Expiration date: 10/2028

Active substance: tofisopam

The drug forms

Tablets: round, flat, disc-shaped, white or grayish-white in color, with a facet, with chamfer on one party and chasing «GRANDAX» - on the other, with little or no odor.

Pharmachologic effect: anxiolytic.

Pharmacodynamics

The preparation of the group of benzodiazepines (atypical benzodiazepine derivative), has an anxiolytic effect, accompanied by little sedative, muscle relaxant, anticonvulsant action. It is psychovegetative regulator eliminates various forms of autonomic disorders. It has a mild stimulating activity.

Due to the lack miorelaksiruyuschego effect of the drug can also be used in patients with myopathy and myasthenia. Because of atypical chemical structure, in contrast to the classical benzodiazepine derivatives, in therapeutic doses Grandaxin® hardly causes the development of physical, psychological dependence and withdrawal.

Grandaxin® refers to the day anxiolytics.

Pharmacokinetics

When ingestion rapidly and almost completely absorbed from the gastrointestinal tract. Blood Cmax is reached within 2 hours after which the plasma concentration is reduced monoexponential. Tofisopam not accumulates in the body. Its metabolites do not possess pharmacological activity. Write mainly in the urine (60-80%) in the form of conjugates with glucuronic acid and to a lesser extent (about 30%) - with the feces. T1 / 2 is 6-8 hours.

Testimony

• neuroses and neurosis-like states (state, accompanied by emotional stress, autonomic disorders, moderate anxiety, apathy, decreased activity, obsessive feelings);
  
• reactive depression with moderately severe psychopathological symptoms;
  
• mental adaptation disorder (PTSD);
  
• climacteric syndrome (as a standalone tool, as well as in combination with hormonal therapy);
  
• premenstrual syndrome;
  
• cardialgia (alone or in combination with other drugs);
  
• alcohol withdrawal syndrome;
  
• myasthenia, myopathy, neurogenic muscular atrophy and other pathological conditions with secondary neurotic symptoms when anxiolytics are contraindicated with pronounced muscle relaxant effect.
  

Contraindications

• Hypersensitivity to the active or any other component of the drug or any other benzodiazepines;
  
• d by severe psychomotor agitation, aggressiveness, or severe depression;
  
• decompensated respiratory failure;
  
• I trimester of pregnancy;
  
• lactation;
  
• apnea syndrome during sleep (in history);
  
• simultaneous application of tacrolimus, sirolimus, cyclosporine;
  
• galactose intolerance, congenital lactase deficiency or malabsorption syndrome of glucose and galactose (product contains lactose monohydrate).
  

Precautions: decompensated chronic respiratory distress, acute respiratory failure in the history of angle-closure glaucoma, epilepsy, organic brain damage (such as atherosclerosis).

Pregnancy and breast-feeding

It contraindicated in I trimester of pregnancy. At the time of treatment should stop breastfeeding.

Side effects

On the part of the digestive tract: loss of appetite, constipation, increased separation of gas, nausea, dry mouth. In some cases, possible congestive jaundice.

CNS: there may be headache, insomnia, irritability, agitation, confusion, seizures may occur in patients with epilepsy.

Allergic reactions: rash, scarlatiniform rash, pruritus.

From the musculoskeletal system: muscle tension, muscle aches.

The respiratory system: respiratory depression.

Interaction

Concomitant use of tacrolimus, sirolimus, cyclosporine and tofizopama contraindicated. plasma concentrations of drugs that are metabolized by CYP3A4, can be increased at the same time taking with tofizopamom.

Application tofizopama with drugs that suppress the central nervous system (analgesics, general anesthetics, antidepressants, H1-antihistamines, sedatives, hypnotics, antipsychotics), reinforces their effects (eg sedation or respiratory depression).

Hepatic enzyme inducers (alcohol, nicotine, barbiturates, antiepileptics) tofizopama may enhance metabolism, which may lead to a decrease in its plasma concentration and therapeutic effect of weakening.

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

Some antihypertensives (clonidine, calcium channel antagonists) may enhance the effects tofizopama. Beta-blockers may slow the metabolism of the drug, but this effect has no clinical significance.

Tofisopam can increase digoxin plasma levels.

Benzodiazepines can affect the anticoagulant effect of warfarin.

Long-term use can inhibit the metabolism of disulfiram tofizopama.

Antacids can interfere with the absorption tofizopama. Cimetidine and omeprazole inhibit metabolism tofizopama.

Oral contraceptives can reduce the intensity of tofizopama metabolism.

Tofisopam weakens the inhibitory effect of alcohol on the central nervous system.

Dosing and Administration: Inside.

The mode set individually, taking into account the patient's condition, the clinical form of the disease and individual sensitivity to the drug. Adults appoint 50-100 mg (1-2 tablets.) 1-3 times a day. At irregular application can take 1-2 tablets. The maximum daily dose - 300 mg.

Elderly patients and patients with kidney failure the daily dose reduced about 2-fold.

Overdose

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

Treatment: in severe suppression of the central nervous system is not recommended to induce vomiting. Rinse the stomach. Appointment of activated charcoal helps to reduce the absorption of the drug. It is necessary to constantly monitor the main physiological parameters and apply the appropriate symptomatic therapy. If respiratory depression can be carried out IVL. The introduction of CNS stimulants are not recommended. Hypotension best addressed in / in a liquid and transfer the patient in the Trendelenburg position. If these steps do not restore normal blood pressure, you can enter the dopamine or norepinephrine. Dialysis and induced diuresis are ineffective.

As an antagonist Flumazenil can be entered, but its use in overdose tofizopama clinically tested.

Special instructions

It should be noted that patients with mental retardation, elderly patients, as well as having disorders of the kidneys and / or liver disease, are more likely than other patients may experience side effects.

Not recommended for use Tofisopam with chronic psychosis, phobias or obsessive-compulsive disorder. In these cases, the risk of suicide attempts and aggressive behavior. Therefore Tofisopam not recommended as monotherapy depression or depression accompanied by anxiety.

Care should be taken when treating patients with depersonalization, and organic brain damage (such as atherosclerosis).

In patients with epilepsy Tofisopam may increase the seizure threshold.

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

Effects on ability to drive and use machines. Grandaxin® not significantly reduce the attention and ability to concentrate.

Release Form

Tablets, 50 mg. According to Table 10. in a blister pack. 2 or 6 blisters in a carton box.

Manufacturer

CJSC "Pharmaceutical plant EGIS." 1106 Budapest, ul. Keresturi, 30-38, Hungary.

In the case of packaging and packing of the drug in Russia further stated:

Pre-packaged, packed: SERDIKS LLC. 142150, Russia, Moscow region., Podolsky district, d. Sofyino, p. 1/1.

Storage conditions

At a temperature of 15-25 ° C.

Keep out of the reach of children.

The shelf life: 5 years.

Do not use beyond the expiration date printed on the package.