Fludiazepam

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 Hoffman-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]

Fludiazepam
Clinical data
Trade namesErispan (JP, TW)
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral (tablets)
ATC code
Legal status
Legal status
Pharmacokinetic data
MetabolismHepatic
ExcretionRenal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H12ClFN2O
Molar mass302.7 g·mol−1
3D model (JSmol)
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See also

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 (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.
  3. "Benzodiazepine Names". non-benzodiazepines.org.uk. Archived from the original on 2008-12-08. Retrieved 2008-12-29.
  4. 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.
  5. US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
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