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Gidazepam

 

Gidazepam

Gidazepam
Systematic (IUPAC) name
2-(9-Bromo-3-oxo-6-phenyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-2-yl)acetohydrazide
Clinical data
Pregnancy cat.
  • ?
Legal status
Routes Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Half-life 86,7 hours
Excretion Renal
Identifiers
CAS number  N
ATC code ?
PubChem
DrugBank
ChemSpider  YesY
UNII  YesY
Chemical data
Formula C17H15BrN4O2 
Mol. mass 387.2
 N   

Gidazepam, also known as hydazepam or hidazepam,[1] is a drug which is an atypical benzodiazepine derivative, developed in the Soviet Union.[2][3] It is a selectively anxiolytic benzodiazepine.[4] It also has therapeutic value in the management of certain cardiovascular disorders.[5][6][7][8][9]

Gidazepam is a prodrug for its active metabolite 7-bromo-5-phenyl-1,2-di-hydro-3H-1,4- benzodiazepine-2-one (desalkylgidazepam or bromo-nordazepam).[10][11] It is used as an antianxiety drug. Its anxiolytic effects can take several hours to manifest after dosing however, as it is the active metabolite which primarily gives the anxiolytic effects.[12]

See also

References

  1. ^ Library of Congress (2006). Library of Congress Subject Headings. Library of Congress. pp. 3300–. 
  2. ^ Spasennikov, BA; Spasennikova, MG (Sep 1991). "The new Soviet tranquilizer--gidazepam". Fel'dsher i akusherka 56 (9): 35–7.  
  3. ^ 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.  
  4. ^ Korkhov, 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.  
  5. ^ 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.  
  6. ^ 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.  
  7. ^ 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.  
  8. ^ Skibitskiĭ, VV; Petrova, TR; Kanorskiĭ, SG (Jun 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.  
  9. ^ Meerson, FZ; Skibitskiĭ, VV (Apr 1992). "Comparative anti-arrhythmia effectiveness of activators of body stress-limiting systems in patients with arrhythmia". Kardiologiia 32 (4): 25–30.  
  10. ^ Andronati, SA; Zin'kovskiĭ, VG; Totrova, MIu; Golovenko, NIa; Stankevich, EA; Zhuk, OV (Jan 1992). "Biokinetics of a new prodrug gidazepam and its metabolite". Biulleten' eksperimental'noi biologii i meditsiny 113 (1): 45–7.  
  11. ^ 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.  
  12. ^ 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.  


5-HT1A agonists
GABAAR PAMs
α2δ VDCC blockers
Antidepressants
Sympatholytics
Others

: PSO/PSI

(, , , , , , ), /,

proc (/), drug (/////)

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)


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