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Flutoprazepam
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| Systematic (IUPAC) name | |
| 7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin-2-one | |
| Identifiers | |
| CAS number | |
| ATC code | none |
| PubChem | |
| Chemical data | |
| Formula | C19H16ClFN2O |
| 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][7]
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.[8]
See also
References
- ^ Sukamoto T, Aikawa K, Itoh K, Nose T. Psychopharmacological and general pharmacological studies of 7-chloro-1-cyclopropylmethyl-1, 3-dihydro-5-(2-fluorophenyl)-2H-1, 4-benzodiazepin-2-one (KB-509). Nippon Yakurigaku Zasshi. 1980 Sep;76(6):447-68. (Japanese).
- ^ Ueki S, Sukamoto T, Watanabe S, Yamamoto T, Kataoka Y, Shibata S, Suwandi D, Shibata K, Takano M, Sato Y. Behavioral effects of flutoprazepam (KB-509) and its metabolites. Nippon Yakurigaku Zasshi. 1982 Jul;80(1):15-30. (Japanese).
- ^ Barzaghi N, Leone L, Monteleone M, Tomasini G, Perucca E. Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects. European Journal of Drug Metabolism and Pharmacokinetics. 1989 Oct-Dec;14(4):293-8.
- ^ Fukuda T, Itoh K, Nose T. 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. 1981 Mar;77(3):273-80. (Japanese).
- ^ Annual Estimates Of Requirements Of Narcotic Drugs, Manufacture Of Synthetic Drugs, Opium Production And Cultivation Of The
- ^ http://www.cnb.gov.sg/ [Central Narcotics Bureau, Singapore]
- ^ "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 on 2007-11-25.
- ^ "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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