GRANDAKSIN
Active material: Tofisopam
When ATH: N05BA23
CCF: Tranquillizer (anxiolytic)
ICD-10 codes (testimony): F10.3, F31, F32, F33, F40, F41.2, F43, F45.3, F48.0, G70.2, G71.0, N94.3, N95.1, N95.3
At KFU: 02.04.01
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)
Pharmaceutical form, composition and packaging
Pills round, flat, a disc-, white or grayish white color, chamfered, Engraved “GRANDAX” on one side and with Valium – on the other side, odorless or almost odorless.
| 1 tab. | |
| Tofisopam | 50 mg |
Excipients: stearic acid, magnesium stearate, gelatin, talc, potato starch, lactose monohydrate, microcrystalline cellulose.
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
Pharmacological action
Tranquillizer. The preparation of the group of benzodiazepines (atypical benzodiazepine). It has anxiolytic effects, not accompanied by a sedative, miorelaksiruyuschim, anticonvulsant effect. Is psychovegetative regulator, eliminates various forms of autonomic disorders. It has a mild stimulating activity.
Due to the lack miorelaksiruyuschego effects the drug can be used in patients with myopathy and myasthenia.
Due to the chemical structure untypicality, Unlike classical benzodiazepines, Grandaksin® at therapeutic doses does not potentiate the effect of alcohol, and practically does not cause the development of physical, psychological dependence and withdrawal syndrome.
Grandaksin® It refers to the day tranquilizers.
Pharmacokinetics
Absorption
Once inside quickly and almost completely absorbed from the gastrointestinal tract. Cmax plasma levels reached within 2 no, then the plasma concentration decreases monoexponential.
Distribution
Tofisopam not accumulates in the body.
Metabolism
Metabolites tofizopama not possess pharmacological activity.
Deduction
T1/2 is 6-8 no.
Write mainly in the urine (60-80%) in the form of conjugates with glucuronic acid and to a lesser extent (about 30%) – with feces.
Testimony
- Neuroses and neurosis-like states (states, accompanied by emotional stress, autonomic disorders, moderate anxiety, apatieй, reduced activity, intrusive experiences);
- Reactive depression with moderately severe psychopathological symptoms;
- Adaptation of mental disorder (post traumatic stress disorder);
- Menopausal syndrome (as an independent means, as well as in combination with hormonal therapy);
- Premenstrual tension;
- Kardialgii (alone or in combination with other drugs);
- Alcohol withdrawal syndrome;
- Myasthenia, myopathies, neurogenic muscle atrophy and other pathological conditions with secondary neurotic symptoms in cases, when anxiolytics contraindicated with severe muscle relaxant action.
Dosage regimen
Set individually based on the patient's condition, Clinical forms of the disease and individual sensitivity to the drug.
Adults appoint 50-100 mg (1-2 tab.) 1-3 times / day. At irregular application can be accepted 1-2 tab. The maximum daily dose – 300 mg.
Elderly patients and patients with renal insufficiency reduce the daily dose of approximately 2 times.
Side effect
CNS: headache, insomnia, irritability, psychomotor agitation, confusion, seizures in patients with epilepsy.
From the digestive system: decreased appetite, constipation, flatulence, nausea, dry mouth; in some cases – cholestatic jaundice.
Allergic reactions: possible itching, rash (incl. scarlatiniform rash).
On the part of the musculoskeletal system: muscle tension, myalgia.
Contraindications
- State, accompanied by severe psychomotor agitation, aggressiveness or deep depression;
- Respiratory failure decompensation;
- A syndrome of sleep apnea (history);
- Simultaneous application of tacrolimus, sirolimusom, cyclosporine;
- I trimester of pregnancy;
- Lactation (breast-feeding);
- Hypersensitivity to the drug or any other benzodiazepines.
FROM caution It should be prescribed to patients with decompensated chronic respiratory distress syndrome, acute respiratory failure history, angle-closure glaucoma, epilepsy, organic brain lesions (eg, in atherosclerosis).
Pregnancy and lactation
Grandaksin® contraindicated for use in the I trimester of pregnancy and lactation (breast-feeding).
Cautions
It should be taken into account, that patients with mental retardation, elderly patients, in patients with impaired renal function and / or liver disease often, than other patients, Side effects may occur.
Not recommended for use in chronic psychosis Tofisopam, phobias or obsessive-compulsive disorder. In these cases, the risk of suicide attempts and aggressive behavior. Therefore Grandaxinum® It not recommended as monotherapy in depression or depression, accompanied by anxiety.
Care should be taken in patients with depersonalization, as well as with organic brain damage (eg, atherosclerosis).
In patients with epilepsy Tofisopam may increase the seizure threshold.
Each tablet Grandaxinum® It contains 92 Lactose mg, which should be considered for patients with lactose intolerance.
Effects on ability to drive vehicles and management mechanisms
Grandaksin® does not significantly reduce the ability to concentrate. The possibility of driving vehicles and management mechanisms should be addressed only after the evaluation of the individual patient's response to drug.
Overdose
Symptoms: after administration at a dose 50-120 mg / kg of body weight may cause vomiting, confusion, Coma, respiratory depression and / or seizures.
Treatment: in severe suppression of the central nervous system is not recommended to induce vomiting, should wash out the stomach. Injection of activated carbon helps reduce the absorption of the drug. It should constantly monitor the main physiological parameters and apply the appropriate symptomatic therapy. If respiratory depression can be carried out artificial respiration. The introduction of CNS stimulants are not recommended. Hypotension best addressed in / in a liquid and transfer the patient to the Trendelenburg position. If these measures do not restore normal blood pressure, You can enter dopamine or norepinephrine (noradrenaline). Dialysis and forced diuresis are not effective. In urgent cases, possible to use a specific benzodiazepine antagonist – flumazenil, but its use in overdose tofizopamom clinically tested.
Drug Interactions
Concomitant use of tacrolimus, sirolimusa, cyclosporine and Grandaxinum® contraindicated. The concentration of drug in the blood plasma, are metabolized by CYP3A4 isoenzyme, with the participation, may increase when taken with tofizopamom.
Application Grandaxinum® with drugs, inhibits the function of the central nervous system (analgesics, funds for general anesthesia, antidepressants, histamine H1-receptors, sedativnыe, sleeping pills, antipsychotics), reinforces their effects (eg, sedation or respiratory depression).
Hepatic enzyme inducers (ethanol, nicotine, barbiturates, antiepileptics) may enhance the metabolism of tofizopama, which can lead to a reduction of its concentration in plasma and the weakening of the therapeutic effect.
Some antifungal drugs (ketoconazole, itraconazole) can slow hepatic metabolism tofizopama, which increases its concentration in blood plasma.
Some antihypertensive drugs (klonidin, Calcium channel blockers) may enhance the effects of Grandaxinum®.
Beta-blockers can slow the metabolism tofizopama, however, this effect is not clinically important.
Tofisopam while the use can increase levels of digoxin in plasma.
Benzodiazepines, incl. Tofisopam, may affect the anticoagulant effect of warfarin.
Prolonged concurrent use of disulfiram can inhibit the metabolism of tofizopama.
Antacids can interfere with the absorption tofizopama.
Cimetidine and omeprazole in odnovremennom primenenii ugnetayut metabolism tofizopama.
Oral contraceptives can reduce the intensity of metabolism tofizopama.
Tofisopam weakens the inhibitory effect of ethanol on the CNS.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children at temperature from 15 ° to 25 ° C. Shelf life – 5 years.
