Universal reference book for medicines
Product name: MAXITOPIR ®

Active substance: topiramate

Type: Anticonvulsant drug

Manufacturer: ACTAVIS hf.
(Iceland)
Composition, form of production and packaging
The tablets covered with a film cover of
white color, round, biconcave, with an inscription "V1" on one side.

1 tab.

topiramate 25 mg

Auxiliary substances: mannitol - 37.81 mg, pregelatinized starch 8.55 mg, microcrystalline cellulose 19 mg, croscarmellose sodium 2.85 mg, colloidal silica 0.36 mg, magnesium stearate 1.43 mg, Opadry II white dye 85F18422 3.8 mg (polyvinyl alcohol , titanium dioxide, macrogol 3350, talc).

10 pieces.
- Strips (1) - packs of cardboard.
10 pieces.
- polyethylene containers (1) - packs of cardboard.
The tablets covered with a film cover of light yellow color, round, biconcave, with an inscription "V3" on one side.

1 tab.

Topiramate 50 mg

Auxiliary substances: mannitol - 75.64 mg, pregelatinized starch - 17.1 mg, microcrystalline cellulose - 38 mg, croscarmellose sodium - 5.7 mg, silicon dioxide colloid - 0.71 mg, magnesium stearate - 2.85 mg, dye Opadry II yellow 85G32312 - 7.6 mg (polyvinyl alcohol , talc, titanium dioxide, macrogol 3350, soy lecithin (E322), iron oxide yellow (E172)).

10 pieces.
- Strips (1) - packs of cardboard.
10 pieces.
- polyethylene containers (1) - packs of cardboard.
The tablets covered with a film cover of yellow color, round, biconcave, with an inscription "V4" on one side.

1 tab.

topiramate 100 mg

Auxiliary substances: mannitol 151.28 mg, pregelatinized starch 34.2 mg, microcrystalline cellulose 76 mg, croscarmellose sodium 11.4 mg, colloidal colloidal silicon 1.42 mg, magnesium stearate 5.7 mg, Opadry II yellow color 85G32313 15.2 mg (polyvinyl alcohol , talc, titanium dioxide, macrogol 3350, iron oxide yellow (E172), soy lecithin (E322)).

10 pieces.
- Strips (1) - packs of cardboard.
10 pieces.
- polyethylene containers (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2012.

PHARMACHOLOGIC EFFECT

Antiepileptic drug, refers to the class of sulfate-substituted monosaccharides.

It blocks sodium channels and suppresses the appearance of action potentials against the background of a prolonged depolarization of the neuron membrane.
Increases the activity of gamma-aminobutyric acid (GABA) against certain subtypes of GABA receptors, prevents the activation of kainate sensitivity of the kainate / AMPK subtype (alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid) receptors to glutamate, does not affect on the activity of N-methyl-D-aspartate against the NMDA receptor subtype. These drug effects are dose-dependent.
In addition, topiramate inhibits the activity of certain isoenzymes of carbonic anhydrase.
In terms of this pharmacological effect, topiramate is significantly inferior to the inhibitor of carbonic anhydrase acetazolamide, therefore this effect of topiramate is not the main component of its antiepileptic activity.
PHARMACOKINETICS

Suction

After taking the drug inside, topiramate is quickly and well absorbed from the digestive tract.
Bioavailability is about 80%. Eating does not have a clinically significant effect on the bioavailability of the drug.
After a single administration of the drug inside the 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 averaged 6.76 μg / ml.

Distribution

Binding to plasma proteins is 13-17%.

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

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

Metabolism

About 20% of the topiramate is metabolized.

Of the plasma, urine and feces of humans, 6 practically inactive metabolites were isolated and identified.

Excretion

Unchanged topiramate and its metabolites are excreted mainly through the kidneys.
Plasma clearance of the drug is 20-30 ml / min.
After repeated administration of the drug at 50 mg and 100 mg 2 times / day, the average T 1/2 was 21 hours.

Pharmacokinetics in special clinical cases

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

In patients with impaired renal function (CC less than 60 ml / min) renal and plasma clearance of topiramate decreases, in patients with the final stage of renal failure, the plasma clearance of topiramate decreases.

In elderly patients in the absence of impaired renal function, the plasma clearance of topiramate does not change.

In patients with moderately severe and severe impairment of liver function, plasma clearance decreases.

In children, as well as in adults, pharmacokinetics is linear.
The clearance of topiramate does not depend on the dose, and C ss in the plasma increases in proportion to the increase in dose. It should be borne in mind that in children the clearance of topiramate is elevated, and its T 1/2 is shorter. Consequently, when taking the drug in equal doses per kg body weight, the concentration of topiramate in the blood plasma may be lower in children than in adults. In children, as in adults, antiepileptic drugs that induce hepatic enzymes cause a decrease in C ss of topiramate in blood plasma.
Topiramate is effectively excreted by hemodialysis.

INDICATIONS

Monotherapy:

- Epilepsy in adults and children older than 3 years (including patients with newly diagnosed epilepsy).

Auxiliary therapy:

- partial or generalized tonic-clonic seizures in adults and children over 3 years of age (with the lack of efficacy of the antiepileptic drug (PEP) of the first choice);

- seizures against the background of Lennox-Gastaut syndrome in adults and children over 3 years old.

DOSING MODE

The drug is taken orally, regardless of food intake.
The tablet should be swallowed whole, without chewing.
To achieve optimal control of epileptic seizures, it is recommended to begin treatment with taking the drug in low doses with subsequent increase to an effective dose.

When using Maxotopy in combination therapy in adults, the minimum effective dose is 200 mg / day.
The average daily dose is 200-400 mg (in 2 divided doses). The maximum daily dose is 1600 mg. It is recommended to start treatment with a dose of 25-50 mg 1 time / day at night for 1 week. Next, you should increase the dose by 25-50 mg / day for 1-2 weeks before choosing the effective dose; frequency of reception - 2 times / day. If this treatment regimen is necessary, the dose is increased by a smaller amount or at longer intervals. The dose and the frequency of reception are selected depending on the clinical effect.
When using Maxotopy in combination therapy in children older than 3 years, the recommended daily dose is 5-9 mg / kg and taken in 2 divided doses.
Selection of the dose begins with 25 mg 1 time / day (overnight) for 1 week. Then the dose is increased by 1-3 mg / kg / day for 1-2 weeks, with the frequency of reception 2 times / day, until the optimal clinical effect.
When carrying out monotherapy for adults, including elderly patients with normal renal function, at the beginning of treatment, Maxitope® is prescribed at 25 mg 1 time per day for 1 week.
Then the dose is increased by 25-50 mg / day for 1-2 weeks, the frequency of reception is 2 times / day. If the treatment regimen is intolerant, the dose is increased by a smaller amount or at longer intervals. The dose and the frequency of reception are selected depending on the clinical effect. The recommended initial dose of topiramate for monotherapy in adults with first established epilepsy is 100 mg / day, the maximum daily dose is 500 mg.
At monotherapy for children older than 3 years in the first week of treatment, topiramate is prescribed in a dose of 0.5-1 mg / kg of body weight 1 time / day for the night.
Then the dose is increased by 0.5-1 mg / kg / day for 1-2 weeks, the daily dose is divided into 2 divided doses. If this mode is intolerant, the dose can be increased by a smaller amount or at longer intervals. The magnitude of the dose and the frequency of reception are determined by the clinical efficacy of the therapy.The recommended dose range for topiramate monotherapy in children older than 3 years is 3-6 mg / kg / day. With newly diagnosed partial seizures, the dose may be up to 500 mg / day.
In days of hemodialysis, topiramate should be prescribed additionally at a dose equal to half the daily dose, in 2 divided doses (before and after the procedure).
The drug should be discontinued gradually (at 100 mg / week) in order to minimize the possibility of an increase in the frequency of seizures.
SIDE EFFECT

From the side of the central nervous system and peripheral nervous system: increased excitability, dizziness, headache, speech and vision impairment, psychomotor inhibition, ataxia, fatigue, impaired concentration, confusion, paresthesia, drowsiness, dyschinesia, diplopia, nystagmus, anorexia, depression , perversion of taste, agitation, cognitive disorders, emotional lability, apathy, psychotic symptoms, aggressive behavior, suicidal thoughts or attempts;
In addition, in children - personality disorders, increased salivation, hyperkinesia, hallucinations.
From the digestive system: symptoms of dyspepsia , nausea, abdominal pain, diarrhea, dry lips;
rarely - increased activity of hepatic transaminases, hepatitis, hepatic insufficiency.
From the side of the organ of vision: it is possible to develop a syndrome characterized by myopia against a background of increased intraocular pressure with a sharp decrease in visual acuity and pain in the eye area;
observed myopia, a decrease in the depth of the anterior chamber of the eye, hyperemia of the mucous membrane of the eye, increased intraocular pressure, mydriasis. A possible mechanism for the development of this syndrome is an increase in supraciliary eudication, leading to a shift in the lens and iris, and as a result, to the development of secondary, closed-angle glaucoma.
Dermatological reactions: erythema multiforme, pemphigus, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Other: weight loss, leukopenia, nephrolithiasis, oligohydrosis (mainly in children), metabolic acidosis.

CONTRAINDICATIONS

- Pregnancy;

- lactation period (breastfeeding);

- children's age till 3 years;

- Hypersensitivity to the components of the drug.

With caution should be used in renal or hepatic insufficiency, nephrourolythiasis (including in the past or in a family history), with hypercalciuria.

PREGNANCY AND LACTATION

The use of the drug during pregnancy and during lactation is contraindicated.

Patients of reproductive age in the period of application of Maxotopy should use reliable methods of contraception.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution should be used for kidney failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should be used for liver failure.

APPLICATION FOR CHILDREN

Contraindication: children under 3 years.

SPECIAL INSTRUCTIONS

To cancel Maxotop ® should be gradual, in order to minimize the possibility of increasing the frequency of seizures.

Patients with mild to severe renal impairment may need 10-15 days to achieve an equilibrium state of plasma concentration, in contrast to 4-8 days for patients with normal renal function.
As with all patients, a gradual increase in dose should be consistent with clinical outcomes (such as seizure control, the incidence of side effects), given that patients with moderate or severe renal failure may need more time to reach a stable state after each dose increase.
When using Maxotopy in patients prone to developing nephrolithiasis, the risk of kidney stones and related symptoms such as renal colic, side pain and kidney problems may increase.
It is recommended to conduct adequate hydration to reduce the risk of kidney stones.
In patients with impaired liver function, topiramate should be used with caution because of the possible decrease in the clearance of this drug.

If a syndrome occurs that involves myopia associated with occlusive glaucoma, Maxotyp ® should be discarded as quickly as the doctor deems it clinically possible and take steps to reduce intraocular pressure.

When using Maxotopy, hyperchloremic, not associated with anion deficiency, metabolic acidosis (eg, a decrease in the bicarbonate concentration in the plasma below the normal level in the absence of respiratory alkalosis) may occur.
This decrease in serum bicarbonate concentration is a consequence of the inhibitory effect of topiramate on renal carboanhydrase. In this regard, in the treatment of topiramate it is recommended to periodically determine the concentration of bicarbonates in the blood serum.
If the weight of the body decreases with the use of Maxotopy, it is advisable to consider the possibility of prescribing additional food.

Impact on the ability to drive vehicles and manage mechanisms

During the period of treatment, the patient should refrain from driving and work, requiring increased attention and speed of psychomotor reactions.

OVERDOSE

Symptoms: convulsions, impaired consciousness right up to coma, decreased blood pressure, severe metabolic acidosis, increased severity of side effects.

Treatment: gastric lavage, symptomatic therapy.
The use of activated carbon is ineffective, because in experiments in vitro it was shown that it does not adsorb topiramate. An effective method of excretion of topiramate from the body is the conduct of hemodialysis.
DRUG INTERACTION

The influence of Maxotopy on the concentration of other antiepileptic drugs (PEP)

With simultaneous administration of Maxotopyr ® does not affect the concentrations of carbamazepine, valproic acid, phenobarbital, primidone.
In some cases, when used with phenytoin, an increase in the concentration of phenytoin in the plasma is possible.
The effect of other PEP on the concentration of topiramate in blood plasma

With the combined use of Maxotopy with phenytoin and carbamazepine, a decrease in the concentration of topiramate in plasma, i.e., is possible.
When adding or canceling phenytoin or carbamazepine, a dose adjustment of Maxitopy is recommended.
Interaction with other medicinal products

With simultaneous use of Maxotopy with digoxin AUC, digoxin decreased by 12%.

When the oral contraceptive containing norethindrone and ethinylestradiol was simultaneously used with Maxotopyr, Maxitopyr ® in doses of 50-800 mg / day had no significant effect on the effectiveness of norethindrone and in doses of 50-200 mg / day - on the efficacy of ethinylestradiol.
A significant dose-dependent decrease in the effectiveness of ethinylestradiol was observed with the use of Maxotopy in doses of 200-800 mg / day. Patients taking oral contraceptives should inform the doctor of any changes in the nature of menstrual bleeding.
With the simultaneous use of metformin with Maxotopyr, the mean values ​​of C max and AUC of metformin are increased by 18% and 25%, respectively, while the average total clearance decreases by 20%.
Topiramate had no effect on the time to reach C max metformin. Plasma clearance of topiramate under the influence of metformin decreases. The clinical significance of the effects of metformin on the pharmacokinetics of topiramate is not clear. When appointing or canceling Maxotopy against the background of metformin therapy, it is necessary to monitor the state of carbohydrate metabolism.
With simultaneous application of Maxotopy with hydrochlorothiazide, the C max and AUC of topiramate increased by 27% and 29%, respectively.

Joint use of Maxotopy with drugs that exert a depressing effect on the central nervous system and with ethanol is not recommended.

With simultaneous application of Maxotopy with pioglitazone, a decrease in AUC of pioglitazone by 15%, without a change in C max .
For active pioglitazone hydroxy metabolite, Cmax and AUC decreased by 13% and 16%, respectively, and a decrease in both C max and AUC by 60% was revealed for active ketometabolite.The clinical significance of this data is unknown.
With the simultaneous use of Maksitopira with other drugs predisposing to the development of nephrolithiasis, in particular with inhibitors of carbonic anhydrase (acetazolamide), there may be an increased risk of kidney stones.
During treatment with Maxotopyr, the use of such drugs should be avoided, as they can cause physiological changes that contribute to the development of nephrolithiasis.
With simultaneous application of Maxitope with valproic acid, the valproic acid AUC is reduced by 11%, topiramate by 14%.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of the reach of children at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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