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tofisopam
Tofisopam〔DE Patent 2122070〕 (Emandaxin, Grandaxin, Sériel) is an anxiolytic that is marketed in several European countries. Chemically, it is a 2,3-benzodiazepine. Unlike other anxiolytic benzodiazepines (which are generally 1,4- or 1,5-substituted) however, tofisopam does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic 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). Tofisopam is indicated for the treatment of anxiety and alcohol withdrawal, and is prescribed in a dosage of 50–300 mg 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.
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,〔 〕 with moderate efficacy demonstrated in clinical trials so far.〔Leventer SM, Raudibaugh K, Frissora CL, Kassem N, Keogh JC, Phillips J, Mangel AW. Clinical trial: dextofisopam in the treatment of patients with diarrhoea-predominant or alternating irritable bowel syndrome. ''Alimentary Pharmacology and Therapeutics''. 2008 Jan 15;27(2):197-206. PMID 17973974〕
Tofisopam is also claimed to be a PDE10A inhibitor, which may provide an alternative mechanism of action for its various therapeutic effects, and this action has been proposed to make tofisopam potentially useful as a treatment for schizophrenia.〔(Nielsen EB, Kehler J, Nielsen J, Brøsen P. Use of Tofisopam as a PDE10A inhibitor. WIPO Patent WO/2007/082546 )〕
Tofisopam has been shown to act as an inhibitor of the liver enzyme CYP3A4,〔Tóth M, Bajnógel J, Egyed A, Drabant S, Tömlo J, Klebovich I. Effect of tofisopam on CYP3A4 enzyme activity on human recombinant 3A4 supersome. (Hungarian) ''Acta Pharmaceutica Hungarica''. 2005;75(4):195-8. PMID 16711396〕 and this could potentially cause dangerous drug interactions with other medications metabolised by this enzyme,〔Drabant S, Tóth M, Bereczki A, Bajnógel J, Tömlö J, Klebovich I. Effect of tofisopam on the single-oral-dose pharmacokinetics and pharmacodynamics of the cyp3a4 probe drug alprazolam. ''European Journal of Clinical Pharmacology''. 2006 Jul;62(7):587-8. PMID 16791582〕〔Tóth M, Drabant S, Varga B, Végso G, Cseh A, Szentpéteri I, Klebovich I. Tofisopam inhibits the pharmacokinetics of CYP3A4 substrate midazolam. ''European Journal of Clinical Pharmacology''. 2008 Jan;64(1):93-4. PMID 17989974〕 although the clinical significance of these findings remains unclear.
==References==
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