Flutoprazepam Explained

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] Its principal active metabolite is n-desalkylflurazepam, also known as norflurazepam, which is also a principal metabolite of flurazepam (trade name Dalmadorm/Dalmane).^{[5] [6]}

Flutoprazepam is typically used for the treatment of severe insomnia and may also be used for treating stomach ulcers.^[7]

Flutoprazepam does not fall under the international Convention on Psychotropic Substances of 1971, and is currently unscheduled in the United States.^[8]

• 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.^[9]

See also

• Benzodiazepine
• Flurazepam
• N-desalkylflurazepam

Notes and References

1. US . 3632574 . patent . PROCESS FOR PRODUCING BENZODIAZEPINE DERIVATIVES . 1968-29-04 . 1972-04-01 . Hisao Yamamoto et al.
2. 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) (author's transl)] . Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica . 76 . 6 . 447–68 . September 1980 . 7203280 . 10.1254/fpj.76.447 . free .
3. Ueki S, Sukamoto T, Watanabe S, Yamamoto T, Kataoka Y, Shibata S, Suwandi D, Shibata K, Takano M, Sato Y . 6 . [Behavioral effects of flutoprazepam (KB-509) and its metabolites] . Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica . 80 . 1 . 15–30 . July 1982 . 6890927 . 10.1254/fpj.80.15 . free .
4. 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 . 14 . 4 . 293–8 . 1989 . 2633923 . 10.1007/BF03190114 . 20710732 .
5. Miyaguchi H, Kuwayama K, Tsujikawa K, Kanamori T, Iwata YT, Inoue H, Kishi T . A method for screening for various sedative-hypnotics in serum by liquid chromatography/single quadrupole mass spectrometry . Forensic Science International . 157 . 1 . 57–70 . February 2006 . 15869852 . 10.1016/j.forsciint.2005.03.011 .
6. 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 . 14 . 4 . 293–8 . 1989 . 2633923 . 10.1007/BF03190114 . 20710732 .
7. 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] . Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica . 77 . 3 . 273–80 . March 1981 . 7052359 . 10.1254/fpj.77.273 . free .
8. Web site: Green List—List of psychotropic substances under international control . August 2016 . 26th . International Narcotics Control Board . 2017-07-30 . https://web.archive.org/web/20170421003842/https://www.incb.org/documents/Psychotropics/greenlist/2016/V1604744_Eng.pdf . 2017-04-21 . dead .
9. Web site: Bilingual Laws Information System . English . The Government of the Hong Kong Special Administrative Region of the People's Republic of China.