Doxefazepam

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Doxefazepam
Doxefazepam.svg
Doxefazepam3d.png
Systematic (IUPAC) name
9-chloro-6-(2-fluorophenyl)-4-hydroxy
-2-(2-hydroxyethyl)-2,5-diazabicyclo
[5.4.0]undeca-5,8,10,12-tetraen-3-one
Clinical data
Pregnancy cat. ?
Legal status Schedule IV(US)
Routes Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Half-life 3-4 hours[1]
Excretion Renal
Identifiers
CAS number 40762-15-0 N
ATC code N05CD12
PubChem CID 38668
DrugBank ?
ChemSpider 35431 YesY
UNII verifiedrevid = 457288969 231RV72C8L verifiedrevid = 457288969 N
KEGG D07327 YesY
ChEMBL CHEMBL64677 YesY
Chemical data
Formula C17H14ClFN2O3 
Mol. mass 348.8
 N (what is this?)

Doxefazepam (marketed under brand name Doxans) is a benzodiazepine derivative drug developed by Schiapparelli in the 1970s.[2] It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is used therapeutically as a hypnotic.[3] According to Babbini and colleagues in 1975, this derivative of flurazepam was between 2 and 4 times more potent than the latter while at the same time being half as toxic in laboratory animals.[4] Section 5.5 of the article Doxefazepam in volume 66 of the World Health Organization's (WHO) and International Agency for Research on Cancer's (IARC) IARC Monographs On The Evaluation Of Carcinogenic Risks To Humans, an article describing the carcinogenic/toxic effects of doxefazepam on humans and experimental animals, states that there is "inadequate evidence in humans for the carcinogenicity of doxefazepam" and limited evidence in experimental for the carcinogenicity of doxefazepam," and concluded that the overall evaluation of the substance's carcinogenicity to humans is "not classifiable."[5]

See also[edit]

References[edit]

  1. ^ http://www.intox.org/databank/documents/pharm/doxefzpm/iarc796.htm
  2. ^ DE Patent 2338058 - BENZODIAZEPINVERBINDUNGEN FUER DIE THERAPIE
  3. ^ Rodriguez, G; Rosadini, G; Sannita, WG; Strumia, E (1984). "Effects of doxefazepam on normal sleep. An EEG and neuropsychological study". Neuropsychobiology 11 (2): 133–9. doi:10.1159/000118066. PMID 6483162. 
  4. ^ Babbini, M.; Torrielli MV, Strumia E, Gaiardi M, Bartoletti M, De Marchi F. (August 1975). "Sedative-hypnotic properties of a new benzodiazepine in comparison with flurazepam. Pharmacological and clinical findings". Arzneimittel-Forschung 25 (8): 1294–1300. PMID 241364. 
  5. ^ "Doxefazepam". IARC Monographs On The Evaluation Of Carcinogenic Risks To Humans (International Agency For Research On Cancer (IARC)) 66: 97–104. 13–20 Feb 1996. Retrieved 10 July 2014. 

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