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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/03/31 04:18:05」(JST)

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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]

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.

English Journal

Muscle relaxants for pain management in rheumatoid arthritis.

Richards BL1, Whittle SL, Buchbinder R.
The Cochrane database of systematic reviews.Cochrane Database Syst Rev.2012 Jan 18;1:CD008922. doi: 10.1002/14651858.CD008922.pub2.
BACKGROUND: Pain management is a high priority for patients with rheumatoid arthritis (RA). Muscle relaxants include drugs that reduce muscle spasm (for example benzodiazepines such as diazepam (Valium), alprazolam (Xanax), lorazepam (Ativan) and non-benzodiazepines such as metaxalone (Skelaxin) or
PMID 22258993

Anticonvulsant properties of 1,4-benzodiazepine derivatives in amygdaloid-kindled seizures and their chemical structure-related anticonvulsant action.

Fukinaga M1, Ishizawa K, Kamei C.
Pharmacology.Pharmacology.1998 Nov;57(5):233-41.
The effects of 14 different 1,4-benzodiazepines on amygdaloid-kindled seizures and their chemical structure-related anticonvulsive actions were studied. The prophylactic effects of 1, 4-benzodiazepines on amygdaloid-kindled seizures were also examined. Male Wistar strain rats were used in this study
PMID 9742288

Propranolol does not alter flutoprazepam kinetics and metabolism in the rat.

Conti I1, Sarati S, Caccia S.
European journal of drug metabolism and pharmacokinetics.Eur J Drug Metab Pharmacokinet.1991 Jan-Mar;16(1):53-8.
The influence of propranolol on the disposition of flutoprazepam, a benzodiazepine derivative extensively biotransformed by hepatic microsomal oxidation, was evaluated in the rat. Propranolol was infused subcutaneously with osmotic minipumps (5 mg/day) to obtain steady-state concentrations of about
PMID 1936062

Japanese Journal

Study on Raffenetti's P File Format in Conventional Ab Initio Self-Consistent-Field Molecular Orbital Calculations in Parallel Computational Environment

Journal of Computer Chemistry, Japan 7(5), 179-184, 2008
NAID 130000107432

Study on Raffenetti's P File Format in Conventional Ab Initio Self-Consistent-Field Molecular Orbital Calculations in Parallel Computational Environment

Journal of Computer Chemistry, Japan 7(5), 179-184, 2008
NAID 120005520441

心身症と考えられる症例におこなった歯科治療

日本歯科心身医学会雑誌 14(1), 65-70, 1999
NAID 130004105490

Related Pictures

★リンクテーブル★

リンク元	「フルトプラゼパム」

「フルトプラゼパム」

Flutoprazepam
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	US: X (Contraindicated); ;
Routes of; administration	Oral, Intravenous
Legal status	Schedule IV(US);
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
	SMILES FC1=CC=CC=C1C2=NCC(N(CC3CC3)C4=C2C=C(C=C4)Cl)=O ;
	InChI InChI=1S/C19H16ClFN2O/c20-13-7-8-17-15(9-13)19(14-3-1-2-4-16(14)21)22-10-18(24)23(17)11-12-5-6-12/h1-4,7-9,12H,5-6,10-11H2 ; Key:OFVXPDXXVSGEPX-UHFFFAOYSA-N ;
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　　[★]

英: flutoprazepam
商: レスタス

抗不安薬;ベンゾジアゼピン系

[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] ttp://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.

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