Gidazepam Explained

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]}

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.

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).^{[10] [11]} Its anxiolytic effects can take several hours to manifest presumably due to the its slow metabolism (half-life 87 hours). The onset and intensity of anxiolytic effects correlate with blood levels of desalkylgidazepam.^[12]

See also

• Phenazepam—another benzodiazepine widely used in Russia and other CIS countries
• Cinazepam
• Cloxazolam

Notes and References

1. Book: Library of Congress. Library of Congress Subject Headings. 2006. Library of Congress. 3300–.
2. Spasennikov BA, Spasennikova MG . [The new Soviet tranquilizer--gidazepam] . Fel'dsher I Akusherka . 56 . 9 . 35–7 . September 1991 . 1684941 .
3. Neznamov GG, Koshelev VV, Voronina TA, Trofimov SS . [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 . Mar 2002 . 12109283 .
4. Korkhov VM, Tkachuk NA, Makan SY, Pavlovsky VI, Andronati SA . Affinities of gidazepam and its analogs for mitochondrial benzodiazepine receptors . Journal of Receptor and Signal Transduction Research . 22 . 1–4 . 411–20 . Feb 2002 . 12503630 . 10.1081/RRS-120014610 . 25403613 .
5. Morozov IS, Barchukov VG, Neznamov GG . [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 . Jan 1998 . 9575408 .
6. Petrova TR, Tatarkin AN . [The neuroregulatory modulation of the hemodynamic reactions to physical loading in patients with cardiac arrhythmias] . Terapevticheskii Arkhiv . 66 . 9 . 65–8 . 1994 . 7992218 .
7. Skibitskiĭ VV, Kanorskiĭ SG . [New pharmacodynamic effects of gidazepam and befol in patients with cardiac arrhythmias] . Eksperimental'naia i Klinicheskaia Farmakologiia . 56 . 5 . 23–7 . Sep 1993 . 7906171 .
8. Skibitskiĭ VV, Petrova TR, Kanorskiĭ SG . [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 . June 1992 . 1405290 .
9. Meerson FZ, Skibitskiĭ VV . [Comparative anti-arrhythmia effectiveness of activators of body stress-limiting systems in patients with arrhythmia] . Kardiologiia . 32 . 4 . 25–30 . April 1992 . 1328745 .
10. Andronati SA, Zin'kovskiĭ VG, Totrova MI, Golovenko NI, Stankevich EA, Zhuk OV . [Biokinetics of a new prodrug gidazepam and its metabolite] . Biulleten' Eksperimental'noi Biologii I Meditsiny . 113 . 1 . 45–7 . January 1992 . 1356504 .
11. Kolyvanov GB, Zherdev VP, Chirkov AM, Otabekova SG, Litvin AA . [Gidazepam biotransformation and pharmacokinetics in different species of animals and man] . Eksperimental'naia i Klinicheskaia Farmakologiia . 56 . 3 . 48–50 . May 1993 . 8106054 .
12. Zherdev VP, Neznamov GG, Kolyvanov GB, Litvin AA, Otabekova SG . [The pharmacokinetic aspects of the clinical action of gidazepam] . Eksperimental'naia i Klinicheskaia Farmakologiia . 56 . 3 . 50–2 . May 1993 . 8106055 .