Gidazepam

Gidazepam

Clinical data
Trade names	Gidazepam IC
Routes of administration	Oral
Legal status
Legal status	CA: Schedule IV US:Unscheduled (UA): Rx-Only [1]
Pharmacokinetic data
Metabolism	Hepatic
Elimination half-life	~87 hours
Excretion	Renal
Identifiers
IUPAC name 2-(9-Bromo-3-oxo-6-phenyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-2-yl)acetohydrazide
CAS Number	129186-29-4
PubChem CID	121919
DrugBank	?  N
ChemSpider	108764  Y
UNII	XMJ87I93Y9
CompTox Dashboard (EPA)	DTXSID00156091
Chemical and physical data
Formula	C17H15BrN4O2
Molar mass	387.237 g·mol−1
3D model (JSmol)	Interactive image
SMILES BrC1=CC2=C(C=C1)N(CC(NN)=O)C(CN=C2C3=CC=CC=C3)=O
InChI 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) Y Key:XLGCMZLSEXRBSG-UHFFFAOYSA-N Y
NY  (what is this?)    (verify)

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]}

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

• Phenazepam—another benzodiazepine widely used in Russia and other CIS countries
• Cinazepam
• Cloxazolam
• List of Russian drugs

References

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. 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. 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.