Active substanceValproic acidValproic acid
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: calcium valproate dihydrate 333.00 mg, which corresponds to the calcium valproate 300.00 mg, which corresponds to valproic acid 265.00 mg;

    Excipients: potato starch 166.40 mg, gelatin 11.00 mg, silicon dioxide 16.50 mg, talc 17.60 mg, magnesium stearate 5.50 mg.

    Description:

    Round, flat tablets of white color with a weak yellowish tinge, with bevelled edges and with a risk on one side.

    Pharmacotherapeutic group:Antiepileptic remedy
    ATX: & nbsp

    N.03.A.G.01   Valproic acid

    Pharmacodynamics:

    Antiepileptic drug, which has central muscle relaxant and sedative effect.

    It shows antiepileptic activity in various types of epilepsy. The main mechanism of action, apparently, is associated with the action of valproic acid on the GABA-ergic system: it increases the content of gamma-aminobutyric acid (GABA) in the central nervous system (CNS) and activates GABA-ergic transmission.

    Pharmacokinetics:

    Absorption - high, food slightly reduces the absorption rate; bioavailability - 100%.The maximum concentration in the plasma is created 3-4 hours after the administration, the equilibrium concentration is reached on the 2-4th day after the start of the reception, which depends on the intervals between the doses. The therapeutic concentrations in the blood plasma range from 50-150 mg / l. The volume of distribution is 0.2 l / kg. Binding with proteins reaches 90-95% at a plasma concentration of up to 50 mg / l and decreases to 80-85% at a concentration of 50-100 mg / l (with uremia, hypoproteinemia, cirrhosis, protein binding is reduced). Penetrates through the placental and blood-brain barrier, excreted in breast milk (concentration in breast milk is 1-10% concentration in the blood plasma of the mother). The content in the cerebrospinal fluid correlates with the size of the protein-unbound fraction. Metabolized by glucuronization and oxidation in the liver, T1/2 - 12-16 hours. 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. When combined with other drugs, the elimination half-life (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 18 months of age can be significantly longer.

    Indications:

    Monotherapy or in combination with other antiepileptic drugs:

    - for treatment of generalized epileptic seizures: clonic, tonic, tonic-clonic, absences, myoclonic, atonic, Lennox-Gastaut syndrome;

    - for the treatment of partial epileptic seizures: partial seizures with or without secondary generalization.

    Contraindications:

    Hypersensitivity to valproic acid, valproate semiotrium, valpromide and other components of the drug; acute and chronic hepatitis (including a history of the patient or a family history), a violation of liver function, severe liver damage with death in close relatives (blood relatives) who took valproic acid; impaired pancreatic function; porphyria; thrombocytopenia; impaired blood clotting; simultaneous use with mefloquine, St. John's wort preparations, lamotrigine, carbapenem; children's age till 6 years.

    Carefully:

    Inhibition of bone marrow function, organic brain disease,impaired renal function, hypoproteinemia, combined antiepileptic therapy (CPET) in children, in children with mental retardation and severe forms of epilepsy, congenital fermentopathies, systemic lupus erythematosus.

    Pregnancy and lactation:

    The use of valproic acid in the first and second trimester of pregnancy is associated with an increased risk of fetal neural tube defects (spina bifida, myelomeningocele, etc.) and other developmental defects along the middle line such as hypospadias in boys, various anomalies of the musculoskeletal system and malformations development of the heart. The overall risk of congenital malformations with valproic acid is not higher than with the use of other antiepileptic drugs (PEP). The risk of developing defects is higher with CPET than with monotherapy with valproic acid. There are reports of the development of bilateral radial dysplasia in the fetus, facial dysmorphia in combination with a delay in intellectual development of varying severity (especially speech development), defects in the development of fingers and nails of the hands and feet.Also reported on the development of various autistic disorders in children exposed to intrauterine effects of valproic acid. Valproic acid penetrates the placenta. The concentration of valproic acid in the fetal blood plasma is higher than in the blood plasma of the mother. In the event that it is not possible to cancel Convulsofin ® in women during the first trimester of pregnancy, especially between the 20th and 40th day of pregnancy, it is necessary to revise the drug treatment plan.

    Convulsofin ® should not be used during pregnancy. The use of the drug in pregnancy is possible only with intolerance or the inability to use other PEP. Women of reproductive age should be informed about the need to use effective methods of contraception. If a woman has planned a pregnancy or has a pregnancy diagnosed, the relationship between the expected benefit of valproic acid for the mother and the risk to the fetus and the baby should be assessed, and the possibility of drug cancellation should be considered.

    During pregnancy, do not interrupt treatment with drugs containing valproic acid, without agreement with the doctor, tk.a sudden discontinuation of therapy or an uncontrolled reduction in the dose of the drug may cause epileptic seizures, which in turn can cause harm to the mother and her future child. If it is not possible to cancel the drug, all measures should be taken to minimize the teratogenic effect of valproic acid. It is recommended to monotherapy with the drug in the minimum effective dose, with the daily dose to be divided into several methods, since the development of fetal defects is apparently associated with a high maximum concentration of valproic acid in the blood plasma. In this connection, during pregnancy, valproic acid should be used in a sustained release dosage form. In addition, even with a constant dose of the drug, the concentration of valproic acid in the plasma should be monitored regularly because it may change during pregnancy. In addition, at the stage of pregnancy planning (one month before conception) and up to the end of the first trimester of pregnancy, it is necessary to add folic acid at a dose of 5 mg per day to antiepileptic treatment to minimize the risk of developing neural tube defects.

    It is recommended to perform prenatal diagnosis (ultrasound and determination of the content of alpha-fetoprotein in the mother's plasma) for early detection of fetal development defects.

    The use of valproic acid during pregnancy can cause hemorrhagic syndrome in newborns, the cause of which, apparently, is hypofibrinogenemia. There were reports of fatal cases of afibrinogenemia. It is possible that hypofibrinogenemia is also accompanied by a deficiency of coagulation factors. However, a distinction should be made between this symptom-complex and the vitamin K-dependent clotting factor deficiency caused by the inducer of microsomal liver enzymes, for example, such as phenobarbital. It is for this reason that neonates need to determine the number of platelets, fibrinogen content and clotting factors. There were no signs of "withdrawal" of valproic acid in newborns.

    Valproic acid is excreted in breast milk. There are reports that the concentration of valproic acid in breast milk was 1-10% of the concentration in the blood plasma of the mother.During the period of breastfeeding, the use of the drug Convulsofin ® is possible only if the expected benefit for the mother exceeds the possible risk for the baby.

    Dosing and Administration:

    Inside, with food or immediately after eating, without chewing, squeezed a little water.

    The daily dose is used in 2-4 admission. Dosage and duration of use of the drug Convulsofin® defines the attending physician individually for each patient. Treatment begins with a minimal dose, gradually increasing it to achieve a clinical effect.

    With monotherapy, the initial dose of Convulsofin ® is 5-10 mg / kg / day. Every 4-7 days the dose is increased by about 5 mg / kg / day.

    Average daily dose in adults and elderly patients reaches 20 mg / kg / day, in children 14-18 years old - 25 mg / kg / day, in children 6-14 years old - 30 mg / kg / day of body weight.

    In some cases, the therapeutic effect of the drug is fully manifested only after 4-6 weeks of treatment. Therefore, care must be taken to increase gradually the daily dose. Usually guided by the following indicative scheme of drug use:

    Age

    Weight bodies (kg)

    Average daily dose (mg / day)

    amount tablets

    Adults

    not less than 60

    1200-2100

    4-7

    Children 14-18 years old

    40-60

    600-1500

    2-5

    Children 6-14 years old

    25-40

    600 -1200

    2-4

    When used with other PETs or the replacement of another PEP with Convulsofin®, the dose of the previously taken PEP, in particular phenobarbital, is immediately lowered. Complete transition to monotherapy with the drug Convulsofin ® is carried out slowly, gradually lowering the dose of the previously taken PEP.

    In patients with renal insufficiency should take into account the possibility of increasing the concentration of free valproic acid in the blood serum and in accordance with this need to reduce the dose of the drug. The dose and duration of the use of the drug Convulsofin® should be determined by the doctor individually for each patient.

    Side effects:

    Side effects are classified according to the following frequency: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%.

    From the side of the blood and lymphatic system: often - thrombocytopenia, leukopenia; very rarely - suppression of bone marrow function, isolated aplasia of red blood cells, leukopenia, neutropenia, pancytopenia, anemia, hypofibrinogenemia.

    From the immune system: rarely - vasculitis, systemic lupus erythematosus.

    From the nervous system: often - drowsiness, slight postural tremor, paresthesia; infrequently - headaches, ataxia, muscle spasm, excitability, hyperactivity, aggression, depression, fatigue, confusion, especially at the beginning of treatment, stupor (partially associated with increased epileptic seizures), lethargy, hallucinations; rarely - chronic encephalopathy, accompanied by neurological symptoms and violation of higher functions of the cerebral cortex, dysarthria, amy, muscle hypotension, impaired movement (choreic dyskinesia) (with high doses and CPET); very rarely - parkinsonism, extrapyramidal symptoms; single cases - dementia with cerebral atrophy, reversible after drug discontinuation; inhibition, cognitive disorders, diffuse changes in the electroencephalogram (with prolonged CPE).

    From the side of the organ of vision: unknown frequency - diplopia, nystagmus, flashing of "flies" before the eyes.

    From the organ of hearing: infrequently, noise in the ears; rarely - reversible or irreversible deafness.

    From the side of metabolism and nutrition: often - increase or decrease in body weight, increased appetite, anorexia.

    From the digestive system: often - diarrhea, nausea, epigastric pain, vomiting (passing without drug withdrawal for several days); infrequently - hypersalivation; very rarely - pancreatitis, including fatal, dose-dependent severe violation of liver function, including fatal.

    From the urinary system: infrequently - enuresis (in children); rarely - reversible Fanconi syndrome (metabolic acidosis, phosphaturia, aminoaciduria, glucosuria).

    On the part of the reproductive system: rarely - amenorrhea, polycystic ovary; unknown frequency - dysmenorrhea, male infertility.

    From the skin and subcutaneous tissues: infrequently - hemorrhage; very rarely erythema; single reports - Stevens-Johnson syndrome, toxic epidermal necrolysis, Lyell's syndrome.

    Allergic reactions: unknown frequency - rash accompanied by eosinophilia, urticaria, angioedema, photosensitivity.

    Laboratory indicators: very often - isolated or moderate hyperammonemia without changes in liver function,not requiring discontinuation of treatment; often - a transient increase in the activity of "hepatic" aminotransferases; infrequently - fermentopathy of unknown origin, reversible after withdrawal of the preparation containing valproic acid; hyperammonemia with simultaneous use with phenobarbital and other PEP; reduction in fibrinogen or coagulation factor VIII, platelet aggregation, prolongation of bleeding time; rarely - an increase in testosterone in the blood plasma, hyponatremia; Very rarely - hypercreatininaemia, hyperglycinemia, hyperbilirubinemia, increased lactate dehydrogenase activity (dose-dependent).

    Other: often - hair loss; infrequent peripheral edema; very rarely - severe weakness, nosebleeds.

    Overdose:

    Symptoms: nausea, vomiting, dizziness, diarrhea, impaired breathing function, muscle hypotension, hyporeflexia, miosis, coma (on EEG increase in slow waves and background activity).

    Treatment: gastric lavage (no later than 10-12 hours after an overdose), reception of activated carbon, forced diuresis, maintenance of vital functions, hemodialysis.

    Interaction:

    With the simultaneous use of valproic acid with other PEP possible their interaction, so you need to monitor the concentration of drugs in the blood plasma.

    The effect of other drugs on the concentration of valproic acid

    With the simultaneous use of microsomal liver enzymes with PEP-inducers, including with phenobarbital, phenytoin, primidon, carbamazepine, the concentration of valproic acid in the blood plasma decreases due to the increase in hepatic metabolism and its antiepileptic effect decreases.

    When used simultaneously with felbamate, the clearance of valproic acid decreases by 22-50%. Depending on the applied dose of felbamate, the concentration of free valproic acid in the blood serum increases linearly by 18%.

    Drug preparations of St. John's wort reduce the concentration of valproic acid in blood plasma.

    Mefloquine enhances the metabolism of valproic acid and has a spasmogenic effect, which can cause an epileptic attack.

    Antibiotics-carbapenems reduce the concentration of valproic acid by 60-100% for 2 days of simultaneous use, which can cause epileptic seizures.As a result of a rapid and significant drop in the concentration of valproic acid in plasma, it is difficult to monitor this interaction (concentration control and dose adjustment of valproic acid). Consider using other antibiotics.

    The concentration of valproic acid in the blood plasma increases with simultaneous use with cimetidine, erythromycin and fluoxetine. At the same time, cases of a decrease in the concentration of valproic acid in blood plasma have been reported when used with fluoxetine.

    With simultaneous application from the reefmPeggthe concentration of valproic acid in the blood plasma may decrease, which may lead to a loss of clinical efficacy of valproic acid.

    When used simultaneously with indirect anticoagulants, the risk of hemorrhagic reactions may increase. It is necessary to monitor the prothrombin index.

    When used simultaneously with drugs that have a high and strong association with blood plasma proteins (acetylsalicylic acid) it is possible to increase the concentration of the free valproic acid fraction (the valproic acid is reduced with plasma proteins) and the effects of valproic acid are possibly increased.

    The effect of valproic acid on other drugs

    Valproic acid may potentiate other psychotropic drugs, including neuroleptics, MAO inhibitors, antidepressants and benzodiazepines, however, while the application is recommended to control the clinical condition of the patient and carry out dose correction if necessary.

    Valproic acid does not affect the concentration of lithium in the blood plasma.

    Valproic acid increases phenobarbital concentration in plasma, resulting in the development can be pronounced inhibition in patients, particularly in children. It is necessary to reduce the dose of phenobarbital and primidone (primidon partially metabolized to phenobarbital) during use of valproic acid and to carry out control of patients during the first 15 days of CHP.

    Addition valproate therapy phenytoin or increasing doses of valproic acid while the use of phenytoin may increase the concentration of free phenytoin (active portion) without increasing the concentration of total phenytoin in blood plasma, which in turn may increase the risk of adverse effects, particularly in patients with brain damage.

    Valproic acid can potentiate the toxic effect of carbamazepine. It is necessary to carefully select the dose when using this combination of drugs.

    Valproic acid displaces diazepam from binding to plasma proteins and suppresses its metabolism. In healthy volunteers valproic acid doubled the fraction of diazepam not associated with plasma proteins, which was accompanied by a significant increase in the apparent volume of distribution and clearance of diazepam (20 and 25%, respectively). The half-life of diazepam remained unchanged.

    With the simultaneous use of lorazepam in healthy volunteers, the clearance of lorazepam decreased to 40%.

    With CPET, clonazepam and phenytoin increased the clearance of phenytoin in children.

    With the simultaneous use of valproic acid and lamotrigine, the risk of developing severe skin reactions increases. Valproic acid inhibits the metabolism of lamotrigine, therefore a correction of the lamotrigine dose is necessary.

    Valproic acid can reduce the clearance of felbamate by 16% and increase its concentration in the blood plasma by about 50%.

    Valproic acid affects metabolism and association with plasma proteins of such drugs as codeine.

    Valproic acid increases the concentration of zivudine in the blood plasma, which increases the manifestation of its toxicity.

    With simultaneous use with nimodipine, the concentration of nimodipine in the blood plasma increases and its hypotensive effect (inhibition of the metabolism of nimodipine by valproic acid) is enhanced.

    Other interactions

    Valproic acid does not induce the induction of microsomal enzymes and does not reduce the effectiveness of oral contraceptives. When used simultaneously with other hepatotoxic drugs and ethanol valproic acid can increase toxic effects on the liver.

    Special instructions:

    Before and during therapy with Konvulsofin®, especially during the first 6 months of treatment, particularly at-risk patients, it is recommended thorough clinical and laboratory investigation, including the liver, pancreas, blood coagulation, metabolic rate (the study hemogram, including the determination of the number of platelets, the concentration of bilirubin,activity of aspartate aminotransferase, alanine aminotransferase, gamma-glutamyltransferase, lipase, alpha-amylase activity in blood plasma glucose, total protein concentration in blood plasma indicator SWIR, partial thromboplastin time, fibrinogen, Factor VIII, other coagulation factors).

    During the first 6 months of treatment, the patient, people close to the patient and the attending physician should regularly contact in order to prevent the development of unwanted effects.

    It is necessary to warn people close to the patient about the possibility of liver function abnormalities and involve them in monitoring the patient's condition.

    Increased risk of developing severe hepatitis, including fatalities, infants and children up to 3 years with severe epilepsy, especially epilepsy, linked with brain damage, mental retardation and / or congenital metabolic or degenerative diseases. At the age of more than 3 years the frequency of such complications decreases significantly and gradually decreases.

    In most cases, liver function abnormalities were observed during the first 6 months of treatment, usually between 2 and 12 weeks, and most often at CPET.

    Of particular importance for the early detection of liver disease are, first, the clinical manifestation of nonspecific symptoms (severe asthenia, intolerance to conventional food, intolerance to valproic acid, anorexia, fatigue, drowsiness, vomiting and abdominal pain, hemorrhages, epistaxis, edema of the eyelids and lower extremities that occur even before the change in laboratory parameters), secondly, relapse or increased frequency and / or change in the severity of epileptic seizures against the background of antiepileptic therapy. It is recommended to inform the patient, if it is a child, then his parents, that if such symptoms appear, you should immediately consult a doctor.

    When detecting an abnormally low prothrombin content, a significant decrease in fibrinogen and clotting factors, an increase in bilirubin concentration and activity of "hepatic" aminotransferases, treatment with valproic acid should be immediately stopped.

    It should be remembered that treatment with Convulsofin ®, like other PEPs, may be accompanied by a small transient increase in the activity of "hepatic" aminotransferases, especially at the beginning of treatment, in the absence of any clinical symptoms.In this case it is recommended to conduct a complete laboratory examination, including the determination of a prothrombin index, and to adjust the dose of the drug.

    In the event that a patient with liver damage takes salicylates, stop taking them; the metabolism of salicylates goes along the same path as the metabolism of valproic acid.

    Children are at increased risk of developing pancreatitis with valproic acid. With age, the risk of developing pancreatitis is reduced. Pancreatitis in combination with liver failure increases the risk of death.

    If severe abdominal pain, nausea, vomiting and / or anorexia occur, the patient should be examined immediately. In case of confirmation of the diagnosis of pancreatitis, in particular when the activity of pancreatic enzymes in the blood plasma increases, the use of Convulsofin® should be stopped and appropriate treatment initiated.

    When used in women of reproductive age, before using the drug Convulsofin®, make sure that the patient is not pregnant, and recommend an effective method of contraception for her.

    In children, valproic acid dosage forms should be used, allowing dosing of the drug.

    In the treatment of patients with renal insufficiency and hypoproteinemia, the concentration of valproic acid in the blood plasma increases. Correction of the dose of Convulsofin® is necessary.

    When taking PEP for various indications, there were reports of cases of suicidal thoughts and suicidal behavior. A meta-analysis of randomized placebo-controlled studies of PEP also revealed a moderately increased risk of suicidal ideation and suicidal behavior. The mechanism of development of this effect is not known and the available data do not allow to exclude the risk of its occurrence with the use of the preparation Convulsofin®.

    Patients should be checked for signs of suicidal thoughts or suicidal behavior. If necessary, appropriate treatment is provided. Patients and people caring for patients should be warned about the need to seek medical help when there are signs of suicidal thoughts or suicidal behavior.

    Drugs containing valproic acid, in rare cases, can cause a reaction of the body's immune system. Nevertheless, in patients with systemic lupus erythematosus, the use of Convulsofin ® is only possible if the expected use benefit exceeds the possible risk.

    The use of Convulsofin® in patients with deficient enzymes of the ornithine urea cycle is not recommended. There have been reports of cases of encephalopathy developing against a background of hyperammonemia with a lethal outcome. In case of symptoms of apathy, drowsiness, vomiting, arterial hypotension and an increase in the number of antiepileptic seizures, the concentration of ammonium and valproic acid in the blood plasma should be determined and, if necessary, the dose of the drug should be reduced. If there is a suspicion of an already existing enzymatic breakdown in the urea cycle, the concentration of ammonia in the blood serum should be determined before using Convulsofin®.

    It should be borne in mind that the initiation of treatment with Convulsofin® may be accompanied by transient symptoms of nausea, vomiting, anorexia, which disappear when the dose is reduced.Before the surgical intervention, it is necessary to conduct a study of the blood coagulation system.

    If there is a symptomatology of the "acute" abdomen before the beginning of surgical intervention, it is recommended to determine the activity of amylase in the blood to exclude acute pancreatitis.

    Patients with oppression of bone marrow function should be under the supervision of a doctor.

    Before taking the drug Convulsofin®, it is necessary to warn the patient about a possible increase or decrease in body weight during treatment and the need to monitor this indicator, including diet.

    Despite the fact that there is no reliable data on the occurrence of a relapse of epileptic seizures after the sudden withdrawal of Convulsofin®, cancellation should be done gradually and only under the supervision of a doctor.

    Patients who receive other antiepileptic drugs should be transferred to receive Convulsofin ® gradually, reaching a clinically effective dose within 2 weeks. After this, a gradual cancellation of other antiepileptic drugs is carried out.

    In patients who do not receive other antiepileptic drugs, a clinically effective dose should be achieved within 1 week.

    At simultaneous application of preparations-antagonists of vitamin A recommend to supervise changes of parameter Kvika. It is necessary to warn patients that they do not use acidic drinks and refrigerated foods at the same time with the use of the drug Convulsofin®.

    Do not drink beverages that contain ethanol.

    During treatment of patients with diabetes should be aware of the possible distortion of the results of urine tests (ketone bodies in the urine).

    Dyspeptic disorders develop less frequently when taking antispasmodics and enveloping agents.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets, 300 mg.

    Packaging:

    For 100 tablets in a plastic bottle of white color with a plastic pull-on lid and control of the first autopsy.

    1 bottle with instructions for use in a cardboard box.

    Storage conditions:

    Store at a temperature not higher than 25 ° C, out of the reach of children.

    Shelf life:

    5 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N014780 / 01
    Date of registration:29.01.2009 / 17.01.2013
    Expiration Date:Unlimited
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp03.02.2018
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