Flutoprazepam
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| Systematic (IUPAC) name | |
|---|---|
|
7-chloro-1-(cyclopropylmethyl)-5-(2-fluorophenyl)-3H-1,4-benzodiazepin-2-one | |
| Clinical data | |
| Trade names | Restas |
| AHFS/Drugs.com | International Drug Names |
| Pregnancy category |
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| Routes of administration | Oral, Intravenous |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | 80-90% |
| Metabolism | Hepatic |
| Biological half-life | 60-90 hours |
| Excretion | Renal |
| Identifiers | |
| CAS Number |
25967-29-7  |
| ATC code | none |
| PubChem | CID 3400 |
| ChemSpider |
3283 |
| UNII |
2GHY1101MM |
| KEGG |
D01279 |
| ChEMBL | CHEMBL2106743 |
| Chemical data | |
| Formula | C19H16ClFN2O |
| Molar mass | 342.795 |
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| (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]
Recreational use 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 misuse commonly happens because 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 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.[8]
See also
References
- ↑ US patent 3632574, Hisao Yamamoto et al, "PROCESS FOR PRODUCING BENZODIAZEPINE DERIVATIVES", published 1968-29-04, issued 1972-04-01
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ http://www.cnb.gov.sg/ [Central Narcotics Bureau, Singapore]
- ↑ "Green List—List of psychotropic substances under international control" (PDF) (23rd ed.). International Narcotics Control Board. August 2003. Retrieved 2007-11-25.
- ↑ "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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