Fludiazepam

Fludiazepam
Clinical data
Trade names Erispan (JP, TW)
AHFS/Drugs.com International Drug Names
Routes of
administration		 Oral (tablets)
ATC code N05BA17 (WHO)
Legal status
Legal status
Pharmacokinetic data
Metabolism Hepatic
Excretion Renal
Identifiers
CAS Number 3900-31-0 YesY
PubChem (CID) 3369
DrugBank DB01567 YesY
ChemSpider 3252 YesY
UNII 7F64A2K16Z YesY
KEGG D01354 YesY
ChEBI CHEBI:31618 YesY
ChEMBL CHEMBL13291 YesY
Chemical and physical data
Formula C16H12ClFN2O
Molar mass 302.7
3D model (Jmol) Interactive image
  (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. 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.


This article is issued from Wikipedia - version of the 4/2/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.