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Tofisopam



Tofisopam
Systematic (IUPAC) name
6-(3,4-dimethoxyphenyl)-2-ethyl-9,10-dimethoxy-3-methyl
-4,5-diazabicyclo[5.4.0]undeca-3,5,7,9,11-pentaene
Identifiers
CAS number 22345-47-7
ATC code N05BA23
PubChem 5502
DrugBank ?
Chemical data
Formula C22H26N2O4 
Mol. mass 382.5
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life 6-8 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

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Legal status

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Routes Oral

Tofisopam (marketed under brand names Emandaxin and Grandaxin) is a drug which is a benzodiazepine derivative. Like other benzodiazepines, it possesses anxiolytic properties but unlike other benzodiazepines it does not have anticonvulsant, sedative,[1] skeletal muscle relaxant, motor skill-impairing or amnestic[2] properties. While it may not be an anticonvulsant in and of itself, it has been shown to enhance the anticonvulsant action of classical 1,4-benzodiazepines such as diazepam (but not sodium valproate, carbamazepine, phenobarbital, or phenytoin).[3] Tofisopam is indicated for the treatment of anxiety and alcohol withdrawal, and is prescribed in a dosage of 50 - 300mg per day divided into three doses. Peak plasma levels are attained two hours after an oral dose. Tofisopam is not reported as causing dependance to the same extent as other benzodiazepines, but is still recommended to be prescribed for a maximum of 12 weeks. [4]

Additional recommended knowledge

Tofisopam is not approved for sale in the United States or Canada. However, Vela Pharmaceuticals of New Jersey is developing the D- enantiomer (dextofisopam) as a treatment for irritable bowel syndrome.[5]

References

  1. ^ Bond, A; M. Lader (1982). "A comparison of the psychotropic profiles of tofisopam and diazepam.". European Journal of Clinical Pharmacology 22 (2): 137-42. PubMed.
  2. ^ Seppala, T; Palva E, Mattila MJ, Korttila K, Shrotriya RC (1980). "Tofisopam, a novel 3,4-benzodiazepine: multiple-dose effects on psychomotor skills and memory. Comparison with diazepam and interactions with ethanol". Psychopharmacology (Berlin) 69 (2): 209-18. PubMed.
  3. ^ Saano, V. (1986). "Tofizopam selectively increases the action of anticonvulsants". Medical Biology 64 (4): 201-6. PubMed.
  4. ^ http://www.biam2.org/www/Sub1469.html
  5. ^ Vela Pharmaceuticals (2005). Vela Announces Positive Phase 2 Results for Dextofisopam in Treating Irritable Bowel Syndrome - IBS: Results Show Effects of Dextofisopam Both in Women and in Men. VelaPharm - News. Retrieved on 21 February, 2006.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Tofisopam". A list of authors is available in Wikipedia.
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