Grandaxin® (Grandaxin®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceTofizopamTofizopam
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  • Grandaxin®
    pills inwards 
    EGIS ZAO Pharmaceutical Plant     Hungary
    • Dosage form: & nbsppills
    Composition:1 tablet contains 50 mg active substance - tofizopama, as well as 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, cellulose microcrystalline 10 mg.
    Description:Round, flat pills in the form of a disc, white or grayish-white, with a bevel, engraved "GRANDAH" on one side and with a risk on the other side, odorless or almost odorless.
    Pharmacotherapeutic group:Anxiolytic agent (tranquilizer)
    ATX: & nbsp

    N.05.B.A.23   Tofizopam

    Pharmacodynamics:
    The drug from the group of benzodiazepine derivatives (an atypical benzodiazepine derivative), has an anxiolytic effect, practically not accompanied by sedative, miorelaxing, anticonvulsant action. It is a psycho-vegetative regulator, it removes various forms of vegetative disorders. Has moderate stimulating activity.
    Due to the lack of a muscle relaxant effect, the drug can be used in patients with myopathy and myasthenia gravis. Due to the atypical nature of the chemical structure,In contrast to classical benzodiazepine derivatives, Grandaxin in therapeutic doses practically does not cause the development of physical, mental dependence and withdrawal syndrome. Grandaxin refers to daytime anxiolytics.
    Pharmacokinetics:When ingested quickly and almost completely absorbed from the gastrointestinal tract. The maximum concentration in the blood is reached within 2 hours, after which the concentration in the plasma decreases monoexponentially. Tofizopam not cumulated in the body. Metabolites do not have pharmacological activity. It is excreted mainly in the urine (60-80%) in the form of conjugates with glucuronic acid and, to a lesser extent (about 30%), with feces. The half-life is 6-8 hours.
    Indications:
    - Neuroses and neurosis-like conditions (conditions accompanied by emotional stress, vegetative disorders, moderately expressed anxiety, apathy, decreased activity, obsessive experiences;
    - Reactive depression with moderate psychopathological symptoms;
    - Disorder of mental adaptation (post-traumatic stress disorder)
    - Climacteric syndrome (as an independent agent, as well as in combination with hormonal drugs);
    - Premenstrual syndrome;
    - Cardialgia (in the form of monotherapy or in combination with other drugs);
    - Alcohol abstinence syndrome;
    - Myasthenia gravis, myopathy, neurogenic muscular atrophy and other pathological conditions with secondary neurotic symptoms, when anxiolytics with pronounced myorelaxing action are contraindicated.
    Contraindications:
    - Hypersensitivity to the active or any other component of the drug or any other benzodiazepines;
    - conditions accompanied by severe psychomotor agitation, aggressiveness or severe depression;
    - Decompensated respiratory failure;
    - I trimester of pregnancy and the period of breastfeeding;
    - respiratory failure syndrome in a dream (in the anamnesis);
    - simultaneous application with tacrolimus, sirolimus, cyclosporin;
    - intolerance to galactose, congenital insufficiency of lactase or glucose malabsorption syndrome and galactose (the preparation contains lactose monohydrate).
    Carefully:Decompensated chronic respiratory distress, acute respiratory failure in history, angle-closure glaucoma, epilepsy, organic brain damage (eg, atherosclerosis).
    Dosing and Administration:
    The dosage regimen is set individually, taking into account the patient's condition, clinical form of the disease and individual sensitivity to the drug.
    Adults appoint 50-100 mg (1-2 tablets) 1-3 times a day.
    With occasional use, you can take 1-2 tablets.
    The maximum daily dose is 300 mg.
    For elderly patients and patients with renal insufficiency, the daily dose is reduced approximately 2-fold.
    Side effects:

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

    From the side of the central nervous system: headache, insomnia, increased irritability, agitation, psychomotor agitation, confusion may occur, convulsive seizures may occur in patients with epilepsy.

    Allergic reactions: exanthema, scarlet fever-like exanthema, itching.

    Musculoskeletal system: muscle tension, muscle pain.

    Respiratory system: respiratory depression.

    Overdose:

    Symptoms: Effects of suppression of the central nervous system function are manifested only after taking high doses (50-120 mg / kg body weight). Such doses may cause vomiting, confused consciousness, coma, respiratory depression and / or epileptic seizures.

    Treatment: When expressed suppression of the functions of the central nervous system is not recommended to induce vomiting. Rinse the stomach. The introduction of activated charcoal helps to reduce the absorption of the drug. It is necessary to constantly monitor the basic physiological parameters and apply appropriate symptomatic therapy. With respiratory depression, it is possible to carry out artificial ventilation of the lungs. Introduction of CNS stimulants is not recommended. Hypotension is best eliminated by intravenous infusion of liquids and transfer of the patient to Trendelenburg position. If these measures do not restore normal blood pressure, you can enter dopamine or norepinephrine. Dialysis and diuresis are not effective. As an antagonist, one can introduce Flumazenil, but its use with an overdose of tophisopam has not been clinically tested.

    Interaction:
    The simultaneous use of tacrolimus, sirolimus, cyclosporine and tofizopama is contraindicated. Plasma concentrations of drugs that are metabolized by CYP3 A4 may increase with simultaneous admission with tofizopam. The use of tofizopam with drugs that suppress the functions of the central nervous system (analgesics, general anesthetics, antidepressants, H1-antigistamine, sedative-hypnotic, antipsychotic) enhances their effects (for example, sedation or respiratory depression).
    Inductors of hepatic enzymes (alcohol, nicotine, barbiturates, antiepileptic drugs) can increase the metabolism of tofizopam, which can lead to a decrease in its concentration in the blood plasma and a weakening of the therapeutic effect. Some antifungal drugs (ketoconazole, itraconazole) can slow the hepatic metabolism of tofizopam, which leads to an increase in its concentration in the blood plasma.
    Some antihypertensive drugs (clonidine, calcium channel antagonists) can potentiate the effects of tofosopam. β-blockers can slow the metabolism of the drug, but this effect has no clinical significance.
    Tofizopam can increase the level of digoxin in the blood plasma. Benzodiazepines can affect the anticoagulant effect of warfarin. Long-term use of disulfiram can inhibit tofizopam metabolism. Antacids can affect the absorption of Tofizopam. Cimetidine and omeprazole inhibit the metabolism of Tofizopam.
    Oral contraceptives can reduce the intensity of tofosopam metabolism.
    Tofizopam weakens the depressant effect of alcohol on the central nervous system.
    Special instructions:
    It should be noted that in patients with mental retardation, elderly patients, as well as those with impaired renal and / or liver function, side effects may be more likely than other patients.
    It is not recommended to apply tophysopam with chronic psychosis, phobia or obsessive states. In these cases, the risk of suicidal attempts and aggressive behavior increases. therefore tophysopam It is not recommended as a monotherapy for depression or depression accompanied by anxiety.
    Care must be taken when treating patients with depersonalization, as well as organic brain damage (eg, atherosclerosis).
    In patients with epilepsy tophysopam can raise the threshold of convulsive readiness. Each Grandaxin® tablet contains 92 mg of lactose, which should be taken into account for patients with lactose intolerance (see Contraindications section).
    Effect on the ability to drive transp. cf. and fur:Grandaxin® significantly reduces attention and the ability to concentrate.
    Form release / dosage:Tablets 50 mg.
    Packaging:10 pieces in a blister pack. 2 or 6 blisters together with instructions for use are packed in a cardboard box.
    Storage conditions:
    Store the drug at a temperature of 15 to 25 ° C. Keep out of the reach of children.
    Shelf life:
    5 years.
    Do not use after the expiration date indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N013243 / 01
    Date of registration:16.09.2011 / 06.12.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Manufacturer: & nbsp
    Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Information update date: & nbsp07.05.2017
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