reduce the risk of dyspeptic phenomena, it is possible to take antispasmodics and coating agents. Abrupt discontinuation of Convulex may lead to an increase in epileptic seizures.

With the simultaneous use of valproic acid with ethanol and other drugs that depress the central nervous system, it is possible to increase the inhibition of the central nervous system. Ethanol and other hepatotoxic drugs increase the likelihood of developing liver damage. Tricyclic antidepressants, MAO inhibitors , neuroleptics and other drugs that reduce the threshold of seizure activity, reduce the effectiveness of valproic acid. Convulex enhances the effects, including side, other antiepileptic drugs (phenytoin, lamotrigine), antidepressants, neuroleptics, tranquilizers, barbiturates, MAO inhibitors, ethanol. Addition of valproate to clonazepam in isolated cases may lead to increased severity of the absence status.

Symptoms: nausea, vomiting, dizziness, diarrhea, impaired respiratory function, muscular hypotonia, hyporeflexia, miosis, coma.
Treatment: gastric lavage (no later than 10–12 h), the appointment of Activated carbon , hemodialysis, forced diuresis, the maintenance of respiration and the cardiovascular system.

In a dry, dark place at a temperature of 15-21 ° C.