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Fludiazepam

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Fludiazepam
Systematic (IUPAC) name
9-chloro-6-(2-fluorophenyl)- 2-methyl-2,5-diazabicyclo [5.4.0]undeca- 5,8,10,12-tetraen-3-one
Clinical data
AHFS/Drugs.com International Drug Names
Pregnancy cat.  ?
Legal status Schedule IV(US)
Routes Oral
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half-life  ?
Excretion Renal
Identifiers
CAS number 3900-31-0
ATC code N05BA17
PubChem CID 3369
DrugBank DB01567
ChemSpider 3252 YesY
UNII 7F64A2K16Z YesY
KEGG D01354 YesY
ChEBI CHEBI:31618 YesY
ChEMBL CHEMBL13291 YesY
Chemical data
Formula C16H12ClFN2O 
Mol. mass 302.7
SMILES eMolecules & PubChem
 YesY(what is this?)  (verify)

Fludiazepam was developed by Hoffman-LaRoche in the 1960s[1] and is marketed in Japan and Taiwan in 0.25mg tablets under the brand name Erispan[2][3] is a drug which is a benzodiazepine derivative and is closely related to diazepam.[4] 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]

Fludiazepam has drug abuse potential.[11]

[edit] See also

[edit] References

  1. ^ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
  2. ^ 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. 
  3. ^ "Benzodiazepine Names". non-benzodiazepines.org.uk. http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html. Retrieved 2008-12-29. 
  4. ^ 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. PMID 7909552. 
  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. 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.. "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.. "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.. "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. 

[edit] External links


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