Flutoprazepam

From Wikipedia, the free encyclopedia
Jump to navigation Jump to search
Flutoprazepam
Flutoprazepam.svg
Flutoprazepam ball-and-stick.png
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
Elimination half-life 60-90 hours
Excretion Renal
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C19H16ClFN2O
Molar mass 342.795
3D model (JSmol)
 ☒N☑Y (what is this?)  (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 does not fall under the international Convention on Psychotropic Substances of 1971, and is currently unscheduled in the United States.[6]

  • In Singapore, flutoprazepam is a Class C-Schedule II drug under the Misuse of Drugs Act.
  • In Thailand, flutoprazepam is a Schedule III psychotropic substance.
  • In Hong Kong, flutoprazepam is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. Flutoprazepam can only be used legally by health professionals and for university research purposes. The substance can be given by pharmacists under a prescription. Anyone who supplies the substance without prescription can be fined $10000 (HKD). The penalty for trafficking or manufacturing the substance is a $5,000,000 (HKD) fine and life imprisonment. Possession of the substance for consumption without license from the Department of Health is illegal with a $1,000,000 (HKD) fine and/or 7 years of jail time.[7]

See also[edit]

References[edit]

  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. ^ "Green List—List of psychotropic substances under international control" (PDF) (26th ed.). International Narcotics Control Board. August 2016. 
  7. ^ "Bilingual Laws Information System" (English). The Government of the Hong Kong Special Administrative Region of the People's Republic of China.