More info
Active ingredients
Release form
Composition
active substance:
tofizopam 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
Pharmacological effect
The drug from the group of benzodiazepine derivatives (an atypical benzodiazepine derivative), has an anxiolytic effect, almost not accompanied by a sedative, muscle relaxant, anticonvulsant action. It is a psycho-vegetative regulator, 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. Due to the atypical nature of the chemical structure, in contrast to the classical benzodiazepine derivatives, Grandaxin® in therapeutic doses practically does not cause the development of physical, psychological dependence and withdrawal syndrome.
Grandaxin® refers to daytime anxiolytics.
Pharmacokinetics
When ingestion quickly 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 not accumulates in the body. Its metabolites do not possess pharmacological activity. It is mainly excreted 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 hours.
Indications
- neuroses and neurosis-like states (conditions accompanied by emotional stress, autonomic disorders, moderate anxiety, apathy, diminished activity, obsessive feelings);
- reactive depression with moderately severe psychopathological symptoms;
- mental adaptation disorder (post-traumatic stress disorder);
- climacteric syndrome (as an independent tool, as well as in combination with hormonal drugs);
- premenstrual syndrome;
- cardialgia (as monotherapy or in combination with other drugs);
- alcohol withdrawal syndrome;
- myasthenia gravis, myopathies, neurogenic muscular atrophies and other pathological conditions with secondary neurotic symptoms, when anxiolytics are contraindicated with a pronounced muscle relaxant effect.
Contraindications
- hypersensitivity to the active or any other component of the drug or any other benzodiazepines;
- conditions accompanied by marked psychomotor agitation, aggressiveness, or severe depression;
- decompensated respiratory failure;
- I trimester of pregnancy;
- breastfeeding period;
- sleep apnea syndrome (in history);
- simultaneous use with tacrolimus, sirolimus, cyclosporine;
- galactose intolerance, congenital lactase deficiency, or malabsorption syndrome of glucose and galactose (the product contains lactose monohydrate).
- Carefully: decompensated chronic respiratory distress, a history of acute respiratory failure, angle-closure glaucoma, epilepsy, organic brain damage (for example, atherosclerosis).
Use during pregnancy and lactation
Contraindicated in the first trimester of pregnancy. At the time of treatment should stop breastfeeding.
Dosage and administration
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 pills) 1–3 times a day. In case of irregular use, 1-2 pills can be taken. The maximum daily dose is 300 mg.
Elderly patients and patients with renal insufficiency reduce the daily dose by about 2 times.
Side effects
- From the digestive tract: loss of appetite, constipation, increased gas, nausea, dry mouth. In some cases, possible stagnant jaundice.
- From the side of the central nervous system: headache, insomnia, increased irritability, psychomotor agitation, confusion, seizures may occur in patients with epilepsy.
- Allergic reactions: rash, scarlet-like rash, itching.
- From the musculoskeletal system: muscle tension, sore muscles.
- On the part of the respiratory system: respiratory depression.
Overdose
Symptoms: The effects of the suppression of the central nervous system function appear only after high doses (50–120 mg / kg). Such doses can cause vomiting, confusion, coma, respiratory depression and / or epileptic seizures.
Treatment: when expressed suppression of the functions of the central nervous system is not recommended to cause vomiting. Rinse the stomach. Appointment of activated carbon helps reduce the absorption of the drug.It is necessary to constantly monitor the basic physiological parameters and apply appropriate symptomatic therapy. With respiratory depression it is possible to carry out mechanical ventilation. The introduction of CNS stimulants is not recommended. Hypotension is best eliminated in / in the introduction of fluids and transfer the patient to the Trendelenburg position. If these measures do not restore normal blood pressure, you can enter dopamine or norepinephrine. Dialysis and induced diuresis are ineffective.
Flumazenil can be administered as an antagonist, but its use in an overdose of tofisopam has not been clinically tested.
Interaction with other drugs
Simultaneous use of tacrolimus, sirolimus, cyclosporine and tofisopam is contraindicated. Plasma concentrations of drugs that are metabolized by CYP3A4 may increase when taken concomitantly with tofisopam.
The use of tofisopam with drugs that suppress the functions of the central nervous system (analgesics, general anesthesia, antidepressants, H1-antihistamines, sedatives, hypnotics, antipsychotics) enhances their effects (for example, sedation or respiratory depression).
Hepatic enzyme inducers (alcohol, nicotine, barbiturates, antiepileptic drugs) can increase the metabolism of tofisopam, which can lead to a decrease in its plasma concentration 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) can enhance the effects of tofisopam. Beta-blockers can slow down the metabolism of the drug, but this effect has no clinical significance.
Tofizopam can increase the level of digoxin in the blood plasma.
Benzodiazepines may affect the anticoagulant effect of warfarin.
Prolonged use of disulfiram may inhibit the metabolism of tofisopam.
Antacids may affect the absorption of tofisopam. Cimetidine and omeprazole inhibit the metabolism of tofisopam.
Oral contraceptives can reduce the intensity of the metabolism of tofisopam.
Tofizopam weakens the inhibitory effect of alcohol on the central nervous system.
special instructions
It should be borne in mind that in patients with mental retardation, elderly patients, as well as those with impaired renal and / or liver function, more often than other patients, side effects may occur.
Tofizopam is not recommended for chronic psychosis, phobias or obsessive-compulsive disorders. In these cases, the risk of suicidal attempts and aggressive behavior increases. Therefore, tofisopam is not recommended as monotherapy for depression or depression accompanied by anxiety.
Care must be taken in treating patients with depersonalization as well as organic brain damage (for example, atherosclerosis).
In patients with epilepsy, tofizopam may increase the threshold of convulsive readiness.
Each Grandaxin® tablet contains 92 mg of lactose, which should be considered for patients suffering from lactose intolerance (see “Contraindications”).
Influence on ability to drive vehicles and work with mechanisms. Grandaxin® does not significantly reduce the attention and ability to concentrate.
Storage conditions
At a temperature of 15–25 ° C.
Keep out of the reach of children.