Fludiazepam

Fludiazepam
Clinical data
Trade names Erispan (JP, TW)
AHFS/Drugs.com International Drug Names
Routes of
administration		 Oral (tablets)
ATC code
Legal status
Legal status
Pharmacokinetic data
Metabolism Hepatic
Excretion Renal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
Formula C16H12ClFN2O
Molar mass 302.7
3D model (JSmol)
  (verify)

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

As with all benzodiazepines, fludiazepam is used recreationally.[11]

See also

References

  1. ↑ Su, TP.; Chen, TJ.; Hwang, SJ.; Chou, LF.; Fan, AP.; Chen, YC. (Aug 2002). "Utilization of psychotropic drugs in Taiwan: an overview of outpatient sector in 2000". Zhonghua Yi Xue Za Zhi (Taipei). 65 (8): 378–91. PMID 12455808.
  2. ↑ "Benzodiazepine Names". non-benzodiazepines.org.uk. Archived from the original on 2008-12-08. Retrieved 2008-12-29.
  3. ↑ Neville, GA.; Beckstead, HD.; Shurvell, HF. (Feb 1994). "A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam". J Pharm Sci. 83 (2): 143–51. doi:10.1002/jps.2600830207. PMID 7909552.
  4. ↑ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
  5. ↑ Tsuchiya, T.; Fukushima, H. (Apr 1978). "Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons". Eur J Pharmacol. 48 (4): 421–4. doi:10.1016/0014-2999(78)90169-3. PMID 648585.
  6. ↑ Nakatsuka, I.; Shimizu, H.; Asami, Y.; Katoh, T.; Hirose, A.; Yoshitake, A. (Jan 1985). "Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity". Life Sci. 36 (2): 113–9. doi:10.1016/0024-3205(85)90089-X. PMID 2857046.
  7. ↑ 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". J Int Med Res. 22 (6): 338–42. PMID 7895897.
  8. ↑ 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". J Int Med Res. 23 (2): 119–22. PMID 7601294.
  9. ↑ 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". J Int Med Res. 23 (5): 377–80. PMID 8529781.
  10. ↑ Inoue, H.; Maeno, Y.; Iwasa, M.; Matoba, R.; Nagao, M. (Sep 2000). "Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry". Forensic Sci Int. 113 (1–3): 367–73. doi:10.1016/S0379-0738(00)00226-7. PMID 10978650.
  11. ↑ 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 (111): 47–56. PMID 7920567.
  • (in Japanese) "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.
  • (in Japanese) Official Dainippon Sumitomo Pharma Website


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