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TOFISOPAM ® (Grandaxin, Emandaxin)

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Buy Tofisopam (Grandaxin®) Online!

Tofisopam (Grandaxin) is an anti-anxiety medication produced in Hungary and available in several European countries. It is a daytime anxiolytic as it does not have sedative, skeletal muscle relaxant, motor skill-impairing, anticonvulsant or amnestic properties.

Check other products from the ANTI-ANXIETY category. 

 


Synonyms Grandaxin, Emandaxin, Sériel
Form: 20 pills of 50mg / 60 pills of 50mg
Form description: Round, flat tablets of white or greyish-white color in the form of a disc, with a facet and a break line on one side and engraving “GRANDAX” on the other side, without or with almost no smell.
Active ingredient: Tofisopam – 50mg
Excipients: Stearic acid, magnesium stearate, gelatin, talc, potato starch, lactose monohydrate, microcrystalline cellulose.
СAS Number: 22345-47-7
ATC code: N05BA23
Pharmacological action: Anxiolytic
Shelf life: 5 years. Do not use it beyond the expiration date printed on the package.
Storage conditions: Store at temperatures no higher than 15-25°C (59-77°F). Keep in a safe place out of reach of children.
Terms of release: Over-the-counter
Manufacturer: EGIS Pharmaceuticals, Hungary https://int.egis.health/

What is Tofisopam (Grandaxin)?

Grandaxin (Tofisopam) is a non-sedating anxiolytic drug with unique pharmacological action. Tofisopam was first synthesized in 1966 in Hungary and is successfully used for anxiety management since the 1970s.

Tofisopam, the active substance of Grandaxin, is a benzodiazepine tranquilizer. Its pharmacological action differs from that of typical benzodiazepine derivatives. Tofisopam belongs to the 2,3-benzodiazepines family, a unique class of psychoactive substances also known as homophthalazines. Unlike 1,4- benzodiazepine derivatives (e.g Diazepam), Tofisopam does not have sedative and anticonvulsant properties and causes almost no physical or psychological dependence or withdrawal syndrome.

As of today, Grandaxin is used in 15 countries across the world, including Russia, Japan, Hungary, and the Czech Republic. Although this drug is not approved for use in North America, its R-enantiomer is in stage II clinical trials for the treatment of irritable bowel syndrome.

What Does Tofisopam Do?

Tofisopam, the active substance of Grandaxin, has a complicated mechanism of action. It does not bind to benzodiazepine receptors and has a limited affinity to the peripheral benzodiazepine receptors, but it improves the binding of 1,4-benzodiazepines to their receptors. The main effects are due to the stimulation of benzodiazepine receptors in the brain, its excitation leads to an increase in the sensitivity of GABA receptors to the mediator. As a result, GABA-ergic transmission is enhanced: chloride channels work more intensively, hyperpolarization of neuron membranes increases, and neuronal activity decreases.

Several studies suggest that the behavioral effects of Grandaxin are likely to be mediated through its effect on dopaminergic and opioid neurotransmission. Tofisopam may enhance the sensitivity of dopamine receptors and modulate opioid signal transduction in the brain without the danger of addiction.

The drug acts as a phosphodiesterase (PDE) inhibitor with the highest affinity to PDE-4A1, PDE-10A1, PDE-3, and PDE-2A3 which can be responsible for its moderate antipsychotic action.

Grandaxin (Tofisopam) does not impair cognitive functions, you can buy it for its mild stimulant action and the ability to potentiate the effect of dopaminergic stimulants.

What is Tofisopam (Grandaxin) Used For?

Grandaxin is prescribed in the following cases:

  • Neurosis, psychopathy and other conditions accompanied by a feeling of emotional stress, anxiety, and fear;
  • Reactive depression with mild psychopathic symptoms;
  • Premenstrual syndrome, climacteric syndrome;
  • Cardialgia (in the form of monotherapy or in combination with other drugs);
  • Myasthenia gravis, myopathies, neurogenic muscular atrophies and other pathological conditions with secondary neurotic symptoms, when anxiolytics with a pronounced muscle relaxant effect are contraindicated; alcohol withdrawal syndrome.

A course of Grandaxin can also be used for alcohol withdrawal.

Where Can I Order Tofisopam (Grandaxin) Online?

You can order Grandaxin online at different vendors. CosmicNootropic offers Grandaxin in packs of 20x50mg and 60x50mg tablets with fast US delivery and worldwide shipping! Always be sure to do your research before purchasing any nootropic supplement to ensure you are getting a quality product.

You can order Grandaxin and get it delivered to the USA, Europe, the UK, Asia, and many other destinations via CosmicNootropic.

 


Legal Disclaimer
This product has not been approved by the US FDA. All statements on this page are for informational purposes only and have not been evaluated by the US FDA.
This product is not intended to diagnose, treat, cure, or prevent any disease. See more

What is Tofisopam (Grandaxin) Dosage, Administration?

For long-term treatment, the recommended dosage is 1-2 pills, 1-3 times a day. If taken occasionally, the dosage is 1-2 pills.

Geriatric patients and patients with kidney deficiency should take twice less.

The maximum daily dose is 300 mg.

For alcohol withdrawal syndrome or prevention and treatment of delirium, treatment duration is from several days to 3–6 weeks.

What are the Side Effects of Tofisopam (Grandaxin)?

This daytime anxiolytic rarely causes side effects, however, they may include:

  • Allergic reactions;
  • Decreased appetite;
  • Constipation;
  • Flatulence;
  • Nausea;
  • Dry mouth;
  • Headache;
  • Insomnia;
  • Irritability;
  • Agitation;
  • May provoke seizures in patients with epilepsy;
  • Skin rash, itching;
  • Muscle tension.

To prevent sleep disorders, the drug should be taken no later than 3-4 p.m.

Overdose

Effects on the central nervous system suppression manifest themselves only after high doses (50–120 mg/kg). Such doses can cause vomiting, confusion, coma, respiratory depression and/or epileptic seizures.

 

Contraindications

  • Hypersensitivity to Tofisopam or other benzodiazepines;
  • Conditions accompanied by severe depression, psychomotor agitation, and aggression;
  • Respiratory failure;
  • Pregnancy and lactation;
  • Sleep apnea;
  • Treatment with tacrolimus, sirolimus, and/or cyclosporine.

 

This drug should be taken with caution in patients with acute respiratory distress syndrome, angle-closure glaucoma, epilepsy, and organic brain syndrome.

How does Tofisopam interact with other drugs?

  • Tofisopam may increase the plasma concentration of the drugs metabolized by CYP3A4. Does potentiate the effects of CNS depressants (e.g analgesics, anesthetics, antidepressants, H1-antihistamines, sedatives, and antipsychotics).
  • Hepatic enzyme inducers (alcohol, nicotine, barbiturates, anticonvulsants) may enhance the metabolism of Tofisopam, thus decreasing its efficacy.
  • Some antifungal drugs (Ketoconazole, Itraconazole) may inhibit the metabolism of Tofisopam and increase its concentration in blood plasma.
  • Some antihypertensive drugs (Clonidine, calcium channel blockers) may potentiate the effect of Tofisopam. Beta-blockers may inhibit the metabolism of the drug without affecting its efficacy significantly.
  • Tofisopam may enhance plasma levels of Digoxin.
  • Benzodiazepines may affect the anticoagulant effect of warfarin.
  • Long-term treatment with disulfiram may inhibit the metabolism of Tofisopam.
  • Antacids may affect the absorption of Tofisopam. Omeprazole and Cimetidine do inhibit the metabolism of Tofisopam.
  • Oral contraceptives may inhibit the metabolism of Tofisopam.
  • Tofisopam does decrease the depressant effect of alcohol on the central nervous system.

 

OFFICIAL INSTRUCTION

  1. Varady et al (1975) The clinical evaluation of Grandaxin used in the treatment of outpatients (a multicentric study) https://www.ncbi.nlm.nih.gov/pubmed/7855
  2. Sladka et al (1978) Placebo controlled study with tofisopam in anxious neurosis https://www.ncbi.nlm.nih.gov/pubmed/32724
  3. A Bond, M Lader (1982) A comparison of the psychotropic profiles of tofisopam and diazepam https://www.ncbi.nlm.nih.gov/pubmed/6124424
  4. C Banki (1983) Comparative study with Grandaxin and diazepam in alcohol withdrawal syndrome and gerontopsychiatric diseases https://www.ncbi.nlm.nih.gov/pubmed/6152821
  5. Szego et al (1993) Excerpts from the clinical-pharmacologic and clinical studies of Grandaxin https://www.ncbi.nlm.nih.gov/pubmed/8100114
  6. Klebovich et al (1993) Pharmacokinetics and metabolism of tofizopam (Grandaxin) https://www.ncbi.nlm.nih.gov/m/pubmed/8100113/
  7. Kalashnikov et al (2002) Immunomodulating effects of tofizopam (Grandaxin) and diazepam in vitro https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1781640/
  8. Baek et al (2002) Analysis of tofisopam in human serum by column-switching semi-micro high-performance liquid chromatography and evaluation of tofisopam bioequivalency https://www.ncbi.nlm.nih.gov/pubmed/11933029
  9. Eros et al (2002) A population-based case-control teratologic study of nitrazepam, medazepam, tofisopam, alprazolum and clonazepam treatment during pregnancy https://www.ncbi.nlm.nih.gov/pubmed/11858890
  10. Kato et al (2003) A case in which tofisopam was effective for treatment of paroxysmal supraventricular tachycardia https://www.ncbi.nlm.nih.gov/pubmed/12772593
  11. Arushanian et al (2004) Peculiarities in the effect of tofisopam and valerian extract on short-term memory and anxiety states in healthy humanshttps://www.ncbi.nlm.nih.gov/pubmed/15707009
  12. E Plotnikova, E Beloborodova (2005) Use of grandaxin in hypermotor dysfunction of the biliary ducts in young people https://www.ncbi.nlm.nih.gov/pubmed/17378391
  13. Rundfeldt et al (2010) The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2993883/
  14. Srivastava et al (2014) Current Update on Evidence Based Literature of Tofisopam. https://www.researchgate.net/publication/323746367_Current_Update_on_Evidence_Based_Literature_of_Tofisopam
  15. Hatayama et al (2015) Acute Effects of Oral Tofisopam on Plasma Concentration and Urinary Excretion of Uric Acid and Oxypurinol “Preliminary Communication” https://pubmed.ncbi.nlm.nih.gov/25619490/
  16. Agamamedova and Nikitina (2016) TOFISOPAM: ANXIETY THERAPY IN NEUROLOGIC PROFILE PATIENTS https://www.researchgate.net/publication/310392912_TOFISOPAM_ANXIETY_THERAPY_IN_NEUROLOGIC_PROFILE_PATIENTS
  17. Pattnaik et al (2021) Role of Tofisopam in Post COVID Neuro-psychiatric Sequelae: A Case Series https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8313453/

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