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{{Drugbox| | {{Drugbox| | ||
|IUPAC_name = ''6-(3,4-dimethoxyphenyl)-2-ethyl-9,10-dimethoxy-3-methyl''<br />''-4,5-diazabicyclo[5.4.0]undeca-3,5,7,9,11-pentaene'' | |IUPAC_name = ''6-(3,4-dimethoxyphenyl)-2-ethyl-9,10-dimethoxy-3-methyl''<br />''-4,5-diazabicyclo[5.4.0]undeca-3,5,7,9,11-pentaene'' | ||
| image = Tofisopam. | | image = Tofisopam Wiki Str.png | ||
| image2 = | | image2 = Tofisopam 3D.png | ||
| width=160 | | width=160 | ||
| CAS_number=22345-47-7 | | CAS_number=22345-47-7 | ||
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| routes_of_administration= Oral | | routes_of_administration= Oral | ||
}} | }} | ||
__NOTOC__ | |||
{{SI}} | |||
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== 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]],<ref name=definitely_not_diazepam>{{cite journal | first = A | last = Bond | coauthors = M. Lader | year = 1982 | title = A comparison of the psychotropic profiles of tofisopam and diazepam. | journal = European Journal of Clinical Pharmacology | volume = 22 | issue = 2 | pages = 137-42 | id = {{PMID|6124424}}}}</ref> [[muscle relaxant|skeletal muscle relaxant]], [[motor skill]]-impairing or [[amnesia|amnestic]]<ref name=not_diazepam>{{cite journal | first = T | last = Seppala | coauthors = Palva E, Mattila MJ, Korttila K, Shrotriya RC | year = 1980 | title = Tofisopam, a novel 3,4-benzodiazepine: multiple-dose effects on psychomotor skills and memory. Comparison with diazepam and interactions with ethanol | journal = Psychopharmacology (Berlin) | volume = 69 | issue = 2 | pages = 209-18 | id = {{PMID|6109345}}}}</ref> 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]]).<ref name=curiouser_and_curiouser>{{cite journal | first = V. | last = Saano | year = 1986 | title = Tofizopam selectively increases the action of anticonvulsants | journal = Medical Biology | volume = 64 | issue = 4 | pages = 201-6 | id = {{PMID|3023768}}}}</ref> 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. <ref> http://www.biam2.org/www/Sub1469.html </ref> | '''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]],<ref name=definitely_not_diazepam>{{cite journal | first = A | last = Bond | coauthors = M. Lader | year = 1982 | title = A comparison of the psychotropic profiles of tofisopam and diazepam. | journal = European Journal of Clinical Pharmacology | volume = 22 | issue = 2 | pages = 137-42 | id = {{PMID|6124424}}}}</ref> [[muscle relaxant|skeletal muscle relaxant]], [[motor skill]]-impairing or [[amnesia|amnestic]]<ref name=not_diazepam>{{cite journal | first = T | last = Seppala | coauthors = Palva E, Mattila MJ, Korttila K, Shrotriya RC | year = 1980 | title = Tofisopam, a novel 3,4-benzodiazepine: multiple-dose effects on psychomotor skills and memory. Comparison with diazepam and interactions with ethanol | journal = Psychopharmacology (Berlin) | volume = 69 | issue = 2 | pages = 209-18 | id = {{PMID|6109345}}}}</ref> 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]]).<ref name=curiouser_and_curiouser>{{cite journal | first = V. | last = Saano | year = 1986 | title = Tofizopam selectively increases the action of anticonvulsants | journal = Medical Biology | volume = 64 | issue = 4 | pages = 201-6 | id = {{PMID|3023768}}}}</ref> 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. <ref> http://www.biam2.org/www/Sub1469.html </ref> | ||
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]].<ref name=dtfp_ibs>{{cite web | author = Vela Pharmaceuticals | year = 2005 | url = http://www.velapharm.com/news/press050104.html | title = 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 | work = VelaPharm - News | accessdate = 21 February | accessyear = 2006}}</ref> | 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]].<ref name=dtfp_ibs>{{cite web | author = Vela Pharmaceuticals | year = 2005 | url = http://www.velapharm.com/news/press050104.html | title = 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 | work = VelaPharm - News | accessdate = 21 February | accessyear = 2006}}</ref> | ||
==References== | ==References== | ||
{{Reflist|2}} | |||
<div class="references-small"> | <div class="references-small"> | ||
</div> | </div> | ||
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{{Benzodiazepines}} | {{Benzodiazepines}} | ||
{{Anxiolytics}} | {{Anxiolytics}} | ||
[[Category:Drug]] | |||
[[Category:Anxiolytics]] | [[Category:Anxiolytics]] | ||
[[Category:Benzodiazepines]] | [[Category:Benzodiazepines]] | ||
Latest revision as of 14:00, 9 April 2015
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| Routes of administration | Oral |
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| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | Hepatic |
| Elimination half-life | 6-8 hours |
| Excretion | Renal |
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| CAS Number | |
| PubChem CID | |
| DrugBank | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
| Chemical and physical data | |
| Formula | C22H26N2O4 |
| Molar mass | 382.5 |
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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
- ↑ 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) - ↑ 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) - ↑ 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 21 February. Unknown parameter
|accessyear=ignored (|access-date=suggested) (help); Check date values in:|accessdate=(help)
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