Grandaxin

Active substance:

tophysopam50 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;

MKC - 10 mg

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

Due to the lack of myorelaxing effect, the drug can also be used in patients with myopathy and myasthenia. 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® belongs to daytime anxiolytics.

Pharmacokinetics

When taken orally, it is quickly and almost completely absorbed from the gastrointestinal tract. Cmax in the blood is achieved within 2 hours, after which the plasma concentration decreases monoexponentially. Tophysopam does not accumulate 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.

• neuroses and neurosis-like conditions (conditions accompanied by emotional tension, vegetative disorders, moderate anxiety, apathy, reduced activity, obsessive experiences);
• reactive depression with moderate psychopathological symptoms;
• mental adaptation disorder (post-traumatic stress disorder);
• menopause syndrome (as an independent remedy, as well as in combination with hormonal drugs);
• premenstrual syndrome;
• cardialgia (in the form of monotherapy or in combination with other drugs);
• alcohol withdrawal syndrome;
• myasthenia, myopathies, neurogenic muscle atrophy and other pathological conditions with secondary neurotic symptoms when anxiolytics with a pronounced myorelaxing effect are contraindicated.

Contraindicated in the first trimester of pregnancy.

Breastfeeding should be stopped during treatment.

• hypersensitivity to the active or any other component of the drug or any other benzodiazepines;
• conditions accompanied by pronounced psychomotor arousal, aggression or severe depression;
• decompensated respiratory failure;
• I trimester of pregnancy;
• breastfeeding period;
• sleep arrest syndrome (in history);
• simultaneous use with tacrolimus, syrolimus, cyclosporin;
• galactose intolerance, congenital lactase deficiency or glucose and galactose malabsorption syndrome (the drug contains lactose monohydrate).

Caution: decompensated chronic respiratory distress, acute respiratory failure in the history, closed-angle glaucoma, epilepsy, organic brain lesions (e.g. atherosclerosis).

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

From the CNS side: there may be headaches, insomnia, increased irritability, psychomotor arousal, confusion, seizures may occur in patients with epilepsy.

Allergic reactions: exanthemum, scarlet-like exanthemum, itching.

From the musculoskeletal system: muscle tension, muscle pain.

From the respiratory system side: respiratory depression.

Simultaneous use of tacrolimus, syrolimus, cyclosporin and tophystopam is contraindicated. The plasma concentration of drugs that are metabolized by CYP3A4 may increase when taken simultaneously with tophysopam.

The use of tophysopam with drugs that suppress CNS functions (analgetics, general anesthesia, antidepressants, H1-antihistamine, sedative, sleeping pills, antipsychotic), enhances their effects (e.g. sedative effect or respiratory depression).

Hepatic enzyme inductors (alcohol, nicotine, barbiturates, antiepileptics) can increase the metabolism of tophysopam, which can lead to a decrease in its concentration in blood plasma and a weakening of the therapeutic effect.

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

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

Tophysopam can increase the level of digoxin in blood plasma.

Benzodiazepines can affect the anticoagulant effect of warfarin.

Prolonged use of disulfiram can inhibit tophysopam metabolism.

Antacid drugs can affect the absorption of tophysopam. Cymethylodine and omeprazole inhibit tophysopam metabolism.

Oral contraceptives can reduce the intensity of tophysopam metabolism.

Tophysopam weakens the oppressive effect of alcohol on the CNS.

Inside.

The dosing regimen is 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 a day. If used irregularly, you can take 1-2 tablets. The maximum daily dose is 300 mg.

For elderly patients and patients with renal failure, the daily dose is reduced by about 2 times.

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

Treatment: in case of pronounced suppression of CNS functions, it is not recommended to cause vomiting. Rinse your stomach. Prescribing activated carbon helps reduce the absorption of the drug. The main physiological parameters should be constantly monitored and appropriate symptomatic therapy should be applied.

In case of respiratory depression, ventilators can be performed. The introduction of CNS stimulants is not recommended. The hypothesis is best eliminated in/in by injecting liquids and transferring the patient to the Trendelenburg position. If these measures do not restore normal blood pressure, you can administer dopamine or norepinephrine. Dialysis and diuresis are ineffective.

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

It should be borne in mind that patients with mental retardation, elderly patients, as well as those with kidney and/or liver dysfunction, may experience side effects more often than other patients.

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

Care is needed in the treatment of patients with depersonalization, as well as organic brain damage (e.g. atherosclerosis).

In epilepsy patients, tophysopam can raise the threshold of convulsive readiness.

Each Grandaxin® tablet contains 92 mg of lactose, which should be taken into account for patients suffering from lactose intolerance (see "Contraindications").

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

tablets