Tofisopamum

Tofisopamum Uses, Dosage, Side Effects, Food Interaction and all others data.

Tofisopamum (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 Tofisopamum 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 Tofisopamum
Generic Tofisopam
Tofisopam Other Names Tofisopam, Tofisopamum
Type
Formula C22H26N2O4
Weight Average: 382.4528
Monoisotopic: 382.18925733
Groups Experimental
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Tofisopamum
Tofisopamum

Uses

For the treatment of anxiety and alcohol withdrawal.

Tofisopamum is also used to associated treatment for these conditions: Anxiety, Depression, Fatigue

How Tofisopamum works

Tofisopamum 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

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*** Taking medicines without doctor's advice can cause long-term problems.
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