GRANDAXIN (TOFISOPAM)

by L F

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.
     
Grandaxin 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.  

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  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).”
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