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Flutoprazepam
Systematic (IUPAC) name
7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin-2-one
Identifiers
CAS number 25967-29-7
ATC code none
PubChem 3400
Chemical data
Formula C 19H16ClFN2O 
Mol. mass 342.795
Pharmacokinetic data
Bioavailability 80-90%
Metabolism Hepatic
Half life 60-90 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat. X(US)
Legal status Schedule IV(US)
Routes Oral, Intravenous

Flutoprazepam (Restas, KB-509) is a drug which is a benzodiazepine derivative. It was invented in Japan in 1972, 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. [1] It is longer acting than diazepam due to its long-acting active metabolites,[2] which contribute significantly to its effects.[3]

Flutoprazepam is typically used for the treatment of severe insomnia and may also be used for treating stomach ulcers.[4]

Abuse of benzodiazepines in Japan is extremely common, with flutoprazepam being one of the most commonly abused, along with the benzodiazepines of abuse nimetazepam, temazepam and triazolam.

Flutoprazepam is currently a Schedule IV drug under the international Convention on Psychotropic Substances of 1971.[5][6]

In Singapore, flutoprazepam is a Class C-Schedule II drug under the Misuse of Drugs Act.

In Hong Kong, flutoprazepam is regulated under Schedule 2 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. Flutoprazepam may be prescribed for the treatment of insomnia by a registered medical doctor. The penalty for trafficking or manufacturing the substance is a $100,000 (HKD) fine and possibly a short imprisonment (1-2 years). Possession of the substance for consumption without valid prescription from a registered medical doctor is illegal and punishable with a $50,000 (HKD) fine.[7]

See also

References

  1. ^ 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. PMID 7203280.  
  2. ^ 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. PMID 6890927.  
  3. ^ 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. PMID 2633923.  
  4. ^ 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. PMID 7052359.  
  5. ^ http://www.cnb.gov.sg/ [Central Narcotics Bureau, Singapore]
  6. ^ "Green List—List of psychotropic substances under international control" (PDF). International Narcotics Control Board. 23rd edition, August 2003. http://www.incb.org/pdf/e/list/green.pdf. Retrieved 2007-11-25.  
  7. ^ "Bilingual Laws Information System" (English). The Government of the Hong Kong Special Administrative Region of the People's Republic of China. http://www.legislation.gov.hk/eng/index.htm.  







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