Fludiazepam Explained

Fludiazepam,^[1] marketed under the brand name Erispan (エリスパン)^{[2] [3]} is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam,^[4] originally developed by Hoffmann-La Roche in the 1960s.^[5] It is marketed in Japan and Taiwan. It exerts its pharmacological properties via enhancement of GABAergic inhibition.^[6] Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam.^[7] It possesses anxiolytic,^{[8] [9] [10]} anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.^[11] Fludiazepam has been used recreationally.^[12]

See also

• Diazepam
• Diclazepam (the 2ʹ-chloro analog)
• Difludiazepam (the 2',6'-difluoro derivative)
• Flunitrazepam (the 7-nitro analog)
• Flualprazolam (the triazolo derivative)
• Ro20-8552

External links

• Web site: 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.. Sumitomo Dainippon Pharma. ja.
• Official Dainippon Sumitomo Pharma Website

Notes and References

1. US Patent 3371085 5-aryl-3h-1,4-benzodiazepin-2(1h)-ones
2. Su TP, Chen TJ, Hwang SJ, Chou LF, Fan AP, Chen YC . 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 . August 2002 . 12455808 .
3. Web site: Benzodiazepine Names . 2008-12-29 . non-benzodiazepines.org.uk . dead . https://web.archive.org/web/20081208054743/http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html . 2008-12-08 .
4. Neville GA, Beckstead HD, Shurvell HF . A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam . Journal of Pharmaceutical Sciences . 83 . 2 . 143–51 . February 1994 . 7909552 . 10.1002/jps.2600830207 .
5. US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
6. Tsuchiya T, Fukushima H . Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons . European Journal of Pharmacology . 48 . 4 . 421–4 . April 1978 . 648585 . 10.1016/0014-2999(78)90169-3 .
7. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A . Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity . Life Sciences . 36 . 2 . 113–9 . January 1985 . 2857046 . 10.1016/0024-3205(85)90089-X .
8. Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z . Effect of an anxiolytic on lipid profile in non-insulin-dependent diabetes mellitus . The Journal of International Medical Research . 22 . 6 . 338–42 . 1994 . 7895897 . 10.1177/030006059402200605 . 9591519 .
9. Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z . Improvement of stress reduces glycosylated haemoglobin levels in patients with type 2 diabetes . The Journal of International Medical Research . 23 . 2 . 119–22 . 1995 . 7601294 . 10.1177/030006059502300205 . 12865838 .
10. Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z . 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 . 1995 . 8529781 . 10.1177/030006059502300508 . 42485678 .
11. Inoue H, Maeno Y, Iwasa M, Matoba R, Nagao M . 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 . September 2000 . 10978650 . 10.1016/S0379-0738(00)00226-7 .
12. Shimamine M, Masunari T, Nakahara Y . [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 . 1993 . 7920567 .