TOFISOPAM (Grandaxin ®)
24 Reviews
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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.
Grandaxin review by Boost Your Biology Expert – Lucas Aoun!
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 from 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
- 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
- Sladka et al (1978) Placebo controlled study with tofisopam in anxious neurosis https://www.ncbi.nlm.nih.gov/pubmed/32724
- A Bond, M Lader (1982) A comparison of the psychotropic profiles of tofisopam and diazepam https://www.ncbi.nlm.nih.gov/pubmed/6124424
- C Banki (1983) Comparative study with Grandaxin and diazepam in alcohol withdrawal syndrome and gerontopsychiatric diseases https://www.ncbi.nlm.nih.gov/pubmed/6152821
- Szego et al (1993) Excerpts from the clinical-pharmacologic and clinical studies of Grandaxin https://www.ncbi.nlm.nih.gov/pubmed/8100114
- Klebovich et al (1993) Pharmacokinetics and metabolism of tofizopam (Grandaxin) https://www.ncbi.nlm.nih.gov/m/pubmed/8100113/
- Kalashnikov et al (2002) Immunomodulating effects of tofizopam (Grandaxin) and diazepam in vitro https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1781640/
- 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
- 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
- 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
- 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
- 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
- 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/
- 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
- 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/
- Agamamedova and Nikitina (2016) TOFISOPAM: ANXIETY THERAPY IN NEUROLOGIC PROFILE PATIENTS https://www.researchgate.net/publication/310392912_TOFISOPAM_ANXIETY_THERAPY_IN_NEUROLOGIC_PROFILE_PATIENTS
- 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/
4.5
Based on 24 Reviews
(19)
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(0)
(2)
05/18/2023
James Q.
Verified BuyerUS
Didn't work for me
I did not experience any effects from Grandaxin (positive or negative).I'm aware that medicines vary in their effectiveness, & I hope that there maybe other medications out there that work for me.
05/19/2023
Hi James, thank you for taking the time to share your experience with Grandaxin. We appreciate your feedback and we're sorry to hear that the product did not provide the desired effects. We hope that you will find a product that will be effective for you. If you have any further questions or concerns, please don't hesitate to reach out to us!
03/26/2023
Nicholas E.
Verified BuyerUS
Subtle effect
I’d describe the effect of this compound as a slight cognitive boost. It’s just effective enough to realize that it’s not a placebo- nothing exceptionally good. I don’t think I’ll repurchase, but yet it was worth trying out.
03/26/2023
Thanks for sharing your review! We hope you will soon find a more suitable product for your needs at our store :)
02/24/2023
John S.
Verified BuyerUS
Drug designed for daytime
It works well. There was lessened anxiety but it didn't annihilate it completely. It does it's job as a DAYTIME tranquilizer, so it's not as effective as Xanax or Phenibut. Phenibut is considered one but not designed for that purpose. You also need to dose consistently.
02/24/2023
Hi John! Thank you for your feedback! We're happy that our product helps you.
01/17/2023
Jacob L.
Verified BuyerUS
Never got to try.
Probably was great but never got to try. Said delivered a long time ago just now getting to review. Unfortunately I never found at my door/mail. Nothing to fault cosmic for!
12/08/2022
Matt S.
Verified BuyerUS
It was good
It was good med overall but it made me jittery it relaxed my mind but not my body
12/08/2022
Hi Matt! Thank you for sharing your experience! For most nootropics, the effect can be varied for different people. It strongly depends on the personal conditions, so we always recommend consulting a specialist before taking any medication.
10/20/2022
Tony
Verified BuyerUS
Does little if anything
So I suffer from panic disorder and PTSD I'm prescribed a regular benzo and I have a high tolerance to benzodiazepines however when I'm off benzos and I started taking this medicine I noticed no difference in my anxiety or any mild stimulant effect either I'm not sure what I'm doing wrong maybe it takes a long time for your body to get used to it I don't know but it's not doing much if anything for me but again that's my experience for other people may differ but I do think this website is amazing and I will continue to use it
10/24/2022
Thank you for your feedback. We're sorry you didn't feel the effect you expected, but hopefully, you can find a product that helps you in the future. Best wishes for your health!
09/04/2022
Eric F.
Verified BuyerUS
Great
Yep worked great
07/25/2022
Nicolas
Verified BuyerUS
Surprisingly Good !!
Trying to wing off of Kratom and Phenibut, and this stuff has definitely worked pretty well. I was able to finally to get off of certain substances and to take my mind off of wanting to take dopamine excitatory substances. It has a slight OCD reduction and doesn’t have that addiction component. But you have to be patient with it, for me it didn’t work until day 3 for the effects to fully work and when it does, it feel like high dose lexapro without the weight gain. I’m truly pleased :)
08/03/2022
Hi Nicolas, Thanks for sharing your experience! We're glad that the product works well for you. :) Please note that we always recommend consulting a specialist before taking any meds.
06/18/2022
Shaun S.
Verified BuyerUS
An interesting alternative to mainstream benzodiazepines
I found this particular nootropic to be useful both for it’s anxiolytic properties as well as, perhaps more so, for its subtle yet synergistic stimulating properties. An anxiolytic that is also stimulating has a two fold recourse either for recovery from benzodiazepine or alcohol dependency or generally in terms of functionality and productivity..
08/01/2022
Hi Shaun, Thanks so much for sharing your experience with us!
06/06/2022
Julia
Verified BuyerUS
Grandaxin
I am very sensitive to all meds, so I couldn't take it every day even at smaller dose due to side effects. However, the customer service is excellent !
08/01/2022
Hi Julia, I'm sorry that Grandaxin didn't suit you. 😔 And thanks for the feedback on our work, it is really important for us!
02/24/2022
Ashley
Verified BuyerUS
Be Careful-Potentially Addicting
Very worried that Grandaxin is now causing me benzo withdrawals despite claims that it is non habit forming. I had taken it for 3 weeks 2x a day or less and am now on day 3 of severe panic attacks and anxiety after it is no longer effective. I switched over to Clonazepam to see if I could get some relief and am also not responding to that benzo. I have never taken Clonazepam so I am very distressed to think that Grandaxin is causing me some kind of crossover tolerance/withdrawal. If I don’t get relief tonight I’m going to end up in the hospital. I went out of my way seeking this drug to provide me relief from tinnitus and anxiety in a non intoxicating non habit forming away. Very very upset it may have caused me an addiction in very little time to deal with.
07/24/2022
Hi Ashley, We're very sorry to hear about your experience. We have not received any reports of such an effect before and are very concerned. Thank you for sharing your experience. We will place a disclaimer based on your feedback.
02/06/2022
Jessica F.
Verified BuyerUS
No more panic
I bought this as well as the afobazole. I have only been taking 1 of each a day and it was just this morning like a month after I started taking them that I realized I have not had a panic attack since I started taking them. So it’s subtle, but for me that’s exactly what I need. I’m a recovering addict so I don’t wanna take all the drugs the doctors in the US would prescribe. But I was having massive panic attacks before taking this. Last time I had one at my doctors office my heart rate was 152. I was miserable, I couldn’t function, it physically hurt. I’m so grateful for this I hope they get it in the US again soon, I’m not familiar with US customs but I don’t have money to spare and can’t risk it getting snatched at customs. Thank you for making this available to people in the US. I feel like it has been life changing so far.
12/04/2021
Jason L.
Verified BuyerUS
Blissful Relief.
fast shipping, quality product.
08/31/2021
Pettclan
Verified BuyerUS
Works well for anxiety, nightmares, stress, and tention.
Ordered this for my 29yo daughter that has severe anxiety and panic attacks due to experiences growing up with her mom and abusive step-dad. Shipping took a bit longer than I expected from USA to USA, but not as long as shipping from outside the USA. She started by taking half of one and about an hour later described the feeling as being just kind of a bit off. I suggested she take the other half which she then did. Asked again about an hour later how she felt. She described it as the anxiety was still there, but in the background instead of raging in the foreground as it usually does. Said it felt a bit odd, but I explained that it might be due to not feeling the same as prescription anti-anxiety medication like Ativan or Xanax that she has had in the past due to this one not having the body effects, amnesiac effects, etc the others do. She was able to function much better throughout the day as she normally has trouble even going outside by herself. She took another half in the late afternoon. She also has night terrors and nightmares, but the next morning told me that although she still had some bad dreams, didn't have any night terrors or nightmares. I personally don't suffer from anxiety, but I also took half of one that same morning to see how it affected me. For me it caused stress and tension I deal with to fade into the background. It was easier to accomplish things I would normally put off. Daughter said she noticed I was more relaxed throughout the day and not as edgy as I normally can be. So all in all it was very worth getting, and I will probably re-order another batch in the future. Just an FYI: everyone has different body chemistry, so it may or may not have the same effects for you. Best suggestion is give it a try. If it works for you, great! If it doesn't, then give something else a shot.
08/13/2021
Mia P.
Verified BuyerUS
Good Quality!
So far, this product has been very helpful using it as-needed for stress and anxiety. It was very helpful on a stressful weekend of traveling, helped me stay calm and collected on a plane without being sedated.
07/14/2021
Bernadine F.
Verified BuyerNL
Good product
Makes me calm without feeling drowsy, just half a tablet is enough for me. Lightning fast shipping from this vendor. Will buy again. Thanks!
05/28/2021
Liudmyla V.
Verified BuyerUS
Works well
Good, lasting long and works with one dose
03/10/2021
Bagz
Verified BuyerAU
It works and works very well!
I've been searching for a Phenibut replacement for some time now since it became prohibited in Australia, Picamilon, Pantogam and others have been unable to scratch that itch. Hello Tofisopam, the first time I tried I tried this was 1 x50mg pill and after an hour I felt a warm and relaxing tingling sensation, I was not expecting it to work and when it was clearly doing something the surprise ironically triggered a panic attack but this is likely due to my own existing issues and not a problem with the drug. Now that I know how the drug works and feels I can confidently use it at 50mg or 100mg doses with a 50mg top-up around midday depending on my level of stress and events planned for that day. It is stimulating and calming which may sound weird but its so much better than anxiolytic meds that sedate you. My only concern is it's strange mechanism of action compared to traditional benzos and the lack of English studies online, but hey it works and is exactly as advertised.
02/16/2020
Sam C.
Verified BuyerGreat product
Really helps my anxiety attacks
01/27/2020
matthew c.
Verified BuyerCalming
First day taking felt an easiness of the day. No surprise moments. Productive and not worried. Good product.
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