Grandaxin (Tofisopam)

grandaxin



Grandaxin (a brand name of Tofisopam) is an anxiolytic drug used in Europe and Russia. It belongs to the benzodiazepine family. However, Grandaxin has a different pharmacological action than other benzodiazepine tranquilizers.

It does not bind to benzodiazepine receptors, does not form dependence and does not have amnesic or muscle relaxant effects in the therapeutic dosage range. The reason for such differences is the chemical structure of Tofisopam. It is a 2,3-benzodiazepine derivative which differs from 1,4-benzodizepines (e.g Alprazolam, Diazepam or Phenazepam)  in the position of the nitrogen atoms.

Grandaxin is marketed as an anxiolytic drug since the 1970s. As of today, it is still popular in Europe and CIS states as an alternative to benzodiazepines.  This drug is not approved for use in the United States. However, its D-enantiomer Dextofisopam is in Phase II clinical trials for Irritable bowel syndrome treatment.


Indications for use


The official indications for use are:

  • Neurosis and neurotic conditions (conditions, accompanied by emotional tension, anxiety, and apathy.)
  • Reactive depression.
  • Adjustment disorder and post-traumatic stress disorder.
  • Climacteric syndrome.
  • Premenstrual syndrome.
  • Alcohol withdrawal syndrome.
  • Myasthenia, myopathy, neurogenic muscle atrophy and other conditions with secondary neurotic symptoms, when the treatment with muscle relaxant anxiolytics is inappropriate.


According to studies, this drug also can be used in the treatment of vertigo, dizziness and/or tinnitus. Several clinical trials performed in Japan suggest that Grandaxin is an effective treatment for these conditions.


Side effects and contraindications


Tofisopam usually tolerated better than typical benzodiazepines. It is not addictive and does not cause sedation. However, it still may cause adverse effects. Possible side effects as suggested by the manufacturer include:

  • Loss of appetite.
  • Constipation.
  • Meteorism.
  • Nausea.
  • Dry mouth.
  • Headaches.
  • Irritability and insomnia.
  • May cause convulsive seizures in epileptic patients.
  • Tension and pain in muscles.
  • Allergic reactions.


The following side effects occur most often in people with developmental disorders, liver and/or kidney disorders, and in elderly patients.

It is not recommended to take Tofisopam for people suffering from chronic psychosis, phobias or obsessive conditions. In this case, treatment can increase the risk of suicidal and aggressive behavior.

Contraindications for use are:

  • Hypersensitivity to the drug.
  • Conditions characterized by pronounced aggressivity, agitation or pronounced depression.
  • Decompensated respiratory failure.
  • Pregnancy and lactation.
  • Sleep apnea.
  • Treatment with cyclosporine, sirolimus and/or tacrolimus.


Should be taken cautiously by patients with acute respiratory failure, respiratory distress, closed glaucoma, epilepsy or organic brain damage (e.g atherosclerosis).


Dosage and how to take


Recommended dosage is 50-100mg 1-3 times a day. The maximum daily dose is 300mg. Elderly patients and patients with renal insufficiency should halve the recommended adult dose.




References
  1. Kyosuke Ichikawa, Yasuo Hattori, Kenji Nakamura “Clinical Evaluation of Tofisopam in the Treatment of Tinnitus and Autonomic Dysfunction.”
  2. Chris Rundfeldt, Katarzyna Socała, Piotr Wlaźcorresponding “The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis.”
  3. Petócz L “Pharmacologic effects of tofizopam (Grandaxin).”
  4. Horváth EJ, Horváth K, Hámori T, Fekete MI, Sólyom S, Palkovits M. “Anxiolytic 2,3-benzodiazepines, their specific binding to the basal ganglia.”
  5. Shruti Srivastava, Manjeet Bhatia, Keshav Gupta, Kartikeya Rajdev “Current update on evidence based literature of Tofisopam.”
  6. Dyukova G.M, Saksonova E.V, Golubev V.L “Grandaxin in Neurologic practice (Multicenter research).”
Here are the user reviews and anecdotal experiences from on-label users. They were translated from Russian language from otzovik website. All kind of reviews included, either negative or positive, sorted by the newest.
5/5

As a person with a volatile temper, I am prone to stress and anxiety. A long road trip, college, then pregnancy, then my husband was recruited to the army. All this has accumulated over time. And one day, when everything seemed to be good, my husband and child were with me, my nerves gave up. I fell into depression. Never experienced it before. Each day my condition gets worse, I eat nothing, left the college, didn’t care about my kid… Everything started going to hell. Went to a doctor but he didn’t

And one day, when everything seemed to be good, my husband and child were with me, my nerves gave up. I fell into depression. Never experienced it before. Each day my condition gets worse, I eat nothing, left the college, didn’t care about my kid… Everything started going to hell. Went to a doctor but he didn’t

Everything started going to hell. Went to a doctor but he didn’t help much.  So I decided to visit a psychiatrist. His diagnosis was: moderate depression with anxiety disorder and exhausted nervous system. He suggested antidepressant for me, but I refused it. Then he offered Grandaxin which pulled me out of this terrible condition.

The drug starts to act after two hours after ingestion.  It brings the feeling of indifference and relieves anxiety. I was prescribed with one pill twice daily. But then I experienced side effects like the apathetic feeling in the first half hour, then slight difficulties breathing, after about an hour these problems goes away and you simply start to see this world from a different angle. Doctor suggested to take half of the pill four times a day, we’ll see what happens. For now I took it for three days and already noticed that it helps me with my depression. My hands no longer shaking from nerves, I stopped crying, became more active and started to come back to life.

Grandaxin was prescribed along with the other medications and vitamins. A very good drug. If your doctor prescribed it for you – take it. I will finish the course and will tell how it helped.

5/5

The doctor prescribed for me Paxil and Grandaxin because of my panic attacks. I decided not to take Paxil because of its huge list of side effects but decided to try Tofisopam. The main problem is the fear of going outside in the morning, the fear was so intense that I always reached my car in presyncope. You need to take two pills daily, one at the morning and one at the lunch, it is not recommended to take it later to avoid sleeping problems. In the first week, I think I felt worse but later I started to feel the effect. I became calmer, less fearful, not suffer from racing heart as much as before, noticed an overall improvement. At least I can reach my car without any problems now which is already good. Taken it for 20 days, now took a break and I think I will take another 20-day course in April, despite my doctor’s suggestion that I can take it for three months without a break. So, my opinion is that this drug helps but does not relieve panic attacks completely. I suggest you hold the breath and let it out slowly, then repeat, it calms you down fast.

4/5

It happened so that all my problems and troubles fell on me simultaneously. Irritability showed up at first, then a mental breakdown, and as a result – insomnia. Even after a hard day full of physical work I was able to fall asleep because of my exhaustion, but not for long. Woke up midnight, with a head full of bad thoughts, and I could just lay in the bed until morning without falling asleep. Of course, at the morning I was broken, tired, with terrible mood. I even had a fever sometimes, that’s so unpleasant! Novo-Passit no longer helps, just as other sedatives like motherwort or valerian root.

Thankfully, my daughter-in-law visited me and suggested to try Grandaxin. I inspected the package insert carefully and decided to take two pills. As for me, this drug helped immediately. I calmed down, can’t say I calmed down completely but my anxious state has gone, I wasn’t nervous about, and what’s the main thing, is that my sleep has normalized. I could not believe my eyes as it was 6 AM when I woke up. Before that, I could sleep only until 3 AM. Started to think less about bad things, my overall condition improved.

It is recommended to take Grandaxin by courses, but I afraid to become dependent on it, so I stopped taking it and will see what happens next. So, for people who have the same symptoms, I suggest to try Tofisopam after consulting with a doctor.

1/5

I heard about Grandaxin long time ago and saw lots of feedbacks. Recently I started to suffer from panic attacks. Went to a doctor and he prescribed this drug for me. Took it for four days, couldn’t take it anymore, didn’t notice anything but side effect. The side effects I’ve noticed is complete loss of appetite, excess saliva production and the panic attacks only got more frequent.

5/5

That’s a good tranquilizer which is available without a prescription. It has a cumulative action, and the only side effect is sleepiness after taking more than two pills in three hours period. After a short nap this effect disappears, but still, it’s better not to take too much or drive a car after taking it. I tried Grandaxin in a stressful situation when I was told that my friend had died. It kicked in about 15 minutes after ingestion, felt a feeling of indifference. It did not affect my actions, I was able to think clearly as before, but my emotional pain has relieved.

The drug is good, I took it regularly for three days and then stopped, but the effects lasted for three days more, calming down my emotions. No negative consequences after that, no drowsiness, sleepiness or any problems with health. If you, god forbid, experience stress – try Grandaxin as a tranquilizer, I liked it.

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