Tofisopam
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Tofisopam
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| 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 |
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| Identifiers | |
| CAS number | |
| ATC code | N05 |
| PubChem | |
| 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. |
? |
| Legal status |
? |
| 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 dependence 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]
[edit] References
- ^ Bond, A; M. Lader (1982). "A comparison of the psychotropic profiles of tofisopam and diazepam.". European Journal of Clinical Pharmacology 22 (2): 137–42. doi:. PMID 6124424.
- ^ 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. doi:. PMID 6109345.
- ^ Saano, V. (1986). "Tofizopam selectively increases the action of anticonvulsants". Medical Biology 64 (4): 201–6. PMID 3023768.
- ^ http://www.biam2.org/www/Sub1469.html
- ^ 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.
[edit] External links
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