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Gidazepam

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Gidazepam
Clinical data
Trade namesGidazepam IC
Pregnancy
category
  • ?
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability?
MetabolismHepatic
Elimination half-life86,7 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 mass387.2 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 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-dihydro-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]

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

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. ISSN 0014-9772. PMID 1684941.
  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. ISSN 0869-2092. PMID 12109283.
  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. doi:10.1081/RRS-120014610. ISSN 1079-9893. PMID 12503630.
  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. ISSN 0869-2092. PMID 9575408.
  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. ISSN 0040-3660. PMID 7992218.
  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. ISSN 0869-2092. PMID 7906171.
  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. ISSN 0022-9040. PMID 1405290.
  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. ISSN 0022-9040. PMID 1328745.
  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. ISSN 0365-9615. PMID 1356504.
  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. ISSN 0869-2092. PMID 8106054.
  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. ISSN 0869-2092. PMID 8106055.
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