Fludiazepam,[2] marketed under the brand name Erispan (エリスパン)[3][4] is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam,[5] originally developed by Hoffmann-La Roche in the 1960s.[6] It is marketed in Japan and Taiwan. [citation needed] It exerts its pharmacological properties via enhancement of GABAergic inhibition.[7] Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam.[8] It possesses anxiolytic,[9][10][11] anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.[12] Fludiazepam has been used recreationally.[13]
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Clinical data | |
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Trade names | Erispan (JP, TW) |
AHFS/Drugs.com | International Drug Names |
Routes of administration | Oral (tablets) |
Drug class | Benzodiazepine |
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Metabolism | Hepatic |
Excretion | Renal |
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ECHA InfoCard | 100.292.343 |
Chemical and physical data | |
Formula | C16H12ClFN2O |
Molar mass | 302.73 g·mol−1 |
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See also
edit- Diazepam
- Diclazepam (the 2ʹ-chloro analog)
- Difludiazepam (the 2',6'-difluoro derivative)
- Flunitrazepam (the 7-nitro analog)
- Flualprazolam (the triazolo derivative)
- Ro20-8552
References
edit- ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
- ^ US Patent 3371085 5-aryl-3h-1,4-benzodiazepin-2(1h)-ones
- ^ Su TP, Chen TJ, Hwang SJ, Chou LF, Fan AP, Chen YC (August 2002). "Utilization of psychotropic drugs in Taiwan: an overview of outpatient sector in 2000". Zhonghua Yi Xue Za Zhi (Chinese Medical Journal; Free China Ed). 65 (8): 378–91. PMID 12455808.
- ^ "Benzodiazepine Names". non-benzodiazepines.org.uk. Archived from the original on 2008-12-08. Retrieved 2008-12-29.
- ^ Neville GA, Beckstead HD, Shurvell HF (February 1994). "A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam". Journal of Pharmaceutical Sciences. 83 (2): 143–51. doi:10.1002/jps.2600830207. PMID 7909552.
- ^ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
- ^ Tsuchiya T, Fukushima H (April 1978). "Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons". European Journal of Pharmacology. 48 (4): 421–4. doi:10.1016/0014-2999(78)90169-3. PMID 648585.
- ^ Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A (January 1985). "Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity". Life Sciences. 36 (2): 113–9. doi:10.1016/0024-3205(85)90089-X. PMID 2857046.
- ^ Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z (1994). "Effect of an anxiolytic on lipid profile in non-insulin-dependent diabetes mellitus". The Journal of International Medical Research. 22 (6): 338–42. doi:10.1177/030006059402200605. PMID 7895897. S2CID 9591519.
- ^ Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z (1995). "Improvement of stress reduces glycosylated haemoglobin levels in patients with type 2 diabetes". The Journal of International Medical Research. 23 (2): 119–22. doi:10.1177/030006059502300205. PMID 7601294. S2CID 12865838.
- ^ Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z (1995). "How blood pressure in patients with non-insulin-dependent diabetes mellitus is influenced by stress". The Journal of International Medical Research. 23 (5): 377–80. doi:10.1177/030006059502300508. PMID 8529781. S2CID 42485678.
- ^ Inoue H, Maeno Y, Iwasa M, Matoba R, Nagao M (September 2000). "Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry". Forensic Science International. 113 (1–3): 367–73. doi:10.1016/S0379-0738(00)00226-7. PMID 10978650.
- ^ Shimamine M, Masunari T, Nakahara Y (1993). "[Studies on identification of drugs of abuse by diode array detection. I. Screening-test and identification of benzodiazepines by HPLC-DAD with ICOS software system]". Eisei Shikenjo Hokoku. Bulletin of National Institute of Hygienic Sciences (111): 47–56. PMID 7920567.
External links
edit- "エリスパンフルジアゼパム錠0.25mg,細粒0.1% Erispan (fludiazepam tablets 0.25 mg, fine granules 0.1%) Prescribing Information" (in Japanese). Sumitomo Dainippon Pharma.[permanent dead link]
- (in Japanese) Official Dainippon Sumitomo Pharma Website Archived 2020-07-01 at the Wayback Machine