Grandaxin 10%
Grandaxin 10% Uses, Dosage, Side Effects, Food Interaction and all others data.
Grandaxin 10% (marketed under brand names Emandaxin and Grandaxin) is a 2,3-benzodiazepine drug which is a benzodiazepine derivative. In contrast to classical 1,4-benzodiazepines, the compound does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor and its psychopharmacological profile differs from such compounds. Although Grandaxin 10% is not approved for sale in North America, it is approved for use in various countries worldwide, including parts of Europe. The D-enantiomer (dextofisopam) is currently in phase II trials in the U.S. for the treatment of irritable bowel syndrome.
Like other benzodiazepines, tofisopam possesses anxiolytic properties but unlike other benzodiazepines it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. It enhances the anticonvulsant activity of 1,4-benzodiazepines like diazepam but not sodium valproate, carbamazepine, phenobarbital, or phenytoin.
| Trade Name | Grandaxin 10% |
| Generic | Tofisopam |
| Tofisopam Other Names | Tofisopam, Tofisopamum |
| Type | |
| Formula | C22H26N2O4 |
| Weight | Average: 382.4528 Monoisotopic: 382.18925733 |
| Groups | Experimental |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Japan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
For the treatment of anxiety and alcohol withdrawal.
Grandaxin 10% is also used to associated treatment for these conditions: Anxiety, Depression, Fatigue
How Grandaxin 10% works
Grandaxin 10% does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor. One study (Rundfeldt C. et al.) has shown that tofisopam acts as an isoenzyme-selective inhibitor of phosphodiesterases (PDEs) with highest affinity to PDE-4A1 (0.42 μM) followed by PDE-10A1 (0.92 μM), PDE-3 (1.98 μM) and PDE-2A3 (2.11 μM).
Toxicity
The onset of impairment of consciousness is relatively rapid in benzodiazepine poisoning. Onset is more rapid following larger doses and with agents of shorter duration of action. The most common and initial symptom is somnolence. This may progress to coma (Grade I or Grade II) following very large ingestions. Oral, rat LD50 is 825 mg/kg.
Half Life
6-8 hours
Innovators Monograph
You find simplified version here Grandaxin 10%
