Convulsofin - instructions for use, analogs, reviews and release forms (300 mg tablets and 500 mg Retard) for the treatment of epilepsy and manic-depressive psychosis in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Convulsofin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Convulsofina 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 Convulsophine in the presence of existing structural analogues. Use for the treatment of epilepsy and bipolar-affective disorders in adults, children, as well as in pregnancy and lactation.Composition and interaction of the drug with alcohol.

Convulsofin antiepileptic drug. Has anticonvulsant, central muscle relaxant and sedative effect. The mechanism of action is associated with an increase in the content of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) in the central nervous system (CNS) due to inhibition of the enzyme GABA-transferase, as well as a decrease in GABA reuptake in the brain tissues. In this case, the excitability and convulsive readiness of the motor zones of the brain decreases. It improves the mental state and mood of patients, has antiarrhythmic activity.

Composition

Valproate calcium dihydrate + excipients.

Pharmacokinetics

Degree of absorption is high, bioavailability is 100%. Simultaneous intake of food slightly reduces the rate of absorption. The therapeutic concentrations in the blood plasma range from 50-150 mg per liter. Binding to blood plasma proteins is 90-95% at a plasma concentration of up to 50 mg per liter and decreases to 80-85% at a concentration of 50-100 mg per liter. Penetrates through the placental barrier and the blood-brain barrier (BBB).It is excreted in breast milk (concentration in breast milk is 1-10% concentration in the mother plasma). The content in the cerebrospinal fluid correlates with the size of the protein-unbound fraction.

Metabolized by glucuronization and oxidation in the liver with the formation of hydroxylated derivatives of valproic acid. Valproic acid (1-3%) and its metabolites (in the form of conjugates, oxidation products, including ketometabolites) are excreted by the kidneys, small amounts are excreted with feces and with exhaled air. With uremia, hypoproteinemia and liver cirrhosis, binding to plasma proteins is reduced. When combined with other drugs, the elimination half-life can be 6-8 hours due to the induction of metabolic enzymes. In patients with impaired liver function, in elderly patients and children under the age of 18 months, the elimination half-life can be significantly longer.

Indications

• epilepsy of various genesis: generalized and partial seizures;
• epileptic seizures against the background of organic brain diseases;
• changes in character and behavior (caused by epilepsy);
• manic-depressive psychosis with a bipolar course, not amenable to treatment with lithium drugs or other drugs;
• febrile convulsions in children;
• children's teak;
• specific syndromes (Vesta, Lennox-Gastaut).

Forms of release

Tablets 300 mg and 500 mg (including Retard).

Instructions for use and dosing regimen

Treatment with Convulsophine begins with low doses of the drug, then they are gradually increased to optimal maintenance doses.

The initial dose of Convulsofina with monotherapy is 5-10 mg per kilogram of body weight. Every 4-7 days, this dose is increased by 5 mg. The average daily dose for adults and elderly and senile age is 20 mg per kilogram of body weight for adolescents older than 14 years - 25 mg per kilogram of body weight, for children aged from 3 to 14 years - 30 mg per kilogram of body weight.

If Convulsophine is prescribed together with other antiepileptic drugs or to replace the previous drug, the dose of the previously taken drug, especially phenobarbital, is immediately lowered. Complete transition to treatment with Convulsophine is slow, gradually lowering the dose of the previous drug.

Usually guided by the following indicative scheme of application of Convulsofina:

• children 3-6 years - daily dose of 300-600 mg;
• children 6-14 years - daily dose of 450-1500 mg;
• adults and adolescents over 14 years of age - daily dose of 1200-2100 mg.

If the renal function is impaired, the daily dose of Convulsofin should be reduced.

The daily dose is divided into 2-4 admission. The drug should be taken during or after a meal, without chewing and washing down with a small amount of liquid.

Side effect

• tremor;
• depression;
• feeling tired;
• hallucinations;
• aggressiveness;
• hyperactive state;
• psychoses;
• unusual agitation;
• motor anxiety or irritability;
• ataxia (impaired coordination of movements);
• dizziness;
• drowsiness;
• headache;
• encephalopathy (non-inflammatory diseases of the brain);
• dysarthria (pronunciation disorder);
• enuresis (urinary incontinence);
• Stupor (oppressed mental state, manifested in inhibition, lack of mobility and taciturnity);
• impaired consciousness;
• coma;
• hearing impairment;
• Diplopia (a visual disorder consisting of a bifurcation of visible objects);
• nystagmus (involuntary vibrational movements of the eyes);
• flickering flies before your eyes;
• nausea, vomiting;
• gastralgia (pain in the epigastric region);
• anorexia (pathological desire to lose weight);
• increased appetite;
• diarrhea, constipation;
• hepatitis (inflammatory liver disease);
• pancreatitis (inflammation of the pancreas);
• Hyperbilirubinemia (increase in the level of bilirubin);
• anemia (lowering of hemoglobin level);
• leukopenia (decrease in the number of leukocytes);
• thrombocytopenia (decrease in the number of platelets);
• reduction of fibrinogen;
• prolonged bleeding time;
• petechial hemorrhages (minor hemorrhages under the skin);
• bruising;
• hematomas;
• increased bleeding;
• skin rash;
• angioedema (swelling of the subcutaneous tissue, skin and mucous membranes);
• Stevens-Johnson syndrome (blisters on the mucous membrane of the mouth, throat, eyes, genitals, other areas of the skin and mucous membranes);
• alopecia (baldness);
• photosensitivity (hypersensitivity to ultraviolet);
• Dysmenorrhea (abdominal pain associated with uterine spasms during menstruation);
• secondary amenorrhea (the cessation of menstruation for six months or more in women of reproductiveage);
• increased mammary glands;
• galactorrhea (excretion of milk or colostrum, not related to feeding);
• increase or decrease in body weight;
• peripheral edema;
• hyperglycinemia (impaired metabolism of amino acids, accompanied by an elevated glycine content in the blood).

Contraindications

• liver failure;
• acute and chronic hepatitis;
• impaired pancreatic function;
• porphyria;
• hemorrhagic diathesis;
• thrombocytopenia;
• children under 3 years;
• liver disease in history;
• hypersensitivity to the drug.

Application in pregnancy and lactation

In pregnancy, the use of Convulsophine is possible only on strict indications, after careful evaluation of the expected benefit of therapy for the mother and the possible risk to the fetus.

When using Convulsofin in the early period of pregnancy, the risk of neural tube nebulization in the embryo (myelomeningocele) increases. Along with this, other abnormalities of fetal development can be noted. The risk of fetal development abnormalities increases with the combined use of Convulsofin with other antiepileptic drugs.

If it is impossible to refuse Convulsophine therapy in the first trimester, the drug is prescribed at the lowest doses, and between 20 and 40 days of pregnancy, the daily dose is divided into several small single doses during the day. It is necessary to regularly monitor the concentration of valproic acid in the blood plasma. For the purpose of early diagnosis of fetal development anomalies, it is recommended to perform ultrasound studies and an alpha-fetoprotein test.

Valproic acid is excreted in mother's milk in small amounts, not representing a danger to the child, therefore, as a rule, the termination of breastfeeding during the period of therapy with Convulsophine is not required.

Use in children

The drug is contraindicated for children under 3 years. Children (especially up to 2 years old) have a higher risk of developing severe liver function abnormalities with Convulsofin.

Application in elderly patients

For the elderly, the dose should be adjusted depending on the level of control of epilepsy. The daily dose is determined depending on the age and body weight of the patient, but a wide range of individual sensitivity to the drug should also be considered.

special instructions

With special care and careful medical supervision, the drug should be prescribed for bone marrow aplasia, pathological changes in the blood, organic brain diseases, hypoproteinemia, renal failure.

The transition from treatment with another anticonvulsant to Convulsophine therapy is slow, reaching a clinically effective dose for 2 weeks and gradually lowering the dose of the previous drug until it is discontinued. In patients who did not receive previous treatment with antiepileptic drugs, a clinically effective dose should be achieved after 1 week.

Side-effects are more likely to occur with combined therapy than with monotherapy with Convulsophine.

Before surgical manipulation of patients taking Convulsofin, should determine the number of platelets, bleeding time, coagulogram indicators.

When developing against the background of taking Convulsofina symptom complex "acute abdomen" before the beginning of surgery it is recommended to determine the level of amylase in the blood to exclude acute pancreatitis.

With the development of spontaneous hematomas and bleeding and the appearance of symptoms such as weakness, lethargic state, swelling, vomiting and jaundice, the drug should be discontinued immediately.

It should be borne in mind that against the background of taking Convulsophine, false-positive reactions are possible to the presence of ketone bodies in the urine, a distortion of the thyroid function indices.

During the treatment with Convulsophine, ethanol-containing (alcohol-containing) drinks are not allowed.

Control of laboratory indicators

On the background of therapy with Convulsofinum it is necessary to periodically monitor the activity of hepatic transaminases, the level of bilirubin, the picture of peripheral blood, the level of fibrinogen in the blood plasma, thromboplastin time, the level of alpha-amylase in the urine (every 3 months).

Impact on the ability to drive vehicles and manage mechanisms

The drug can reduce the speed of psychomotor reactions and the ability to concentrate, so patients taking Convulsofin should refrain from potentially dangerous activities.

Drug Interactions

With the simultaneous use of Convulsophine with ethanol (alcohol) and other drugs that depress the central nervous system, it is possible to increase the depression of the central nervous system (CNS).

With simultaneous use of Convulsofin and other antiepileptic drugs, antipsychotics, antidepressants, tranquilizers, barbiturates, MAO inhibitors, thymoleptics, it is possible to enhance their effects, including side effects.

Simultaneous administration of tricyclic antidepressants (imipramine) or phenytoin with Convulsophine may cause generalized epileptic seizures, and clonazepam-absense.

With the simultaneous use of Convulsofin with other anticonvulsant drugs (phenobarbital, phenytoin, carbamazepine, mefloquine), valproic acid in the serum can be decreased (acceleration of its metabolism).

With the simultaneous use of Convulsophine and anticoagulants (coumarin and indanedione derivatives, heparin, thrombolytic agents and antiaggregants), a mutual potentiation of the effect on the coagulating system of blood occurs and the risk of bleeding increases.

With simultaneous use with Convulsofin, in addition to CNS depression, tricyclic antidepressants, bupropion, clozapine, haloperidol, loxapine, maprotiline, molindone, MAO inhibitors, phenothiazines, pimozide, thioxanthenes can reduce the threshold of convulsive activity.

Convulsofin does not induce the induction of hepatic enzymes and does not reduce the effectiveness of oral contraceptives.

With the simultaneous use of Convulsophine with hepatotoxic drugs and ethanol, it is possible to increase the toxic effect of Convulsofin on the liver.

With the simultaneous use of Convulsophine with salicylates, its effects are enhanced (displacement from the bond with proteins).

With the simultaneous use of Convulsofin with barbiturates and primidon there is an increase in the concentration of the latter in blood plasma.

Convulsofin increases the half-life of lamotrigine up to 70 hours in adults and up to 45-55 hours in children.

Convulsofin reduces zidovudine clearance by 38%, while its half-life does not change.

Felbamate increases the concentration of valproic acid in plasma by 35-50%.

Valproic acid can also affect the metabolism and binding of blood plasma proteins to other drugs(e.g., codeine).

Analogues of the drug Convulsofin

Structural analogs for the active substance:

• Valopixime;
• Valparin;
• Valproate sodium;
• Valproic acid;
• Depakin;
• Dipromal;
• Convulex;
• Convulsofin-Retard;
• Enkorat.

Analogues for the pharmacological group (antiepileptic drugs):

• Actinerval;
• Algerian;
• Acetazolamide;
• Benzobarbital;
• Benzon;
• Briviak;
• Wimpat;
• Gabagamma;
• Gabapentin;
• Habitryl;
• Halodiff;
• Gapentec;
• Hexamidine;
• Depamid;
• Diazepam;
• Diakarb;
• Diphenine;
• Zagreton;
• Zenicetam;
• Zeptol;
• Zonegran;
• Inovevelon;
• Carbaleshin Retard;
• Carbamazepine;
• Carbapine;
• Caten;
• Kepayra;
• Keppra;
• Clonazepam;
• Clonotril;
• Convalis;
• Convilept;
• Convulsant;
• Lameptil;
• Lamyctal;
• Lamitor;
• Lamolope;
• Lamotrigine;
• Lamotriks;
• Levetinol;
• Levetiracetam;
• Lethiram;
• Lyrics;
• Mazepine;
• Maxitope;
• Maliazine;
• Mysolin;
• Neuronthin;
• Paglyuferal;
• Prabiegin;
• Pregabalin;
• Primidone;
• Relium;
• Replica;
• Rivotril;
• Ropimat;
• Seizar;
• Sibazon;
• Stasepine;
• Storilate;
• Suxilep;
• Tebantin;
• Tegretol;
• Thirapol;
• Topalepsin;
• Topamax;
• Topiramate;
• Topiromax;
• Topsaver;
• Thoreal;
• Trileptal;
• Phenobarbital;
• Finlepsin;
• Chloracon;
• Egipentin;
• Exalieff;
• Eltator;
• Epial;
• Epikepran;
• Epimax;
• Epitera;
• Epitope;
• Epitropyl;
• Eplorontin.

Review of the neurologist's doctor

Patients with generalized and partial seizures in the absence of contraindications often prescribe the drug Convulsofin. The active substance of this drug is valproic acid. It has an effective anticonvulsant, muscle relaxant and sedative effect. With the constant intake of tablets in patients improves mental state, mood. In addition, Confulfsin differs marked antiarrhythmic activity. With absences, temporal pseudoabsances, the drug exhibits high efficacy, and in psychomotor seizures the efficacy is much lower.

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