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Fludiazepam

 

Fludiazepam

Fludiazepam
Systematic (IUPAC) name
7-chloro-5-(2-fluorophenyl)-1-methyl-1H-benzo[e][1,4]diazepin-2(3H)-one
Clinical data
AHFS/Drugs.com
Pregnancy cat.
  • ?
Legal status
Routes Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Half-life ?
Excretion Renal
Identifiers
CAS number  YesY
ATC code N05
PubChem
DrugBank
ChemSpider  YesY
UNII  YesY
KEGG  YesY
ChEBI  YesY
ChEMBL  YesY
Chemical data
Formula C16H12ClFN2O 
Mol. mass 302.7
 YesY   

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]

See also

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.  
  3. ^ "Benzodiazepine Names". non-benzodiazepines.org.uk. 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.  
  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.  
  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.  
  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.  
  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.  
  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.  
  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.  
  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.  

External links

  • (Japanese) Erispan フルジアゼパム錠，細粒 (PDF) Dainippon Sumitomo Pharma. November 2005.
  • (Japanese) Official Dainippon Sumitomo Pharma Website
1,4-Benzodiazepines
1,5-Benzodiazepines
2,3-Benzodiazepines *
Triazolobenzodiazepines
Imidazobenzodiazepines
Oxazolobenzodiazepines
Thienodiazepines
Pyridodiazepines
Pyrazolodiazepines
Pyrrolodiazepines
Tetrahydroisoquinobenzodiazepines
Pyrrolobenzodiazepines *
Benzodiazepine prodrugs
* atypical activity profile (not GABAA receptor ligands)
5-HT1A agonists
GABAAR PAMs
α2δ VDCC blockers
Antidepressants
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