Grandaxinum

General characteristics. Structure:

Tablets of 1 table.
active agent:  Tofizopamum of 50 mg
excipients: stearic acid — 1 mg; magnesium stearate — 1 mg; gelatin — 3,5 mg; talc — 2 mg; potato starch — 20,5 mg; lactoses monohydrate — 92 mg; MKTs — 10 mg  

Description of a dosage form

Tablets are round, flat, in the form of a disk, white or grayish-white color, with a facet, with risky on one party and an engraving of "GRANDAX" — on another, without or almost inodorous.

Pharmacological properties:

Pharmacological action - anxiolytic.
Pharmacodynamics. Drug from group of derivatives of benzodiazepine (atypical derivative benzodiazepine), renders the anxiolytic effect which is almost not followed by sedative, myorelaxation, anticonvulsant action. Is the psychovegetative regulator, eliminates various forms of vegetative frustration. Has the moderate stimulating activity.

Owing to lack of myorelaxation effect drug can be used also at patients with a myopathy and a myasthenia. Owing to an atipichnost of chemical structure, unlike classical benzodiazepine derivatives, Grandaksin® in therapeutic doses practically does not cause development of physical, mental dependence and a withdrawal.

Грандаксин® treats day anxiolytics.

Pharmacokinetics. At intake quickly and almost it is completely soaked up from a GIT. Cmax in blood is reached during 2 h then concentration in plasma decreases monoeksponentsialno. Tofizopamum does not kumulirutsya in an organism. Its metabolites have no pharmacological activity. It is removed mainly with urine (60–80%) in the form of conjugates with glucuronic acid and to a lesser extent (about 30%) — with a stake. T1/2 makes 6–8 h.

Indications to use:

- neurosises and neurosis-like states (the state which are followed by emotional pressure, vegetative frustration, moderately expressed concern, apathy, hypoactivity, persuasive experiences);

- situational depression with moderately expressed psychopathological symptoms;

- disorder of mental adaptation (posttraumatic stressful frustration);

- a menopausal syndrome (as independent means, and also in a combination with hormonal drugs);

- premenstrual syndrome;

- cardialgias (in the form of monotherapy or in a combination with other drugs);

- alcoholic abstinence syndrome;

- a myasthenia, myopathies, neurogenic muscular atrophies and other morbid conditions with secondary neurotic symptoms when anxiolytics with the expressed myorelaxation action are contraindicated.

Route of administration and doses:

Inside.

The mode of dosing is set individually taking into account a condition of the patient, a clinical form of a disease and individual sensitivity to drug. The adult appoint 50–100 mg (1–2 tab.) 1–3 times a day. At irregular use it is possible to accept 1–2 table. The maximum daily dose — 300 mg.

To patients of advanced age and patients with a renal failure the daily dose is reduced approximately twice.

Features of use:

It is necessary to consider that at patients with a delay of mental development, elderly patients, and also having renal failures and/or a liver more often than at other patients, side effects can be observed.

It is not recommended to apply Tofizopamum at chronic psychosis, a phobia or persuasive states. The risk of suicide attempts and an agressive behavior increases in these cases. Therefore Tofizopamum is not recommended as monotherapy of the depression or a depression which is followed by alarm.

Care at treatment of patients with depersonalization, and also organic lesion of a brain is necessary (for example atherosclerosis).

At patients with epilepsy Tofizopamum can raise a threshold of convulsive readiness.

Each tablet Grandaksin® contains 92 mg of lactose that should be considered the patient having a lactose intolerance (see. "Contraindications").

Influence on ability to drive the car or to perform the works demanding the increased speed of physical and mental reactions. Грандаксин® significantly does not reduce attention and ability to concentrate.

Side effects:

From a GIT: a loss of appetite, a lock, the raised department of gases, nausea, dryness in a mouth. Congestive jaundice is in some cases possible.

From TsNS: the headache, sleeplessness, the increased irritability, psychomotor arousing, confusion of consciousness can be observed, there can be convulsive attacks at patients with epilepsy.

Allergic reactions: dieback, scarlatiniform dieback, itch.

From a musculoskeletal system: muscle tension, muscle pain.

From respiratory system: respiratory depression.

Interaction with other medicines:

Simultaneous use of a takrolimus, sirolimus, cyclosporine and Tofizopamum contraindicated. Concentration in a blood plasma of drugs which are metabolized by CYP3A4 can increase at a concomitant use with Tofizopamum.

Use of Tofizopamum with the drugs suppressing the TsNS functions (analgetics, means of the general anesthesia, antidepressants, H1 - antihistaminic, sedative, somnolent, antipsychotic), strengthens their effects (for example sedation or respiratory depression).

Inductors of liver enzymes (alcohol, nicotine, barbiturates, antiepileptic means) can strengthen metabolism of Tofizopamum that can lead to decrease in its concentration in a blood plasma and to easing of therapeutic effect.

Some antifungal drugs (кетоконазол, итраконазол) can slow down hepatic metabolism of Tofizopamum that leads to increase in its concentration in a blood plasma.

Some anti-hypertensive drugs (a clonidine, antagonists of calcium channels) can strengthen effects of Tofizopamum. Beta adrenoblockers can slow down drug metabolism, however this effect has no clinical value.

Tofizopamum can increase digoxin level in a blood plasma.

Benzodiazepines can affect anticoagulating effect of warfarin.

Prolonged use of Disulfiramum can oppress metabolism of Tofizopamum.

Antiacid means can influence absorption of Tofizopamum. Cimetidinum and омепразол oppress metabolism of Tofizopamum.

Peroral contraceptive means can reduce intensity of metabolism of Tofizopamum.

Tofizopamum weakens the oppressing effect of alcohol on TsNS.

Contraindications:

- hypersensitivity to active or any other component of drug or any other benzodiazepines;

- the states which are followed by the expressed psychomotor excitement, aggression or the expressed depression;

- dekompensirovanny respiratory insufficiency;

- I trimester of pregnancy;

- feeding period breast;

- an apnoea syndrome in a dream (in the anamnesis);

- simultaneous use with takrolimusy, sirolimusy, cyclosporine;

- intolerance of a galactose, inborn insufficiency of lactase or a sprue of glucose and a galactose (drug contains lactoses monohydrate).

With care: a dekompensirovanny chronic respiratory distress, acute respiratory insufficiency in the anamnesis, closed-angle glaucoma, epilepsy, organic lesions of a brain (for example atherosclerosis).

Use at pregnancy and feeding by a breast

Contraindicated in the I trimester of pregnancy. For the period of treatment it is necessary to stop breastfeeding.

Overdose:

Symptoms: effects of suppression of the TsNS function are shown only after reception of high doses (50–120 mg/kg). Such doses can cause vomiting, confusion of consciousness, a coma, respiratory depression and/or epileptic seizures.

Treatment: at the expressed suppression of the TsNS functions it is not recommended to cause vomiting. To wash out a stomach. Purpose of absorbent carbon helps to reduce drug absorption. It is necessary to watch constantly the key physiological parameters and to apply the corresponding symptomatic therapy. At respiratory depression it is possible to carry out IVL. Introduction of stimulators of TsNS is not recommended. It is the best of all to eliminate hypotension in/in administration of liquids and transfer of the patient in the provision of Trendelenburga. If these measures do not recover normal the ABP, it is possible to enter dopamine or noradrenaline. Dialysis and the caused diuresis are inefficient.

As the antagonist it is possible to enter Flumazenil, however its use at overdose of Tofizopamum is clinically not tested.

Storage conditions:

Period of validity of 5 years. List B.: At a temperature of 15-25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets, 50 mg. According to 10 tab. in the blister. 2 or 6 blisters are packed into a cardboard pack.