Konvuleks - anticonvulsant drug.
Release form and composition
Convolux dosage forms:
- Enteric capsules: 150 and 500 mg - 10 pcs. in blisters, in a cardboard box of 10 blisters; 300 mg - 20 pcs. in blisters, in a cardboard bundle 5 blisters;
- Film-coated tablets with prolonged action: 50 or 100 pcs. in polypropylene / dark glass bottles, in a cardboard bundle one bottle;
- Drops for oral administration: in dark glass bottles with a dosing device with a volume of 100 ml, in a cardboard bundle one bottle;
- Syrup for children: in bottles of dark glass with a volume of 100 ml, in a cardboard bundle one bottle complete with a measuring syringe;
- Solution for intravenous (iv) administration: 5 ml each in ampoules of colorless glass, 5 ampoules in plastic pallets, in a carton pack 1 pallet.
The active ingredient of the drug is valproic acid. Its content corresponding to sodium valproate:
- 1 capsule - 150, 300 or 500 mg;
- 1 tablet - 300 or 500 mg;
- 1 ml of drops - 300 mg;
- 1 ml of syrup - 50 mg;
- 1 ml of solution - 100 mg.
Auxiliary components of capsules:
- The composition of the capsule body: gelatin, carion 83 (sorbitol, hydrogenated starch, mannitol), titanium dioxide, glycerol 85%, hydrochloric acid 25%, iron red oxide (E172);
- The composition of the enteric coating: glyceryl monostearate 45-55 type II, macrogol 6000, triethyl citrate, 30% dispersion of a copolymer of methacrylic acid and ethyl acrylate (1: 1) dry (polysorbate-80 and sodium lauryl sulfate);
- The composition of the ink labeling: shellac, isopropanol, propylene glycol, water, denatured ethanol (methylated alcohol), titanium dioxide, butanol, black iron oxide dye.
Additional components of tablets:
- Excipients: citric acid, colloidal silicon dioxide, ethyl cellulose, magnesium stearate, talc, methyl methacrylate copolymer, trimethylammonio ethyl methyl acrylate chloride and ethyl acrylate (1: 2: 0.1) (Eudragit RS30D);
- The composition of the shell: a copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2): 0.1) (Eudragit RS30D), a copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2: 0.2) (Eudragit RL30D type apt, and a kind of acylacrylate chloride) and ethyl acrylate (1: 2: 0.2) (Eudragit RL30D type apt, a kind of acylate and acrylate chloride). , triethyl citrate, vanillin.
Auxiliary components of the drops: sodium hydroxide, sodium saccharinate, purified water, hydrochloric acid 37%, flavor with orange flavor.
Syrup auxiliaries: methyl parahydroxybenzoate, maltitol liquid (licasin 80/55), sodium saccharinate, sodium cyclamate, propyl parahydroxybenzoate, sodium chloride, purified water, peach flavoring 9/030307, raspberry flavoring 9/372710.
Auxiliary components of the solution: disodium hydrogen phosphate dodecahydrate, sodium hydroxide, injectable water.
Indications for use
- Epilepsy of various etiologies (cryptogenic, idiopathic, symptomatic);
- Behavioral disorders due to epilepsy;
- Specific syndromes - Lennox-Gasto, Vesta;
- Febrile convulsions in children, children's teak;
- Partial epileptic seizures in adults and children (simple, secondarily generalized, complex);
- Generalized epileptic seizures (clonic, myoclonic, tonic, atonic, tonic-clonic, mixed, as well as absences);
- Bipolar affective disorders.
- Acute and chronic hepatitis;
- Liver failure;
- Severe thrombocytopenia;
- Pancreas dysfunction;
- Hemorrhagic diathesis;
- Disorders of urea metabolism (including in the family history);
- Lactation period;
- Simultaneous use with lamotrigine, mefloquine or hunter perforated;
- Hypersensitivity to valproic acid, its salts or auxiliary components of the drug.
- A history of liver and pancreas diseases, including familial ones;
- Inhibition of bone marrow hematopoiesis (leukopenia, anemia, thrombocytopenia);
- Renal failure;
- Congenital fermentopathies;
- Organic diseases of the brain;
- Mental retardation in children;
- Pregnancy (especially the I trimester).
Restrictions on the use of Konvuleks:
- Capsules: children under 3 years;
- Tablets: children under 3 years old or with a body weight less than 20 kg;
- Drops: children weighing less than 7.5 kg.
- Drops: children weighing more than 7.5 kg;
- Solution: children under 3 years of age and those who are shown simultaneous treatment with several antiepileptic drugs.
Dosing and Administration
Capsules and tablets should be taken orally, without chewing, with a small amount of water, with meals or immediately after a meal: capsules - 2-3 times a day, tablets - 1-2 times a day.
Drops and syrup are taken orally with a small amount of water 2-3 times a day, regardless of the meal.
The initial daily dose for adults is 600 mg. Gradually (once every 3 days) it is increased by 150-250 mg to achieve a clinical effect.
When using Konvuleks as a monopreparation, the daily dose is calculated taking into account the patient's weight - at the rate of 5-15 mg / kg, then it is gradually increased - by 5-10 mg / kg per week.
The recommended daily dose is 20-25 mg / kg, about 1000-2000 mg. If necessary, it is increased to the maximum permissible dose - 2500 mg per day or 30 mg / kg. For patients with an accelerated metabolism of valproic acid, if absolutely necessary, the daily dose may be increased to 60 mg / kg. However, treatment should be carried out under careful control of the concentration of sodium valproate.
When applying Konvuleks as part of combination therapy, the daily dose is 10-30 mg / kg, then it is increased by 5-10 mg / kg per week.
The initial daily dose for children weighing more than 25 kg - 5-15 mg / kg (300 mg), gradually (5-10 mg / kg per week), it is increased to achieve a clinical effect. As a rule, further dose is 20-30 mg / kg / day (1000-1500 mg).
Daily doses for children weighing 7.5-25 kg:
- With monotherapy: the average - 15-45 mg / kg, maximum - 50 mg / kg;
- With combined therapy - 30-100 mg / kg.
Patients with renal insufficiency may require a reduction in the dose of Convolux. It is necessary to select the dose according to the monitoring of the clinical condition, since the indicators of plasma valproic acid concentration may not be sufficiently informative.
The average dose of the drug in the form of drops and syrup, taking into account the weight of the patient:
- 7.5-14 kg - 150-450 mg / day: 15-45 drops or 3-9 ml of syrup;
- 14-21 kg - 300-600 mg / day: 30-60 drops or 6-12 ml of syrup;
- 21-32 kg - 600-900 mg / day: 60-90 drops or 12-18 ml of syrup;
- 32-50 kg - 900-1500 mg / day: 90-150 drops;
- 50-90 kg - 1500-2500 mg / day: 150-250 drops.
In the form of syrup, Konvuleks is prescribed only for children.
In the form of a solution, the drug is administered intravenously slowly or infusionally.
Recommended daily doses:
- With the on / in the slow introduction - 5-10 mg / kg of body weight of the patient;
- With the / in infusion introduction - 0.5-1 mg / kg / hour.
When transferring a patient from oral administration of Konvuleks to the i / v use, the doses do not change, only the first administration is carried out 12 hours after the last administration of the drug inside. As soon as the patient’s condition permits, the injection solution is replaced with an oral form, and the first dose is also recommended 12 hours after the last injection.
If it is necessary to quickly achieve a high concentration of sodium valproate in the blood plasma, the following dosing regimen is recommended: intravenously at a dose of 15 mg / kg for 5 minutes, 30 minutes later, intravenous infusion at a rate of 1 mg / kg / hour with constant monitoring Valproic acid concentration to reach a plasma level of about 75 μg / ml.
The maximum permissible daily dose is 2500 mg.
Average daily doses: for adults - 20 mg / kg, for adolescents - 25 mg / kg, for children - 30 mg / kg.
Ringer's solution, 5% glucose solution or isotonic sodium chloride solution is used as an infusion solution for Konvuleks. The prepared infusion solution should be used within 24 hours. If any other drugs are used at the same time, they should be administered on a separate infusion system.
In general, Konvuleks well tolerated. Side effects often occur during combination therapy or plasma concentrations of more than 100 mg / l:
- Digestive system: decrease or increase in appetite, gastralgia, diarrhea, nausea, constipation, vomiting, hepatitis, pancreatitis, up to severe lesions with a fatal outcome (in the first 6 months of treatment, usually at 2-12 weeks);
- Central nervous system: flashing of “flies” before eyes, nystagmus, diplopia, tremor, drowsiness, dizziness, headache, ataxia, encephalopathy, stupor, enuresis, impairment of consciousness, dysrhythmia, changes in behavior, mood or mental state (feeling tired, anxious , aggressiveness, psychosis, hyperactive condition, irritability, hallucinations, unusual agitation, depression), coma;
- The hematopoietic system: thrombocytopenia, leukopenia, anemia, a decrease in the content of fibrinogen and platelet aggregation, leading to the development of hypocoagulation (accompanied by an increase in bleeding time, hemorrhages, bleeding, petechial hemorrhages, hematomas);
- Metabolism: decrease or increase in body weight;
- Endocrine system: secondary amenorrhea, dysmenorrhea, galactorrhea, breast enlargement;
- Allergic reactions: skin rash, urticaria, photosensitivity, angioedema, malignant exudative erythema;
- Other: hair loss (usually reversible), peripheral edema;
- Laboratory indicators: hyperbilirubinemia, hyperammonemia, hypercreatininemia, a slight increase in liver transaminase activity and a dose-dependent increase in lactate dehydrogenase.
Due to the fact that there are reports of severe and even lethal cases of pancreatitis and liver failure when using valproic acid preparations, it is important to consider the following:
- Children at the age of 3 years with severe epilepsy are at increased risk. It is associated with congenital degenerative or metabolic diseases, brain damage;
- Liver dysfunction in most cases developed in the first 6 months of treatment (usually between 2 and 12 weeks), more often with combination therapy;
- Cases of pancreatitis were observed in patients of all ages, regardless of the duration of treatment, although the risk decreased with age;
- Hepatic impairment with pancreatitis increases the risk of death;
- Early diagnosis (up to the icteric stage) is based mainly on clinical observation, i.e. to identify early symptoms, such as anorexia, asthenia, drowsiness, extreme fatigue, and sometimes vomiting and abdominal pain. A relapse of epileptic seizures is possible, despite ongoing anti-epileptic therapy.
If any of the above symptoms appear, you should immediately consult a doctor. For the same reason, during treatment, especially in the first six months (and especially with combination therapy), it is necessary to periodically monitor liver function — the activity of hepatic transaminases and amylase, the concentration of bilirubin, the level of prothrombin and fibrinogen, coagulation factors, and also a picture of peripheral blood ( particular blood platelets).
Patients receiving other antiepileptic drugs should be transferred to Konvuleks gradually, reaching an effective dose within 2 weeks. Only then can another anti-convulsant medication be discontinued. For patients who have not received antiepileptic therapy, an effective clinical dose should be achieved after 1 week.
If surgery is necessary, a complete blood test should be done (including to establish the number of platelets), examine the indicators of the coagulogram, determine the bleeding time.
It should be borne in mind that Konvulex can distort the results of urine tests for diabetes mellitus and indicators of thyroid function.
To reduce the risk of dyspeptic disorders, antispasmodics or coating agents can be prescribed.
If symptoms of acute abdomen appear before the operation, it is recommended to determine the activity of amylase in the blood in order to rule out acute pancreatitis.
Abrupt withdrawal of the drug may lead to increased epileptic seizures.
During the period of treatment Konvulexom:
- It is forbidden to consume alcoholic beverages;
- Care should be taken when engaging in activities that require quick reactions and increased concentration of attention, including when driving.
- Mefloquine - increases the risk of epileptic seizures due to increased metabolism of valproic acid and a decrease in its concentration in the blood plasma, as well as the probability of the convulsive effect of mefloquine;
- St. John's wort - increases the probability of reducing the concentration of sodium valproate in the plasma.
It is not recommended to use Konvuleks in combination with lamotrigine, because severe skin reactions, such as toxic epidermal necrolysis, may develop. If the use of such a combination is still necessary, careful laboratory and clinical monitoring is required.
Due to the likelihood of undesirable, sometimes severe reactions, special precaution should be taken when the following medicines are prescribed at the same time: carbamazepine, phenobarbital, primidone, phenytoin, clonazepam, ethosuximide, topiramate, felbamate, antipsychotics, antidepressants, monoamine oxidase inhibitors, benzodiazythynehydroxyphene, zychidazychidazychyazychazychyazychimy, zykhaza zykhazykhyy, zykhaza zykhy, zyyroxamate, zyrophamate, neuroleptics, antidepressants, monoamine oxidase inhibitors, prophylactic mecholines, antipsychotics, anti-depressants, monoamine oxidases, prophylactic agents, anti-depressants, anti-depressants, anti-depressants, anti-depressants, anti-depressants, anti-depressants, anti-depressants, anti-depressants, anti-depressants, anti-depressants, anti-depressants. carbapenems, monobactam.
Combinations to be taken into account:
- Indirect anticoagulants - enhancing their action. Careful monitoring of the prothrombin index is necessary;
- Acetylsalicylic acid - mutual enhancement effect;
- Nimodipine - enhancing its hypotensive action;
- Myelotoxic drugs - increase the risk of oppression of bone marrow hematopoiesis;
- Ethanol and hepatotoxic drugs - the likelihood of liver damage.
Terms and conditions of storage
Store in a dark place, out of reach of children, at a temperature of: capsules - up to 30 ºС, tablets, drops and solution - up to 25 ºС, syrup - 15-25 ºС. Tablets - in tightly closed package.
Shelf life - 5 years.