Gidazepam

Benzodiazepine medication From Wikipedia, the free encyclopedia

Gidazepam, also known as hydazepam or hidazepam,[2] is a drug which is an atypical benzodiazepine derivative, developed in the Soviet Union.[3][4] It is a selectively anxiolytic benzodiazepine.[5] It also has therapeutic value in the management of certain cardiovascular disorders.[6][7][8][9][10]

Trade namesGidazepam IC
Routes of
administrationOral
Legal status
MetabolismHepatic
Quick facts Clinical data, Trade names ...
Gidazepam
Clinical data
Trade namesGidazepam IC
Routes of
administration		Oral
Legal status
Legal status
Pharmacokinetic data
MetabolismHepatic
Elimination half-life~87 hours
ExcretionRenal
Identifiers
  • 2-(9-Bromo-3-oxo-6-phenyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-2-yl)acetohydrazide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H15BrN4O2
Molar mass387.237 g·mol−1
3D model (JSmol)
  • BrC1=CC2=C(C=C1)N(CC(NN)=O)C(CN=C2C3=CC=CC=C3)=O
  • InChI=1S/C17H15BrN4O2/c18-12-6-7-14-13(8-12)17(11-4-2-1-3-5-11)20-9-16(24)22(14)10-15(23)21-19/h1-8H,9-10,19H2,(H,21,23) checkY
  • Key:XLGCMZLSEXRBSG-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)
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Pharmacology

Gidazepam and several of its analogs, in contrast to other benzodiazepines, are comparatively more selective agonists of TSPO (formerly the peripheral benzodiazepine receptor) than the benzodiazepine receptor.[5]

Gidazepam acts as a prodrug to its active metabolite 7-bromo-2,3-dihydro-5-phenyl-1H-1,4-benzodiazepin-2-one (desalkylgidazepam or bromo-nordazepam).[11][12] Its anxiolytic effects can take several hours to manifest presumably due to its slow metabolism (half-life 87 hours). The onset and intensity of anxiolytic effects correlate with blood levels of desalkylgidazepam.[13]

Gidazepam active metabolite (desalkylgidazepam or bromonordiazepam), responsible for its therapeutic effects

See also

References

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