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Gidazepam

From Wikipedia, the free encyclopedia
Benzodiazepine medication
Pharmaceutical compound
Gidazepam
Clinical data
Trade namesGidazepam IC
Routes of
administration
Oral
Legal status
Legal status
Pharmacokinetic data
MetabolismHepatic
Eliminationhalf-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
PubChemCID
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)

Gidazepam, also known ashydazepam orhidazepam,[2] is a drug which is an atypicalbenzodiazepine derivative, developed in theSoviet Union.[3][4] It is a selectivelyanxiolytic benzodiazepine.[5] It also has therapeutic value in the management of certain cardiovascular disorders.[6][7][8][9][10]

Pharmacology

[edit]

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

Gidazepam acts as aprodrug 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

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References

[edit]
  1. ^https://mozdocs.kiev.ua/likiview.php?id=33305 "Категорія відпуску. За рецептом."/"Leave Status: By Prescription"
  2. ^Library of Congress (2006).Library of Congress Subject Headings. Library of Congress. pp. 3300–.
  3. ^Spasennikov BA, Spasennikova MG (September 1991). "[The new Soviet tranquilizer--gidazepam]".Fel'dsher I Akusherka.56 (9):35–7.PMID 1684941.
  4. ^Neznamov GG, Koshelev VV, Voronina TA, Trofimov SS (Mar 2002). "[Experimental and clinical rationale for complex treatment of mental disorders in clean-up workers of the Chernobyl nuclear plant accident]".Eksperimental'naia i Klinicheskaia Farmakologiia.65 (2):12–6.PMID 12109283.
  5. ^abKorkhov VM, Tkachuk NA, Makan SY, Pavlovsky VI, Andronati SA (Feb 2002). "Affinities of gidazepam and its analogs for mitochondrial benzodiazepine receptors".Journal of Receptor and Signal Transduction Research.22 (1–4):411–20.doi:10.1081/RRS-120014610.PMID 12503630.S2CID 25403613.
  6. ^Morozov IS, Barchukov VG, Neznamov GG (Jan 1998). "[The effect of gidazepam on the cardiovascular system function in patients with neurotic reactions and in healthy subjects under aggravated conditions]".Eksperimental'naia i Klinicheskaia Farmakologiia.61 (1):30–2.PMID 9575408.
  7. ^Petrova TR, Tatarkin AN (1994). "[The neuroregulatory modulation of the hemodynamic reactions to physical loading in patients with cardiac arrhythmias]".Terapevticheskii Arkhiv.66 (9):65–8.PMID 7992218.
  8. ^Skibitskiĭ VV, Kanorskiĭ SG (Sep 1993). "[New pharmacodynamic effects of gidazepam and befol in patients with cardiac arrhythmias]".Eksperimental'naia i Klinicheskaia Farmakologiia.56 (5):23–7.PMID 7906171.
  9. ^Skibitskiĭ VV, Petrova TR, Kanorskiĭ SG (June 1992). "[Comparative analysis of antiarrhythmic action and electrophysiological effects of a new benzodiazepine derivative gidazepam and ethacizin in arrhythmias of various genesis]".Kardiologiia.32 (6):35–7.PMID 1405290.
  10. ^Meerson FZ, Skibitskiĭ VV (April 1992). "[Comparative anti-arrhythmia effectiveness of activators of body stress-limiting systems in patients with arrhythmia]".Kardiologiia.32 (4):25–30.PMID 1328745.
  11. ^Andronati SA, Zin'kovskiĭ VG, Totrova MI, Golovenko NI, Stankevich EA, Zhuk OV (January 1992). "[Biokinetics of a new prodrug gidazepam and its metabolite]".Biulleten' Eksperimental'noi Biologii I Meditsiny.113 (1):45–7.PMID 1356504.
  12. ^Kolyvanov GB, Zherdev VP, Chirkov AM, Otabekova SG, Litvin AA (May 1993). "[Gidazepam biotransformation and pharmacokinetics in different species of animals and man]".Eksperimental'naia i Klinicheskaia Farmakologiia.56 (3):48–50.PMID 8106054.
  13. ^Zherdev VP, Neznamov GG, Kolyvanov GB, Litvin AA, Otabekova SG (May 1993). "[The pharmacokinetic aspects of the clinical action of gidazepam]".Eksperimental'naia i Klinicheskaia Farmakologiia.56 (3):50–2.PMID 8106055.
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