Gidazepam

Gidazepam
Gidazepam.svg
Gidazepam ball-and-stick model.png
Clinical data
Trade names Gidazepam IC
Routes of
administration
Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Elimination half-life 86,7 hours(for active metabolite)
Excretion Renal
Identifiers
CAS Number
PubChem CID
DrugBank
  • ? ☒N
ChemSpider
UNII
Chemical and physical data
Formula C17H15BrN4O2
Molar mass 387.2 g·mol−1
3D model (JSmol)
 ☒N☑Y (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, and Gidazepam’s half-life is among the longest of all GABA-ergic agonists.[12]

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

See also[edit]

References[edit]

  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.