Flutazolam Trade names Coreminal (JP ) Other names 13-chloro- 2-(2-fluorophenyl)- 9-(2-hydroxyethyl)- 3-oxa- 6,9-diazatricyclo[8.4.0.02,6 ] tetradeca-1(10),11,13- trien- 8-one AHFS /Drugs.com International Drug Names Routes of administration Oral Legal status
US : Unscheduled
In general: unscheduled, ℞-only in Japan
Metabolism Hepatic Elimination half-life 3.5 hours
10-chloro-11b -(2-fluorophenyl)-7-(2-hydroxyethyl)-3,5-dihydro-2H -[1,3]oxazolo[3,2-d ][1,4]benzodiazepin-6-one
CAS Number PubChem CID ChemSpider UNII KEGG ChEMBL CompTox Dashboard (EPA ) Formula C 19 H 18 Cl F N 2 O 3 Molar mass 376.81 g·mol−1 3D model (JSmol )
Fc1ccccc1C42OCCN2CC(=O)N(c3c4cc(Cl)cc3)CCO
InChI=1S/C19H18ClFN2O3/c20-13-5-6-17-15(11-13)19(14-3-1-2-4-16(14)21)22(8-10-26-19)12-18(25)23(17)7-9-24/h1-6,11,24H,7-10,12H2
Y Key:WMFSSTNVXWNLKI-UHFFFAOYSA-N
Y
N Y (what is this?)
Flutazolam [1] (Coreminal , MS-4101) is a drug which is a benzodiazepine derivative. It was invented in Japan, and this is the main country in which it has been used medically. It has sedative , muscle relaxant , anticonvulsant , and anxiolytic effects similar to those produced by other benzodiazepine derivatives, and though it is around the same potency as diazepam , it produces a more marked sedation and impaired coordination. It is indicated for the treatment of insomnia .[2] Its major active metabolite is n-desalkylflurazepam , also known as norflurazepam, which is also a principal metabolite of flurazepam (trade name Dalmane).[3]
Flutazolam is closely related in structure to another benzodiazepine, haloxazolam .[4] [5]
See also [ ]
Benzodiazepine
Flurazepam
N-desalkylflurazepam
References [ ]
^ DE 1952486
^ Mitsushima T, Ueki S. Psychopharmacological effects of flutazolam (MS-4101). Nippon Yakurigaku Zasshi . 1978 Nov;74(8):959-79. (Japanese).
^ Miyaguchi H, Kuwayama K, Tsujikawa K, Kanamori T, Iwata YT, Inoue H, Kishi T (February 2006). "A method for screening for various sedative-hypnotics in serum by liquid chromatography/single quadrupole mass spectrometry". Forensic Science International . 157 (1): 57–70. doi :10.1016/j.forsciint.2005.03.011 . PMID 15869852 .
^ Kuwayama T, Kurono Y, Muramatsu T, Yashiro T, Ikeda K (January 1986). "The behavior of 1,4-benzodiazepine drugs in acidic media. V. Kinetics of hydrolysis of flutazolam and haloxazolam in aqueous solution" . Chemical and Pharmaceutical Bulletin (Tokyo) . 34 (1): 320–6. doi :10.1248/cpb.34.320 . PMID 2870816 .
^ Yashiro T, Kuwayama T, Kawazura H, Suzuki T (October 1987). "[The behavior of 1,4-benzodiazepine drugs in acidic media. IX. Effect of hydrolyzate of flutazolam on the central nervous system]" . Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan (in Japanese). 107 (10): 830–4. doi :10.1248/yakushi1947.107.10_830 . PMID 2894449 .
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L-655,708
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Ro15-4513
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Ro4938581
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SH-053-R-CH3-2′F
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