Tofisopam

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Tofisopam
Clinical data
Other names6-(3,4-Dimethoxyphenyl)-2-ethyl-9,10-dimethoxy-3-methyl-4,5-diazabicyclo[5.4.0]undeca-3,5,7,9,11-pentaene
AHFS/Drugs.comInternational Drug Names
Routes of
administration		By mouth (tablets)
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
MetabolismHepatic
Elimination half-life3 hours[1][2]
ExcretionRenal
Identifiers
  • 1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine
JSmol)
SMILES
  • O(c3ccc(C\2=N\N=C(/C(c1c/2cc(OC)c(OC)c1)CC)C)cc3OC)C
  • InChI=1S/C22H26N2O4/c1-7-15-13(2)23-24-22(14-8-9-18(25-3)19(10-14)26-4)17-12-21(28-6)20(27-5)11-16(15)17/h8-12,15H,7H2,1-6H3 checkY
  • Key:RUJBDQSFYCKFAA-UHFFFAOYSA-N checkY
  (verify)

Tofisopam

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,[9] with moderate efficacy demonstrated in clinical trials so far.[10]

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.[11]

Tofisopam has been shown to act as an inhibitor of the liver enzyme CYP3A4,[12][13] and some researches suspect that this could cause dangerous drug interactions with other medications metabolised by this enzyme,[14][15] although the clinical significance of these findings remains unclear.

References

  1. PMID 8100113
    .
  2. PMID 20967473
    .
  3. ^ DE Patent 2122070
  4. ISBN 978-3-88763-075-1
    .
  5. S2CID 30776062
    .
  6. S2CID 24063885
    .
  7. PMID 3023768
    .
  8. PMID 8100112
    .
  9. ^ 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. Archived from the original on May 2, 2005. Retrieved February 21, 2006.
  10. S2CID 8557111
    .
  11. ^ Nielsen EB, Kehler J, Nielsen J, Brøsen P. Use of Tofisopam as a PDE10A inhibitor. WIPO Patent WO/2007/082546
  12. ^ "Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers". FDA. May 26, 2021.
  13. PMID 16711396
    .
  14. S2CID 32545296
    .
  15. S2CID 35022772
    .
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