Grandaxin, tablets 50 mg, 20 pcs.

Pharmacodynamics

Tophizopam is a mild anxiolytic with short-term action and a broad therapeutic index. The exact mechanism of action is unknown. Tofizopam differs from other 1,4-benzodiazepines both in its chemical structure and in its clinical and pharmacological effects.

The drug is effective in treating anxiety disorders, including those accompanied by vegetative manifestations, fatigue, apathy. Unlike other benzodiazepines, tofizopam has no sedative, hypnotic, muscle relaxant and anticonvulsant activity. The drug does not have adverse effects on memory, psychomotor and cognitive function, but has moderate stimulant activity.

Because of absence of muscle relaxant effect the drug can also be used in patients with myopathy, myasthenia gravis and neurogenic muscle atrophy in which the use of muscle relaxants is contraindicated or undesirable. With long-term use, tofizopam does not cause the development of physical or mental dependence.

Pharmacokinetics

Intake. When administered orally, it is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax is reached within 1-1.5 h.

Distribution. About 50% of tofizopam is bound to blood proteins.

Metabolism. After absorption, tofizopam undergoes significant presystemic metabolism in the liver. The main metabolic pathway is demethylation.

Elimation. It is excreted mainly by the kidneys (about 60%) and in the form of metabolites through the intestine. T1/2 is 6-8 hours.

Indications

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

• .Treatment of mental (neurotic) and psychosomatic disorders accompanied by emotional tension, anxiety, vegetative disorders, apathy, fatigue and depressed mood;

• alcohol withdrawal syndrome.

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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;

MC, 10 mg

How to take, the dosage

Internal.

Adults. The usually recommended dose is 1 to 2 tablets 1 to 3 times a day (total daily dose 50 to 300 mg). If used irregularly, 1 to 2 tablets may be taken. The maximum dose is 300 mg. Gradual increase in dose is usually not necessary; treatment can be started at the required dose, as the drug is well tolerated and during its administration there is usually no decrease in activity and mental wakefulness.

Children and adolescents under the age of 18 years. Use in children and adolescents under 18 years of age is contraindicated. There is insufficient experience with the drug in children and adolescents under 18 years of age.

Particular patient groups. There is no information about special patient groups. Clinical studies of efficacy and safety of Grandaxin® Tablets 50 mg (tofizopam) in elderly patients with renal and hepatic impairment have not been conducted.

Interaction

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

The use of tofizopam with drugs that have CNS depressant effect (analgesics, general anesthetics, antidepressants, sedatives, hypnotics), H1-histamine receptor blockers, antipsychotics increases their effects (for example, sedative effect or respiratory depression).

Opioids: Co-administration of sedative drugs such as benzodiazepines or similar drugs such as Grandaxin® with opioids increases the risk of sedation, respiratory depression, coma and death due to the additive CNS depressant effect of these drugs. Doses and duration of co-administration of these drugs should be limited.

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 hypotensive drugs (clonidine, BMCC) may increase the effects of tofizopam. β-adrenoblockers may slow down the metabolism of the drug, but this effect is of no clinical significance.

Digoxin: Tofizopam may increase plasma concentrations of digoxin.

Warfarin: benzodiazepines may affect the anticoagulant effect of warfarin.

Disulfiram: prolonged use of disulfiram may inhibit the metabolism of tofizopam.

Antacids have different effects on absorption of tofizopam. Cimetidine and omeprazole inhibit the metabolism of tofizopam.

The oral contraceptives may decrease the metabolic rate of tofizopam.

Alcohol: tofizopam attenuates the suppressive effect of alcohol on perception.

Special Instructions

Particular caution is required when treating patients with compensated chronic respiratory failure or those who have previously suffered from acute respiratory failure.

Caution is required when treating elderly patients and those with psychiatric degeneration, as well as those with renal and/or liver function disorders, because they are more likely than other patients to have adverse reactions of the drug.

When combining Grandaxin® with drugs that suppress CNS function (antidepressants, sedatives, hypnotics, opioid analgesics, general anesthetics), antihistamines, antipsychotics, alcohol may increase mutual effects.

It is not recommended to use the drug in chronic psychosis, phobia or compulsive states. With decreased inhibition, the risk of suicidal attempts and aggressive behavior increases. Therefore, Grandaxin® is not recommended as monotherapy for depression or depression accompanied with anxiety.

Caution is necessary when treating patients with personality disorders (psychopathies).

The drug should be used with extreme caution in organic brain lesions (e.g., atherosclerosis).

In patients with epilepsy, Grandaxin® may provoke seizures.

It is not recommended to use this drug in patients with closed-angle glaucoma.

Risk when combined with opioids. Co-administration of Grandaxin® with opioids increases the risk of sedation, respiratory depression, coma and death. Due to the increased risk, concomitant use of sedatives is possible only in patients for whom alternative therapies cannot be used. If it is decided to concomitantly prescribe Grandaxin® with other sedative drugs, the lowest effective dose should be used, and the duration of treatment should be as short as possible. Such patients need careful monitoring of respiratory depression and sedation symptoms. It is therefore strongly recommended that patients and caregivers (if any) be made aware of the symptoms of respiratory depression and sedation.

Grandaxin® contains lactose. Each tablet of Grandaxin® contains 92 mg of lactose monohydrate. This should be considered in patients with rare hereditary diseases, including galactose intolerance, complete lactase deficiency and glucose-galactose malabsorption.

Impact on driving and operating machinery.