Grandaxin, tablets 50 mg, 60 pcs.

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

Because of its myorelaxant effect the drug can also be used in patients with myopathy and myasthenia gravis. Due to the atypicality of the chemical structure, unlike classical benzodiazepine derivatives, Grandaxin® practically does not cause physical and psychological dependence and withdrawal syndrome in therapeutic doses.

Grandaxin® is a daytime anxiolytic.

Pharmacokinetics

In oral administration, it is quickly and almost completely absorbed from the gastrointestinal tract. Cmax in blood is reached within 2 h, after which plasma concentrations decrease monoexponentially. Tofizopam does not cumulate in the body. Its metabolites have no pharmacological activity. It is excreted mainly with 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 h.

Indications

Stress, Neurosis, Alcoholism, Cardialgia (heart pain), Anxiety, Premenstrual syndrome, Climax, Seizures, Vascular disorders, Asthenia

• neuroses and neurosis-like states (states accompanied by emotional tension, autonomic disorders, moderately expressed anxiety, apathy, decreased activity, obsessive feelings);
• reactive depression with moderately pronounced psychopathological symptoms;
• disorder of mental adaptation (post-traumatic stress disorder);
• climacteric syndrome (as an independent agent, as well as in combination with hormonal drugs);
• predmenstrual syndrome;
• cardialgia (as monotherapy or in combination with other drugs);
• Acid withdrawal syndromealcohol withdrawal syndrome;
• myasthenia, myopathies, neurogenic muscle atrophies and other pathological conditions with secondary neurotic symptoms, when anxiolytics with pronounced muscle relaxant effect are contraindicated.

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Active ingredient

Tofizopam

Composition

Active substance:

Tofizopam50 mg;

Supplements:

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

How to take, the dosage

Internal administration.

The dosage regimen is determined individually with consideration of the patient’s condition, 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. If used irregularly, 1-2 tablets may be taken. Maximum daily dose is 300 mg.

In elderly patients and patients with renal insufficiency, the daily dose is reduced by about half.

Interaction

Simultaneous use of tacrolimus, sirolimus, cyclosporine and tofizopam is contraindicated. Plasma concentrations of drugs that are metabolized by CYP3A4 may increase with concomitant use of tofizopam.

The use of tofizopam with drugs that suppress CNS function (analgesics, general anesthetics, antidepressants, H1-antihistamines, sedatives, hypnotics, antipsychotics), increases their effects (e.g. sedative effect or respiratory depression).

Hepatic enzyme inducers (alcohol, nicotine, barbiturates, antiepileptic drugs) may increase the metabolism of tofizopam, which may lead to a decrease in its plasma concentration and weaken therapeutic effect.

Some antifungal drugs (ketoconazole, itraconazole) may slow hepatic metabolism of tofizopam, which leads to an increase in its plasma concentration.

Some antihypertensive drugs (clonidine, calcium channel antagonists) may increase the effects of tofizopam. Beta-adrenoblockers may slow down the metabolism of the drug, but this effect is of no clinical significance.

Tofizopam may increase plasma levels of digoxin.

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.

The oral contraceptives may decrease the metabolic rate of tofizopam.

Tofizopam attenuates the CNS depressant effect of alcohol.

Special Instructions

Patients with mental retardation, elderly patients, and those with renal and/or liver dysfunction are more likely than other patients to have side effects.

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

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

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

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

Impact on the ability to drive and operate machinery: During the use of the drug it is prohibited to drive vehicles and / or work with complex mechanisms requiring increased concentration.

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Contraindications

• high sensitivity to the active or any other component of the drug or any other benzodiazepines;
• conditions accompanied by marked psychomotor agitation, aggressiveness, or marked depression;
• decompensated respiratory failure;
• I trimester of pregnancy;
• breastfeeding period;
• syndrome of sleep apnea (history);
• 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, acute respiratory failure in anamnesis, closed-angle glaucoma, epilepsy, organic brain lesions (such as atherosclerosis).

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Side effects

Gastrointestinal disorders: decreased appetite, constipation, increased gas excretion, nausea, dry mouth. In some cases, congestive jaundice may occur.

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

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

Musculoskeletal disorders: muscle tension, pain in the muscles.

Respiratory system: respiratory depression.

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Overdose

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

Treatment: If CNS function is severely depressed, it is not recommended to induce vomiting. Flush the stomach. Administration of activated charcoal helps to reduce absorption of the drug. Basic physiological parameters should be monitored at all times and appropriate symptomatic therapy should be used.

In case of respiratory depression, ventilatory ventilation may be performed. Administration of CNS stimulants is not recommended. Hypotension is best managed with IV fluids and Trendelenburg. If these measures do not restore normal BP, dopamine or norepinephrine may be administered. Dialysis and induced diuresis are ineffective.

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

Pregnancy use

It is contraindicated in the first trimester of pregnancy.

Breastfeeding should be stopped during treatment.