Tofisopam

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Tofisopam
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Clinical data
Pregnancy
category
  •  ?
Routes of
administration
Oral
ATC code
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Legal status
  •  ?
Pharmacokinetic data
Bioavailability?
MetabolismHepatic
Elimination half-life6-8 hours
ExcretionRenal
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
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Chemical and physical data
FormulaC22H26N2O4
Molar mass382.5

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

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]

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 (1982). "A comparison of the psychotropic profiles of tofisopam and diazepam". European Journal of Clinical Pharmacology. 22 (2): 137–42. PMID 6124424. Unknown parameter |coauthors= ignored (help)
  2. Seppala, T (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. PMID 6109345. Unknown parameter |coauthors= ignored (help)
  3. Saano, V. (1986). "Tofizopam selectively increases the action of anticonvulsants". Medical Biology. 64 (4): 201–6. PMID 3023768.
  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 21 February. Unknown parameter |accessyear= ignored (|access-date= suggested) (help); Check date values in: |accessdate= (help)

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