Grandaxinum is a medication tranquilizing drug that reduces anxiety, suppresses fears and emotional and mental stress. Included in the group of anxiolytic drugs, or ataraxics (anti-anxiety drugs), II generation and refers to medications of the benzodiazepine series, which today occupy a leading position in terms of breadth of use among tranquilizers.

Release form, composition and packaging

"Grandaxin" is produced by the company "EGIS" (Hungary). Pharmacies receive paper packs containing 2 or 6 cell plastic-aluminum blisters with 10 packs of tablets - white cylindrical with a central dividing line and the word GRANDAX extruded on opposite sides.

The therapeutic basis of the medication is tofisopam, which in an amount of 50 mg is in 1 tablet. In tablets, formative inactive constituents are also present.

Pharmacological action, pharmacodynamics and pharmacokinetics

The drug is considered as a daytime tranquilizer, that is, it can be used in the daytime, since it does not cause a drowsiness.

Anxiolytic "Grandaxin" moderately affects the nervous system, which is expressed by:

  • in tranquilizing (calming) effect;
  • in easing mental stress;
  • in suppressing anxiety and anxiety (anxiolytic);
  • in reducing the severity of fears (antifobic), the frequency and severity of panic attacks;
  • in moderate stimulating effect (eliminates abnormal weakness, depression).

Also, the drug has a stress-protective effect (protects nerve cells from the damaging effects of stress).

In addition to these effects, “Grandaxin” is active and eliminates various forms of disorders in the psycho-vegetative area, regulating the flow of physiological processes, the work of muscles, glands, blood and lymph vessels.

Clinically, this effect of the drug is expressed in the fact that the medication reduces the physiological manifestations of fear and anxiety, including the state in panic attacks:

  • eliminates jumps in blood pressure;
  • relieves the feeling of suffocation and the "onset of death";
  • expanding the coronary vessels, normalizes the frequency of contractions of the heart (tachycardia) and the phenomenon of arrhythmia (uneven contractions), relieves neurotic pain in the heart;
  • stabilizes the disturbed functions of the stomach and intestines - relieves nausea, vomiting, stomach, esophageal and intestinal cramps, psychogenic diarrhea with frequent urges;
  • reduces sweating, tremors (trembling fingers), spastic convulsive muscle contractions, weakness in the legs, a feeling of exhaustion.

The advantage of “Grandaxin” over other psychotropic medicines of a number of benzodiazepines:

  • anxiolytic does not cause daytime inhibition and drowsiness, but on the contrary, acts as a moderate stimulant of nerve functions, therefore, the medicine is prescribed for daily intake;
  • the tranquilizer does not relieve convulsive attacks, does not have a relaxing effect on the muscles, so it can be used for atrophic processes in muscle fibers;
  • rarely shows a weakening of the therapeutic effect with long-term use (if used in the recommended dosages), does not lead to dependence, does not cause antipsychotic manifestations in a patient who stops treatment.

A feature of this anxiolytic is the active and complete absorption of the active component into the blood through the mucous membranes of the stomach and intestines, which ensures the rapid manifestation of healing properties. About 2 hours after the tablet enters the stomach, the highest amount of tofisopam is observed in plasma.

In the body, the therapeutic substance does not accumulate and after 7 - 9 hours it is removed by 68 - 75% in the urine and partially through the intestines. Intermediate substances (metabolites) formed during the treatment of tofisopam in the liver do not have pharmaceutical properties. Therefore, even with long-term therapy, addiction to the medication develops rather slowly, and overdose, subject to the frequency of administration and doses, is practically eliminated.

Why is Grandaxin prescribed?

A medication is required for the development of the following conditions:

  • moderate severity of anxiety neurological disorders;
  • neurotic disorders in seriously ill people;
  • vegetative vascular and other disorders against the background of a panic attack, emotional overload, stress;
  • weakening of myocardial function, neurogenic pain behind the sternum, arrhythmias;
  • manifestations of premenstrual and menopausal syndrome;
  • post-traumatic disorder after emotional shocks and injuries;
  • hidden current moderate depression;
  • atrophic processes in muscles of a neurogenic nature and other pathologies accompanied by neurological manifestations in which muscle relaxants tranquilizers are contraindicated (with muscle-relaxing effect).

A tranquilizer allows you to quickly eliminate the symptoms associated with these pathologies:

  • internal nervous tension;
  • inadequate constant anxiety without meaningful reasons;
  • apathy, decreased activity, depression;
  • physiological manifestations of panic disorders (tremors, panic, fear of death, pressure surges, muscle cramps, head and heart pains, neurotic diarrhea, sweating).

In addition, "Grandaxinum" is prescribed as one of the medications in the treatment of alcohol and drug withdrawal.

In a short time, tofisopam successfully removes or alleviates manifestations such as:

  • agitation, nervous tension, irritability, aggressiveness;
  • lack of coordination;
  • chills, tremors, nausea;
  • Depression accompanying addiction treatment
  • risk of developing hallucinations and delirium.

Instructions for use and dosage

The dose and regimen are developed for a separate medical history.

A neurologist, psychotherapist or psychiatrist takes into account the nature of the disease, age, severity of symptoms, and necessarily - concomitant diseases, among which there may be those in which the medication is contraindicated.

Since the drug stimulates the nervous system a little, for normal falling asleep, the last dose of the drug is best taken no later than 15 hours before the expected bedtime.

The recommended adult dose for 1 dose is from 50 to 100 mg, which is determined by the severity of the condition. The standard reception mode is up to 3 times in 24 hours. The largest amount of tofisopam that an adult patient can receive is 300 mg.

A single dose of the drug is allowed for rarely manifested neurological disorders. In conditions of irregular intake, you can once drink 1 - 2 tablets of the medication.

How to take a tranquilizer for minors?

In pediatrics, anxiolytic is prescribed from the age of 14 years. And only in exceptional cases - to younger patients (only with the permission of a specialist).

The application for adolescents from 14 years of age involves taking 25-100 mg (from half a tablet to 2) 1 to 2 times in 24 hours. A child can receive no more than 200 mg of tofisopam per day.

The duration of therapy is also individual. Standard - from 2 weeks to 2 to 3 months. In case of alcohol and drug withdrawal, as well as for the prevention of delirium, the drug is prescribed in a course of 3 to 7 days to 4 to 6 weeks.

Application Features:

  1. For age-related patients from 70 years old, people with renal failure or developmental delay, the daily dose of Grandaxinum is reduced by 1.5 - 2 times, since this category of patients is more likely to have adverse reactions. In elderly people, tofisopam negatively affects memory function and motor coordination.
  2. Patients with chronic psychosis, severe depression and phobias (fears), depersonalization (self-consciousness disorder) or acute obsessive states are not recommended to appoint tofizopam to avoid the risk of aggression and suicidal attacks. In this case, “Grandaxin” is combined with other psychotropic drugs and antidepressants.
  3. With epilepsy, tofisopam can lead to more frequent seizures.

With special care, a tranquilizer is prescribed:

  • patients with decompensated respiratory distress (inflammatory, life-threatening lung damage);
  • patients with a previous episode of acute respiratory failure;
  • people with angle-closure glaucoma.

Grandaxin practically does not reduce the level of attention and the speed of mental and physical reactions when the patient controls vehicles and sophisticated equipment.

During pregnancy and breastfeeding

Grandaxin tablets are not prescribed:

  1. In the first 13 to 14 weeks of gestation. Further, only in rare cases, if the degree of the likely therapeutic effect in a pregnant patient is much higher, compared with the risk of negative effects of tofisopam on the fetus.
  2. To nursing mothers. Tofisopam passes into breast milk, and its effect on the baby’s body can cause unpredictable and serious complications. If the mother needs therapy, then at the time of treatment it is necessary to transfer the child to artificial feeding.

Drug interaction

With the simultaneous use of "Grandaxin" with other drugs, their pharmaceutical interaction should be considered.

The parallel reception of "Grandaxinum" is forbidden:

  • with immunosuppressants - tacrolimus ("Prograf"), sirolimus ("Rapamun"), cyclosporine ("Sandimmun-Neoral");
  • H1-antihistamines (diphenhydramine, diphenhydramine, doxylomine, promethazine);
  • with medicines that depress the central nervous system;
  • phenobarbital, antipsychotics (e.g. chlorpromazine, haloperidol, levomepromazine, clozapine);
  • sleeping pills ("Imovan");
  • clonidine;
  • tranquilizers (diazepam, nitrazepam);
  • anesthetics (sodium oxyburate, pentotal for anesthesia);
  • antidepressants, anticholinergics (trihexyphenidyl, atropine);
  • opiates (morphine, methylfentanyl, methadone).

With the combined use of a medication with these drugs, there is a high probability of a mutual strengthening of their action, leading to inhibition of the functions of the nervous system and respiratory center.

"Grandaxin" increases the concentration in the blood:

  • Digoxin;
  • drugs that are processed in the liver by the enzyme CYP3A4.

"Grandaxin" changes the anticoagulant effect of "Heparin", "Warfarin".

The therapeutic effect of "Grandaxin" weaken:

  • barbiturates, alcohol, nicotine and anti-epilepsy medicines, since they accelerate the metabolism (treatment with hepatic enzymes) of tofisopam, thus reducing its plasma content;
  • antacids ("Maalox", "Rennie", "Fosfalugel"), slowing down the absorption of tofisopam.

Increase the content of tofisopam in the blood, slowing down its processing in the liver:

  • antifungal drugs based on ketoconazole, itraconazole;
  • long-term use of "Disulfiram";
  • birth control pills, proton pump inhibitors Omez, Creon, Omeprazole, H2-histamine receptor blockers (Ranitidine, Cimetidine).

The therapeutic effect of “Grandaxin” is enhanced by some drugs that lower blood pressure, namely “Clonidine” and calcium channel blockers.

Metoclopramide accelerates the action of tofisopam, increasing its absorption.

Grandaxin's compatibility with alcohol

"Grandaxin" and alcohol are incompatible, although "Grandaxin" is used to eliminate withdrawal symptoms in alcohol dependence. But it is forbidden to use a tranquilizer if the patient is not able to refuse drinks with ethanol during treatment.

With the combined use of tofisopam and ethanol, the risk is high:

  • severe poisoning of the liver tissue;
  • amplification of all side effects of the drug and alcohol on the nervous system, leading to loss of consciousness, a drop in blood pressure, respiratory depression and a coma.

Contraindications, side effects and overdose

The medication is contraindicated in the following cases:

  • special sensitivity to the components of the medication or other benzodiazepines;
  • acute psychosis, neurotic states with severe aggression, overexcitation, severe depression;
  • severe respiratory failure, difficult to treat;
  • previous respiratory arrest during sleep;
  • first 13 weeks of gestation;
  • breastfeeding;
  • age up to 14 years;
  • intolerance or malabsorption (malabsorption) of galactose and glucose, congenital lactase deficiency.

Patients who do not tolerate lactose should be warned about the presence of 92 mg of lactose in each tablet of the drug.

Side effects of anxiolytics are often expressed in such manifestations as:

  • dry mouth
  • loss of appetite, constipation, gas, nausea;
  • yellowing of the skin and eye proteins;
  • headache, poor night sleep, irritability, overexcitation (usually if the medicine is taken after three to four hours of the day);
  • rash of a different nature, red spots, itching of the skin (more often in patients with allergies);
  • muscle tension and soreness;
  • confusion of consciousness;
  • seizures in patients with epilepsy;
  • respiratory depression.

In some cases, adverse reactions can be reduced by lowering the dose of Grandaxinum.If allergic manifestations, shortness of breath and severe sleep disturbances are not eliminated, then taking the medicine should be stopped.

An overdose often develops with long-term use of the maximum doses of tofisopam or a single use of a large amount of medication. There are signs of depression of the central nervous system: drowsiness, shortness of breath, confusion, cramps, in severe cases - a sharp drop in blood pressure and coma.

In case of mild manifestations of an overdose, one should rinse the stomach and give the patient adsorbents - Polysorb or activated charcoal, which will absorb the excess medicine. In the event of a drop in pressure, the patient is raised his legs at an angle of 45 degrees, slightly lowering the head end of the bed.

In the hospital, detoxification therapy, restoration of respiratory function, cardiac and vascular system function, norepinephrine and dopamine infusion are performed to normalize the pressure. In critical cases, the hospital uses the introduction of "Flumazenil" (a benzodiazepine antagonist) into the blood.

Analogues of the drug

A synonym for the drug according to the therapeutic substance is “Tofizopam”.

Grandaxin's analogs in therapeutic effect: Diazepam, Phenazepam, Relium, Tazepam, Relanium, Afobazol.

Comparative characteristics with Afobazole and Phenibut

When comparing any drugs with a similar therapeutic effect, one should take into account the indications for each of them, the severity of symptoms in which a particular drug helps better, the speed of medicines, contraindications and limitations.

“Afobazole” or “Grandaxin” - which of the two drugs that are similar in effect to the drugs, but having different therapeutic substances as the active ingredient, is the best?

The following facts should be highlighted:

  1. Grandaxin is a stronger and faster-acting medication compared to Afobazol. A stable therapeutic effect is already evident on the 2nd – 3rd day of administration, and the effect of Afobazole is felt no earlier than the 7th – 9th day of treatment.
  2. However, unlike Afobazole, Grandaxinum gives more negative side reactions and has an extensive list of contraindications and warnings.
  3. Afobazol does not cope with manifestations of severe stress and a more pronounced dysfunction of the nervous system, which Grandaksin can eliminate.

Therefore, from the point of view of the frequency and severity of adverse reactions, Afobazole is preferable, but it should be chosen only on condition that the medicine really helps the patient. Otherwise, it may be necessary to use "Grandaxinum" as a more active tranquilizer.

What is better to take - Phenibut or Grandaxin? After all, these are medicines with a different medical basis.

If "Grandaxinum" is only a tranquilizer, then "Phenibut", first of all, is prescribed to activate cerebral circulation and stimulate memory, learning and attention, mental reactions. And its anti-anxiety effect is considered as an additional property that allows the use of "Phenibut" in mild mental disorders. It will support normal sleep, relieve anxiety, help with tics, enuresis and stuttering, soothe elderly patients with abrupt alcohol withdrawal, insomnia and nightmares.

"Grandaxinum" also has a more narrowly targeted effect in more serious disorders of the nervous system. This is a more "difficult" medicine, and it is used only from adolescence.

Phenibut has far fewer contraindications and is allowed in pediatrics for babies from 2 years old and pregnant women from 13 to 15 weeks of gestation. But he, unlike "Grandaksin", causes inhibition and drowsiness.

Therefore, in order to judge the effectiveness of two medications, you need to know the diagnosis and analyze the pathological manifestations that need to be addressed.

You should know that "Grandaxinum" and "Phenibut" are compatible and even mutually enhance the therapeutic effects, so they can be drunk together.Especially if you need to not only relieve anxiety and reassure the patient, but also improve blood circulation and brain function. In addition, Phenibut can reduce the overexcitation that often accompanies treatment with Grandaxin.

However, concurrent administration of these drugs is prohibited if the patient develops a paradoxical (reverse) reaction to Phenibut. In this case, Grandaxin will only increase the restless behavior and panic state of the patient.

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