Flutoprazepam

Flutoprazepam
Clinical data
Trade names Restas
AHFS/Drugs.com International Drug Names
Pregnancy
category
  • US: X (Contraindicated)
Routes of
administration
Oral, Intravenous
ATC code none
Legal status
Legal status
Pharmacokinetic data
Bioavailability 80-90%
Metabolism Hepatic
Biological half-life 60-90 hours
Excretion Renal
Identifiers
CAS Number 25967-29-7 YesY
PubChem (CID) 3400
ChemSpider 3283 YesY
UNII 2GHY1101MM YesY
KEGG D01279 YesY
ChEMBL CHEMBL2106743
Chemical and physical data
Formula C19H16ClFN2O
Molar mass 342.795
3D model (Jmol) Interactive image
  (verify)

Flutoprazepam (Restas) is a drug which is a benzodiazepine. It was patented in Japan by Sumitomo in 1972[1] and its medical use remains mostly confined to that country. Its muscle relaxant properties are approximately equivalent to those of diazepam - however, it has more powerful sedative, hypnotic, anxiolytic and anticonvulsant effects and is around four times more potent by weight compared to diazepam.[2] It is longer acting than diazepam due to its long-acting active metabolites,[3] which contribute significantly to its effects.[4]

Flutoprazepam is typically used for the treatment of severe insomnia and may also be used for treating stomach ulcers.[5]

Flutoprazepam is currently a Schedule IV drug under the international Convention on Psychotropic Substances of 1971.[6][7]

See also

References

  1. US patent 3632574, Hisao Yamamoto et al, "PROCESS FOR PRODUCING BENZODIAZEPINE DERIVATIVES", published 1968-29-04, issued 1972-04-01
  2. Sukamoto, T.; Aikawa, K.; Itoh, K.; Nose, T. (Sep 1980). "[Psycopharmacological and general pharmacological studies of 7-chloro-1-cyclopropylmethyl-1, 3-dihydro-5-(2-fluorophenyl)-2H-1, 4-benzodiazepin-2-one (KB-509) (author's transl)]". Nippon Yakurigaku Zasshi. 76 (6): 447–68. doi:10.1254/fpj.76.447. PMID 7203280.
  3. Ueki, S.; Sukamoto, T.; Watanabe, S.; Yamamoto, T.; Kataoka, Y.; Shibata, S.; Suwandi, D.; Shibata, K.; et al. (Jul 1982). "[Behavioral effects of flutoprazepam (KB-509) and its metabolites]". Nippon Yakurigaku Zasshi. 80 (1): 15–30. doi:10.1254/fpj.80.15. PMID 6890927.
  4. Barzaghi, N.; Leone, L.; Monteleone, M.; Tomasini, G.; Perucca, E. (1989). "Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects.". Eur J Drug Metab Pharmacokinet. 14 (4): 293–8. doi:10.1007/BF03190114. PMID 2633923.
  5. Fukuda, T.; Itoh, K.; Nose, T. (Mar 1981). "[Antiulcerogenic action of 7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin-2-one (KB-509), a new benzodiazepine derivative]". Nippon Yakurigaku Zasshi. 77 (3): 273–80. doi:10.1254/fpj.77.273. PMID 7052359.
  6. http://www.cnb.gov.sg/ [Central Narcotics Bureau, Singapore]
  7. "Green List—List of psychotropic substances under international control" (PDF) (23rd ed.). International Narcotics Control Board. August 2003. Retrieved 2007-11-25.
  8. "Bilingual Laws Information System" (English). The Government of the Hong Kong Special Administrative Region of the People's Republic of China.
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