Grandaxin
Grandaxin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Use in childhood
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Grandaxin
ATX code: N05BA23
Active ingredient: Tofisopam (Tofisopam)
Producer: JSC Pharmaceutical Plant EGIS, Hungary
Description and photo update: 2019-07-08
Prices in pharmacies: from 324 rubles.
Buy
Grandaxin is a drug with anxiolytic action.
Release form and composition
Grandaxin is produced in the form of tablets: grayish-white or white, round, flat, beveled, odorless or almost odorless, with the inscription "GRANDAX" on one side and with a line on the other (10 pcs. In blisters, each 2 or 6 blisters in a cardboard box).
The composition of 1 tablet includes:
- Active ingredient: tofisopam - 50 mg;
- Auxiliary components: stearic acid - 1 mg; magnesium stearate - 1 mg; gelatin - 3.5 mg; talc - 2 mg; potato starch - 20.5 mg; lactose monohydrate - 92 mg; microcrystalline cellulose - 10 mg.
Pharmacological properties
Pharmacodynamics
Tofisopam - the active ingredient of Grandaxin - is an atypical benzodiazepine derivative, which is characterized by an anxiolytic effect, practically not accompanied by anticonvulsant, muscle relaxant and sedative effects. It refers to psychovegetative regulators that eliminate various forms of autonomic disorders. Tofisopam is characterized by moderate stimulating activity. Since there is no muscle relaxant effect, it is allowed to prescribe Grandaxin to patients with myasthenia gravis and myopathy.
Due to the atypical chemical structure, the drug, when taken in recommended doses, practically does not lead to the development of withdrawal syndrome, as well as physical and mental dependence. Grandaxin is a daytime anxiolytic.
Pharmacokinetics
When taken orally, tofisopam is rapidly and almost completely absorbed from the gastrointestinal tract. The maximum concentration of the substance in the blood plasma is reached 2 hours after ingestion, after which its level falls monoexponentially. Tofisopam is not characterized by a cumulative effect, and its metabolites have no pharmacological activity. The active component of Grandaxin is excreted mainly through the kidneys (60-80%) in the form of conjugates with glucuronic acid and to a lesser extent (about 30%) through the intestines. The half-life is 6-8 hours.
Indications for use
- Neurosis-like states (conditions accompanied by autonomic disorders, emotional stress, apathy, moderate anxiety, obsessive experiences, decreased activity) and neuroses;
- Cardialgia (as monotherapy or concurrently with other drugs);
- Reactive depression with mild psychopathological symptoms;
- Post-traumatic stress disorder (mental adjustment disorder);
- Premenstrual tension syndrome;
- Climacteric syndrome (as monotherapy or simultaneously with hormonal drugs);
- Myopathies, neurogenic muscle atrophy, myasthenia gravis and other pathological conditions with secondary neurotic symptoms in cases where it is contraindicated to use anxiolytic drugs with a pronounced muscle relaxant effect;
- Alcohol withdrawal syndrome.
Contraindications
- Respiratory failure in the stage of decompensation;
- Conditions that are accompanied by severe psychomotor agitation, deep depression or aggressiveness;
- Sleep apnea syndrome (history);
- Simultaneous use with sirolimus, tacrolimus, cyclosporine;
- Congenital lactase deficiency, galactose intolerance, glucose and galactose malabsorption syndrome (Grandaxin contains lactose monohydrate);
- First trimester of pregnancy and lactation (breastfeeding);
- Hypersensitivity to the components of the drug or any other benzodiazepines.
Grandaxin should be taken with caution in patients with a history of acute respiratory failure, decompensated chronic respiratory distress syndrome, epilepsy, angle-closure glaucoma, organic brain lesions (for example, with atherosclerosis).
Instructions for the use of Grandaxin: method and dosage
The dosage regimen is set individually, taking into account the clinical form of the disease, the patient's condition and individual sensitivity to the action of the drug.
For adults, Grandaxin is prescribed 1-3 times a day, 1-2 tablets (50-100 mg). The maximum daily dose is 300 mg. With irregular use of the drug, you can take 1-2 tablets.
With renal failure and elderly patients, the daily dose of Grandaxin should be reduced by about 2 times.
Side effects
During therapy with Grandaxin, the development of disorders from some body systems is possible:
- Digestive system: dry mouth, nausea, constipation, decreased appetite, flatulence; in some cases - cholestatic jaundice;
- Central nervous system: confusion, insomnia, headache, psychomotor agitation, increased irritability, seizures in patients with epilepsy;
- Respiratory system: respiratory depression;
- Musculoskeletal system: muscle pain, muscle tension;
- Allergic reactions: exanthema (including scarlet fever), pruritus.
Overdose
When Grandaxin is taken orally in high doses (50–120 mg / kg body weight), symptoms of inhibition of the central nervous system may occur: blurred consciousness, vomiting, depression of the respiratory center and / or epileptic seizures, coma.
With pronounced suppression of central nervous system functions, vomiting should not be induced. Gastric lavage is recommended. The appointment of activated carbon reduces the absorption of the drug. It is necessary to constantly monitor the basic physiological parameters and conduct appropriate symptomatic therapy. Respiratory depression is an indication for mechanical ventilation. Administration of CNS stimulants is not recommended.
The hypotension is preferably treated by intravenous fluids and placing the patient in a Trendelenburg position. If these measures do not lead to normalization of blood pressure, administration of norepinephrine (norepinephrine) or dopamine is allowed. The effectiveness of dialysis and forced diuresis has not been proven. In emergency cases, it is possible to use flumazenil, a specific benzodiazepine antagonist, but its use in case of an overdose of tofisopam has not been studied enough.
special instructions
In elderly patients, as well as in patients with impaired liver and / or kidney function, delayed mental development, side effects may be observed more often than others.
According to the instructions, Grandaxin is not recommended to be taken as monotherapy for depression or depressive conditions accompanied by anxiety (due to the high risk of suicidal attempts and aggressive behavior).
Care should be taken when using Grandaxin in patients with depersonalization, as well as with organic brain lesions (for example, with atherosclerosis).
In patients with epilepsy, tofisopam may increase the seizure threshold.
Each tablet contains 92 mg of lactose, which must be taken into account by patients with lactose intolerance.
Grandaxin has no significant effect on attention and ability to concentrate.
Pediatric use
In pediatric practice, Grandaxin is not used.
Drug interactions
Simultaneous use of Grandaxin with tacrolimus, sirolimus and cyclosporine is contraindicated.
Tofisopam reduces the depressing effect of ethanol on the central nervous system.
With the simultaneous use of Grandaxin with certain drugs, the following undesirable effects may occur:
- Drugs that suppress the functions of the central nervous system (analgesics, antidepressants, agents for general anesthesia, blockers of histamine H1 receptors, hypnotics, sedatives and antipsychotic drugs) - enhance their effects;
- Some antifungal drugs (itraconazole, ketoconazole) - it is possible to slow down the hepatic metabolism of tofisopam, which leads to an increase in its concentration in the blood plasma;
- Liver enzyme inducers (barbiturates, ethanol, antiepileptic drugs, nicotine) - it is possible to increase the metabolism of tofisopam, which can lead to a weakening of its therapeutic effect;
- Beta-blockers - it is possible to slow down the metabolism of tofisopam (has no clinical significance);
- Oral contraceptives - a decrease in the metabolic rate of tofisopam is possible;
- Some antihypertensive drugs (calcium channel blockers, clonidine) - may increase the effects of Grandaxin;
- Benzodiazepines, including tofisopam - possibly affecting the anticoagulant effect of warfarin;
- Digoxin - an increase in its level in blood plasma is possible;
- Antacids - it is possible to change the absorption of tofisopam;
- Disulfiram (long-term simultaneous use) - it is possible to inhibit the metabolism of tofisopam;
- Omeprazole and cimetidine - inhibition of the metabolism of tofisopam.
Analogs
Analogues of Grandaxin are: Afobazol, Diazepam, Gidazepam, Relanium, Neurol, Tazepam, Phenazepam.
Terms and conditions of storage
Store in a dark, dry place out of reach of children at a temperature of 15-25 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Grandaxin
Reviews about Grandaxin among doctors are mostly positive. With a properly selected treatment regimen, side effects during treatment are practically not observed.
The drug is often prescribed for nervous disorders. It has a sedative effect and relieves anxiety and tension well.
Patients note that clinically significant improvement is observed approximately one week after the start of therapy. Some patients report the occurrence of adverse reactions: weakness, drowsiness, dizziness.
Grandaxin effectively eliminates one of the most characteristic symptoms of menopause - neurotic disorder.
Price for Grandaxin in pharmacies
The approximate price for Grandaxin is 385-430 rubles for a pack of 20 tablets, or 810-900 rubles for a pack of 60 tablets.
Grandaxin: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Grandaxin 50 mg tablets 20 pcs. 324 r Buy |
|
Grandaxin tablets 50mg 20 pcs. 391 r Buy |
|
Grandaxin 50 mg tablets 60 pcs. 765 RUB Buy |
|
Grandaxin tablets 50mg 60 pcs. 813 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
