Flutoprazepam

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Flutoprazepam
Flutoprazepam.svg
Flutoprazepam ball-and-stick.png
Systematic (IUPAC) name
7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin-2-one
Clinical data
AHFS/Drugs.com International Drug Names
Pregnancy cat.
Legal status
Routes Oral, Intravenous
Pharmacokinetic data
Bioavailability 80-90%
Metabolism Hepatic
Half-life 60-90 hours
Excretion Renal
Identifiers
CAS number 25967-29-7 YesY
ATC code None
PubChem CID 3400
ChemSpider 3283 YesY
UNII 2GHY1101MM YesY
KEGG D01279 YesY
Chemical data
Formula C19H16ClFN2O 
Mol. mass 342.795
 YesY (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]

Abuse of benzodiazepines in Japan is extremely common, with flutoprazepam, nimetazepam, temazepam and triazolam being the four most often sought after by drug users. Triazolam and temazepam make-up 65% of all prescription forgeries for benzodiazepines, while flutoprazepam and nimetazepam make up all the rest of the cases of benzodiazepine prescription forgeries. Diazepam and oxazepam are also commonly misused due to the fact that they are easily obtainable by prescription from doctors.

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

  • 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.[8]

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. ^ 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.