Analogues of the drug according to ATC codes:
VALPARINE VALPARINE HR DEPAKINE CHRONO DEPAKINE CHRONOSPHERE CONVULEX CONVULEX CONVULEX CONVULSOFIN ENCORATE ENCORATE CHRONO All
Before using CONVULEX you should consult your doctor. These instructions for use are for informational purposes only. For more complete information, please refer to the manufacturer's instructions.
Reviews of Konvulex, opinions of patients and doctors
60% of positive reviews about a product account for 40% of negative ones. Some patients note the obvious effectiveness of the medication. This applies to the greatest extent to cases of treatment of children. Negative consumer reactions are usually due to persistent side effects. Some of the respondents could not stand the deterioration of their condition and stopped the course on their own, provoking relapses. According to doctors, most of the body’s negative reactions to therapy can be dealt with. The main thing is to act according to the scheme developed by a neurologist and contact a professional with all questions.
Release form, composition and packaging
Enteric-soluble soft gelatin capsules, pink, enteric-coated, marked “150” in gray ink; the contents of the capsules are a colorless or colorless liquid with a slightly yellowish tint, with a weak characteristic odor.
| 1 caps. | |
| valproic acid | 150 mg |
Excipients:
Capsule body composition: carion 83 (mannitol 2-4%, sorbitol 27-32%, hydrogenated starch 61-71%) - 15.14 mg, glycerol 85% - 21.63 mg, gelatin - 71.56 mg, titanium dioxide - 0.67 mg, iron oxide red (E172) - 0.17 mg, hydrochloric acid 25% - 0.57 mg.
Composition of the enteric coating: 30% dispersion of copolymer of methacrylic acid and ethyl acrylate (1:1) dry (sodium lauryl sulfate 0.7%, polysorbate-80 2.3%) - 17.55 mg, triethyl citrate - 2.81 mg, macrogol 6000 - 0.88 mg, glyceryl monostearate 45-55 type II - 0.53 mg.
Composition of capsule marking ink: shellac - 47.5%, titanium dioxide, black iron oxide dye, butanol, water, propylene glycol, denatured ethanol (methylated alcohol), isopropanol.
10 pieces. - blisters (10) - cardboard packs.
Enteric-soluble soft gelatin capsules, pink, enteric-coated, marked “300” in gray ink; the contents of the capsules are a colorless or colorless liquid with a slightly yellowish tint, with a weak characteristic odor.
| 1 caps. | |
| valproic acid | 300 mg |
Excipients:
Capsule body composition: carion 83 (mannitol 2-4%, sorbitol 27-32%, hydrogenated starch 61-71%) - 24.94 mg, glycerol 85% - 35.63 mg, gelatin - 117.86 mg, titanium dioxide - 1.1 mg, iron oxide red (E172) - 0.28 mg, hydrochloric acid 25% - 0.94 mg.
Composition of the enteric coating: 30% dispersion of copolymer of methacrylic acid and ethyl acrylate (1:1) dry (sodium lauryl sulfate 0.7%, polysorbate-80 2.3%) - 28.83 mg, triethyl citrate - 4.61 mg, macrogol 6000 - 1.44 mg, glyceryl monostearate 45-55 type II - 0.86 mg.
Composition of capsule marking ink: shellac 47.5%, titanium dioxide, black iron oxide dye, butanol, water, propylene glycol, denatured ethanol (methylated alcohol), isopropanol.
20 pcs. - blisters (5) - cardboard packs.
Enteric-soluble soft gelatin capsules, pink, enteric-coated, marked “500” in gray ink; the contents of the capsules are a colorless or colorless liquid with a slightly yellowish tint, with a weak characteristic odor.
| 1 caps. | |
| valproic acid | 500 mg |
Excipients:
Capsule body composition: carion 83 (mannitol 2-4%, sorbitol 27-32%, hydrogenated starch 61-71%) - 40.97 mg, glycerol 85% - 58.53 mg, gelatin - 193.64 mg, titanium dioxide - 1.81 mg, iron oxide red (E172) - 0.46 mg, hydrochloric acid 25% - 1.54 mg.
Composition of the enteric coating: 30% dispersion of copolymer of methacrylic acid and ethyl acrylate (1:1) dry (sodium lauryl sulfate 0.7%, polysorbate-80 2.3%) - 47.62 mg, triethyl citrate - 7.62 mg, macrogol 6000 - 2.38 mg, glyceryl monostearate 45-55 type II - 1.43 mg.
Composition of capsule marking ink: shellac 47.5%, titanium dioxide, black iron oxide dye, butanol, water, propylene glycol, denatured ethanol (methylated alcohol), isopropanol.
10 pieces. - blisters (10) - cardboard packs.
pharmachologic effect
Antiepileptic drug. It also has a central muscle relaxant and sedative effect.
The mechanism of action is primarily due to an increase in GABA content in the central nervous system due to inhibition of the GABA transferase enzyme. GABA reduces the excitability and convulsive readiness of the motor areas of the brain. In addition, in the mechanism of action of the drug, a significant role is played by the effect of valproic acid on GABAA receptors (activation of GABA-ergic transmission), as well as the effect on voltage-dependent sodium channels. According to another hypothesis, it acts on sites of postsynaptic receptors, simulating or enhancing the inhibitory effect of GABA. A possible direct effect on membrane activity is associated with changes in conductivity for potassium ions. Improves the mental state and mood of patients, has antiarrhythmic activity.
Pharmacokinetics
Suction
Valproic acid is almost completely absorbed from the gastrointestinal tract, bioavailability when taken orally is 100%. Eating does not reduce the rate of absorption. Cmax in plasma is observed after 2-3 hours. The therapeutic concentration of valproic acid in blood plasma is 50-150 mg/l.
Distribution
Css is achieved on days 2-4 of treatment, depending on the intervals between doses.
At a concentration in blood plasma of up to 50 mg/l, the binding of valproic acid to plasma proteins is 90-95%, at a concentration of 50-100 mg/l - 80-85%.
Concentration values in the cerebrospinal fluid correlate with the value of the non-protein-bound fraction of the active substance. Valproic acid penetrates the placental barrier and is excreted in breast milk. The concentration in breast milk is 1-10% of the concentration in maternal blood plasma.
Metabolism
Valproic acid undergoes glucuronidation and oxidation in the liver.
Removal
Valproic acid (1-3% of the dose) and its metabolites are excreted by the kidneys, small amounts - with feces and exhaled air. T1/2 with monotherapy and in healthy volunteers is 8-20 hours.
Pharmacokinetics in special clinical situations
With uremia, hypoproteinemia and cirrhosis, the binding of valproic acid to plasma proteins decreases.
When combined with other drugs, T1/2 can be 6-8 hours due to the induction of metabolic enzymes.
In patients with impaired liver function, elderly patients and children under the age of 18 months, a significant increase in T1/2 is possible.
Compound
A 5 ml ampoule contains 500 mg sodium valproate (corresponding to 433.9 mg valproic acid ).
1 ml of syrup contains 50 mg of active substance. The syrup is intended for treatment in pediatrics, therefore it has a peculiar fruity smell. Additional components: sodium cyclamate , methyl parahydroxybenzoate, peach or raspberry flavor, sodium saccharinate, liquid maltitol.
The capsule contains 150, 300 or 500 mg of active ingredient. Additional components: hydrochloric acid, hydrogenated starch, sorbitol, carion.
CONVULEX: DOSAGE
Capsules are taken orally, without chewing, 2-3 times a day, during or immediately after meals, with a small amount of water.
Adults are prescribed an initial dose of 600 mg/day with a gradual increase in dose by 150-250 mg every 3 days until a clinical effect is achieved (disappearance of seizures).
The initial dose for monotherapy is 5-15 mg/kg/day, then the dose is gradually increased by 5-10 mg/kg per week.
The recommended daily dose is about 1-2 g, i.e. 20-25 mg/kg. If necessary, the dose can be increased to a maximum dose of 2.5 g/day (30 mg/kg).
The maximum dose is 30 mg/kg/day (in patients with accelerated metabolism of valproic acid, the maximum dose can be increased to 60 mg/kg/day under monitoring of the concentration of valproic acid in the blood plasma).
When carrying out combination therapy, the dose is 10-30 mg/kg/day, followed by an increase of 5-10 mg/kg per week.
Children weighing more than 25 kg are prescribed an initial dose of 300 mg/day (5-15 mg/kg/day), with a gradual increase by 5-10 mg/kg per week until a clinical effect is achieved (disappearance of seizures), while the dose , as a rule, is 1-1.5 g/day (20-30 mg/kg/day).
The maximum dose is 30 mg/kg/day (in patients with accelerated metabolism of valproic acid, the maximum dose can be increased to 60 mg/kg/day under monitoring of the concentration of valproic acid in the blood plasma).
For children weighing 7.5-25 kg with monotherapy, the average dose is 15-45 mg/kg/day, the maximum is 50 mg/kg/day. With combination therapy - 30-100 mg/kg/day.
Average daily doses of Convulex
Although the pharmacokinetics of valproic acid may vary in the elderly, this is of limited clinical significance and dosing should be based on clinical effect. Due to decreased binding to serum albumin, the proportion of unbound drug in plasma increases. This makes it advisable to more carefully select the dose of the drug in the elderly, with the possible use of smaller doses of the drug.
In patients with renal failure, it may be necessary to reduce the dose of the drug. The dose should be selected based on monitoring of the clinical condition, since plasma concentrations may not be sufficiently informative.
Patient's body weight (kg) Dose (mg/day) Number of capsules 150 mg Number of capsules 300 mg Number of capsules 500 mg 7.5-14 150-450 1-3 – – 14-21 300-600 2-4 1-2 – 21-32 600-900 4-6 2-3 – 32-50 900-1500 – 3-5 2-3 50-90 1500-2500 – – 3-5
Convulex price, where to buy
The cost of an antiepileptic drug depends on the dosage form, sales region and pharmacy chain. The price of Convulex in tablet form is 500 rubles (500 mg, 50 pcs), in the form of a solution – 1400 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Konvulex syrup for children
50mg/ml 100ml G.L.Pharma GmbH/Gerot Pharmaceuticals GmbH RUB 139 order - Konvulex tablets p.p.o. prolonged action 300 mg 50 pcs. G.L.Pharma GmbH/ Gerot Pharmaceuticals GmbH
RUB 303 order
- Konvulex tablets p.p.o. prolonged action 500 mg 50 pcs. G.L.Pharma GmbH/Gerot Pharmaceuticals GmbH
RUR 498 order
- Konvulex drops for internal use. approx. 300mg/ml 100mlG.L.Pharma GmbH/Gerot Pharmaceuticals GmbH
RUB 211 order
Pharmacy Dialogue
- Konvulex (long-acting tablet 300 mg No. 50)Gerot Pharm.
RUB 322 order
- Convulex (syrup 50mg/ml 100ml)Gerot Pharm.
RUB 143 order
- Konvulex (long-acting tablet 500 mg No. 50)Gerot Pharm.
RUR 521 order
- Convulex 30% bottle 100mlGerot Pharm.
RUB 208 order
show more
Pharmacy24
- Convulex 100 mg/ml 5 ml No. 5 solution for injection G.L Pharma GmbH, Austria
1263 UAH.order
PaniPharmacy
- Konvulex retard tablets Konvulex retard tablets. p/o 500 mg No. 50 Austria, GL Pharma
631 UAH. order
show more
Drug interactions
Contraindicated combinations
Mefloquine: risk of epileptic seizures due to increased metabolism of valproic acid and a decrease in its plasma concentration and, on the other hand, the convulsant effect of mefloquine.
St. John's wort: risk of reducing the concentration of valproic acid in the blood plasma.
Not recommended combinations
Lamotrigine: increased risk of severe skin reactions (toxic epidermal necrolysis). Valproic acid inhibits microsomal liver enzymes that ensure the metabolism of lamotrigine, which slows down its T1/2 to 70 hours in adults and up to 45-55 hours in children and increases plasma concentrations. If the combination is necessary, careful clinical and laboratory monitoring is required.
Combinations requiring special precautions
Carbamazepine: Valproic acid increases the plasma concentration of the active metabolite of carbamazepine to the point of signs of overdose. In addition, carbamazepine enhances the hepatic metabolism of valproic acid and reduces its concentration. These circumstances require the attention of a doctor and determination of drug concentrations in plasma and a possible revision of their doses.
Phenobarbital, primidone: Valproic acid increases plasma concentrations of phenobarbital or primidone to the point of signs of overdose, more often in children. In turn, phenobarbital or primidone enhance the hepatic metabolism of valproic acid and reduce its concentration. Clinical observation is recommended during the first 2 weeks of combination treatment with an immediate reduction in the dose of phenobarbital or primidone when signs of sedation appear, and determination of the level of anticonvulsants in the blood.
Phenytoin: changes in the concentration of phenytoin in plasma are possible; phenytoin increases the hepatic metabolism of valproic acid and reduces its concentration. Clinical observation is recommended, determining the level of anticonvulsants in the blood, changing dosages if necessary.
Clonazepam: The addition of valproic acid to clonazepam in isolated cases may lead to an increase in the severity of absence status.
Ethosuximide: Valproic acid can either increase or decrease the serum concentrations of ethosuximide due to changes in its metabolism. Clinical observation is recommended, determining the level of anticonvulsants in the blood, changing dosages if necessary.
Topiramate: Increases the risk of hyperammonemia and encephalopathy.
Felbamate: increased plasma concentrations of valproic acid by 35-50%, with risk of overdose. Clinical observation, determination of the level of valproic acid in the blood, and changes in the dosage of valproic acid when combined with felbamate and after its discontinuation are recommended.
Neuroleptics, MAO inhibitors, antidepressants, benzodiazepines: neuroleptics, tricyclic antidepressants, MAO inhibitors, which lower the seizure threshold, 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 plasma concentration.
Zidovudine: Valproic acid increases the plasma concentration of zidovudine, leading to increased toxicity.
Carbapenems, monobactams: meropenem, panipenem, as well as aztreonam and imipenem reduce the concentration of valproic acid in plasma, which may lead to a decrease in the anticonvulsant effect.
Combinations to consider
Acetylsalicylic acid: increased effects of valproic acid due to its displacement from plasma proteins. Valproic acid enhances the effect of acetylsalicylic acid.
Indirect anticoagulants: valproic acid enhances the effect of indirect anticoagulants; careful monitoring of the prothrombin index is necessary when administered together with vitamin K-dependent anticoagulants.
Nimodipine: increased hypotensive effect of nimodipine due to an increase in its concentration in plasma due to the suppression of its metabolism by valproic acid.
Myelotoxic drugs: increased risk of suppression of bone marrow hematopoiesis.
Ethanol and hepatotoxic drugs: increase the likelihood of developing liver damage.
Other combinations
Oral contraceptives: valproic acid does not induce liver microsomal enzymes and does not reduce the effectiveness of hormonal oral contraceptives.
Pregnancy and lactation
During treatment, pregnancy should be protected. Experiments on animals revealed the teratogenic effect of valproic acid. The incidence of neural tube defects in children born to women who took valproate in the first trimester of pregnancy is 1-2%. In this regard, it is advisable to use folic acid preparations. In the first trimester of pregnancy, treatment with Convulex should not be started. If a pregnant woman is already receiving the drug, treatment should not be interrupted due to the risk of increased seizures. The drug should be used in the lowest effective doses, avoiding combination with other anticonvulsants and, if possible, regularly monitoring the concentration of valproic acid in plasma.
Overdose of the drug Convulex, symptoms and treatment
Symptoms: severe sedation, impaired balance and coordination of movements, myasthenia gravis, hyporeflexia, miosis, heart block, metabolic acidosis, coma (on the EEG - an increase in slow waves and background activity). Treatment: there is no specific antidote. Therapy should be aimed at accelerating the elimination of valproate from the body and maintaining vital body functions. It is advisable to carry out hemodialysis and hemoperfusion, the use of activated carbon and intravenous administration of naloxone.
CONVULEX: SIDE EFFECTS
In general, Konvulex® is well tolerated by patients. Side effects are possible mainly when the drug concentration in plasma is above 100 mg/l or during combination therapy.
From the digestive system: nausea, vomiting, gastralgia, decreased or increased appetite, diarrhea, hepatitis, constipation, pancreatitis, up to severe injuries with a fatal outcome (in the first 6 months of treatment, more often for 2-12 weeks).
From the side of the central nervous system: tremor, diplopia, nystagmus, flickering of “floaters” before the eyes, changes in behavior, mood or mental state (depression, fatigue, hallucinations, aggressiveness, hyperactive state, psychosis, unusual agitation, restlessness or irritability), ataxia, dizziness, drowsiness, headache, encephalopathy, dysarthria, enuresis, stupor, impaired consciousness, coma.
From the hematopoietic system: anemia, leukopenia, thrombocytopenia, decreased fibrinogen content and platelet aggregation, leading to the development of hypocoagulation (accompanied by prolongation of bleeding time, petechial hemorrhages, bruises, hematomas, bleeding).
From the metabolic side: decrease or increase in body weight.
From the endocrine system: dysmenorrhea, secondary amenorrhea, breast enlargement, galactorrhea.
Laboratory parameters: hypercreatininemia, hyperammonemia, hyperbilirubinemia, slight increase in the activity of liver transaminases, LDH (dose-dependent).
Allergic reactions: skin rash, urticaria, angioedema, photosensitivity, malignant exudative erythema (Stevens-Johnson syndrome).
Other: peripheral edema, hair loss (usually restored after discontinuation of the drug).
Solution for intravenous administration Convulex
Instructions for medical use of the drug
Description of pharmacological action
Konvulex® is an antiepileptic drug that also has a central muscle relaxant and sedative effect. The mechanism of action is primarily due to inhibition of the GABA transferase enzyme and an increase in GABA content in the central nervous system. GABA inhibits pre- and postsynaptic discharges and thereby prevents the spread of seizure activity into the central nervous system. In addition, in the mechanism of action of the drug, a significant role is played by the effect of valproic acid on GABAA receptors, as well as the effect on voltage-dependent sodium channels. According to another hypothesis, it acts on sites of postsynaptic receptors, simulating or enhancing the inhibitory effect of GABA. A possible direct effect on membrane activity is associated with changes in potassium conductance. Improves the mental state and mood of patients, has antiarrhythmic activity.
Indications for use
- status epilepticus; - treatment of epileptic seizures (generalized - absences, myoclonic seizures, tonic-clonic, atonic, mixed; partial - simple, complex, secondary generalized seizures; specific syndromes (West, Lennox-Gastaut).
Release form
solution for intravenous administration 100 mg/ml; ampoule 5 ml, contour plastic packaging (pallets) 5, cardboard pack 1; solution for intravenous administration 100 mg/ml; ampoule 5 ml, contour plastic packaging (pallets) 5, cardboard pack 1; Composition Solution for intravenous administration 5 ml valproic acid 433.9 mg (corresponding to 500.0 mg sodium valproate) excipients: sodium hydroxide - 117 mg, disodium hydrogen phosphate dodecahydrate - 71.8 mg, water for injection - up to 5 ml in ampoules 5 ml; in contour plastic packaging 5 ampoules; in a cardboard pack 1 package.
Pharmacodynamics
Konvulex® is an antiepileptic drug that also has a central muscle relaxant and sedative effect. The mechanism of action is primarily due to inhibition of the GABA transferase enzyme and an increase in GABA content in the central nervous system. GABA inhibits pre- and postsynaptic discharges and thereby prevents the spread of seizure activity into the central nervous system. In addition, in the mechanism of action of the drug, a significant role is played by the effect of valproic acid on GABAA receptors, as well as the effect on voltage-dependent sodium channels. According to another hypothesis, it acts on sites of postsynaptic receptors, simulating or enhancing the inhibitory effect of GABA. A possible direct effect on membrane activity is associated with changes in potassium conductance. Improves the mental state and mood of patients, has antiarrhythmic activity.
Pharmacokinetics
Steady-state concentrations with intravenous administration are achieved within a few minutes and can be maintained by slow infusion. The therapeutic concentration of the drug in blood plasma ranges from 50–150 mg/l. Valproic acid is bound to plasma proteins by 90–95% at plasma concentrations up to 50 mg/l and by 80–85% at concentrations of 50–100 mg/l; with uremia, hypoproteinemia and cirrhosis, protein binding is reduced. Cerebrospinal fluid concentration levels correlate with the non-protein bound fraction of the drug, being approximately 10% of serum levels. Valproic acid penetrates the placental barrier and is excreted in breast milk. Concentrations in breast milk are 1–10% of maternal plasma concentrations. The drug undergoes glucuronidation and oxidation in the liver, metabolites and unchanged valproic acid (1–3% of the dose) are excreted by the kidneys, small amounts are excreted in feces and exhaled air. T1/2 of the drug in healthy subjects and with monotherapy is from 8 to 20 hours; when combined with other drugs, T1/2 can be 6–8 hours due to the induction of metabolic enzymes; in patients with impaired liver function and elderly patients - may be significantly longer.
Use during pregnancy
Use during pregnancy. During treatment, pregnancy should be protected. Experiments on animals revealed the teratogenic effect of valproic acid. The incidence of neural tube defects in children born to women who took valproate in the first trimester of pregnancy is 1–2%. In this regard, it is advisable to use folic acid preparations. In the first trimester of pregnancy, treatment with Convulex® should not be started. If a pregnant woman is already receiving the drug, treatment should not be interrupted due to the risk of increased seizures. The drug should be used in the lowest effective doses, avoiding combination with other anticonvulsants and, if possible, regularly monitoring drug plasma levels. Convulex® is contraindicated during lactation. At the same time, breastfeeding is possible, because the concentration in milk does not exceed 1–10% of the drug level in the mother’s blood plasma.
Use for renal impairment
Patients with renal failure may require a dose reduction. The dose is set by monitoring the patient’s clinical condition, because values for the concentration of valproic acid in blood plasma may not be sufficiently informative.
Other special occasions at reception
Contraindicated in severe liver dysfunction. The drug should be prescribed with extreme caution if there is a history of liver disease.
Contraindications for use
- hypersensitivity to valproic acid; - severe dysfunction of the liver and/or pancreas; - porphyria; - hemorrhagic diathesis; - severe thrombocytopenia. With caution: - in children when treated with several antiepileptic drugs; - in children and adolescents with multiple concomitant diseases and severe forms of seizures; - in case of renal dysfunction; - in patients with anamnestic data on diseases of the liver and pancreas; - with suppression of bone marrow hematopoiesis: leukopenia, anemia, thrombocytopenia; - for congenital enzymopathies; - with organic brain lesions; - with hypoproteinemia.
Side effects
In general, Konvulex® is well tolerated by patients. Side effects are possible mainly when the drug level in plasma is above 100 mg/l or during combination therapy. From the gastrointestinal tract: nausea, vomiting, gastralgia, anorexia or increased appetite, diarrhea, hepatitis; rarely - constipation, pancreatitis, up to severe injuries with a fatal outcome (in the first 6 months of treatment, more often - at 2-12 weeks). From the side of the central nervous system: tremor; rarely - changes in behavior, mood or mental state (depression, feeling tired, hallucinations, aggressiveness, hyperactive state, psychosis, unusual agitation, restlessness or irritability), ataxia, dizziness, drowsiness, headache, encephalopathy, dysarthria, stupor, impaired consciousness , coma. From the sensory organs: diplopia, nystagmus, flashing “spots” before the eyes. From the hematopoietic organs and hemostasis system: anemia, leukopenia; thrombocytopenia, decreased fibrinogen content, platelet aggregation and blood clotting, accompanied by prolongation of bleeding time, petechial hemorrhages, bruises, hematomas, bleeding. Metabolism: loss or increase in body weight. Allergic reactions: skin rash, urticaria, angioedema, photosensitivity, Stevens-Johnson syndrome. Laboratory indicators: hypercreatininemia, hyperammonemia, hyperglycinemia, hyperbilirubinemia, slight increase in the activity of liver transaminases, LDH (dose-dependent). From the endocrine system: dysmenorrhea, secondary amenorrhea, breast enlargement, galactorrhea. Other: peripheral edema, alopecia (as a rule, hair growth is restored after discontinuation of the drug).
Directions for use and doses
IV. The recommended daily dose for slow intravenous administration is 5–10 mg/kg; with intravenous infusion - 0.5–1 mg/kg/hour. When switching from oral administration to intravenous administration, the doses do not change; the first intravenous administration is recommended 12 hours after the last oral administration. The injection solution should be replaced by taking the drug orally as soon as the patient's condition allows it. The first oral administration is also recommended 12 hours after the last injection. If it is necessary to quickly achieve and maintain high plasma concentrations, the following approach is recommended: intravenous administration of 15 mg/kg over 5 minutes, after 30 minutes, begin infusion at a rate of 1 mg/kg/h with constant monitoring of concentrations until a plasma level reaches about 75 µg/ml. The maximum daily dose of the drug should not exceed 2500 mg. Average daily doses are 20 mg/kg in adults and elderly patients, 25 mg/kg in adolescents, 30 mg/kg in children. Isotonic sodium chloride solution, 5% glucose solution, and Ringer's solution can be used as an infusion solution for Convulex®. The prepared solution for infusion can be used within 24 hours; the unused volume of the solution is destroyed. If other drugs are also used intravenously, Convulex® should be administered via a separate infusion system.
Overdose
Symptoms: nausea, vomiting, dizziness, diarrhea, respiratory dysfunction, muscle hypotonia, hyporeflexia, miosis, coma. Treatment: gastric lavage (no later than 10–12 hours), administration of activated carbon, hemodialysis; ensuring forced diuresis, maintaining breathing and the cardiovascular system.
Interactions with other drugs
Pharmacodynamic interaction. With simultaneous use of valproic acid with ethanol and other drugs that depress the central nervous system (tricyclic antidepressants, MAO inhibitors and antipsychotics), increased central nervous system depression may occur. Ethanol and other hepatotoxic drugs increase the likelihood of developing liver damage. Tricyclic antidepressants, MAO inhibitors, antipsychotics and other drugs that lower the threshold for seizure activity reduce the effectiveness of valproic acid. Convulex® enhances the effects, incl. side effects, other antiepileptic drugs (phenytoin, lamotrigine), antidepressants, neuroleptics, tranquilizers, barbiturates, MAO inhibitors, thymoleptics, ethanol. The addition of valproate to clonazepam in isolated cases can lead to increased severity of absence status. Pharmacokinetic interaction. With the simultaneous use of valproic acid with barbiturates or primidone, an increase in their concentration in the blood plasma is observed. Increases T1/2 of lamotrigine (inhibits liver enzymes, causes a slowdown in the metabolism of lamotrigine, as a result of which its T1/2 is extended to 70 hours in adults and to 45–55 hours in children). Reduces the clearance of zidovudine by 38%, while its T1/2 does not change. When combined with salicylates, an increase in the effects of valproic acid is observed (displacement from plasma proteins). Konvulex® enhances the effect of antiplatelet agents (acetylsalicylic acid) and indirect anticoagulants. When combined with phenobarbital, phenytoin, carbamazepine, mefloquine, the content of valproic acid in the blood serum decreases (acceleration of metabolism). Felbamate increases plasma concentrations of valproic acid by 35–50% (dose adjustment required). Valproic acid does not induce liver enzymes and does not reduce the effectiveness of oral contraceptives.
Special instructions for use
During treatment, it is advisable to monitor the activity of liver transaminases, bilirubin levels, peripheral blood patterns, blood platelets, the state of the blood coagulation system, amylase activity (every 3 months, especially when combined with other antiepileptic drugs). In patients receiving other antiepileptic drugs, transition to valproic acid should be gradual, reaching a clinically effective dose after 2 weeks, after which gradual withdrawal of other antiepileptic drugs is possible. In patients not treated with other antiepileptic drugs, a clinically effective dose should be achieved after 1 week. The risk of side effects from the liver is increased during combination anticonvulsant therapy, as well as in children. During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Drinks containing ethanol are not allowed. Before surgery, a general blood test (including platelet count), determination of bleeding time, and coagulogram parameters are required. If symptoms of an “acute” abdomen occur during treatment, it is recommended to determine the level of amylase in the blood before surgery to exclude acute pancreatitis. During treatment, one should take into account the possible distortion of the results of urine tests in diabetes mellitus (due to an increase in the content of keto products) and indicators of thyroid function. If any acute serious side effects develop, you should immediately discuss with your doctor the advisability of continuing or stopping treatment. To reduce the risk of developing dyspeptic disorders, it is possible to take antispasmodics and enveloping agents. Abruptly stopping taking Convulex® may lead to an increase in epileptic seizures.
Storage conditions
List B: In a place protected from light, at a temperature not exceeding 25 °C.
Best before date
36 months
ATX classification:
N Nervous system
N03 Antiepileptic drugs
N03A Antiepileptic drugs
N03AG Fatty acid derivatives
N03AG01 Valproic acid
Indications
- epilepsy of various etiologies (idiopathic,
- cryptogenic and symptomatic);
- generalized epileptic seizures in adults and children (clonic,
- tonic,
- tonic-clonic,
- absence seizures,
- myoclonic,
- atonic);
- partial epileptic seizures in adults and children (with or without secondary generalization);
- specific syndromes (Vesta,
- Lennox-Gastaut);
- behavioral disorders,
- caused by epilepsy;
- febrile seizures in children,
- baby tic;
- treatment and prevention of bipolar affective disorders.
Contraindications
- liver failure;
- acute and chronic hepatitis;
- pancreatic dysfunction;
- porphyria;
- hemorrhagic diathesis;
- severe thrombocytopenia;
- disorders of urea metabolism (incl.
- in family history);
- combination with mefloquine,
- St. John's wort,
- lamotrigine;
- lactation period;
- children's age (up to 3 years);
- hypersensitivity to valproic acid and its salts or components of the drug.
Carefully:
- with anamnestic data on diseases of the liver and pancreas (incl.
- in family history);
- with suppression of bone marrow hematopoiesis (leukopenia,
- thrombocytopenia,
- anemia);
- with renal failure;
- for congenital enzymopathies;
- for organic diseases of the brain;
- with hypoproteinemia;
- during pregnancy (especially the first trimester);
- children with mental retardation.
Analogs
Pharmacies offer many synonyms and analogues of the product "Convulex". The former also contain valproic acid, which gives them the necessary characteristics. The group includes: “Apilepsin”, “Valparin”, “Depakine”, “Encorat”.
You can learn more about Valparin here.
Drug analogues contain other active ingredients or their composition is supplemented with excipients. These include drugs such as Keppra, Levetiracetam, Comviron and many others.
You will learn more about the drug "Depakine" here.
special instructions
Due to reports of severe and fatal cases of liver failure and pancreatitis when using valproic acid preparations, the following should be kept in mind:
- the high-risk group includes 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 dysfunction 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 regardless of the patient’s age and duration of treatment,
- although the risk of developing pancreatitis decreased with patient age;
- insufficiency of liver function with pancreatitis increases the risk of death;
- early diagnosis (before the icteric stage) is based mainly on clinical observation - identifying early symptoms,
- such as asthenia,
- anorexia,
- extreme fatigue
- drowsiness,
- sometimes accompanied by vomiting and abdominal pain; in this case, a relapse of epileptic seizures may occur against the background of unchanged antiepileptic therapy.
In such cases, you should immediately consult a doctor for a clinical examination and liver function test.
During treatment, especially in the first 6 months, it is necessary to periodically check liver function - liver transaminase activity, levels of prothrombin, fibrinogen, coagulation factors, bilirubin concentration, as well as amylase activity (every 3 months, especially when combined with other antiepileptic drugs) and picture of peripheral blood, in particular blood platelets.
In patients receiving other antiepileptic drugs, transfer to valproic acid should be carried out gradually, reaching a clinically effective dose after 2 weeks, after which gradual withdrawal of other antiepileptic drugs is possible. In patients not treated with other antiepileptic drugs, a clinically effective dose should be achieved after 1 week.
The risk of side effects from the liver is increased during combination anticonvulsant therapy, as well as in children. Drinks containing ethanol are not allowed.
Before surgery, a general blood test (including platelet count), determination of bleeding time, and coagulogram parameters are required.
If symptoms of an “acute” abdomen occur during treatment, before surgery, it is recommended to determine the activity of amylase in the blood to exclude acute pancreatitis.
During treatment, one should take into account the possible distortion of the results of urine tests in diabetes mellitus (due to an increase in the content of ketone bodies) and indicators of thyroid function.
If any acute serious side effects develop, you should immediately discuss with your doctor the advisability of continuing or stopping treatment.
To reduce the risk of developing dyspeptic disorders, it is possible to take antispasmodics and enveloping agents.
Abruptly stopping taking Convulex may lead to an increase in epileptic seizures.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Overdose
Symptoms appear depending on the dose. In mild cases, drowsiness , nausea , dizziness , and sedation . With severe intoxication, breathing is depressed, hyporeflexia, metabolic acidosis , miosis, and hyptonus develop. Rarely, cerebral edema and increased intracranial pressure . Enterosorbents are prescribed and syndromic therapy is carried out.
