Grandaxin, pills 50 mg, 60 pcs.

Composition

Active ingredient:

tofizopam 50 mg;

Auxiliary substances:

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

Pharmacological action

Grandaxin – a drug from the group of benzodiazepine derivatives (atypical benzodiazepine derivative), has an anxiolytic effect, practically not accompanied by sedative, muscle relaxant, anticonvulsant action. It is a psychovegetative regulator, eliminates various forms of vegetative disorders. It has 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 classical 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. Tofizopam does not accumulate in the body. Its metabolites do not have pharmacological activity. It is mainly excreted in the urine (60-80%) in the form of conjugates with glucuronic acid and to a lesser extent (about 30%) “with feces. ” T1 / 2 is 6-8 hours.

Indications

• neurosis and neurosis-like States (state, accompanied by emotional stress, autonomic disorders, moderate anxiety, apathy, decreased activity, Intrusive experiences);
• reactive depression with moderate psychopathological symptoms;
• disorder of mental adaptation (PTSD);
• climacteric syndrome (as a standalone tool, as well as in combination with hormonal therapy);
• premenstrual syndrome;
• cardialgia (as monotherapy or in combination with other drugs);
• alcohol withdrawal syndrome;
• myasthenia gravis, myopathy, neurogenic muscular atrophy and other pathological conditions with secondary neurotic symptoms when anxiolytics are contraindicated with pronounced muscle relaxant effect.

Use during pregnancy and lactation

Contraindicated in the first trimester of pregnancy.

Breast-feeding should be discontinued for the duration of treatment.

Contraindications

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

With caution: decompensated chronic respiratory distress, a history of acute respiratory failure, angle-closure glaucoma, epilepsy, organic brain damage (for example, atherosclerosis).

Side effects

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

From the central nervous system: there may be headache, insomnia, increased irritability, psychomotor agitation, confusion, convulsive seizures may occur in patients with epilepsy.

Allergic reactions: exanthema, scarlet fever-like exanthema, pruritus.

From the musculoskeletal system: muscle tension, muscle pain.

Respiratory system disorders: respiratory depression.

Interaction

Concomitant use of tacrolimus, sirolimus, cyclosporine and tofizopam is contraindicated. Plasma concentrations of drugs that are metabolized by CYP3A4 may increase when co-administered with tofizopam.

The use of tofizopam with drugs that suppress the functions of the central nervous system (analgesics, general anesthesia, antidepressants, H1-antihistamines, sedatives, sleeping pills, antipsychotics) increases their effects (for example, sedation or respiratory depression).

Inducers of liver enzymes (alcohol, nicotine, barbiturates, antiepileptic drugs) can increase the metabolism of tofizopam, which can lead to a decrease in its concentration in blood plasma and weaken the therapeutic effect.

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

Some antihypertensive medications (clonidine, calcium channel antagonists) may increase the effects of tofizopam. Beta-blockers may slow down the drug’s metabolism, but this effect is not clinically relevant.

Tofizopam may increase plasma digoxin levels.

Benzodiazepines may affect the anticoagulant effect of warfarin.

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

Antacids may affect the absorption of tofizopam. Cimetidine and omeprazole inhibit the metabolism of tofizopam.

Oral contraceptives may reduce the metabolic rate of tofizopam.

Tofizopam weakens the depressing effect of alcohol on the central nervous system.

How to take, course of administration and dosage

Inside.

The dosage regimen is set individually, taking into account the patient’s condition, the clinical form of the disease and individual sensitivity to the drug. Adults are prescribed 50-100 mg (1-2 tablets) 1-3 times a day. With irregular use, you can take 1-2 tablets. The maximum daily dose is 300 mg.

In elderly patients and patients with renal insufficiency, the daily dose is reduced approximately 2 times.

Overdose

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

Treatment: with severe suppression of CNS functions, it is not recommended to induce vomiting. Wash out the stomach. The use 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.

If you have respiratory depression, you can perform mechanical ventilation. Administration of CNS stimulants is not recommended. Hypotension is best treated by intravenous fluids and placing the patient in the Trendelenburg position. If these measures do not restore normal blood pressure, dopamine or norepinephrine can be administered. Dialysis and induced diuresis are ineffective.

Flumazenil can be administered as an antagonist, but its use in overdose of tofizopam has not been clinically tested.

Special instructions

It should be taken into account that patients with mental retardation, elderly patients, as well as those with impaired renal and/or liver function, may experience side effects more often than other patients.

It is not recommended to use tofizopam for chronic psychosis, phobia or obsessive states. In these cases, the risk of suicidal attempts and aggressive behavior increases. Therefore, tofizopam is not recommended as a monotherapy for depression or depression accompanied by anxiety.

Caution is necessary when treating patients with depersonalization, as well as organic brain damage (for example, atherosclerosis).

In patients with epilepsy, tofizopam may increase the seizure alert threshold.

Each tablet of Grandaxin® contains 92 mg of lactose, which should be considered in patients suffering from lactose intolerance (see “Contraindications”).

Influence on the ability to drive a car or perform work that requires an increased rate of physical and mental reactions. Grandaxin® does not significantly reduce attention and concentration.

Composition

Tablet Form of production

Storage conditions

At a temperature of 15-25 °C

Shelf life

5 years

Active ingredient

Tofizopam

Conditions of release from pharmacies

By prescription

Dosage form

of the tablet

Purpose

For adults as prescribed by a doctor, For pregnant women in the second and third trimester as prescribed by a doctor

Indications

Menopause, Asthenia, Alcoholism, Vegetative-vascular disorders, Neurosis, Stress, Premenstrual syndrome

Weight

Weight: 25 gr.