Topalepsin - Instructions For Use, Price, Reviews, Analogs Of Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Topalepsin

Topalepsin: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Topalepsin

ATX code: N03AX11

Active ingredient: topiramate (Topiramate)

Producer: JSC "Chemical and Pharmaceutical Plant" AKRIKHIN "(Russia)

Description and photo update: 2020-04-03

Prices in pharmacies: from 192 rubles.

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Topalepsin is an antiepileptic drug belonging to the class of sulfate-substituted monosaccharides.

Release form and composition

Dosage form - film-coated tablets: biconvex, round, the color at the break - from white to white with a grayish or creamy shade, the color of the film shell - from light pink to pink with a creamy shade (tablets with a dosage of 25, 50 and 100 mg - 10 pcs. in a blister, in a cardboard box 3 packages and instructions for use of Topalepsin; tablets with a dosage of 200 mg - 4 pcs. in a blister strip or 28 pcs. in a polypropylene / polyethylene can, 7 packs or 1 can in pack of cardboard along with instructions for use of the drug).

1 tablet contains:

• active ingredient: topiramate (in terms of 100% substance) - 25/50/100/200 mg;
• additional ingredients: MCC (microcrystalline cellulose) - 12.5 / 25/50/100 mg; pregelatinized starch - 12/24/48/96 mg; corn starch - 7.5 / 15/30/60 mg; crospovidone - 2.5 / 5/10/20 mg; croscarmellose sodium - 1.5 / 3/6/12 mg; lactose monohydrate - 17.5 / 35/70/140 mg; colloidal silicon dioxide - 1/2/4/8 mg; magnesium stearate - 0.5 / 1/2/4 mg;
• film shell: lactose monohydrate - 0.24 / 0.48 / 0.96 / 1.92 mg; titanium dioxide - 0.432 / 0.864 / 1.728 / 3.456 mg; glycerol - 0.32 / 0.64 / 1.28 / 2.56 mg; hypromellose - 2/4/8/16 mg; talc - 0.68 / 1.36 / 2.72 / 5.44 mg; macrogol 6000 - 0.32 / 0.64 / 1.28 / 2.56 mg; iron dye red oxide - 0.008 / 0.016 / 0.032 / 0.064 mg.

Pharmacological properties

Pharmacodynamics

Topalepsin is an antiepileptic drug. Due to the effect it exerts, the frequency of the appearance of action potentials, which are characteristic of a neuron in a state of persistent depolarization, decreases. This is evidence of the dependence of the blocking action of topiramate on sodium channels on the state of the neuron; there is an increase in the activity of GABA (gamma-aminobutyric acid) in relation to some subtypes of GABA receptors (including GABAA receptors), as well as modulation of the activity of the GABAA receptors themselves. Topiramate prevents kainate from activating the sensitivity of kainate / AMPK receptors (alpha-amino-3-hydroxy-5 methylisoxazole-4-propionic acid) to glutamate, does not affect the activity of N-methyl-D-aspartate towards NMDA receptors. These effects are dose-dependent at plasma concentrations of the active substance from 1 to 200 μM, with a minimum activity in the range from 1 to 10 μM.

Topiramate inhibits the activity of some isoenzymes of carbonic anhydrase (II – IV), but this effect is much weaker than that of acetazolamide, and, most likely, is not the main one in the anticonvulsant activity of the substance.

Pharmacokinetics

Pharmacokinetic characteristics of topiramate:

• absorption: topiramate is characterized by a high degree of absorption, its bioavailability is 80% (this parameter does not depend on meal time). The maximum concentration of the substance (C _max) in the blood plasma is reached 2 hours after taking the drug orally at a dose of 400 mg. After repeated oral administration at a dose of 100 mg 2 times a day, C _max is 6.76 μg / ml;
• distribution: the volume of distribution after taking a dose of 1200 mg is 0.55–0.8 l / kg, depending on the patient's sex (in women it is equal to 50% of the values observed in men). Reaches an equilibrium concentration after 4-8 days, with impaired renal function, this period increases to 10-15 days. The connection with plasma proteins varies in the range of 13-17%. The substance is found in breast milk;
• metabolism: topiramate is metabolized in the liver by hydrolysis, hydroxylation and glucuronidation, in the process six metabolites are formed that do not have pharmacological activity. The nature of pharmacokinetics after a single oral administration is linear, plasma clearance is constant (20-30 ml / min). The area under the concentration-time curve (AUC) in the dose range from 100 to 400 mg increases in proportion to the dose;
• excretion: after repeated administration of topiramate at a dose of 50 and 100 mg 2 times a day, the half-life is 21 hours. In persons with severe renal impairment (with creatinine clearance less than 60 ml / min) and hepatic insufficiency, renal and plasma clearance are reduced. From the body, the substance is excreted in the urine mainly unchanged - up to 70% of the dose taken, the rest is excreted in the form of metabolites. Topiramate is removed from plasma by hemodialysis.

Indications for use

Topalepsin is used for the following conditions / diseases:

• epilepsy diagnosed for the first time (as a means of monotherapy);
• epileptic seizures against the background of Lennox-Gastaut syndrome, partial / generalized tonic-clonic seizures (as an adjunct drug in therapy in adults and children over 3 years old).

Contraindications

Absolute:

• children under 3 years old;
• gestation period;
• breast-feeding;
• established hypersensitivity to topiramate or other components of the drug.

Relative (Topalepsin should be taken with precautions):

• nephrourolithiasis (including history, including familial);
• renal / hepatic impairment;
• hypercalciuria.

Topalepsin, instructions for use: method and dosage

Topalepsin tablets are taken orally, regardless of food intake. It is not recommended to divide the tablet into parts.

When using the drug as a means of monotherapy, it should be borne in mind that the withdrawal of concomitant anticonvulsant therapy may affect the frequency of seizures. If abrupt withdrawal of concomitant anticonvulsant therapy is undesirable, the dose of the previously taken drug is gradually reduced, reducing it by 1/3 every 14 days.

With the cancellation of drugs that are inducers of microsomal hepatic enzymes, plasma concentrations of topiramate will increase. In this case, in the presence of clinical indications, the dose may be reduced.

Recommended dosing regimen for Topalepsin monotherapy:

• adult patients: at the beginning of monotherapy - 25 mg 1 time per day before bedtime for 7 days. In the future, the dose is increased by 25-50 mg / day, observing an interval of 7-14 days (the daily dose must be divided into 2 doses). If there is intolerance to such a therapy regimen, the dose should be increased by a smaller amount or set at longer intervals. The selection of the dose depends on the effect produced. The recommended dose is 100 mg / day, the maximum daily dose should not exceed 500 mg. When conducting monotherapy refractory to the treatment of epilepsy, in some cases, the daily dose of topiramate is increased to 1000 mg;
• children and adolescents aged 3 to 18 years: with monotherapy in the first week of treatment, appoint 0.5-1 mg / kg / day (the daily dose must be divided into 2 doses) Depending on the clinical efficacy and tolerability of therapy, the dose of topiramate and the rate of increase are determined. The recommended dose range for monotherapy with the drug in children 3–18 years old is from 3 to 6 mg / kg / day. In the case of recently diagnosed partial seizures - up to 500 mg / day.

The recommended dosing regimen when taking Topalepsin in combination with other anticonvulsant drugs:

• adult patients: the initial dose is 50 mg once a day at night for 7 days. In the future, the dose is increased by 25-50 mg every 7 days until the effective dose is reached. The average dose is 200-400 mg / day (it should be divided into 2 doses). If necessary, the daily dose can be increased to a maximum of 1600 mg. When selecting a dose, the criterion is the clinical effect, which in some patients can be achieved by taking the drug once a day;
• children and adolescents aged 3 to 18 years: the recommended total daily dose is from 5 to 9 mg / kg in 2 doses. Dose selection begins with 25 mg / day at night for 7 days. In the future, it is allowed to increase the dose by 1–3 mg / kg, observing an interval of 7–14 days (the daily dose must be divided into 2 doses). A daily dose of 30 mg / kg is generally well tolerated.

On the days of hemodialysis, an additional dose of Topalepsin is required in a dose equal to half the daily dose. The additional dose is divided into 2 doses (before and after the hemodialysis procedure).

To minimize the possibility of increasing the frequency of seizures, Topalepsin is withdrawn gradually (by 100 mg / week).

Side effects

Possible side reactions from systems and organs when taking Topalepsin:

• mental disorders: depression, confusion, pathologically increased distractibility, perseveration of thinking, impaired reading skills, slow thinking, severe speech disorders, mood lability, tearfulness, depressed mood, auditory and visual hallucinations, lack of spontaneous speech, decreased / loss of libido, dysfemia, falling asleep disorder, sleep disturbances, early awakening in the morning, insomnia, lethargy, disorientation, agitation, anger, psychotic disorder, euphoria, flattening of emotions, cognitive disorders, anxiety, aggression, emotional / affective lability, inappropriate behavior, apathy, anxiety, paranoid conditions, panic attack, pathological thinking, intrasomnic disorder, mania, panic disorder, panic reaction, feelings of despair,hypomanic state, suicidal ideation or attempts;
• central nervous system (CNS): paresthesias, intentional tremors (dynamic), psychomotor disturbances, seizures, seizures of the type of large convulsive seizures, complex partial seizures, sensory disturbances, tremor, essential tremor, psychomotor hyperactivity, dyskinesia, hypesthesia, cerebellar syndrome, peripheral neuropathy, sedation, drowsiness, disturbance of the circadian rhythm of sleep, poor sleep quality, lethargy, depression of consciousness, fainting, hypokinesia, burning sensation, parosmia, dystonia, akinesia, dizziness, postural dizziness, lightheadedness, stupor, clumsiness, improper coordination, imbalance, anosmia, hyposmia, memory impairment, impaired attention, learning difficulties, lack of response to stimuli, speech disorder, amnesia, dysgeusia, nystagmus, dysgraphia,dysphasia, articulation disorder, visual field defects, aura, aphasia, salivation, repetitive speech, loss of sensation, hypogeusia, dysesthesia, apraxia, hyperesthesia;
• musculoskeletal system: muscle spasms, muscle cramps, muscle stiffness, muscle fatigue, muscle weakness, pain in the side, muscle pain in the chest, arthralgia, myalgia, swelling of the joints, discomfort in the limbs;
• urinary system: stress urinary incontinence, urgent painful urge to urinate, pollakiuria, hematuria, dysuria, nephrolithiasis, pain in the kidney area, ureteral stones, urinary calculi, renal colic, renal tubular acidosis;
• reproductive system: sexual dysfunction, erectile dysfunction;
• respiratory system: dysphonia, nosebleeds, nasal congestion, rhinorrhea, hypersecretion in the paranasal sinuses, nasopharyngitis, dyspnea, cough, shortness of breath on exertion;
• immune system: conjunctival edema, allergic edema, hypersensitivity;
• digestive system: nausea / vomiting, pain in the mouth, dry mouth, hypersecretion of the salivary glands, bleeding gums, oral paresthesia, oral hypoesthesia, halitosis, constipation, diarrhea, dyspepsia, abdominal discomfort, abdominal pain, pain in the upper / lower abdomen, pain throughout the abdomen, stomach discomfort, gastritis, pancreatitis, bloating, flatulence, epigastric discomfort, glossodynia, gastroesophageal reflux disease, liver failure, hepatitis;
• hematopoietic system: lymphadenopathy, anemia, neutropenia, leukopenia, eosinophilia, thrombocytopenia;
• heart and blood vessels: rapid heartbeat, hot flushes, bradycardia, sinus bradycardia, hyperemia, orthostatic hypotension, Raynaud's phenomenon;
• metabolism: increased / decreased appetite, anorexia, polydipsia, hypokalemia, hyperchloremic acidosis, metabolic acidosis;
• skin and subcutaneous tissues: rash, urticaria, macular rash, localized urticaria, erythema, erythema multiforme, allergic dermatitis, pruritus, generalized pruritus, alopecia, anhidrosis, facial edema, facial hypesthesia, periorbital edema, unpleasant skin odor, skin discoloration, toxic epidermal necrolysis, Stevens-Johnson syndrome;
• organ of vision: visual impairment, blurred vision, decreased visual acuity, impaired visual depth perception, blepharospasm, pathological sensations in the eyes, oculomotor disorders, transient blindness, one-sided blindness, night blindness, dry eyes, increased lacrimation, impaired accommodation, eyelid edema, diplopia, photophobia, photopsia, glaucoma, myopia, scotoma, atrial fibrillation, mydriasis, amblyopia, presbyopia, maculopathy, angle-closure glaucoma;
• organ of hearing and balance: hearing impairment, deafness, sensorineural deafness, one-sided deafness, discomfort in the ears, vertigo, ear pain, ringing in the ears;
• general reactions: irritability, fatigue, malaise, flu-like condition, unusual sensations, inertia, thirst, facial edema, hyperthermia, cold extremities, asthenia, pyrexia, calcification, anxiety, drunkenness, gait disturbance;
• laboratory parameters: increased activity of liver enzymes, hypokalemia, leukopenia, crystalluria, increase / decrease in body weight, abnormal test for tandem walking, decrease in the content of hydrocarbons in the blood.

Overdose

With an overdose of Topalepsin, an increase in side effects is observed.

To normalize the condition, gastric lavage is performed, symptomatic therapy is prescribed. The use of activated carbon is ineffective, since, as was found in in vitro experiments, it does not adsorb topiramate. The most effective way to remove topiramate from the body is hemodialysis.

special instructions

The use of Topalepsin for the relief of acute migraine attacks has not been studied.

Patients with nephrourolithiasis (including a personal and family history), renal and hepatic failure, hypercalciuria should be careful when taking the drug.

In patients with impaired renal function and patients on hemodialysis, it is necessary to adjust the dosage regimen of the drug.

To minimize the possibility of an increase in the frequency of convulsive seizures, it is recommended that Topalepsin be withdrawn gradually. In the course of clinical trials in adult patients with epilepsy therapy, the doses were reduced by 50–100 mg at intervals of 7 days and by 25–50 mg in adult patients who received topiramate at a dose of 100 mg / day for the prevention of migraine. When conducting clinical studies in children over 3 years of age, topiramate was discontinued gradually, over a period of 14–56 days. In cases where, for medical reasons, a quick cancellation of Topalepsin is required, careful monitoring of the patient's condition is necessary.

In order to reduce the risk of developing nephrolithiasis during therapy with topiramate, the patient should increase the amount of fluid consumed.

Against the background of the use of Topalepsin, it is possible to reduce sweating and the appearance of hyperthermia in conditions of an elevated ambient temperature (especially in young children). To avoid an increased risk of complications from overheating, fluid loss must be replenished in a timely manner before and during exercise or other exercise-related activities and during high temperatures.

Throughout the course of therapy, the patient's condition should be monitored to identify signs of suicidal idealization in them and appropriate treatment should be prescribed in time. It is necessary to inform patients or their caregivers about the need to immediately seek medical attention if signs of suicidal idealization or suicidal behavior appear.

If there are visual impairments (including a syndrome including myopia associated with angle-closure glaucoma), the attending physician discontinues topiramate as soon as he considers it possible. If necessary, measures are taken to lower the intraocular pressure.

To prevent the development of metabolic acidosis, during the period of therapy with topiramate, the necessary studies are carried out, including the determination of the concentration of bicarbonates in the serum. When metabolic acidosis occurs and persists, either reduce the dose of topiramate or cancel Topalepsin completely. In pediatric patients, chronic metabolic acidosis can cause growth retardation. The effect of topiramate on growth and possible bone-related complications in adults and children has not been systematically studied.

With a decrease in body weight against the background of the use of topiramate, it is necessary to correct the diet.

The combined use of Topalepsin with other drugs that have a depressing effect on the central nervous system is not recommended.

During the period of treatment, the patient should avoid drinking alcohol.

Influence on the ability to drive vehicles and complex mechanisms

During the period of application of Topalepsin, patients need to be careful when driving a car and operating other complex and potentially dangerous mechanisms, since topiramate causes side reactions of the central nervous system in the form of drowsiness and dizziness, as well as visual impairment.

Application during pregnancy and lactation

Topalepsin is contraindicated in pregnant and breastfeeding women.

Adequate and strictly controlled clinical studies on the safety of the use of topiramate in women carrying a child have not been conducted.

Topalepsin therapy during pregnancy can cause fetal damage. According to the register of pregnant women, with intrauterine exposure to topiramate on the fetus, the likelihood of congenital malformations, for example, craniofacial defects (cleft palate or cleft lip), hypospadias and anomalies in the development of various body systems, increases. The above malformations were observed with the use of topiramate both as a means of monotherapy and as an auxiliary drug in combination treatment. According to the register of pregnant women, women who were prescribed monotherapy with topiramate during gestation were more likely to have babies with low body weight (less than 2500 mg) compared with the group of patients not taking antiepileptic drugs. The causal relationship of this phenomenon has not been established.

Before prescribing Topalepsin tablets to women of childbearing age, it is necessary to assess the expected benefits of therapy for the mother and the potential risk to the fetus and consider alternative treatment options. The doctor must necessarily warn the patient about the existing risks to fetal health when taking topiramate during gestation or when pregnancy occurs during drug therapy.

Based on a limited number of observations, it is assumed that topiramate is excreted in breast milk. Therefore, if it is necessary to use Topalepsin during lactation, it is necessary to interrupt breastfeeding.

Pediatric use

Topalepsin is contraindicated in pediatric patients under 3 years of age.

With impaired renal function

Patients with impaired renal function should take Topalepsin with caution.

For violations of liver function

Patients with impaired liver function should take Topalepsin with precautions.

Use in the elderly

There are no special instructions on the Topalepsin dosage regimen for elderly patients.

Drug interactions

Possible interactions of topiramate with other substances / drugs:

• oral contraceptives containing estrogen: topiramate reduces their effectiveness;
• digoxin: AUC of digoxin decreases by 12%;
• ethanol and other drugs that depress the central nervous system: simultaneous administration is not recommended;
• carbamazepine: in combination therapy with topiramate, the AUC of carbamazepine does not change or changes slightly (less than 10%), while the AUC of topiramate decreases by 40%;
• phenytoin: when combined with topiramate, phenytoin AUC does not change or increases by 25%, while topiramate's AUC decreases by 48%; correction of the dosage regimen of the latter may be required;
• valproic acid: simultaneous use with topiramate leads to a decrease in its AUC by 14%, valproic acid AUC by 11%;
• Carbonic anhydrase inhibitors (acetazolamide): Increases the risk of renal calculi.

Analogs

Topalepsin's analogues are Maxitopyr, Ropimat, Topamax, Topiromax, Epimax, Topsaver, Toreal, Torapimat, Topiramate, Topiramat Canon, Topiramat Sandoz, Topiramat-ALSI, Topiramat-Vial, Topiramat-Teva, Topiramat-other TL, Epitop and

Terms and conditions of storage

Store in a place out of the reach of children, protected from light and moisture, at a temperature not exceeding 25 ° C.

Shelf life is 2 years. It is not allowed to use the drug after the expiration date.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Topalepsin

The reviews about Topalepsin found on the Internet are positive. Mostly they are left by the relatives of patients taking the drug. It is noted that since the drug is manufactured in Russia, its cost is significantly lower than imported analogues. Compared to other domestic antiepileptic drugs, Topalepsin is more effective and allows you to prevent epileptic seizures for a long time.

Most users consider a very large list of adverse reactions to be a disadvantage of the drug, although little is reported about their manifestation during therapy. Some patients express dissatisfaction with the fact that Topamax, which was previously included in the list of free drugs (an imported analogue of the drug), has been replaced by Topalepsin under the additional drug provision program.

Price for Topalepsin in pharmacies

In pharmacies, the price of Topalepsin, film-coated tablets, can be (per pack of 30 pcs.): Dosage of 25 mg - from 189 to 237 rubles; dosage of 50 mg - from 320 to 475 rubles; dosage of 100 mg - from 465 to 616 rubles.

Topalepsin: prices in online pharmacies

Drug name Price Pharmacy

Topalepsin 25 mg film-coated tablets 30 pcs. 192 RUB Buy

Topalepsin 50 mg film-coated tablets 30 pcs. 229 r Buy

Topalepsin 100 mg film-coated tablets 30 pcs. 529 r Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!