Description
Release form
Tablets
Pharmacological action
Grandaxin – a drug from the group of benzodiazepine derivatives (an atypical benzodiazepine derivative), has an anxiolytic effect, which is almost not accompanied by a sedative, muscle relaxant, anticonvulsant effect. It is a psycho-vegetative regulator that eliminates various forms of autonomic disorders. It has moderate stimulating activity.
Due to the lack of muscle relaxant effect, the drug can also be used in patients with myopathy and myasthenia gravis. Due to the atypical nature of the chemical structure, in contrast to the classic benzodiazepine derivatives, Grandaxin ® in therapeutic doses practically does not cause the development of physical, mental dependence and withdrawal syndrome.
Grandaxin ® is a daily anxiolytic.
Pharmacokinetics
When taken orally, it is rapidly and almost completely absorbed from the digestive tract. Cmax in the blood is reached within 2 hours, after which the plasma concentration decreases monoexponentially. Tofisopam is not cumulated in the body. Its metabolites do not have pharmacological activity. It is excreted mainly in 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.
Contraindications
Conditions accompanied by severe psychomotor agitation, aggressiveness, or deep depression.
Respiratory failure at the stage of decompensation.
Syndrome of respiratory arrest in a dream (history).
Concomitant use with tacrolimus, sirolimus, cyclosporine.
I trimester of pregnancy.
Lactation (breastfeeding).
Hypersensitivity to the drug or any other benzodiazepine.
Caution is advised to prescribe the drug in the following cases:
Uncompensated chronic respiratory distress syndrome.
A history of acute respiratory failure.
Angle-closure glaucoma.
epilepsy.
Organic brain damage (e.g., atherosclerosis).
Use during pregnancy and lactation
Grandaxin is contraindicated for use in the first trimester of pregnancy and during lactation (breastfeeding).
Special instructions
Treatment with Grandaxin in patients with myasthenia gravis should be carried out under strict constant medical supervision.
In case of affective-shock reactions in the framework of reactive psychosis, as well as in deep depression, active combination therapy with antidepressants is indicated.
The appearance of increased irritability during treatment with Grandaxin, dyspepsia in some cases can be eliminated by reducing the dose of the drug.
With the development of insomnia, the last dose should be taken no later than 15 hours. The occurrence of exanthema during treatment with Grandaxin requires discontinuation of the drug.
In case of allergic reactions to the drug or serious sleep disorders, Grandaxin should be discontinued.
Effect on the ability to drive vehicles and control mechanisms
Grandaxin does not cause a significant decrease in the ability to concentrate.
The question of the possibility of driving vehicles and controlling mechanisms should be decided only after assessing the individual patient’s response to the drug.
Composition
1 tablet contains:
Active substances: tofisopam 50 mg.
Excipients: stearic acid, magnesium stearate, gelatin, talc, potato starch, lactose monohydrate, microcrystalline cellulose.
Dosage and administration
Set individually, taking into account 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 / day. The maximum daily dose of 300 mg.
Children over 14 years of age are prescribed up to 200 mg / day.
To prevent the disorder of falling asleep, the drug is recommended to be taken no later than 15-16 hours a day.
In elderly patients and patients with renal failure, the daily dose is reduced by about 2 times.
In case of alcohol withdrawal syndrome, a short course of therapy is indicated for the prevention and treatment of delirium: from several days to 3-6 weeks.
Side effects of
From the gastrointestinal tract: decreased appetite, constipation, increased gas separation, nausea, dry mouth. In some cases, congestive jaundice is possible.
From the side of the central nervous system: headache, insomnia, increased irritability, psychomotor agitation, confusion may be observed, convulsive seizures may occur in patients with epilepsy.
Allergic reactions: exanthema, scarlet fever-like exanthema, pruritus.
From the side of the musculoskeletal system: muscle tension, muscle pain.
From the respiratory system: respiratory depression.
Drug Interactions
The simultaneous use of tacrolimus, sirolimus, cyclosporine and tofisopam is contraindicated. The plasma concentration of drugs that are metabolized by CYP3A4 may increase while taking tofisopam.
The use of tofisopam with drugs that suppress the central nervous system (analgesics, general anesthesia, antidepressants, H1 antihistamines, sedatives, hypnotics, antipsychotics), enhances their effects (for example, sedation or respiratory depression).
Inducers of liver enzymes (alcohol, nicotine, barbiturates, antiepileptic drugs) can enhance the metabolism of tofisopam, which can lead to a decrease in its concentration in blood plasma and a weakening 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.
Benzodiazepines may affect the anticoagulant effect of warfarin.
Prolonged use of disulfiram may inhibit tofisopam metabolism.
Antacids may affect the absorption of tofisopam. Cimetidine and omeprazole inhibit the metabolism of tofisopam.
Oral contraceptives may decrease the intensity of tofisopam metabolism.
Tofisopam weakens the inhibitory effect of alcohol on the central nervous system.
Overdose
Symptoms: drowsiness, slight respiratory depression, in severe cases – coma.
Treatment: conducting activities aimed at restoring respiratory function and cardiovascular activity. Gastric lavage and activated charcoal are recommended. In emergency cases, the use of a specific benzodiazepine antagonist flumazenil may be possible.
Storage Conditions
The product should be stored at 15 ° C to 25 ° C.
shelf life
5 years
Deystvuyushtee substance
tofisopam
dosage form
tablets
Possible product names
GRANDAXIN 0.05 N20 TABLE
Grandaxin 0.05g No. 20
Grandaxin 50mg Tab. X20
Grandaxin 50mg No. 20 tab
GRANDAKSIN 50MG. No. 20 TAB.
