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Topapepsin - instructions for use, analogs, reviews and release forms (tablets 25 mg, 50 mg, 100 mg and 200 mg) of the drug for the treatment of epilepsy, Lennox-Gastaut syndrome and migraine prevention in adults, children and pregnancy. Composition and alcohol

Topapepsin - instructions for use, analogs, reviews and release forms (tablets 25 mg, 50 mg, 100 mg and 200 mg) of the drug for the treatment of epilepsy, Lennox-Gastaut syndrome and migraine prevention in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Topaleptsin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Topaleptsin 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 Topaleptsin in the presence of existing structural analogues.Use for the treatment of epilepsy, Lennox-Gastaut syndrome and migraine prevention in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

 

Topaleptsin - antiepileptic agent, refers to the class of sulfate-substituted monosaccharides.

 

Topiramate (active ingredient of Topalepsin) reduces the incidence of action potentials that are characteristic of a neuron in a state of persistent depolarization, which indicates the dependence of the blocking action of the drug on the sodium channels on the state of the neuron. Topiramate potentiates the activity of gamma-aminobutyric acid (GABA) against certain subtypes of GABA receptors (including GABAA receptors), and also modulates the activity of the GABAA receptors themselves, inhibits the activation of kainate sensitivity of kainate receptors and alpha-aminomethylisoxazole propionic acid receptors (AMPK- receptors) to glutamate, does not affect the activity of N-methyl-D-aspartate against ionotropic glutamate receptors that selectively bind N-methyl-D-aspartate (NMDA receptors). These effects of topiramate are dose-dependent with a plasma topiramate concentration of 1 μM to 200 μM, with minimal activity ranging from 1 μM to 10 μM.

 

In addition, topiramate inhibits the activity of certain isoenzymes of carbonic anhydrase, but this effect in the topiramate is weaker than that of acetazolamide and, apparently, is not the main antiepileptic activity of topiramate.

 

Composition

 

Topiramate + auxiliary substances.

 

Pharmacokinetics

 

After ingestion, topiramate is absorbed quickly and efficiently. Bioavailability - 81%. Eating does not have a clinically significant effect on the bioavailability of topiramate. Binding to plasma proteins is 13-17%. After ingestion, about 20% of the dose is metabolized. In the plasma, urine and feces of humans, 6 practically inactive metabolites were identified. It is excreted mainly by the kidneys in unchanged form (70%) and in the form of metabolites.

 

 Indications

  • epilepsy - as a monotherapy for initial treatment in patients older than 2 years (partial or primary generalized tonic-clonic seizures);
  • epilepsy - as part of complex therapy in patients older than 2 years (partial or generalized tonic-clonic seizures);
  • seizures on the background of the Lennox-Gastaut syndrome;
  • prevention of migraine attacks in adults.

 

Forms of release

 

Tablets coated with a coating, 25 mg, 50 mg, 100 mg and 200 mg.

 

Instructions for use and dosing regimen

 

Inside, regardless of food intake. Tablets should not be divided.

 

For optimal control of seizures, it is recommended to begin treatment with low doses with subsequent increase to an effective dose. When used as a monotherapy, it is necessary to take into account the possible effect of withdrawal of antiepileptic drugs (PEP) on the frequency of seizures. In cases where there is no need to abruptly cancel PEP, their dose is recommended to be reduced gradually, decreasing by 1/3 every 2 weeks. With the withdrawal of drugs (LS), which are inducers of microsomal liver enzymes, the concentration of topiramate in the blood plasma will increase, which should be taken into account in the therapy.

 

Monotherapy

 

Adults: at the beginning of the monotherapy - 25 mg once a day at night for 1 week. Then the dose is increased at intervals of 1-2 weeks by 25-50 mg per day (the daily dose is divided into 2 divided doses). If this mode of treatment is intolerant, the dose is increased by a smaller amount or at large intervals. The dose is selected depending on the effectiveness and tolerability of the therapy.The recommended initial target dose is 100-200 mg per day, the maximum daily dose should not exceed 500 mg with monotherapy. Dosing recommendations apply to all adults, including elderly patients who are not suffering from kidney disease.

 

Children: older than 6 years with monotherapy with topaleptsin in the 1st week of treatment - 0.5-1 mg per 1 kg of body weight before bedtime. Then the dose is increased with an interval of 1-2 weeks by 0.5-1 mg per 1 kg of body weight per day (the daily dose is divided into 2 divided doses). If this mode of therapy is intolerant, the dose is increased more smoothly or at large intervals between dose increases. The magnitude of the dose and the rate of its increase are determined by the clinical efficacy and tolerability of therapy. The recommended dose range for topiramate monotherapy in children - 100 mg per day, depends on the clinical efficacy (in children 6-16 years this dose is about 2 mg per 1 kg of body weight per day).

 

Combination Therapy

 

Adults: with the appointment as part of combination therapy with other anticonvulsant drugs in adults, the initial dose is 25-50 mg once a day at night for 1 week. The dose is then increased by 25-50 mg every week until the effective dose is reached.The minimum effective dose is 200 mg per day, the average daily dose is 200-400 mg, the frequency of administration is 2 times a day. Doses over 1600 mg per day have not been studied. The criterion for choosing the dose is the clinical effect and tolerability, in some patients this effect can be achieved with the drug once a day. Dosing recommendations apply to all adults, including elderly patients who are not suffering from kidney disease.

 

Children: when prescribed as part of combined anticonvulsant therapy in children older than 3 years, the recommended total daily dose is 5-9 mg per 1 kg of body weight in 2 divided doses. Selection of the dose begins with 25 mg per day (at a rate of 1-3 mg per 1 kg of body weight per day) overnight for 1 week. In the future, the dose can be increased by 1-3 mg per 1 kg of body weight for 1-2 weeks and taken in 2 divided doses. The criterion for correct dose selection is a stable clinical effect and good tolerability. The daily dose to 30 mg per 1 kg of body weight is usually well tolerated.

 

Prevention of migraine

 

The recommended total daily dose is 100 mg in 2 divided doses. Begin treatment with a dose of 25 mg or less at bedtime for 1 week. Then the dose is increased by 25 mg per day with an interval of 1 week.If this regime is intolerant, the dose is increased by a smaller amount or at longer intervals. The dose is selected depending on the clinical effect. In some patients, a positive result is achieved with a daily dose of 50 mg per day. When applying a dose of more than 100 mg per day, an additional effect in the prevention of migraine is not observed.

 

Side effect

  • drowsiness;
  • dizziness;
  • violation of attention;
  • amnesia (memory impairment);
  • psychomotor disorders;
  • convulsions;
  • incorrect coordination;
  • tremor (trembling of limbs or trunk);
  • lethargy (a painful condition characterized by slowness, lethargy, fatigue);
  • disturbance of balance;
  • Articulation disorder (speech), pronounced speech disorders;
  • oppression of consciousness;
  • convulsions of the type of large convulsive seizures;
  • visual field defect;
  • fainting;
  • salivation;
  • repetitive speech;
  • poor sleep quality;
  • loss of sensitivity;
  • depression;
  • slow thinking;
  • cognitive disorders (decreased memory, mental performance);
  • insomnia;
  • confusion, disorientation;
  • aggression, mood lability;
  • anxious arousal, anger;
  • inadequate behavior, suicidal ideation or attempt;
  • auditory and visual hallucinations;
  • decreased libido (sexual desire);
  • tearfulness, euphoria;
  • violation of reading skills;
  • flattening of emotions;
  • blurred vision, diplopia (double vision), decreased visual acuity;
  • dry eyes, photophobia, increased lacrimation;
  • one-sided blindness, transient blindness;
  • glaucoma;
  • violation of accommodation (adaptation of the eyes to changes in external conditions);
  • swelling of the eyelids;
  • night blindness;
  • oculomotor disorders;
  • anemia, leukopenia, thrombocytopenia, eosinophilia, neutropenia;
  • allergic edema, edema of the conjunctiva;
  • anorexia (eating disorder), decreased appetite, increased appetite;
  • constant thirst;
  • ringing in the ears, discomfort in the ears, pain in the ear;
  • deafness, one-sided deafness, neurosensory deafness;
  • bradycardia (decrease in heart rate), heart palpitations;
  • flushes of blood;
  • nasopharyngitis (inflammation of the nasal mucosa and posterior pharyngeal wall);
  • nosebleeds, nasal congestion;
  • cough, shortness of breath during physical exertion;
  • nausea, diarrhea, vomiting, constipation;
  • abdominal pain;
  • dry mouth;
  • gastritis (inflammation of the gastric mucosa);
  • pancreatitis (inflammation of the pancreas);
  • flatulence (increased gassing in the intestine);
  • bleeding gums;
  • hypersecretion of the salivary glands;
  • pain in the oral cavity, bad breath;
  • hepatitis (inflammation of the liver), liver failure;
  • alopecia (baldness);
  • skin itching, rash, urticaria, erythema (redness of the skin);
  • allergic dermatitis;
  • swelling of the face;
  • Stevens-Johnson syndrome, erythema multiforme;
  • arthralgia (joint pain);
  • muscle spasms, myalgia (muscle pain), muscle cramps, muscle weakness, muscle pain in the chest;
  • swelling of the joints;
  • nephrolithiasis (formation of kidney stones);
  • pollakiuria (frequent urination), dysuria (urination disorder);
  • urinary incontinence;
  • hematuria (blood in the urine);
  • an urgent painful urge to urinate;
  • pain in the kidneys;
  • erectile dysfunction, sexual dysfunction;
  • irritability;
  • violation of gait;
  • influenza-like condition;
  • coldness of limbs;
  • feeling of intoxication;
  • weight loss, weight gain;
  • crystalluria (crystals of salts in urine);
  • an increase in the activity of hepatic enzymes, hypokalemia, a decrease in the content of hydrocarbonates in the blood.

 

Contraindications

  • hypersensitivity to topiramate;
  • children under 2 years.

 

Application in pregnancy and lactation

 

Adequate and strictly controlled clinical trials of the safety of topiramate in pregnancy have not been conducted.

 

The use of topaleptsin during pregnancy can cause damage to the fetus. The data of the register of pregnant women show that when the intrauterine effect of topiramate on the fetus increases the risk of developing congenital malformations (for example, craniofacial defects, such as "hare lip" and "wolf mouth", hypospadias and abnormalities of development of various body systems). These developmental anomalies were recorded both with monotherapy with topiramate and with its use in combination therapy. In comparison with the group of patients not taking antiepileptic drugs, the data of the register of pregnant women with monotherapy with topiramate testifies to an increase in the frequency of the birth of children with a low body weight (less than 2500 grams). Causal link is not established.

 

When treating women of childbearing age, the expected benefit of therapy for the mother and the potential risk to the fetus should be weighed and alternative treatment options considered. If topiramate is used in pregnancy or if pregnancy occurs during the treatment period, the patient should be warned about the potential risk to the fetus.

 

A limited number of observations suggest that topiramate is excreted in breast milk. If it is necessary to use during the lactation period, the question of stopping breastfeeding should be solved.

 

Use in children

 

Do not use in children under 2 years of age.

 

Application in elderly patients

 

In elderly patients, dose adjustment is not required.

 

special instructions

 

The use of topiramate for the treatment of acute migraine attacks has not been studied.

 

It should be used with caution in renal and hepatic insufficiency, nephrourolythiasis (including personal and family history), hypercalciuria.

 

Patients with impaired renal function and patients on hemodialysis require correction of the topiramate dosage regimen.

 

To abolish Topalepsin should be gradual in order to minimize the possibility of increasing the frequency of convulsive seizures.In clinical studies in adults in the treatment of epilepsy, the doses were reduced by 50-100 mg at intervals of 1 week and by 25-50 mg in adults receiving topiramate at a dose of 100 mg per day to prevent migraine. In children, in clinical trials, topiramate was gradually withdrawn within 2-8 weeks. If the medical indications require a rapid withdrawal of topiramate, it is recommended to monitor the patient's condition.

 

To reduce the risk of developing nephrolithiasis during the treatment period, you should increase the amount of fluid consumed.

 

Against the background of the use of topiramate, sweating and hyperthermia can be reduced, especially in young children, in conditions of high ambient temperature. Sufficient replenishment of fluid loss before and during activities such as exercise or staying at high temperatures can reduce the risk of complications caused by overheating.

 

During the treatment period, patients should be monitored to identify signs of suicidal ideation and prescribe appropriate treatment. It is necessary to recommend to patients (and, if necessary,caregivers) immediately seek medical help in case of signs of suicidal idealization or suicidal behavior.

 

If abnormalities occur on the part of the eye, including a syndrome involving myopia associated with occlusive glaucoma, Topapepsin should be discontinued as soon as the attending physician deems it possible. If necessary, measures should be taken to lower the intraocular pressure.

 

To avoid the occurrence of metabolic acidosis, during the treatment with topiramate it is recommended to carry out the necessary studies, including determination of the concentration of hydrocarbonates in the serum. When there is metabolic acidosis and its persistence, it is recommended to reduce the dose or stop taking topiramate. In children, chronic metabolic acidosis can lead to slower growth. The effect of topiramate on growth and possible complications associated with the bone system has not been systematically studied in children and adults.

 

If the weight of the body decreases, the diet should be adjusted.

 

It is not recommended the simultaneous use of other drugs,which exert a depressing effect on the central nervous system (CNS).

 

During treatment, the patient should avoid drinking alcohol.

 

Impact on the ability to drive vehicles and manage mechanisms

 

With caution should be used in patients engaged in potentially dangerous activities requiring increased attention and speed of psychomotor reactions, since topiramate can cause drowsiness, dizziness, visual impairment.

 

Drug Interactions

 

With simultaneous application with Topalepsin phenytoin and Carbamazepine reduce its concentration in the blood plasma. This is due to the induction of enzymes under the influence of phenytoin and carbamazepine, with the participation of which the metabolism of topiramate is carried out. In some cases, with the use of topiramate, there was an increase in the concentration of phenytoin in the blood plasma.

 

With simultaneous application of a single dose of topiramate and digoxin, it is possible to reduce the area under the pharmacokinetic curve (AUC) of digoxin.

 

With the simultaneous use of an oral contraceptive containing norethindrone and ethinyl estradiol, topiramate did not significantly affect the clearance of norethindrone, however, the plasma clearance of ethinyl estradiol increased significantly.Thus, with the simultaneous administration of topiramate with oral contraceptives, their effectiveness may be reduced.

 

Patients taking metformin, pioglitazone, glibenclamide with simultaneous application or cancellation of topiramate may fluctuate in plasma glucose. With these combinations, you should monitor the plasma glucose level.

 

With the simultaneous use of topiramate with drugs that predispose to the development of nephrolithiasis, there may be an increased risk of kidney stones.

 

Analogues of the drug Topaleptsin

 

Structural analogs for the active substance:

  • Maxitope;
  • Ropimat;
  • Topamax;
  • Topiramate;
  • Topiromax;
  • Topsaver;
  • Thoreal;
  • Torapimat;
  • Epimax;
  • The epitope.

 

Analogues for the pharmacological group (antiepileptic drugs):

  • Actinerval;
  • Algerian;
  • Acetazolamide;
  • Benzobarbital;
  • Benzon;
  • Briviak;
  • Valopixime;
  • Valparin;
  • Valproic acid;
  • Vero-Lamotrigine;
  • Wimpat;
  • Gabagamma;
  • Gabapentin;
  • Halodiff;
  • Gapentec;
  • Hexamidine;
  • Depakin;
  • Depamid;
  • Diazepam;
  • Dipromal;
  • Diphenine;
  • Zagreton;
  • Zenicetam;
  • Zeptol;
  • Zonegran;
  • Inovevelon;
  • Carbaleptin retard;
  • Carbamazepine;
  • Caten;
  • Keppra;
  • Clonazepam;
  • Convalis;
  • Convulex;
  • Convulsant;
  • Lameptil;
  • Lamyctal;
  • Lamitor;
  • Lamotrigine;
  • Lamotriks;
  • Levetiracetam;
  • Lethiram;
  • Mazepine;
  • Mysolin;
  • Neuronthin;
  • Prigabilon;
  • Relium;
  • Rivotril;
  • Ropimat;
  • Sabril;
  • Sibazon;
  • Stasepine;
  • Suxilep;
  • Tebantin;
  • Topamax;
  • Topiromax;
  • Thoreal;
  • Trileptal;
  • Phenobarbital;
  • Finlepsin;
  • Chloracon;
  • Exalieff;
  • Enkorat;
  • Epimax;
  • Epitera;
  • Epitropyl;
  • Eplorontin.

 

Response of a pediatric neurologist

 

I can say that the antiepileptic drug Topaleptsin usually gives a good therapeutic effect in patients of childhood, both in monotherapy and in combination with other medicines. The frequency of convulsive attacks decreases, many children experience persistent remission of the disease. But the side effects when taking Topaleptsin are registered in almost every patient. Parents complain of lethargy and drowsiness in children, anorexia and weight loss, impaired vision and memory disorders. I do not remember in my practice a single case where the treatment with this drug was absolutely problem-free.

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