Directory of medicines. Directory of medicines Release form and composition of Topamax

pharmachologic effect

Antiepileptic drug, belongs to the class of sulfamate-substituted monosaccharides.

Topiramate blocks sodium channels and suppresses the occurrence of repeated action potentials against the background of prolonged depolarization of the neuron membrane. Topiramate increases the activity of GABA (GABA) in relation to some subtypes of GABA receptors (including GABA A receptors), and also modulates the activity of GABA A receptors themselves, prevents kainate from activating the sensitivity of the kainate / AMPK subtype (alpha-amino-3 -hydroxy-5-methylisoxazole-4-propionic acid) glutamate receptors, does not affect NMDA activity against the NMDA receptor subtype. These effects of the drug are dose-dependent at a plasma concentration of topiramate from 1 μmol to 200 μmol, with a minimum activity ranging from 1 μmol to 10 μmol.

In addition, topiramate inhibits the activity of some isoenzymes of carbonic anhydrase. In terms of the severity of this pharmacological effect, topiramate is significantly inferior to acetazolamide, a well-known inhibitor of carbonic anhydrase, therefore, this activity of topiramate is not the main component of its antiepileptic activity.

Pharmacokinetics

Suction

After taking the drug inside, topiramate is quickly and effectively absorbed from the gastrointestinal tract. Bioavailability is 81%. Food intake does not have a clinically significant effect on the bioavailability of the drug.

Pharmacokinetics of topiramate is linear, plasma clearance remains constant, and AUC in the dose range from 100 mg to 400 mg increases in proportion to the dose.

After repeated oral administration at a dose of 100 mg 2 times / day, C max averages 6.76 μg / ml.

Distribution

Plasma protein binding is 13-17%.

After a single oral administration in a dose of up to 1200 mg, the average Vd is 0.55-0.8 l / kg. The V d value depends on gender. In women, the values ​​are approximately 50% of the values ​​observed in men, which is associated with a higher content of adipose tissue in the body of women.

In patients with normal renal function, it may take 4 to 8 days to reach equilibrium.

Metabolism

After oral administration, about 20% of the dose is metabolized.

Six practically inactive metabolites were isolated and identified from human plasma, urine and feces.

Withdrawal

Topiramate (70%) and its metabolites are excreted mainly by the kidneys.

After oral administration, the plasma clearance of the drug is 20-30 ml / min.

After repeated administration of the drug 50 mg and 100 mg 2 times / day, the average T 1/2 averaged 21 hours.

Pharmacokinetics in special clinical situations

The rate of excretion of topiramate by the kidneys depends on renal function and does not depend on age.

In patients with moderate and severe renal impairment (CC ≤ 70 ml / min), the renal and plasma clearance of topiramate decreases, as a consequence, an increase in C ss of topiramate in blood plasma is possible compared with patients with normal renal function. The time to reach C ss topiramate in blood plasma in patients with moderate or severe renal impairment is 10 to 15 days. Patients with moderate to severe renal impairment are advised to use half the recommended starting and maintenance dose.

In elderly people who do not suffer from kidney disease, the plasma clearance of topiramate does not change.

In patients receiving concomitant therapy with antiepileptic drugs that induce enzymes involved in drug metabolism, the metabolism of topiramate increased by 50%.

Topiramate is effectively eliminated by hemodialysis. Long-term hemodialysis can lead to a decrease in the concentration of topiramate in the blood below the amount required to maintain anticonvulsant activity. To avoid a rapid drop in plasma topiramate concentration during hemodialysis, an additional dose of Topamax® may be required. When adjusting the dose, you should take into account:

1) the duration of hemodialysis;

2) the value of the clearance of the used hemodialysis system;

3) effective renal clearance of topiramate in a patient on dialysis.

Plasma clearance of topiramate is reduced by an average of 26% in patients with moderate to severe hepatic impairment. Therefore, patients with hepatic impairment should use topiramate with caution.

In children under 12 years of age, the pharmacokinetic parameters of topiramate, as in adults receiving the drug as an adjuvant therapy, are linear, while its clearance does not depend on the dose, and C ss in plasma increases in proportion to the dose increase. It should be borne in mind that in children, the clearance of topiramate is increased, and its T 1/2 is shorter. Therefore, at the same dose per 1 kg of body weight, plasma concentrations of topiramate in children may be lower than in adults. In children, as in adults, antiepileptic drugs that induce liver enzymes cause a decrease in the concentration of topiramate in the blood plasma.

Indications

Epilepsy:

- as monotherapy in adults and children over 2 years of age with epilepsy (including in patients with newly diagnosed epilepsy);

- as part of complex therapy in adults and children over 2 years of age with partial or generalized tonic-clonic seizures, as well as for the treatment of seizures against the background of Lennox-Gastaut syndrome.

- prevention of migraine attacks in adults (the use of Topamax ® for the treatment of acute migraine attacks has not been studied).

Dosage regimen

The drug is taken orally, regardless of food intake.

The capsules should be opened carefully, mixed with a small amount (about 1 teaspoon) of any soft food. This mixture should be swallowed immediately without chewing. Do not store the drug mixed with food until the next dose. Topamax ® capsules can be swallowed whole.

To achieve optimal control of epileptic seizures in adults and children, it is recommended to start treatment with low doses of the drug, followed by titration to the effective dose.

The capsules are intended for patients who have difficulty swallowing tablets (for example, children and elderly patients).

Partial or generalized tonic-clonic seizures, as well as seizures associated with Lennox-Gastaut syndrome

Combination anticonvulsant therapy in adults. The minimum effective dose is 200 mg / day. Usually the total daily dose ranges from 200 mg to 400 mg and is taken in 2 divided doses. Some patients may need to increase the daily dose to a maximum of 1600 mg. It is recommended to start treatment with a low dose, followed by a gradual selection of the effective dose. The selection of the dose begins with 25-50 mg, taking them at night for 1 week. In the future, at intervals of 1-2 weeks, the dose can be increased by 25-50 mg and taken in 2 divided doses. When choosing a dose, it is necessary to be guided by the clinical effect. In some patients, the effect can be achieved by taking the drug 1 time / day. To achieve the optimal effect of treatment with Topamax ® it is not necessary to control its plasma concentration.

Combined anticonvulsant therapy in children over 2 years of age. The recommended total daily dose of Topamax ® as an adjunctive therapy is 5 to 9 mg / kg and is taken in 2 divided doses. Dose selection should be started at 25 mg (or less, based on an initial dose of 1 to 3 mg / kg / day) at night for 1 week. In the future, the dose can be increased with an interval of 1-2 weeks by 1-3 mg / kg and taken in 2 divided doses. When choosing a dose, it is necessary to be guided by the clinical effect. A daily dose of up to 30 mg / kg is usually well tolerated.

Epilepsy (including newly diagnosed epilepsy)

At withdrawal of concomitant anticonvulsants with the aim of monotherapy with topiramate, the possible effect of this step on the frequency of seizures should be considered. In cases where there is no need to abruptly discontinue concomitant anticonvulsants for safety reasons, it is recommended to reduce their doses gradually, reducing the dose of concomitant antiepileptic drugs by 1/3 every 2 weeks.

With the abolition of drugs that are inducers of liver microsomal enzymes, the concentration of topiramate in the blood will increase. In such situations, if there are clinical indications, the dose of Topamax ® can be reduced.

At monotherapy for adults at the beginning of treatment Topamax ® is prescribed at a dose of 25 mg at bedtime for 1 week. Then the dose is increased at intervals of 1-2 weeks by 25 mg or 50 mg in 2 divided doses. If the patient does not tolerate such a dose escalation regimen, then the intervals between dose increases can be increased, or the dose can be increased more smoothly. When choosing a dose, it is necessary to be guided by the clinical effect. The initial dose for monotherapy with topiramate in adults is 100 mg / day, and the maximum daily dose should not exceed 500 mg. Some patients with refractory forms of epilepsy tolerate topiramate monotherapy at doses up to 1000 mg / day. These dosing recommendations apply to all adults, including elderly patients without kidney disease.

At monotherapy for children over 2 years of age in the first week of treatment, Topamax ® is prescribed at a dose of 0.5-1 mg / kg of body weight before bedtime. Then the dose is increased at intervals of 1-2 weeks by 0.5-1 mg / kg / day in 2 divided doses. If the child does not tolerate such a dose escalation regimen, then the dose can be increased more smoothly or the intervals between dose increases can be increased. The size of the dose and the rate of its increase depend on the clinical effect. The recommended dose range for monotherapy with topiramate in children over the age of 2 years is 100-400 mg / day. Children with newly diagnosed partial seizures can be prescribed up to 500 mg / day.

Migraine

For prevention of migraine attacks The recommended daily dose of topiramate is 100 mg in 2 divided doses. At the beginning of treatment, 25 mg is prescribed at bedtime for 1 week. Then the dose is increased by 25 mg / day with an interval of 1 week. In case of intolerance to such a therapy regimen, the dose is increased by a smaller amount or at longer intervals. The dose is selected depending on the clinical effect. In some cases, a positive result is achieved with a daily dose of 50 mg topiramate. In clinical trials, patients received various doses of topiramate, but not more than 200 mg / day.

Special patient groups

In patients with moderate to severe renal failure dose reduction may be necessary. It is recommended to use half of the recommended starting and maintenance dose.

Hemodialysis: since topiramate is removed from the plasma during hemodialysis, an additional dose of Topamax® should be administered on the days of hemodialysis, equal to approximately half the daily dose. The additional dose should be divided into two doses, taken at the beginning and after the end of the hemodialysis procedure. The additional dose may vary depending on the characteristics of the equipment used in the hemodialysis.

Have patients with hepatic impairment Topiramate should be used with caution.

Side effect

Determination of the frequency of side effects: very often (≥1 / 10), often (≥1 / 100,<1/10), нечасто (≥1/1000 и <1/100), редко (≥1/10 000 и <1/1000) и очень редко (<1/10 000).

From the center anal nervous system: very often - drowsiness, dizziness, paresthesia, in children - apathy, impaired attention; often - impaired coordination of movements, nystagmus, lethargy, memory impairment, tremor, amnesia, improper gait, hypesthesia, perversion of taste, impaired thinking, cognitive impairment, apathy, decreased mental activity, psychomotor impairment, sedative effect; infrequently - loss of gustatory sensitivity, akinesia, loss of smell, aphasia, apraxia, aura, burning sensation in the limbs or on the face, cerebellar syndrome, disturbance of the circadian rhythm of sleep, complex partial seizures, convulsions, postural dizziness, dysesthesia, sensory disorder, dysgraphia, dyskinesia , dysphasia, dystonia, feeling of "goosebumps" on the body, tonic-clonic seizures of the grand mal type, hyperesthesia, hypogeusia, hypokinesia, hyposmia, peripheral neuropathy, parosmia, pre-syncope, repetitive speech, impaired touch, stupor, fainting, lack of reactions to stimuli, in children - psychomotor hyperactivity.

Mental disorders: often - slow thinking, severe speech disorders, confusion, depression, insomnia, aggressive reactions, agitation, disorientation, emotional lability, erectile dysfunction, in children - behavior change, learning disabilities (difficulties with reading, writing, counting); infrequently - anorgasmia, sexual dysfunction, tearfulness, impaired sexual arousal, dysfemia, early awakening in the morning, euphoric mood, auditory and visual hallucinations, hypomanic states, decreased libido, mania, panic, paranoid states, perseveration of thinking, impaired reading skills, disorders sleep, suicidal ideation or attempts, tearfulness; very rarely - a feeling of despair.

From the digestive system: very often - decreased appetite, anorexia; often - nausea, diarrhea; infrequently - abdominal pain, constipation, stomach discomfort, dyspeptic symptoms, dry mouth, impaired sensitivity in the oral cavity, gastritis, gastroesophageal reflux, bleeding gums, heaviness in the stomach, in children - vomiting, bad breath, epigastric discomfort areas, flatulence, glossodynia, pain in the oral cavity, pancreatitis, hypersecretion of the salivary glands, thirst.

From the musculoskeletal system: often - myalgia (including in the chest), muscle spasms, muscle cramps, arthralgia; infrequently - pain in the side, muscle fatigue, muscle weakness, muscle stiffness; very rarely - joint swelling, discomfort in the limbs.

On the part of the cardiovascular system: sometimes - bradycardia, heart palpitations, hot flushes, orthostatic hypotension, Raynaud's phenomenon.

On the part of the organ of vision: often - diplopia, blurred vision, dry eyes; infrequently - accommodation disorder, amblyopia, blepharospasm, transient blindness, one-sided blindness, increased lacrimation, mydriasis, night blindness, photopsia, presbyopia, scotoma (including atrial fibrillation), decreased visual acuity; very rarely - discomfort in the eyes, angle-closure glaucoma, involuntary movements of the eyeballs, eyelid edema, myopia, maculopathy, conjunctival edema.

On the part of the organ of hearing: often - ear pain, ringing in the ears, in children - vertigo; infrequently - deafness (including sensorineural and unilateral), discomfort in the ears, hearing impairment.

From the respiratory system: often - shortness of breath, nosebleeds; infrequently - hoarseness, shortness of breath on exertion, nasal congestion, hypersecretion in the paranasal sinuses, in children - rhinorrhea; very rarely - nasopharyngitis.

From the hematopoietic system: often - anemia; infrequently - leukopenia, lymphadenopathy, thrombocytopenia, in children - eosinophilia; very rarely - neutropenia.

On the part of the skin and subcutaneous tissues: often - rash, alopecia, itching, decreased sensitivity of the facial skin; infrequently - lack of sweating, allergic dermatitis, skin redness, skin pigmentation disorders, facial edema, unpleasant skin odor, urticaria; very rarely - erythema multiforme, paraorbital edema, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the urinary system: often - nephrolithiasis, dysuria, pollakiuria; infrequently - exacerbation of urolithiasis, hematuria, urinary incontinence, frequent urge to urinate, renal colic, pain in the kidney area; very rarely - renal tubular acidosis.

On the part of laboratory parameters: infrequently - a decrease in the content of bicarbonates in the blood (by an average of 4 mmol / l), crystalluria, leukopenia, hypokalemia (a decrease in the level of potassium in the blood serum below 3.5 mmol / l).

General violations: very often - fatigue, irritability, weight loss; often - asthenia, anxiety, in children - fever; infrequently - facial edema, allergic reactions, hyperchloremic acidosis, hypokalemia, increased appetite, metabolic acidosis, polydipsia, cold extremities, fatigue, weakness, calcification; very rarely - generalized edema, flu-like illness, angioedema, weight gain.

Contraindications for use

- children under 2 years old;

- hypersensitivity to the components of the drug.

WITH caution should be used for renal or hepatic failure, nephrourolithiasis (including in the past or in a family history), with hypercalciuria.

Application during pregnancy and lactation

There have been no special controlled studies in which Topamax ® was used to treat pregnant women. Pregnancy registration data indicate a possible connection between the use of Topamax® during pregnancy and congenital malformations (for example, craniofacial defects such as cleft lip / cleft palate, hypospadias and developmental abnormalities of various body systems). These malformations were recorded both with topiramate monotherapy and with its use within the framework of polytherapy. Compared with the group of patients not taking antiepileptic drugs, the data on the registration of pregnancies with monotherapy with Topamax ® indicate the likelihood of the birth of children with low body weight (less than 2500 g). The relationship of the observed phenomena with the intake of the drug has not been established.

In addition, pregnancy records and other studies indicate that the risk of teratogenic effects with combined treatment with antiepileptic drugs may be higher than with monotherapy. The use of Topamax® during pregnancy is justified only if the potential benefit of therapy to the mother outweighs the possible risk to the fetus.

When treating and counseling women of childbearing potential, the treating physician should weigh the benefits / risks of treatment and consider alternative treatment options. If Topamax ® is used during pregnancy, or if the patient becomes pregnant while taking this drug, she should be warned of the potential risk to the fetus.

The limited number of observations suggests that topiramate is excreted in breast milk in women. If it is necessary to use Topamax® during lactation, the question of stopping breastfeeding should be resolved.

Application in children

The drug is contraindicated for use in children under 2 years of age.

Overdose

Symptoms: convulsions, drowsiness, speech and vision disorders, diplopia, thinking disorders, coordination disorders, lethargy, stupor, arterial hypotension, abdominal pain, dizziness, agitation and depression. In most cases, the clinical consequences were not severe, but deaths have been observed after overdose with the use of a mixture of several drugs, including topiramate. The development of severe metabolic acidosis is possible.

There is a known case of overdose when the patient took a dose of topiramate from 96 to 110 g, which led to a coma, which lasted 20-24 hours. After 3-4 days, the symptoms of overdose resolved.

Treatment: if the patient has eaten shortly before taking an excessive dose of the drug, it is necessary to immediately flush the stomach or induce vomiting. In vitro studies have shown that activated carbon adsorbs topiramate. If necessary, symptomatic therapy should be carried out. An effective way to remove topiramate from the body is hemodialysis. Patients are advised to adequately increase the volume of fluid intake.

Drug interactions

Influence of Topamax ® on the concentration of other antiepileptic drugs (AEDs)

Simultaneous administration of Topamax® with other AEDs (phenytoin, carbamazepine, valproic acid, phenobarbital, primidone) does not affect the values ​​of their C ss in plasma, with the exception of certain patients in whom the addition of Topamax® to phenytoin may cause an increase in the concentration of phenytoin in plasma. This may be due to the inhibition of a specific polymorphic isoform of the enzyme of the cytochrome P450 system (CYP2Cmeph). Therefore, when symptoms of toxicity develop in patients receiving phenytoin, it is necessary to control the concentration of phenytoin in blood plasma.

In a study of pharmacokinetics in patients with epilepsy, the addition of topiramate to lamotrigine did not affect the C ss of the latter in blood plasma at doses of topiramate 100-400 mg / day. During and after the discontinuation of lamotrigine (average dose 327 mg / day) C ss topiramate did not change.

Effect of other AEDs on plasma topiramate concentration

Phenytoin and carbamazepine, when used simultaneously with Topamax ®, reduce the plasma concentration of topiramate. The addition or withdrawal of phenytoin or carbamazepine during treatment with Topamax® may require a change in the dose of the latter. The dose is selected depending on the development of the required clinical effect. The addition or withdrawal of valproic acid does not cause clinically significant changes in the concentration of topiramate in the blood plasma and, therefore, does not require a change in the dose of Topamax®.

Interaction with other medicinal products

In the studies conducted with the simultaneous use of Topamax® in a single dose, the AUC of digoxin decreased by 12%. The clinical significance of this effect has not been established. When prescribing or discontinuing Topamax® in patients receiving digoxin, it is necessary to monitor the serum digoxin concentration.

Within the framework of clinical studies, the consequences of the combined use of Topamax ® with drugs that depress the functions of the central nervous system, as well as with ethanol, have not been studied. Combined use of Topamax ® with drugs that have a depressant effect on the central nervous system, and with ethanol is not recommended.

With the joint administration of Topamax and drugs based on St. John's wort (Hypericum perforatum), the concentration of topiramate in the plasma may decrease and, as a result, the effectiveness of the drug may also decrease. Clinical studies of the interaction of Topamax ® and preparations based on St. John's wort have not been conducted.

With the simultaneous use of an oral contraceptive containing norethisterone (1 mg) and ethinylestradiol (35 μg), Topamax® at doses of 50-800 mg / day did not significantly affect the effectiveness of norethisterone and at doses of 50-200 mg / day - on the effectiveness of ethinylestradiol. A significant dose-dependent decrease in the effectiveness of ethinylestradiol was observed at doses of Topamax ® 200-800 mg / day. The clinical significance of the described changes is not clear. The risk of reduced effectiveness of contraceptives and increased breakthrough bleeding should be considered in patients taking oral contraceptives in combination with Topamax®. Patients taking estrogen-containing contraceptives should inform their doctor about any changes in the timing and nature of menstruation. Contraceptive effectiveness can be reduced even in the absence of breakthrough bleeding.

In healthy volunteers, a decrease in lithium AUC by 18% was observed while taking topiramate at a dose of 200 mg / day. In patients with manic-depressive psychosis, the use of topiramate at doses up to 200 mg / day did not affect the pharmacokinetics of lithium; however, at higher doses (up to 600 mg / day), the AUC of lithium was increased by 26%. With the simultaneous use of topiramate and lithium, the concentration of the latter in the blood plasma should be monitored.

Drug interaction studies conducted with single and multiple administration of topiramate to healthy volunteers and patients with manic-depressive psychosis yielded similar results. With the simultaneous use of topiratam in daily doses of 250 mg or 400 mg, the AUC of risperidone taken at doses of 1-6 mg / day decreases by 16% and 33%, respectively. At the same time, the pharmacokinetics of 9-hydroxyrisperidone did not change, and the total pharmacokinetics of active substances (risperidone and 9-hydroxyrisperidone) did not change significantly. The change in the level of systemic exposure to risperidone / 9-hydroxyrisperidone and topiramate was not clinically significant, and this interaction is unlikely to be of clinical significance.

Drug interactions were studied in healthy volunteers with separate and co-administration of hydrochlorothiazide (25 mg) and topiramate (96 mg). The research results showed that with the simultaneous administration of topiramate and hydrochlorothiazide, there is an increase in C max of topiramate by 27% and its AUC by 29%. The clinical significance of these studies has not been identified. When hydrochlorothiazide is prescribed to patients taking topiramate, topiramate dose adjustment may be required. There were no significant changes in the pharmacokinetic parameters of hydrochlorothiazide with concomitant therapy with topiramate.

Drug interactions were studied in healthy volunteers who received metformin or a combination of metformin and topiramate. The research results showed that with the simultaneous administration of topiramate and metformin, there is an increase in C max and AUC of metformin by 18% and 25%, respectively, while the clearance of metformin with simultaneous administration with topiramate decreased by 20%. Topiramate had no effect on Tmax of metformin in blood plasma. The clearance of topiramate when administered together with metformin decreases. The extent of the identified changes in clearance has not been studied. The clinical significance of the effects of metformin on the pharmacokinetics of topiramate is unclear. In case of addition or withdrawal of Topamax ® in patients receiving metformin, the condition of patients with diabetes should be monitored.

Drug interactions were studied in healthy volunteers with separate and joint administration of pioglitazone and topiramate. There was a decrease in the AUC of pioglitazone by 15%, without changing the C max of the drug. These changes were not statistically significant. Also, for the active hydroxymetabolite pioglitazone, a decrease in C max and AUC was revealed by 13% and 16%, respectively, and for the active ketometabolite, a decrease in both C max and AUC by 60% was revealed. The clinical significance of these data has not been clarified. With the joint appointment of Topamax ® and pioglitazone to patients, the patient's condition should be carefully monitored to assess the course of diabetes mellitus.

A drug interaction study was conducted to study the pharmacokinetics of glibenclamide (5 mg / day) in an equilibrium state, used alone or simultaneously with topiramate (150 mg / day) in patients with type 2 diabetes mellitus. When using topiramate, the AUC of glibenclamide decreased by 25%. The level of systemic exposure to active metabolites, 4-trans-hydroxy-glibenclamide and 3-cis-hydroxy-glibenclamide, was also reduced (by 13% and 15%, respectively). Glibenclamide did not affect the pharmacokinetics of topiramate at steady state. A statistically insignificant decrease in the AUC of pioglitazone by 15% was found in the absence of a change in its C max. When prescribing topiramate to patients receiving glibenclamide (or prescribing glibenclamide to patients receiving topiramate), the patient's condition should be carefully monitored to assess the course of diabetes mellitus.

With the simultaneous use of Topamax ® with other drugs that predispose to the development of nephrolithiasis, the risk of kidney stones may increase. During the period of treatment with Topamax ®, the use of such drugs should be avoided, since they can cause physiological changes that contribute to the development of nephrolithiasis.

The combined use of topiramate and valproic acid in patients who tolerate each drug well individually is accompanied by hyperammonemia with or without encephalopathy. In most cases, symptoms and signs disappear after one of the drugs is discontinued. This adverse event is not due to pharmacokinetic interactions. The relationship between hyperammonemia and the use of topiramate alone or in combination with other drugs has not been established.

When topiramate and valproic acid are taken together, hypothermia (an unintentional decrease in body temperature below 35 ° C) may occur in combination with hyperammonemia or independently. This phenomenon can occur both after the start of joint administration of valproic acid and topiramate, and with an increase in the daily dose of topiramate.

Clinical studies have been conducted to evaluate potential drug interactions between topiramate and other drugs. The results of this interaction are summarized in the table.

Added drug	Concentration of added drug *	Topiramate concentration *
Amitriptyline	increase in C max and AUC of nortriptyline (amitriptyline metabolite) by 20%	not studied
Dihydroergotamine (orally and s / c)	**	**
Haloperidol	an increase in the AUC of the metabolite by 31%	not studied
Propranolol	increase in C max of 4-OH propranolol by 17% (topiramate 50 mg)	an increase in C max by 9% and 16%, an increase in AUC by 9% and 17% (propranolol 40 mg and 80 mg every 12 hours, respectively)
Sumatriptan (orally and s / c)	**	not studied
Pizotifen	**	**
Diltiazem	decrease in AUC of diltiazem by 25% and deacetyldyltiazem by 18% and ** for N-demethyldyltiazem	increase in AUC by 20%
Venlafaxine	**	**
Flunarizine	increase in AUC by 16% (50 mg every 12 hours) 1	**

* expressed as% of C max and AUC values ​​with monotherapy
** no changes in C max and AUC (≤ 15% of the initial data)
1 with repeated administration of flunarizine (monotherapy), an increase in AUC was observed by 14%, which may be associated with the accumulation of the drug in the process of reaching an equilibrium state

Conditions of dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

The drug should be stored out of the reach of children, in a dry place at a temperature not exceeding 25 ° C. Shelf life is 2 years.

Application for violations of liver function

It should be used with caution in liver failure. In patients with moderate to severe impaired liver function, plasma clearance decreases.

Application for impaired renal function

When prescribing the drug to patients with moderate to severe renal impairment it should be borne in mind that it may take 10-15 days to reach an equilibrium state in this category of patients, as opposed to 4-8 days in patients with normal renal function. Since topiramate is removed from the plasma during hemodialysis, an additional dose of the drug equal to half the daily dose should be prescribed on the days of it, in 2 divided doses (before and after the procedure).

It should be used with caution in renal failure, nephrourolithiasis (including in the past or in a family history), with hypercalciuria.

special instructions

Cancellation of Topamax ® (like other antiepileptic drugs) should be gradual in order to minimize the possibility of an increase in the frequency of seizures. To reduce the dose by 25-50 mg, Topamax® is used in the form of capsules at a dosage of 15 mg or 25 mg. In clinical studies, the dose of the drug was reduced by 50-100 mg once a week - for adults in the treatment of epilepsy and by 25-50 mg - in adults receiving Topamax® at a dose of 100 mg / day for the prevention of migraine. In children in clinical trials, Topamax was gradually discontinued over a period of 2-8 weeks. If, for medical reasons, a quick cancellation of Topamax ® is necessary, it is recommended to carry out appropriate monitoring of the patient's condition.

As with any disease, the dosage regimen should be established in accordance with the clinical effect (i.e., the degree of seizure control, the absence of side effects) and take into account the fact that in patients with impaired renal function, to establish a stable plasma concentration for each dose it will take a longer time.

With topiramate therapy, oligohydrosis (reduced sweating) and anhidrosis may occur. Decreased sweating and hyperthermia (increased body temperature) can occur in children exposed to high ambient temperatures. With topiramate therapy, it is very important to adequately increase the volume of fluid consumed, which helps to reduce the risk of developing nephrolithiasis, as well as side effects that may occur under the influence of physical exertion or high temperatures.

There is an increased incidence of mood disorders and depression with topiramate treatment.

When using antiepileptic drugs, including Topamax ®, the risk of suicidal thoughts and suicidal behavior increases in patients taking these drugs for any of the indications.

In double-blind clinical trials, the incidence of suicidal events (suicidal thoughts, attempts at suicide, suicide) was 0.5% in patients receiving topiramate (46 out of 8652), which is about 3 times higher than in patients. who received placebo (0.2%; 8 people out of 4045). One case of suicide was reported in a double-blind study of bipolar disorder in a patient receiving topiramate.

Thus, it is necessary to monitor the condition of patients in order to identify signs of suicidal thoughts and prescribe appropriate treatment. Patients (and, if necessary, caregivers of patients) should be advised to seek immediate medical attention if signs of suicidal thoughts or suicidal behavior appear.

In some patients, especially those with a predisposition to nephrolithiasis, there may be an increased risk of kidney stones and associated symptoms such as renal colic. To reduce this risk, an adequate increase in fluid intake is required. Risk factors for the development of nephrolithiasis are a history of nephrolithiasis (including family history), hypercalciuria, concomitant therapy with other drugs that contribute to the development of nephrolithiasis.

Caution should be exercised when prescribing Topamax ® to patients with renal insufficiency (CC<70 мл/мин). Это связано с тем, что у таких пациентов клиренс препарата понижен.

In patients with impaired liver function, Topamax ® should be used with caution because of a possible decrease in the clearance of topiramate.

When using Topamax ®, a syndrome has been described that includes acute myopia with concomitant secondary angle-closure glaucoma. Symptoms include an acute decrease in visual acuity and / or eye pain. Ophthalmological examination may reveal myopia, flattening of the anterior chamber of the eye, hyperemia (redness) of the eyeball, increased intraocular pressure. Mydriasis may occur. This syndrome can be accompanied by the secretion of fluid, leading to the displacement of the lens and iris forward with the development of secondary angle-closure glaucoma. Symptoms usually appear 1 month after you start using Topamax®. Unlike primary open-angle glaucoma, which is rarely observed in patients under 40 years of age, secondary angle-closure glaucoma is observed when topiramate is used in both adults and children. If a syndrome occurs, including myopia associated with angle-closure glaucoma, treatment includes discontinuation of Topamax® as soon as the attending physician considers it possible, and appropriate measures aimed at lowering intraocular pressure. Usually, these measures lead to the normalization of intraocular pressure.

Increased intraocular pressure of any etiology in the absence of adequate treatment can lead to serious complications, including loss of vision.

With the use of topiramate, hyperchloremic, not associated with anion deficiency, metabolic acidosis may occur (for example, a decrease in the concentration of bicarbonates in the blood by an average of 4 mmol / l in the absence of respiratory alkalosis). This decrease in serum bicarbonate concentration is a consequence of the inhibitory effect of topiramate on renal carbonic anhydrase. In most cases, a decrease in bicarbonate concentration occurs at the beginning of the drug intake, although this effect can manifest itself at any time during treatment with topiramate. The level of decrease in concentration is usually weak or moderate (the average value is 4 mmol / l when used in adult patients at a dose of more than 100 mg / day and about 6 mg / kg / day when used in pediatric practice). In rare cases, patients showed a decrease in concentration below 10 mmol / l. Certain diseases or treatments that predispose to acidosis (eg, kidney disease, severe respiratory illness, status epilepticus, diarrhea, surgery, ketogenic diet, certain medications) may be additional factors that enhance the bicarbonate-reducing effect of topiramate.

In children, chronic metabolic acidosis can lead to stunted growth. The effect of topiramate on growth and possible complications associated with the skeletal system has not been systematically studied in children and adults.

In connection with the above, during treatment with topiramate, it is recommended to carry out the necessary studies, including the determination of the concentration of bicarbonate in serum. If metabolic acidosis occurs and persists, it is recommended to reduce the dose or stop taking Topamax ®.

If, while taking Topamax ®, the patient's body weight decreases, then the question of the advisability of enhanced nutrition should be considered.

Laboratory indicators

Hypokalemia, defined as a decrease in serum potassium concentration below 3.5 mmol / L, was observed in 0.4% of patients receiving topiramate.

Influence on the ability to drive vehicles and use mechanisms

Topamax ® acts on the central nervous system and can cause drowsiness, dizziness, blurred vision and other symptoms. These adverse effects can be dangerous for patients who drive and move machinery, especially during the period until the patient's response to the drug is established.

Topamax is an anticonvulsant drug used to treat epilepsy.

Release form and composition of Topamax

Topamax is available in the form of tablets and capsules.

The main active ingredient of Topamax is topiramate.

As auxiliary substances of Topamax tablets are: lactose monohydrate, pregelatinized starch, carnauba wax, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, titanium dioxide, polysorbate 80, polyethylene glycol, hydroxypropylmethyl cellulose.

Excipients of Topamax capsules are: sucrose, starch syrup; povidone; cellulose acetate.

Pharmacological action of Topamax

Topamax is an antiepileptic drug of the sulfate-substituted monosaccharide class.

By blocking sodium channels, topiramate suppresses re-emerging action potentials against the background of prolonged depolarization of the neuronal membrane.

Topiramate also reduces the activity of certain isoenzymes of carbonic anhydrase. But this type of activity of a substance is not the main component of its antiepileptic activity.

Indications for the use of Topamax

According to the instructions Topamax is used:

• as monotherapy for first-time diagnosed epilepsy;
• as an adjunct drug in children over the age of 2 years and adults with partial or generalized tonic-clonic seizures;
• with epileptic seizures occurring against the background of Lennox-Gastaut syndrome;
• as a prophylaxis for migraine (capsules).

Contraindications

According to the instructions Topamax is not used:

• with increased sensitivity to the constituent components of the drug;
• under the age of 2;

Topamax is prescribed with caution when:

• hepatic and renal failure;
• nephrourolithiasis;
• hypercalciuria.

Method of application and dosage of Topamax

According to the instructions, Topamax is taken orally.

When taking capsules by children and elderly patients, you must open the capsule and mix its contents with 1 teaspoon of soft food. The mixture must be swallowed quickly.

Treatment with Topamax should be started with taking 25-50 mg of the drug at night for one week. Further, the dose is increased every 1-2 weeks by 25-50 mg and is divided into two doses.

When using Topamax as a combination therapy in children over two years of age, the recommended daily dose of Topamax is 5-9 mg per kg of body weight per day (2 doses). Dose selection starts at 25 mg. Further, the dose may be increased by 1-3 mg per kg of body weight every 1-2 weeks.

The initial dose when using Topamax as monotherapy in adults is 100 mg per day. In this case, the daily dose should not exceed 500 mg.

For children over 2 years of age, in the first week of therapy, Topamax is prescribed at a dosage of 0.5-1 mg per kg of body weight at night. Further, the dose is increased by 0.5-1 mg per kg of body weight per day (2 doses) every 1-2 weeks.

The daily dose of Topamax for the prevention of migraine is 100 mg (2 doses).

Side effects

According to reviews, Topamax can often cause side effects.

Central and peripheral nervous system: dizziness, drowsiness, paresthesia, impaired attention, memory, thinking, speech, coordination, lethargy, nystagmus, tremor, amnesia, improper gait, changes in taste, hypesthesia, dysarthria, psychomotor disturbances.

Mental disorders: speech disorders, slow thinking, depression, confusion, insomnia, aggression, irritability, disorientation, erectile dysfunction.

Digestive system: changes in appetite, nausea, anorexia, diarrhea.

Musculoskeletal system: myalgia, muscle pain, spasms and cramps, arthralgia.

Organs of vision: diplopia, dry eyes, visual impairment.

Hearing organ: pain and ringing in the ears.

Respiratory system: epistaxis, shortness of breath.

Dermatological reactions: alopecia, rash, itching, decreased sensitivity of the face.

Urinary system: nephrolithiasis, pollakiuria, dysuria.

Hematopoietic system: anemia.

General disorders: irritability, fatigue, weight loss, anxiety, asthenia.

According to reviews of Topamax, a syndrome may occur, which is characterized by myopia, which occurs against the background of increased intraocular pressure.

Overdose

According to reviews of Topamax, an overdose of the drug is manifested by convulsions, drowsiness, impaired vision and speech, diplopia, impaired thinking, coordination, arterial hypotension, stupor, dizziness, agitation and depression, lethargy.

In reviews of Topamax, there were fatal cases of overdose with a mixture of several drugs, including Topamax.

For the treatment of an overdose with Topamax, it is used: gastric lavage, intake of activated charcoal, symptomatic therapy, hemodialysis.

Application during pregnancy and lactation

Despite the fact that studies on the safety of using Topamax during pregnancy have not been conducted, it is possible to use the drug during pregnancy only when the potential benefit to the mother is higher than the risk to the child.

Presumably, Topamax can be excreted in breast milk. Therefore, if it becomes necessary to take the drug during breastfeeding, you must stop feeding the baby with breast milk.

Interaction of Topamax with other drugs

Topamax reduces the effectiveness of estrogen-containing oral contraceptives.

The drug reduces the AUC of digoxin.

When used simultaneously with carbamazepine and phenytoin, the AUC of topiramate decreases.

When used simultaneously with valproic acid, the AUC of topiramate and valproic acid decreases.

Carbonic anhydrase inhibitors increase the risk of renal calculi formation.

special instructions

Topamax should be withdrawn gradually so that the possibility of an increase in the frequency of seizures is minimized.

It is necessary to select the dosage of the drug in accordance with the clinical effect.

When treating Topamax, it is necessary to adequately increase the volume of fluid consumed in order to reduce the risk of developing nephrolithiasis and side effects.

During therapy with Topamax, it is necessary to abandon the performance of potentially hazardous activities that require quick response and high concentration of attention.

Topamax's analogs

Analogues of Topamax are drugs such as Topilepsin, Droplet, Epiramat, Topiramine, Topirol, Topiromax.

Before using an analogue of Topamax, you should definitely consult with your doctor.

Storage conditions Topamax

The drug is stored in a dark and dry place with a temperature of no more than 25 °.

1 capsule of Topamax contains 50, 25 or 15 mg topiramate .

Additional substances: sugar crumbs ( sucrose, starch syrup), povidone, cellulose acetate.

Capsule shell composition: water, Gelatin, Sorbitan Laurate, Sodium Lauryl Sulfate, Titanium Dioxide, Opacode Black ink black (black o iron oxide , glaze solution in ethyl alcohol, isopropyl alcohol, butyl alcohol, propylene glycol, ammonium hydroxide ).

Release form

Topamax is a hard gelatin white capsule labeled "50 mg" in black ink and a colorless cap labeled "TOP" in black ink; the inner contents of the capsules are white granules.

pharmachologic effect

Anticonvulsant .

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Antiepileptic drug, belongs to the group of fructose derivatives.

Topiramate suppresses sodium channels and inhibits the appearance of repeated action potentials during prolonged depolarization of the neuron wall. Increases activity gamma-aminobutyric acid for a number of subtypes GABA receptors and regulates activity GABAA receptors , blocks activation kainatom receptors for glutamate ... These effects of Topamax are dose-dependent over a range of concentrations topiramate in the blood 1-200 μmol.

Topiramate inhibits the activity of some isomers carbonic anhydrase ... However, in terms of the severity of this pharmacological effect, it is much inferior to - inhibitor carbonic anhydrase ... This activity of the drug is not the main component of it. antiepileptic activity .

Pharmacokinetics

After taking topiramate quickly absorbed from the intestines. Bioavailability reaches 81%. Food intake does not affect the bioavailability of the drug. Plasma protein binding - 13-17%.

In individuals with healthy kidney function, it will take 4-8 days to reach equilibrium. Transformation undergoes up to 20% of the dose taken. There are 6 known inactive metabolites. Topiramate and its derivatives are excreted by the kidneys. The half-life is on average 21 hours.

Indications for use

• :
  - prevention migraine .
• :
  - as monotherapy in children from 2 years of age and adults with epilepsy and in persons with newly diagnosed epilepsy;
  - as a component of complex therapy in children from 2 years of age and adults with generalized or partial tonic-clonic seizures ; for the treatment of seizures in Lennox-Gastaut syndrome .

Contraindications

• Age up to two years.
• to the components of the drug.
• It is necessary to use Topamax with caution when, hepatic or , hypercalciuria .

Side effects

• Disturbances from the nervous system: apathy, impaired thinking, speech, memory and concentration, lethargy , tremor , , changes in taste sensations, cognitive disorders, psychomotor disorders, loss of sense of taste and smell, akinesia, apraxia, aphasia, cerebellar syndrome , burning sensation, disturbed sleep rhythm, impaired coordination, convulsions , increased salivation, dysgraphia, dysesthesia, dyskinesia, dystonia, dysphasia, tonic-clonic seizures, hyperesthesia, hypokinesia, hypogeusia, hyposmia, parosmia, repetitive speech, stupor , violation of the sense of touch, fainting .
• Mental disorders: confusion, slow thinking, aggressive reactions, agitation, emotional lability, disorientation, anorgasmia , cry , sexual dysfunction, dysfemia , euphoric mood, hallucinations , decrease libido, hypomanic states, manias, paranoid states , a state of panic, perseveration of thinking, restlessness , suicidal ideation, tearfulness .
• Digestive system disorders:, change in appetite, abdominal pain, dry mouth, changes in sensitivity in the mouth, gastroesophageal reflux, , bleeding gums, thirst, glossodyny, symptoms.
• Musculoskeletal system disorders: myalgia, spasms , muscle pain, convulsions, arthralgia , muscle stiffness, joint swelling.
• Cardiovascular disorders: orthostatic hypotension, bradycardia, .
• Visual impairment: visual impairment, diplopia , dry eyes, violation of accommodation, blepharospasm, one-sided blindness, mydriasis, photopsia , night blindness, presbyopia , decreased visual acuity, closed-angle , swelling of the eyelids, conjunctival edema, maculopathy .
• Hearing organ damage: pain and ringing in the ears, deafness, hearing impairment.
• Respiratory system disorders: epistaxis, hoarseness, dyspnea , nasal congestion, rhinorrhea, nasopharyngitis .
• Skin lesions:, lack of perspiration, skin redness, skin pigmentation disorders, unpleasant odor, erythema multiforme , paraorbital edema.
• Lesions of the urinary system: pollakiuria, hematuria, nephrolithiasis, , , dysuria, urinary incontinence, kidney pain, renal tubular acidosis .
• Damage to the hematopoietic system: anemia , leukopenia, thrombocytopenia, lymphadenopathy, eosinophilia, neutropenia.
• Changes in laboratory parameters: a decrease in the concentration of bicarbonates in the blood, leukopenia, crystalluria, hypokalemia.
• General disorders: fatigue, decrease or increase in body weight, anxiety , swelling of the face, hyperchloremic or metabolic acidosis , cold extremities, weakness , fatigue, calcification , flu-like diseases, generalized edema .

Application instruction of Topamax (Way and dosage)

According to the instructions for Topamax, the drug is taken orally, regardless of food intake. The capsule must be opened, its contents must be mixed with a small amount of soft food. Then swallow quickly without chewing. Also, the capsules are allowed to be swallowed whole.

For better control of epileptic seizures in patients of all ages, it is recommended to start therapy with low doses of the drug, then titrate to the effective dose.

Tonic-clonic seizures (partial, generalized ), seizures at Lennox-Gastaut syndrome ... The smallest effective dose in adults is 200 mg per day. The daily dose ranges from 200 mg to 400 mg and is taken in two doses. Some patients may be shown to consume a maximum daily dose of 1600 mg. The dose is selected from 25-50 mg at night, once a day for a week. Then the dose can be increased by 25-50 mg and divided into 2 doses. In a number of patients, the effect is achieved when taken once a day.

Epilepsy ... In adults, with monotherapy, at the beginning, 25 mg of Topamax is prescribed once a day for a week. Subsequently, the dose is increased at intervals of 7-14 days by 25-50 mg. If necessary, it is possible to make longer intervals between dose increases, or to increase the dose in smaller increments. The initial dose for epilepsy in adults is 100 mg per day, the maximum daily dose is 500 mg.

Migraine ... For the prevention of migraine, the daily dose of the drug should be 50 mg twice a day. If necessary, you can practice increasing the dose until the onset of the clinical effect.

Overdose

Symptoms: drowsiness , convulsions , impairment of the function of speech and vision, impaired thinking and coordination, diplopia, lethargy, arterial hypotension, dizziness, ... Development is possible metabolic acidosis severe degree.

Treatment: gastric lavage or vomiting; reception that effectively adsorbs topiramate ; symptomatic therapy, an increase in the volume of fluid consumed.

Interaction

The effects caused by the joint intake of funds that cause depression of nervous functions, alcohol and Topamax have not been studied.

Joint reception Hypericum perforatum lowers concentration topiramate in blood.

When using high doses topiramate (less than 600 mg / day) and lithium preparations , the concentration of the latter may increase.

When used together topiramate and there is an increase in concentration topiramate in blood.

With the simultaneous appointment of patients and their condition should be monitored to assess the nature of the course.

Simultaneous use of Topamax with drugs that predispose to development nephrolithiasis may further increase the risk of kidney stone production. Such combinations should be avoided.

Combined use valproic acid and topiramate often accompanied by hyperammonemia in some cases with the development encephalopathy .

Terms of sale

Topamax is on the list of prescription drugs.

Storage conditions

Store at temperatures up to 26 degrees. Keep out of the reach of children.

Shelf life

Two years.

special instructions

Topamax should be withdrawn slowly over 2-8 weeks to minimize the possibility of an increase in the frequency of seizures.
With drug treatment, there is an increased incidence of mood disorders, suicidal thoughts, depression and suicidal behavior.

If the patient loses weight during therapy with Topamax, it is advisable to consider switching to enhanced nutrition.

Topamax can cause dizziness, blurred vision, drowsiness and a number of other symptoms that pose a serious danger to people driving.

Analogs

Matching ATX level 4 code:

Topamax analogs: Topilex, Topiramine, Toprakar, Epiramate, Epiramate-Teva .

For children

It is forbidden to admit children under two years of age.

With alcohol

During pregnancy (and lactation)

During the period either it is necessary to interrupt treatment with Topamax.

Topamax (Topiramate), Topalepsin, Topsaver, Maxitopyr, Epitop, Toreal, Epimax are a group of drugs with the same active ingredient and the same pharmacological action.

Characteristics of the substance Topiramate

Topiramate is an anticonvulsant, which is aimed at antiepileptic action by relieving muscle cramps.

This component is also able to quickly eliminate psychoses, due to the fact that Topiramate has anti-manic characteristics, it eliminates, as well as manic-depressive disorders.

Topiramate has the empirical formula C12H21NO8S. It is a fructose derivative and has a complex structure with a high molecular weight - 339.33 units. In pharmacology, Topiramate is classified as a substance with antiepileptic action.

Topamax and its generics

Topomax is an antiepileptic drug that belongs to fructose derivatives. The active substance of this drug, topiramate, suppresses sodium channels, and also slows down the development of repeated action potentials during prolonged depolarization of the walls of neurons.

This drug is prescribed for epileptic seizures, convulsive conditions, as well as for the elimination of manic-depressive conditions.

The drugs Topalepsin, Topsaver, Maxitopyr, Epitop, Toreal, Epimax are all Topomax analogues that have the same properties and indications. The active substance of all these funds is topiramate.

The action of all funds is aimed at eliminating epileptic seizures, manic-depressive states. All of these drugs are available as capsules and tablets for internal use.

Pharmacological properties

Topomax is a drug that has an antiepileptic effect. This agent increases the activity of GABA receptors, and also contributes to the normalization of AMPK receptors. It is used in therapeutic therapy when symptoms appear in the initial stages, spasmodic conditions with various etiologies.

Topomax also has anti-spasmodic, analgesic, anti-inflammatory effects.

Many patients who have used this drug note that it is able to quickly remove seizure activity and reduce nervous irritability.

Pharmacokinetics of the drug

Topiramate is instantly absorbed in the stomach and intestines. The bioavailability of the drug is independent of food intake. The bioavailability level is about 81%.

The protein binding of the active ingredient is about 13-17%. The average level of distribution volume depends on gender. The volume of distribution in women is almost 2 times lower than in men, this is due to the fact that women have a high level of body fat.

The distribution rate is 0.55 to 0.8 liters per kilogram for single dosages up to 1200 mg. The highest level of concentration in the blood usually reaches a few hours after taking the drug at a dosage of 400 mg. The average period of the equilibrium concentration in the blood serum is 4 to 8 days.

The excretion of the active substance occurs through the kidneys. 70% of the active ingredient is removed unchanged. The half-life is about 21 hours.

Release form and composition

Topomax is produced in capsule form. The dosage of the capsules is 15, 25 and 50 mg. The capsules are contained in blisters of 10 pieces. Blisters are packed in cardboard boxes. Also on sale there are plastic bottles with the number of capsules 28 and 60 pieces.

Component components:

Components of the shell:

• gelatin;
• silicon dioxide;
• titanium dioxide;
• purified water;
• sodium lauryl sulfate;
• Opakod ink black S-1-17822 / 23.

Under what indications is it assigned?

Topomax, like all its analogues based on the active substance, topiramate is prescribed for the following indications:

• to relieve seizures and myoclonic nature;
• relieves from;
• eliminates;
• assigned when;
• at ;
• helps to relieve tonic-clonic seizures.

In many patient reviews about Topomax found on the Internet, it is noted that this drug is also effective for relieving smooth muscle spasms.

It is impossible to use Topomax, as well as its analogs, during the following conditions:

• pregnant women;
• when breastfeeding;
• if there is an increased sensitivity to the active ingredient and other constituent elements of the drug;
• in the presence of renal failure;
• with heart failure;
• if there are severe brain disorders;
• the presence of malignant tumors;
• not recommended for children under 2 years of age.

With extreme caution, drugs with the active ingredient topiramate are taken for osteoporosis, nephrourolithiasis, as well as in old age.

Features of reception and dosage

Topomax must be taken by mouth. The medicine should be taken at a dosage of 200 mg twice a day. If suddenly there is such a need, the contents of the capsule are allowed to be mixed with water, but only with a small amount.

For adult patients, the drug can be taken in conjunction with others, but the dose level should only be set by the attending physician.

At the initial stage of therapy for epileptic conditions, it is recommended to take 25 mg of the drug per day. An increase in the dose should be made only depending on the clinical manifestations of the disease.

It is not recommended to take Topomax by children under 2 years of age. From the age of two to 10 years, the dosage per day should not exceed 50 mg. If patients have kidney problems, then they should be prescribed the drug in sufficiently low dosages.

If Topomax is used as an additional antiepileptic drug, it is recommended to take the drug at a dosage of 9 mg twice a day. The duration of the therapeutic treatment is about 7 days.

For migraines, it is necessary to apply 100 mg twice a day. If very severe migraine attacks occur, it is recommended to increase the dosage to 200 mg twice a day. During preventive treatment, drugs based on topiramate are taken at 25 mg once a day for one week.

Reception by pregnant women and during lactation

Clinical and adequate studies of the effect of topiramate during pregnancy on the fetus have not been conducted. But in practice, there are cases when during the period of use of Topimax as monotherapy in women during pregnancy there were serious pathologies and deviations in the development of the baby.

Children were born with craniofacial defects, cleft palate or lips, and other defects. Also, children are often born with a low body weight, no more than 2500 kilograms. Thus, the use of drugs based on topiramate during pregnancy is highly undesirable.

During the period of breastfeeding, the use of the drug is contraindicated. It is better at the time of treatment with this medication to refuse breastfeeding or not to take the drug during breastfeeding.

Overdose and side effects

Overdose symptoms are rare. It is usually accompanied by the following symptoms:

• the appearance of seizures;
• the occurrence of problems with speech;
• deterioration of vision;
• increased sleepiness;
• disorder of coordination;
• thinking problems;
• the appearance of a stupor;
• excitation;
• depressive state;
• the appearance of pain in the abdomen.

During the use of Topomax, the following unpleasant conditions may appear:

special instructions

When using Topomax, you should pay attention to the following points:

• withdrawal of the drug should be done slowly in order to reduce the frequency of seizures and prevent the appearance of unwanted symptoms;
• if the drug is taken during hemodialysis, then the dosage should be increased, the drug must be taken before and after the hemodialysis procedure;
• if during the use of the drug there is a decrease in body weight, then it is recommended to adjust the diet;
• at the time of using the drug, it is not recommended to drive a car and perform work that requires increased attention.

A doctor's review of Topamax and similar drugs based on topimarat, as well as reviews of patients who took these drugs, can shed light on unclear points regarding the intake and effectiveness of this group of drugs.

Physician Review

Topomax, as well as Topalepsin, Topsaver, Maxitopyr, Epitop, Toreal, Epimax are the same drugs with the active ingredient topiramate. All these drugs have the same effect - they reduce the activity and frequency of epileptic seizures, stop migraine attacks, as well as seizures of a partial and myoclonic nature. During the use of this remedy, a decrease in seizures is observed, the nervous system and psyche are restored.

Psychotherapist

The opinion of ordinary people

I have had epilepsy for a long time, about 10 years. At first, it practically did not bother me, but over time the attacks began to become more frequent, and they could occur at the most inopportune moments.

After examination by a neurologist, I was prescribed. But as soon as I started taking this remedy, I felt very bad, I had so many side effects, I myself do not remember.

I again decided to go to a doctor for a psychotherapist, only after a complete examination I was prescribed Topomax. At first, I took 25 mg. At the moment he was replaced by Topalepsin for me. I take it 20 mg in the morning and 20 mg at night. I forgot about the attacks.

Svetlana, 28 years old

The son is 12 years old and he is already 6 years old with epileptic seizures. At first, they bothered him 2-3 times a month. After a complete examination, we were prescribed Topomax. He has been taking this remedy for 4 years, during this period this remedy was not always in the pharmacy, so we replaced him with Topalepsin, Topsaver, Epimax. All drugs have a similar effect. The son's attacks hardly bother him, it happens 1-2 times a year, but not more.

Marina, 33 years old

Price question

The price of a Topomax package with 60 capsules and a dosage of 25 mg is from 1,735 rubles. Packing Topomax with the number of capsules 60 pieces and a dosage of 50 mg costs from 2500 rubles.

Toreal costs from 150 rubles, Topalepsin from 200 rubles, Maxitopir from 350 rubles.

Topamax's analogs for the effect on the body:

• Gabagamma;
• Neurontin;
• Pagluferal;
• Epiramat-Teva.

Forbidden during pregnancy

Forbidden while breastfeeding

Has restrictions for children

Has restrictions for seniors

Has limitations for liver problems

Has limitations for kidney problems

Topamax is an antiepileptic drug used in neurology in many European countries and beyond. The medicine has earned numerous positive reviews from both doctors themselves and patients. Topamax is taken exclusively on the recommendation of a specialist, but even in this case, it is important to study in detail the instructions for its use.

General information about the drug

Topamax is an anticonvulsant used for epilepsy. International non-proprietary name - Topiramate (topiramate). The drug is used in neurology.

Forms of release, composition and cost of drugs

The medicine is dispensed in the form of oral capsules. Contains the active ingredient topiramate in a dosage of 25 or 50 mg for 1 pc. The price for Topamax (approximate) may be as follows:

It should be noted that this cost of an imported (Belgian) drug is relatively low. But if necessary, the doctor can always recommend a cheaper analogue of the medication in question.

Pharmacodynamics and pharmacokinetics

The drug has an anticonvulsant effect based on blocking sodium channels and suppressing the re-emergence of action potentials, provoked by prolonged depolarization of neuronal membranes.

Topiramate enhances the function of GABA in relation to some receptors (in particular, GABAA), and also modifies the work of the GABAA receptors themselves. The effectiveness of the active ingredient of the drug depends on its dose.

Also, topiramate reduces the action of certain isoenzymes of carbonic anhydrase. But this property is much weaker than that of another similar drug, acetazolamide, so Topiramate is rarely the drug of choice for epilepsy.

Absorption of topiramate occurs in the gastrointestinal tract. Usually excreted by the kidneys, but in different concentrations. The rate of excretion of the drug is directly influenced by the work of the patient's urinary system.

Indications and contraindications

There are several indications for the use of Topamax. The medication is prescribed for patients with epilepsy and migraine:

1. Adults and children from 2 years old with different forms of epileptic seizures as part of complex therapy or monotherapy.
2. For adult patients for the prevention of the development of migraine attacks.

Note. The effectiveness of Topamax for the relief of acute migraine attacks has not been studied.

Topamax has a list of absolute contraindications. The drug is not prescribed to patients:

• under 2 years of age;
• with hypersensitivity to topiramate or auxiliary components.

You should not drink capsules and women of reproductive age who are not taking effective contraceptives.

The drug is not prescribed for women during pregnancy. Topiramate passes into breast milk, so capsules are not taken during lactation either. If such a need arises, breastfeeding should be suspended for the entire period of treatment.

The drug is prescribed for children over 2 years of age, but only for the treatment of partial or generalized epileptic seizures (as monotherapy or as part of a complex treatment). For therapeutic or prophylactic purposes for migraines, the medicine is strictly contraindicated for children.

Detailed Application Guide

Medication treatment should be started with the lowest effective dosage. It must be gradually increased until the expected therapeutic effect is achieved.

Note. There is no need for regular monitoring of the content of topiramate in the blood to optimize the treatment process. But before starting therapy, a laboratory test must be prescribed without fail.

Features of dosage of the drug for adults

The dosage of drugs is titrated depending on the therapeutic response of the patient's body to the treatment. It is necessary to start with 25 mg of the drug. It must be taken once a day before bedtime. Such a dose of Topamax will be relevant for 1-2 weeks, after which it will be doubled or quadrupled. In this case, the daily dosage is divided into 2 doses - morning and evening.

If the patient does not tolerate such a Topamax dosing regimen, then the number of capsules taken should be increased at a greater interval than 1-2 weeks. Or increase the dose not by 50, but by 25 mg. For monotherapy, adult patients are prescribed an initial dosage of 100-200 mg / day. Taking the medicine is divided into 2 approaches - morning and evening. The maximum allowable dose of the drug is 500 mg.

Note. In some patients suffering from refractory forms of epilepsy, a high therapeutic response was noted when taking the medication in a daily dose of 1000 mg.

The above dosages of Topamax are suitable for all - adults and elderly patients - with normal kidney and liver function.

Features of dose titration for children from 6 to 16 years old

Treatment of epilepsy in children over 6 should be started with a dose of 0.5-1 mg / kg body weight. The capsule is taken once a day, preferably before going to bed. This dosage regimen should be followed for 7 or 14 days. After that, the dose is doubled, or increased fourfold, and is divided into 2 daily doses. The amount of drug taken is increased until the expected effect of treatment is achieved.

As a monotherapy, Topamax is prescribed for pediatric patients from 6 years of age at an initial dose of 100 mg. This is equal to about 2 mg / kg body weight. Such features of the dosage of the drug are used for children 6-16 years old.

Treatment of children 2-5 years old

It is recommended to start therapy with 1 capsule of 25 mg of topiramate. You can start the treatment process with a lower dosage (for example, 1-3 mg per kg of the child's weight). Due to possible differences in dose titration for each child, Topamax cannot be used for self-medication.

Topamax is intended to prevent migraine attacks, not to treat them in the acute phase. For this purpose, the drug is prescribed exclusively for adult patients.

The generally accepted dosage in this case is 100 mg Topamax, divided into 2 applications within 24 hours. Features of therapy:

Some patients managed to achieve a clinical response from the use of 50 mg / 24 hours, in others - 200 mg / 24 hours. Thus, each situation is individual and requires an appropriate approach.

Possible side reactions and signs of overdose

Usually Topamax therapy is well tolerated by patients. If side effects occur, then they proceed mainly in a mild or moderate degree. But drug overdose should be avoided. If the daily dose of the drug prescribed by the doctor has been exceeded, you must immediately seek medical help. Even with the complete absence of ailments associated with this fact.

Side effect symptoms

There are quite a few possible side reactions associated with its use described in the official instructions for Topamax. However, below are only those ailments that occur in most cases, that is, very often. These include:

Changes in the clinical parameters of the blood test are often observed. In particular, patients taking Topamax develop anemia. Less often, cases of leukopenia, thrombocytopenia, eosinophilia are recorded. Development of lymphadenopathy is possible.

Such side effects may not cause any harm to the patient's body, since they often go away on their own. If they persist or their intensity increases, in this case it may even be necessary to completely cancel the drug or replace it with analogues.

Overdose

Cases of overdose with Topamax are known. At the same time, the following symptoms appeared in patients:

Important! Long-term and severe overdose of Topamax can provoke the development of severe metabolic acidosis.

The peculiarities of the dosage treatment, due to the absence of the topiramax antidote, consist in carrying out the following measures:

1. Cleansing the stomach by enema or vomiting.
2. Reception of an adsorbent (in particular, activated carbon).
3. Drinking a lot of fluids.
4. If necessary, carry out symptomatic therapy (pain relieving).

One of the most effective methods to help eliminate the symptoms of Topamax overdose is the hemodialysis procedure.

Special instructions and drug interactions

Topamax should be withdrawn as gradually as its dosage is increased. If it is necessary to abruptly stop taking capsules, you should carefully monitor the patient's condition. A sudden cessation of therapy with any drugs based on topiramate can provoke the development of another epileptic seizure.

Patients suffering from kidney and liver diseases require special attention when treating Topamax. Also, the drug is prescribed with caution to persons with chronic alcoholism.

Throughout the entire therapeutic course, you need to carefully monitor the mental and psychological state of the patient. In some patients, the appearance of depression and suicidal thoughts was noted. If such deviations appear, psychotherapy should be started immediately.

Monitoring of the urinary system is important when treating Topamax in patients with diagnosed nephro- or urolithiasis. Increased control requires the condition of patients prone to similar diseases (the presence of urolithiasis in a personal or family history).

Important! Topamax contains sucrose in its composition. Patients suffering from intolerance to this substance are not advised to take this medication. If its appointment is due to vital indications, the patient's condition must be carefully monitored by a doctor!

• phenytoin;
• carbamazepine;
• digoxin;
• alcohol;
• drugs that inhibit the work of the central nervous system;
• Hypericum perforatum;
• valproic acid;
• lithium preparations;
• risperidone;
• hydrochlorothiazide;
• drugs that promote the development of nephrolithiasis.

Combine Topamax with Metformin, Pioglitazone and Glyburide with caution. While taking these drugs, the patient's diabetic profile should be carefully monitored.

Analogs

Today in pharmacies you can find the following Topamax analogues (by active ingredient):

All of the above generics of Topamax have almost completely identical composition. But the auxiliary components of drugs may differ, therefore, replacing Topamax with an analogue must be carried out extremely carefully, taking into account the possible hypersensitivity of the patient's body to certain auxiliary components.