Flutazolam[1] (Coreminal, MS-4101) is a central nervous system depressant and sedative drug. Derived from the benzodiazepine structure, it was invented and [[[approved drug|approved for medical use]] in Japan.
Flutazolam exhibits 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] While flutazolam has a very short half-life of only 3.5 hours, n-desalkylflurazepam has a long half-life of between 47–100 hours.[4]
Flutazolam is closely related in structure to another benzodiazepine, haloxazolam.[5][6]
See also
- Flurazepam (Dalmane, Slipam) and *N-desalkylflurazepam, primary metabolite
- Mexazolam (Melex, Sedoxil)
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.
- ↑ "Dalmane Prescribing Information" (PDF). Prescribing Information for Dalmane. FDA. Archived from the original (PDF) on January 18, 2017. Retrieved 3 April 2022.
- ↑ 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. 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.