The description is up to date 31.03.2014

• Latin name: Grandaxin
• ATX code: N05BA23
• Active substance: Tofisopam (Tofisopam)
• Manufacturer: OJSC Pharmaceutical Plant EGIS, Hungary

Compound

Active substance - tofisopam , 1 tablet contains 50 mg of tofisopam. Excipients: magnesium stearate ,talc , stearic acid , gelatin , MCC , potato starch ,lactose monohydrate .

Release form

The drug Grandaxin (INN - Tofisopam) is available in the form of tablets of 50 mg, 10 tablets are contained in a blister, 2 or 6 blisters are in a carton.

Tablets are white or grayish, flat, scored on one side, almost odorless.

pharmachologic effect

The annotation to the drug states that the drug has an anxiolytic effect.

Pharmacodynamics and pharmacokinetics

The drug is a tranquilizer from the group of derivatives benzodiazepine , eliminates the variety different forms . Grandaxin also has stimulating activity. The drug can be used for patients with and myopathy . It does not cause any physical or mental dependence, nor a withdrawal syndrome. Refers to daytime anxiolytics .

Quickly and almost completely absorbed into the blood from the gastrointestinal tract when taken orally. After 2 hours, the maximum concentration of the substance in the blood is reached. The half-life of Grandaxin is 6-8 hours. About 60% is excreted in the urine, the rest - in the feces.

Indications for the use of Grandaxin

What are Grandaxin tablets for? Here are the indications for the use of the drug:

• mental adjustment disorder ;
• alcoholic withdrawal syndrome ;
• cardialgia ;
• myopathies , ;
• neurogenic muscular atrophy , as well as other pathological conditions (in case anxiolytics with muscle relaxant action are contraindicated);
• neurosis-like states (emotional stress, anxiety, vegetative disorder, apathy, anxiety, decreased activity).

Grandaksin is also prescribed for ( vegetative-vascular dystonia ).

Contraindications

The drug is prohibited to take in the following cases:

• hypersensitivity to any component of the drug;
• 1st trimester of pregnancy, lactation ;
• psychomotor agitation, aggressiveness,;
• decompensated respiratory failure ;
• respiratory arrest syndrome (during sleep).

The drug contains lactose monohydrate, so it is not recommended for patients with galactose intolerance , With congenital lactase deficiency as well as patients suffering from glucose malabsorption syndrome and malactose .

The drug should be used with caution when:

• acute respiratory failure ;
• decompensated chronic respiratory distress ;
• organic brain lesions ( and etc.)

Side effects

When taking Grandaxin, you may experience such side effects how:

• ,nausea , loss of appetite ,dry mouth , in some cases - congestive jaundice ;
• , irritability, psychomotor agitation, patients with epilepsy may begin seizures , ;
• ,exanthema (including scarlet fever);
• pain and tension in the muscles;
• difficulty breathing.

Application instruction of Grandaksin (Way and dosage)

The medicine is taken orally. The dosage size is set individually depending on general condition patient, individual tolerability of the drug and clinical form diseases. Adults are usually prescribed 1-2 tablets per day (50-100 mg.) Up to 3 times a day. With irregular consumption, the dose is set in the amount of 1-2 tablets.

The maximum allowed dose per day is 300 mg.

Instructions for Grandaxin for old people (over 65) and patients with kidney failure : the daily dose of taking the medicine is reduced by 2 times.

Before taking the medicine, be sure to consult your doctor.

Overdose

In the case of taking doses of 50-150 mg / kg, effects of reducing the function of the central nervous system may occur. This dose may cause vomit , , respiratory depression , confusion , epileptic seizures .

If symptoms of an overdose occur, do not induce vomiting. It is necessary to wash the stomach, take , which will reduce the absorption of the substance, apply symptomatic treatment.

In case of respiratory depression, IVL CNS stimulants should not be administered.

In case of hypotension, intravenous administration of fluids is recommended, moving the patient to trendelenburg pose . If the above measures did not lead to the normalization of pressure, you should enter norepinephrine or .

Interaction

Simultaneous use of Grandaxin with tacrolimus , cyclosporine , sirolimus forbidden.

When taking Tofisopam with drugs that suppress the functions of the central nervous system ( sedative , hypnotic , analgesics , antipsychotic , antidepressants , facilities general anesthesia etc.) their sedative effect is enhanced.

Nicotine , alcohol , anti-elpileptic drugs , barbiturates can accelerate metabolism, which will lead to a decrease in the concentration of the drug in the blood and a decrease in its therapeutic effect.

Part antifungal drugs (such as the and) may slow the metabolism of the drug and lead to an increase in its concentration in the blood.

Antihypertensive drugs such as antagonists calcium channels and clonedin can enhance the effect active substance Grandaxin.

Terms of sale

V different countries Grandaxin is available by prescription or not. In Russia and Ukraine this drug not sold without a prescription.

Storage conditions

Store the medicine in a place that is inaccessible to children, at a temperature not exceeding 25 ° C.

Best before date

special instructions

More often than in other patients, side effects may occur in the elderly, in patients with delayed mental development , in those who suffer kidney dysfunction or liver.

Tofisopam should not be used for phobias, chronic psychosis or obsessive states as there may be a risk of increased suicide attempts and aggressive behavior.

Grandaxin does not affect the ability to concentrate and attention, so it can be used when driving and working where a fast physical and mental reaction is needed.

Grandaksin's analogs

Coincidence in the ATX code of the 4th level:

Which is better: Grandaxin or Afobazol?

Both drugs have the same indications for use, however, Afobasalo fewer contraindications and side effects. With regard to the therapeutic effect that both drugs have sedative effect and reduce anxiety in patients. Before you start taking Grandaxin or Afobazol, be sure to consult your doctor.

Alcohol and Grandaxin

Alcohol reduces the effectiveness of any drug, so Grandaxin's compatibility with alcohol is not possible. Simultaneous use increases the load on the liver, and also increases the likelihood of side effects.

Reviews about Grandaxin

Expert reviews: with proper dosage and use of the drug, it has a positive effect with minimal side effects.

Reviews of doctors on Grandaxin: this drug is often prescribed by doctors for nervous disorders, it has a sedative effect and helps relieve anxiety and tension.

Constant stress weakens nervous system person, which can cause severe mental disorders. For stabilization mental background doctors often prescribe the highly effective drug Grandaxin. Reception of the drug is associated with a number of special indications and contraindications, the lists of which are given in the instructions.

Composition and form of release

The drug Grandaxin (Grandaxini) is produced in the form of flat round tablets of white or white-gray color, with a bevel, odorless. On one side there is a risk, on the other the inscription "GRANDAX". Tablets are packaged in blisters, which are placed in cardboard packs of 2 or 6 pieces. Composition of one tablet:

Pharmacodynamics and pharmacokinetics

The drug Grandaxin is a tranquilizer that belongs to the group of atypical benzodiazepine derivatives. The drug has an anxiolytic effect (reducing anxiety), it has practically no muscle relaxant, sedative, anticonvulsant effects. Psychovegetative tranquilizer-anxiolytic eliminates various forms autonomic disorders, exhibits moderate stimulating activity.

Due to the fact that the drug does not have a muscle relaxant effect, it can be used for myopathy and myasthenia gravis. Due to the atypical chemical structure compared with classical benzodiazepines, therapeutic doses of Grandaxin do not potentiate the effect of alcohol, do not cause the development of mental and physical dependence, withdrawal syndrome. Grandaxin group - daytime tranquilizers.

After oral administration of tablets, the substance is rapidly absorbed into the blood through gastrointestinal tract, reaches a maximum concentration after two hours, after which it decreases exponentially. Tofisopam does not accumulate, its metabolites are inactive, their half-life is 6-8 hours. The remains of the drug are excreted in the urine (in the form of glucuronic conjugates) and feces.

Indications for the use of Grandaxin

The manufacturer's instructions contain a list of diseases and disease states that serve as a reason for the appointment of Grandaxin:

• neuroses of various origins (apathy, anxiety, obsessive experiences, etc.);
• reactive form depression with moderate psychopathological symptoms;
• post-traumatic stress;
• cardialgia (as part of complex treatment or in monotherapy mode);
• premenstrual emotional disorder;
• climacteric condition (as part of complex treatment or in monotherapy);
• withdrawal syndrome;
• muscle atrophy due to neurotic disorders;
• myasthenia gravis, myopathies and other painful conditions with neurotic signs, provided that the use of anxiolytic drugs with a strong muscle relaxant effect is contraindicated;
• vegetative-vascular dystonia

How to take Grandaxin

Tablets are intended for oral administration. Accurate dosage chosen individually according to general well-being patient, tolerability of the components and the clinical degree of the disease. According to instructions, adult patients are prescribed Grandaxin 1-3 times a day, 50-100 mg (1-2 tablets). Maximum allowable daily dosage- 300 mg. With occasional use of the drug, the dose will be one or two tablets. For age categories patients (over 65 years of age), as well as for those suffering from renal insufficiency, the dose is halved.

special instructions

Features of the active substance Grandaxin on the body made it necessary to note the following in the instructions special instructions:

1. Grandaxin is not recommended for monotherapy. depressive states, as the risk of aggression and suicidal mood increases.
2. With a slowdown in mental development or impaired kidney and liver function, the likelihood of side effects increases.
3. Under regular medical supervision, it is necessary to take medicine for patients with depersonalization and organic brain damage (for example, atherosclerosis).
4. If you are lactose or galactose intolerant, you should know that the preparation contains 92 mg of lactose monohydrate. The drug is not prescribed for deficiency of the lactase enzyme.
5. Tofisopam ( active substance) may increase the seizure threshold.
6. The drug does not affect concentration.

drug interaction

The sedative Grandaxin has a number of restrictions on drug interaction. The instructions for use indicate possible combinations:

1. The simultaneous use of the drug with Tacrolimus, Cyclosporine, Sirolimus, Clonidine is contraindicated.
2. Tofisopam increases the plasma concentration of drugs that are metabolized by the same isoenzyme as it.
3. Grandaxin enhances the effects of drugs that suppress the functions of the central nervous system. These include general anesthesia, blockers histamine receptors, analgesics, antipsychotics, antidepressants, sleeping pills, dopamines. The combination of such medicines can lead to respiratory depression, sedation.
4. Ethanol, liver enzyme inducers, antiepileptic drugs, barbiturates, nicotine increase the metabolism of tofisopam, which reduces its concentration in the blood and weakens the effect.
5. Antifungal agents Ketoconazole, Itraconazole slow down the hepatic metabolism of Grandaxin, which increases its plasma concentration.
6. Antihypertensive drugs, calcium channel blockers increase the effectiveness of the drug.
7. Beta-blockers slow down the metabolism of the active substance.
8. Tofisopam increases the level of Digoxin in the blood, negatively affects the anticoagulant effect of warfarin.
9. Long-term use of disulfiram inhibits the metabolism of the active ingredient.
10. Antacids adversely affect the rate of absorption of the drug.

grandaxin and alcohol

Tofisopam reduces the negative effect of ethanol on the nervous system, and alcoholic beverages increase the metabolism of the drug. This leads to a decrease in the effectiveness of the tool. Because of this during drug therapy, it is forbidden to take alcohol and alcohol-containing drinks or medicines. Side effects of this combination will increase the load on the liver, high risk poisoning.

Side effects of Grandaxin

During therapy with Grandaxin, manifestations are possible adverse reactions. Instructions for use highlight the following:

• seizures, headache, confusion, insomnia;
• congestive jaundice, decreased appetite, dry mouth, constipation, nausea, flatulence;
• allergy, scarlet fever exanthema, pruritus;
• muscle pain, tension;
• psychosis, irritability, phobias;
• respiratory depression.

Overdose

If you take Grandaxin tablets at a dose higher than the instructions indicate (over 50-120 mg per kg of body weight), then suppression of the functions of the central nervous system is possible. This is manifested by vomiting, coma, confusion, epileptic seizures, respiratory depression. With severe symptoms, it is recommended to wash the stomach, do not induce vomiting. Reception shown activated carbon to prevent drug absorption. Physicians should monitor the patient's basic physiological parameters.

With respiratory depression, artificial ventilation of the lungs is indicated, the introduction of stimulants of the central nervous system is not recommended. Hypotension is eliminated intravenous administration solutions, transferring the patient to a prone position, legs above the head. In the absence of recovery efficiency normal pressure using the usual methods, it is possible to administer norepinephrine, dopamine, norepinephrine. Forced diuresis and dialysis are ineffective. Emergencies require the use of a specific benzodiazepine antagonist, flumazenil.

Contraindications

With caution, the drug should be used in persons with angle-closure glaucoma, respiratory failure (acute), epilepsy, respiratory distress (chronic, decompensated). Clinical researches and pharmacokinetic features led to the introduction of a number of direct contraindications into the instructions:

• stage of decompensation in respiratory failure;
• conditions associated with aggression severe depression or noticeable psychomotor agitation;
• diagnosed withdrawal syndrome respiratory function in a dream;
• first trimester of pregnancy and period breastfeeding;
• galactose intolerance, lactase deficiency (congenital), galactose and glucose malabsorption syndrome;
• hypersensitivity to the constituent components.

Terms of sale and storage

The drug Grandaxin is a prescription drug. It is stored at a temperature of 15-25 degrees for five years.

Grandaksin's analogs

The drug can be replaced with agents from the benzodiazepine group - they have the same effect and have a similar or slightly different composition. Analogues of the drug include:

• Afobazole - tablets with anxiolytic action based on afobazole (morphodihydrochloride);
• Gidazepam is an anticonvulsant tablet medicine containing the same name component gidazepam;
• Diazepam - tranquilizing pills and ampoules with a solution based on diazepam;
• Neurol is an analogue of Grandaxin in the form of tablets with a muscle relaxant effect based on alprazolam;
• Relanium - anti-anxiety solution for parenteral administration containing diazepam as active component;
• Tazepam - sedative tablets based on oxazepam;
• Phenazepam - anxiolytic tablets and injection containingzepine.

Grandaxin price

Tranquilizer Grandaxin is sold in pharmacies at prices that depend on the number of tablets in the package, the price policy of sellers. In Moscow, the approximate cost of the drug will be:

Pharmacy name	Type of drug release	Price, rubles
	Tablets 50 mg 20 pcs.
	Tablets 50 mg 60 pcs.
ZdravZone	50 mg 20 tablets
	50 mg 60 tablets
Pharmacy IFK	60 tablets of 50 mg
	20 tablets of 50 mg
pills.ru	Tablets 50 mg 20 pcs.
	Tablets 50 mg 60 pcs.

According to its pharmacological properties, it belongs to tranquilizers (anxiolytic drugs). Produced in tablet form. INN: Tofisopam.

1 tablet contains 50 mg of tofisopam, excipients are stearic acid, magnesium stearate, gelatin, talc, complex carbohydrates(lactose monohydrate, potato starch, microcrystalline cellulose).

Externally, Grandaxin is a round, flat, disc-shaped tablet. white color, sometimes with a grayish tint, there is a chamfer, with a risk on one side of the tablet and the inscription "GRANDAX" on the other side, almost odorless.

Release form - tablets of 50 mg. 2 or 6 blisters of 10 tablets, together with the instructions, are placed in a separate carton.

Pharmacodynamically, tofisopam is a representative of a group of atypical benzodiazepine derivatives, capable of exerting an anxiolytic effect, practically not accompanied by sedative, muscle relaxant effects. Gradaxin acts as a psycho-vegetative corrector-regulator, eliminates different kinds autonomic disorders, also has a moderate stimulating activity.

Due to the absence of a muscle relaxant effect, the agent can also be used in patients with myopathy and myasthenia gravis. Unlike classical benzodiazepine drugs, tofisopam, being its atypical derivative, at therapeutic doses weakens the effects of alcohol and practically does not cause withdrawal symptoms, as well as physical and mental dependence. Grandaxin is a daytime tranquilizer.

Pharmacokinetically, after oral administration, tofisopam is rapidly and almost completely absorbed from digestive tract, while reaching a maximum concentration in the blood within 2 hours, after which the concentration in plasma decreases rapidly. Tofisopam does not accumulate in the body.

Metabolites of the drug are not pharmacologically active. Tofisopam is excreted mainly in the urine (up to 80 percent) in the form of compounds with glucuronic acid, to a lesser extent (about a third), through bile with feces. The half-life is about 7 hours.

Indications

Grandaxin is used in the presence of neuroses and neurosis-like conditions (conditions that are accompanied by emotional stress, obsessive experiences, moderate anxiety, autonomic disorders, as well as apathy and decreased activity).

The indication for use is the presence of reactive depression with moderate psychopathological symptoms; mental adjustment disorder (post-traumatic stress).

climacteric syndrome (as individual treatment, and in combination with hormone replacement therapy), premenstrual syndrome.

Grandaxin is used in the treatment of cardialgia (as a monotherapy, also in combination with other drugs).

The drug Grandaxin can be prescribed for alcohol withdrawal.

Overdose

Signs of overdose are CNS suppression effects, which can usually only occur after doses of 50-120 mg/kg body weight. High doses may cause vomiting, confusion, respiratory depression and/or seizures, and coma.

Treatment. When suppressing the functions of the central nervous system, one should not achieve a gag reflex (to avoid asphyxia with vomit).

It is necessary to wash the stomach, take activated charcoal, which will help reduce the absorption of the drug. Along with this, it is necessary to constantly monitor the main physiological parameters of the body and conduct symptomatic therapy. In case of respiratory depression, it is permissible to carry out artificial ventilation lungs.

The introduction of CNS stimulant drugs is not indicated. Hypotension should be corrected by intravenous administration of colloid and crystalloid solutions, as well as by transferring the patient to the Trendelenburg position. With the ineffectiveness of these measures, the introduction of norepinephrine or dopamine is indicated. Dialysis and increased diuresis in this case are not effective.

As an antagonist, the administration of flumazenil is acceptable, at the same time, its use in case of an overdose of Grandaxin has not been clinically tested.

special instructions

When using Grandaxin, it is important to remember that in patients with current and history of mental retardation, in the elderly and patients, as well as those with a history of impaired renal and hepatic function, the likelihood of negative effects is higher than in others. sick.

It is not recommended to take Grandaxin in chronic psychosis, various phobias, obsessive-compulsive disorders, due to an increased risk of suicidal attempts and aggressive behavior. Based on this, tofisopam is not indicated as a monotherapy for depression or depression in combination with anxiety.

When Grandaxin is used in patients with epilepsy, there is a possibility of an increase in the threshold for convulsive readiness.

Each tablet of Grandaxin contains about 90 mg of lactose, which should be taken into account for people with lactose intolerance.

The use of the drug does not significantly reduce attention and the ability to concentrate.

Plasma concentrations of drugs metabolized by cytochrome CYP3A4 may increase when taken concomitantly with Grandaxin. The use of tofisopam with drugs that can suppress the functions of the central nervous system (antidepressants, antihistamines, analgesics and anesthetics central action, hypnotics, antipsychotics) enhances their therapeutic or side effects (in particular, respiratory depression and sedation).

Hepatic enzyme inducers (antiepileptic drugs, for example, barbiturates, alcohol, nicotine) can increase the metabolism of tofisopam, while leading to a decrease in its plasma concentration and a weakening of the therapeutic effect.

Row antifungal agents(ketoconazole, itraconazole) can slow down the metabolism of Grandaxin in the liver, which, in turn, can lead to an increase in its plasma concentration.

Part antihypertensive drugs(calcium channel antagonists and clonidine) can stimulate the action of tofisopam. Beta-blockers may slightly slow down the metabolism of tofisopam without significant clinical effect.

Taking tofisopam and digoxin at the same time can lead to an increase in the level of the latter in the blood plasma.

Benzodiazepines may interfere with the anticoagulant effect of warfarin.

Antacids in some cases affect the level of absorption of tofisopam. Cimetidine and omeprazole slow down the metabolism of tofisopam. Oral contraceptives, along with long-term use disulfiram, can also reduce the intensity of Grandaxin's metabolism.

Video from the author

Storage conditions

Grandaxin is stored at room temperature, access to the storage place should be limited to children. Shelf life 5 years.

Analogues

Grandaxin is original drug firm Egis. Analogues of the drug for this moment no.

Price

Grandaxin is released in the pharmacy chain by prescription. Average prices are:

• Packing 20 tablets 290-465 rubles.
• Packing 60 tablets 740-1050 rubles.

You can not self-medicate, it can pose a threat to health and life. Before using Grandaxin, consult a specialist!

Name:

Grandaxin (Grandaxinum)

Pharmacological
action:

Pharmacodynamics

A drug from the group of benzodiazepine derivatives ( atypical benzodiazepine derivative), renders anxiolytic effect, practically not accompanied by a sedative, muscle relaxant, anticonvulsant action. It is a psycho-vegetative regulator, eliminates various forms vegetative disorders. It has a moderate stimulating activity.

Due to the lack of a muscle relaxant effect, the drug can also be used in patients with myopathy and myasthenia gravis. Due to the atypical chemical structure, unlike the classic benzodiazepine derivatives, Grandaxin® in therapeutic doses practically does not cause the development of physical, mental dependence and withdrawal syndrome.

Grandaxin® refers to daytime anxiolytics.

Pharmacokinetics

When taken orally, it is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax in the blood is reached within 2 hours, after which the plasma concentration decreases monoexponentially. Tofisopam does not accumulate in the body. Its metabolites do not have pharmacological activity. It is excreted mainly in the urine (60-80%) in the form of conjugates with glucuronic acid and to a lesser extent (about 30%) in the feces. T1 / 2 is 6-8 hours.

Indications for
application:

- neurosis and neurosis-like states(conditions accompanied by emotional stress, autonomic disorders, moderate anxiety, apathy, decreased activity, obsessive feelings);
- reactive depression with moderately severe psychopathological symptoms;
-mental adjustment disorder(post-traumatic stress disorder);
- climacteric syndrome(how independent remedy, as well as in combination with hormonal drugs);
- premenstrual syndrome;
- cardialgia(in the form of monotherapy or in combination with other drugs);
- alcohol withdrawal syndrome;
- myasthenia gravis, myopathies, neurogenic muscular atrophy and other pathological conditions with secondary neurotic symptoms when anxiolytics with a pronounced muscle relaxant effect are contraindicated.

Mode of application:

Set individually, taking into account the patient's condition, the clinical form of the disease and individual sensitivity to the drug.
Adults appoint 50-100 mg (1-2 tab.) 1-3 times / day. The maximum daily dose is 300 mg.
Children over 14 years old prescribe up to 200 mg / day.
To prevent sleep disorders, the drug is recommended to be taken no later than 15-16 hours of the day.
Elderly patients and patients with renal insufficiency daily dose reduced by about 2 times.
With alcohol withdrawal syndrome, for the prevention and treatment of delirium, a short course of therapy is indicated: from several days to 3-6 weeks.

Side effects:

From the gastrointestinal tract: decreased appetite, constipation, increased flatus, nausea, dry mouth. In some cases, congestive jaundice is possible.

From the CNS: headache, insomnia, irritability, psychomotor agitation, confusion may occur, seizures may occur in patients with epilepsy.

allergic reactions: exanthema, scarlatiniform exanthema, itching.

From the side of the musculoskeletal system: muscle tension, muscle pain.

From the side respiratory system : respiratory depression.

Contraindications:

- hypersensitivity to the active or any other component drug or any other benzodiazepine;
- conditions accompanied by severe psychomotor agitation, aggressiveness or severe depression;
- decompensated respiratory failure;
- I trimester of pregnancy;
- the period of breastfeeding;
- sleep apnea syndrome (in history);
- simultaneous use with tacrolimus, sirolimus, cyclosporine;
- intolerance to galactose, congenital deficiency lactase or glucose and galactose malabsorption syndrome (the drug contains lactose monohydrate).

Carefully: decompensated chronic respiratory distress, history of acute respiratory failure, angle-closure glaucoma, epilepsy, organic brain lesions (eg atherosclerosis).

Interaction
other medicinal
by other means:

Simultaneous application tacrolimus, sirolimus, cyclosporine and tofisopam is contraindicated. Plasma concentrations of drugs that are metabolized by CYP3A4 may increase when taken concomitantly with tofisopam.

Application tofisopam with drugs that suppress the functions of the central nervous system(analgesics, general anesthetics, antidepressants, H1-antihistamines, sedatives, hypnotics, antipsychotics), enhances their effects (for example, sedation or respiratory depression).

Liver enzyme inducers(alcohol, nicotine, barbiturates, antiepileptic drugs) can increase the metabolism of tofisopam, which can lead to a decrease in its concentration in blood plasma and a weakening of the therapeutic effect.

Some antifungal drugs (ketoconazole, itraconazole) can slow down the hepatic metabolism of tofisopam, which leads to an increase in its concentration in blood plasma.

Some antihypertensive drugs(clonidine, calcium channel antagonists) may enhance the effects of tofisopam. Beta-blockers can slow down the metabolism of the drug, but this effect has no clinical significance.

Tofisopam may increase plasma digoxin levels blood.

Benzodiazepines may affect anticoagulant effect warfarin.

Long-term use disulfiram may inhibit the metabolism of tofisopam.

Antacids may interfere with the absorption of tofisopam. Cimetidine and omeprazole inhibit the metabolism of tofisopam.

Oral contraceptives means can reduce the intensity of metabolism of tofisopam.

Tofisopam weakens the inhibitory effect of alcohol on the central nervous system.

Pregnancy:

Contraindicated in the first trimester of pregnancy. At the time of treatment should stop breastfeeding.

Overdose:

Symptoms: effects of suppression of the CNS function appear only after taking high doses (50-120 mg / kg). Such doses may cause vomiting, confusion, coma, respiratory depression and/or epileptic seizures.

Treatment: in case of severe suppression of the central nervous system, it is not recommended to induce vomiting. Rinse the stomach. The appointment of activated charcoal helps to reduce the absorption of the drug. It is necessary to constantly monitor the main physiological parameters and apply appropriate symptomatic therapy. With respiratory depression, you can carry out IVL. The introduction of CNS stimulants is not recommended. Hypotension is best treated with IV fluids and placing the patient in the Trendelenburg position. If these measures do not restore normal blood pressure, dopamine or noradrenaline can be administered. Dialysis and induced diuresis are ineffective.

As an antagonist Flumazenil can be administered, but its use in tofisopam overdose has not been clinically tested.

Release form:

- Tablets of 0.01 g in a package of 50 pieces;
- Granules for suspension preparation;
- Mezapam granules for children white with a yellowish tint;

Produced in orange glass jars with a capacity of 150 ml with a label indicating 100 ml. Each jar contains 20 g of granules containing 0.04 g (40 mg) of mezapam.

Storage conditions:

The drug should be stored at a temperature of 15° to 25°C.

Best before date- 5 years.
Conditions for dispensing from pharmacies - dispensed on prescription.

Tablets round shape, white or greyish-white, with two flat sides, one with a notch, the other engraved with "GRANDAX", odorless or almost odorless.

1 tablet contains:
active substance: tofisopam 50 mg
Excipients: stearic acid - 1 mg; magnesium stearate - 1 mg; gelatin - 3.5 mg; talc - 2 mg; potato starch - 20.5 mg; lactose monohydrate - 92 mg; MCC - 10 mg

Grandaxin is a tranquilizer that reduces the level of anxiety.

The active substance is a benzodiazepine derivative. It differs in its characteristics from its other derivatives (atypical benzodiazepine).

Unlike many other drugs in this group, the instruction positions Grandaxin as a strong anti-anxiety agent and a light stimulant that has a barely noticeable sedative effect. The difference lies in the fact that when it is taken, there is practically no anticonvulsant and muscle relaxant activity of the active substance.

On this page you will find all the information about Grandaxin: complete instructions on application to this drug, average prices in pharmacies, complete and incomplete analogues of the drug, as well as reviews of people who have already used Grandaxin. Want to leave your opinion? Please write in the comments.

Clinical and pharmacological group

Tranquilizer (anxiolytic).

Terms of dispensing from pharmacies

Released by prescription.

Prices

How much does Grandaxin cost? average price in pharmacies is at the level of 450 rubles.

Release form and composition

Release form - tablets of 50 mg. 2 or 6 blisters of 10 tablets, together with the instructions, are placed in a separate carton.

• 1 tablet contains 50 mg of tofisopam, excipients are stearic acid, magnesium stearate, gelatin, talc, complex carbohydrates (lactose monohydrate, potato starch, microcrystalline cellulose).

Outwardly, Grandaxin is a round, flat disc-shaped tablet of white color, sometimes with a grayish tinge, there is a chamfer, with a risk on one side of the tablet and the inscription "GRANDAX" on the other side, it has almost no smell.

Pharmacological effect

Grandaxin is a benzodiazepine tranquilizer. The main action is anxiolytic (calming). Unlike other benzodiazepine tranquilizers, it does not have sedative, hypnotic, muscle relaxant, anticonvulsant effects.

The drug regulates psycho-vegetative, relieves various autonomic disorders. It has a moderate stimulating effect. Specified pharmacological properties determine the belonging of the drug to daytime anxiolytics. Due to the lack of a muscle-relaxing effect, the drug can be taken by patients with myasthenia gravis and myopathy.

Atypical chemical formula Tofizopam, which is very different from the structure of classical benzodiazepine anxiolytics, provides the drug with a number of advantages:

• in a therapeutic dose does not enhance the effect of ethanol;
• does not give rise to a withdrawal syndrome;
• does not cause mental or physiological addiction.

The mechanism of action is associated with a stimulating effect on benzodiazepine receptors in the brain. Their excitation leads to an increase in the sensitivity of GABA receptors to the neurotransmitter. As a result, chloride channels begin to work more efficiently, membrane hyperpolarization increases. nerve cells weakened neural activity.

Indications for use

What helps? Grandaxin is used to treat:

1. premenstrual syndrome;
2. Alcohol withdrawal syndrome;
3. Cardialgia (both as a monotherapeutic agent and in combination with other drugs);
4. Reactive (psychogenic) depression with moderately severe psychopathological symptoms;
5. Serious mental post-traumatic disorders associated with a single psychotraumatic situation or systematically recurring episodes;
6. Neuroses and pseudo-neurotic conditions (neuropsychiatric disorders characterized by emotional stress, a moderate increase in anxiety, apathy, decreased activity, the appearance of obsessive experiences, vegetative disorders);
7. neurogenic muscular atrophy, myopathy, myasthenia gravis and others pathological conditions, which are accompanied by secondary neurotic symptoms and in which the use of anxiolytics (tranquilizers), which have a pronounced muscle relaxant effect, is contraindicated;
8. Pathological (in the annotation it is indicated that with climacteric syndrome the drug can be prescribed both as an independent agent and as an addition to hormone therapy).

Contraindications

Contraindications to taking the medication are:

1. Decompensated respiratory failure.
2. The period of pregnancy (in particular, the first trimester) and breastfeeding (lactation).
3. Hypersensitivity to the active substance or other auxiliary components drug.
4. Conditions accompanied by aggressiveness, irritability, pronounced psychomotor agitation or depression.
5. Co-administration with cyclosporine, sirolimus, tacrolimus.
6. Congenital lack of lactase, galactose intolerance or malabsorption syndrome of galactose and glucose (Grandaxin contains lactose monohydrate).
7. Syndrome of respiratory arrest during sleep (available in the patient's history).

Grandaxin is prescribed with extreme caution for: acute respiratory failure in the patient's history, epilepsy, angle-closure glaucoma, decompensated chronic respiratory distress, organic brain damage (for example, with atherosclerosis).

Use during pregnancy and lactation

Grandaxin is contraindicated for use in the first trimester of pregnancy and during lactation (breastfeeding).

Instructions for use

The instructions for use indicate that the dosage of Grandaxin is set individually, taking into account the patient's condition, the clinical form of the disease and individual sensitivity to the drug.

1. Usually, adults are prescribed 50-100 mg (1-2 tablets) 1-3 times / day.
2. At irregular use you can take 1-2 tab.
3. The maximum daily dose is 300 mg.

For elderly patients and patients with renal insufficiency, the daily dose is reduced by about 2 times.

Side effects

The use of Grandaxin can cause the following side effects from the central nervous system:

• Psychomotor agitation;
• Seizures (in patients with epilepsy);
• Headache;
• confusion;
• Insomnia;
• Increased irritability.

Grandaxin may cause the following gastrointestinal side effects:

• dry mouth;
• Flatulence;
• Cholestatic jaundice (in some cases);
• Decreased appetite;
• Nausea;
• constipated

On the part of the respiratory system, the use of Grandaxin can lead to respiratory depression, musculoskeletal system- to muscle pain and muscle tension.

Against the background of the use of the drug, in some cases, there are allergic reactions in the form of exanthema (including scarlatiniform exanthema) and pruritus.

Overdose

When Grandaxin is taken orally in high doses (50–120 mg/kg of body weight), symptoms of depression of the central nervous system functions may be observed: clouded consciousness, vomiting, depression respiratory center and / or epileptic seizures, coma.

With severe suppression of the functions of the central nervous system, vomiting should not be induced. Gastric lavage is recommended. The appointment of activated charcoal reduces the absorption of the drug. It is necessary to constantly monitor the main physiological parameters and conduct appropriate symptomatic therapy. Respiratory depression is an indication for mechanical ventilation. The introduction of CNS stimulants is not recommended.

Hypotension is preferably treated with intravenous fluids and placing the patient in the Trendelenburg position. If these measures do not lead to normalization blood pressure, the introduction of norepinephrine (norepinephrine) or dopamine is allowed. The effectiveness of dialysis and forced diuresis has not been proven. Flumazenil, a specific benzodiazepine antagonist, can be used in emergency cases, but its use in tofisopam overdose has not been sufficiently studied.

special instructions

1. Avoid alcoholic beverages during treatment with this drug.
2. Each Grandaxin tablet contains 92 mg of lactose, which should be taken into account in patients with lactose intolerance.
3. In patients with epilepsy, tofisopam may increase the seizure threshold.
4. It should be borne in mind that in patients with mental retardation, elderly patients, in patients with impaired renal and / or liver function, side effects may occur more often than in other patients.
5. Caution is needed when treating patients with depersonalization, as well as those with organic lesion brain (for example, with atherosclerosis).
6. It is not recommended to use tofisopam in chronic psychosis, phobias or obsessive-compulsive disorders. In these cases, the risk of suicidal attempts and aggressive behavior increases. Therefore, Grandaxin is not recommended as a monotherapy for depression or depression accompanied by anxiety.

Grandaxin does not significantly reduce attention and ability to concentrate.

drug interaction

Interaction medicines can occur both with drugs taken earlier, and with those that are planned to be taken in the future. Please tell your doctor or pharmacist if you are currently taking or have recently taken any medicines even non-prescription ones. If you need to start taking any other drug (especially if it affects the central nervous system) during treatment with Grandaxin or within one month after completion of treatment, please inform your doctor about the treatment with Grandaxin.

Caution (medical supervision) is necessary if Grandaxin tablets are taken simultaneously with the following drugs:

• if you are taking drugs that act on the central nervous system (for example, sedatives, drugs for the treatment of depression, epilepsy, allergies, psychotic conditions, general anesthetics, sleeping pills), immunosuppressive drugs, anticoagulants, antifungal drugs, antiarrhythmic drugs, cardiac glycosides ( such as digoxin), antihypertensive drugs, antacids and oral contraceptives, be sure to tell your doctor. Also report if you regularly drink alcoholic beverages.

In these cases, direct medical supervision or dose adjustment of concomitant medications may be necessary.