Gidazepam

Gidazepam Alerta sobre risco à saúde


Nome IUPAC	2-(9-Bromo-3-oxo-6-phenyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-2-yl)acetohydrazide
Identificadores
Número CAS	129186-29-4
PubChem	121919
ChemSpider	108764
SMILES	`BrC1=CC2=C(C=C1)N(CC(NN)=O)C(CN=C2C3=CC=CC=C3)=O`
Propriedades
Fórmula molecular	C17H15BrN4O2
Massa molar	387.2
Farmacologia
Biodisponibilidade	?
Via(s) de administração	Oral
Metabolismo	Hepático
Meia-vida biológica	86.7 horas (para o metabólito ativo)
Excreção	Renal
Página de dados suplementares
Estrutura e propriedades	n, ε_r, etc.
Dados termodinâmicos	Phase behaviour Solid, liquid, gas
Dados espectrais	UV, IV, RMN, EM
Exceto onde denotado, os dados referem-se a materiais sob condições normais de temperatura e pressão Referências e avisos gerais sobre esta caixa. Alerta sobre risco à saúde.

Gidazepam, também conhecido como hidazepam,^[1] é um medicamento atípico derivado das benzodiazepinas, desenvolvido na União Soviética.^[2]^[3] É uma benzodiazepina seletivamente ansiolítica.^[4] Ele também tem valor terapêutico no tratamento de certas doenças cardiovasculares.^[5]^[6]^[7]^[8]^[9] Também pode ser usado no tratamento da tontura .

O gidazepam é um pró-fármaco de seu metabólito ativo 7-bromo-5-fenil-1,2-di-hidro- 3H-1,4-benzodiazepina-2-ona (desalquilgidazepam ou bromo-nordazepam).^[10]^[11] É usado como um ansiolítico. Os efeitos ansiolíticos podem levar várias horas para se manifestar após a dosagem, pois é altamente dependente de seu metabólito ativo, e a meia-vida do Gidazepam está entre as mais longas de todos os agonistas GABAérgicos.^[12]

Ver também[editar | editar código-fonte]

Fenazepam - outro benzodiazepínico amplamente utilizado na Rússia e em outros países da Comunidade dos Estados Independentes
Cinazepam
Cloxazolam
Lista de benzodiazepinas

Referências

↑ Library of Congress (2006). Library of Congress Subject Headings. Library of Congress. [S.l.: s.n.] pp. 3300–
↑ Spasennikov BA, Spasennikova MG. «[The new Soviet tranquilizer--gidazepam]». Fel'dsher I Akusherka. 56: 35–7. PMID 1684941
↑ 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: 12–6. PMID 12109283
↑ 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: 411–20. PMID 12503630. doi:10.1081/RRS-120014610
↑ 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: 30–2. PMID 9575408
↑ Petrova TR, Tatarkin AN (1994). «[The neuroregulatory modulation of the hemodynamic reactions to physical loading in patients with cardiac arrhythmias]». Terapevticheskii Arkhiv. 66: 65–8. PMID 7992218
↑ Skibitskiĭ VV, Kanorskiĭ SG. «[New pharmacodynamic effects of gidazepam and befol in patients with cardiac arrhythmias]». Eksperimental'naia i Klinicheskaia Farmakologiia. 56: 23–7. PMID 7906171
↑ 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: 35–7. PMID 1405290
↑ Meerson FZ, Skibitskiĭ VV. «[Comparative anti-arrhythmia effectiveness of activators of body stress-limiting systems in patients with arrhythmia]». Kardiologiia. 32: 25–30. PMID 1328745
↑ 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: 45–7. PMID 1356504
↑ 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: 48–50. PMID 8106054
↑ 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: 50–2. PMID 8106055

[Congress2006-1] Library of Congress (2006). Library of Congress Subject Headings. Library of Congress. [S.l.: s.n.] pp. 3300–

[2] Spasennikov BA, Spasennikova MG. «[The new Soviet tranquilizer--gidazepam]». Fel'dsher I Akusherka. 56: 35–7. PMID 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: 12–6. PMID 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: 411–20. PMID 12503630. doi:10.1081/RRS-120014610

[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: 30–2. 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: 65–8. PMID 7992218

[7] Skibitskiĭ VV, Kanorskiĭ SG. «[New pharmacodynamic effects of gidazepam and befol in patients with cardiac arrhythmias]». Eksperimental'naia i Klinicheskaia Farmakologiia. 56: 23–7. PMID 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: 35–7. PMID 1405290

[9] Meerson FZ, Skibitskiĭ VV. «[Comparative anti-arrhythmia effectiveness of activators of body stress-limiting systems in patients with arrhythmia]». Kardiologiia. 32: 25–30. PMID 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: 45–7. PMID 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: 48–50. PMID 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: 50–2. PMID 8106055

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]

[10]

[11]

[12]

v d e Benzodiazepinas
1,4-benzodiazepínicos	2-oxoquazepam 3-hidroxifenazepam Bromazepam BMS-906024 Camazepam Carburazepam Clordiazepóxido Cinazepam Cinolazepam Clonazepam Cloniprazepam Clorazepato Ciprazepam Delorazepam Demoxepam Desmetilflunitrazepam Devazepida* Diazepam Diclazepam Difludiazepam Doxefazepam Elfazepam Carfluzepato de etilo Dirazepato de etila Loflazepato de etilo Flubromazepam Fletazepam Fludiazepam Flunitrazepam Flurazepam Flutemazepam Flutoprazepam Fosazepam Gidazepam Halazepam Iclazepam Irazepina Quenazepina Cetazolam Lorazepam Lormetazepam Lufuradom* Meclonazepam Medazepam Menitrazepam Metaclazepam Motrazepam Norflurazepam Nifoxipam Nimetazepam Nitemazepam Nitrazepam Nitrazepato Nordazepam Nortetrazepam Oxazepam Fenazepam Pinazepam Pivoxazepam Prazepam Proflazepam Quazepam QH-II-66 Reclazepam RO4491533* Ro05-4082 Ro5-4864* SH-I-048A Sulazepam Temazepam Tetrazepam Tifluadom* Timelotem* Tolufazepam Triflunordazepam Tuclazepam Uldazepam
1,5-benzodiazepínicos	Arfendazam Clobazam CP-1414S Lofendazam Triflubazam
2,3-benzodiazepínicos*	Girisopam GYKI-52466 GYKI-52895 Nerisopam Talampanel
Triazolobenzodiazepinas	Adinazolam Alprazolam Balovaptan* Bromazolam Clonazolam Estazolam Flualprazolam Flubromazolam Flunitrazolam Nitrazolam Fenazolam Pirazolam Rilmazolam (metabólito ativo de Rilmazafona) Triazolam
Imidazobenzodiazepinas	Bretazenil Climazolam EVT-201 FG-8205 Flumazenil GL-II-73 Imidazenil L-655.708 Loprazolam Midazolam PWZ-029 Remimazolam Ro15-4513 Ro48-6791 Ro48-8684 Ro4938581 Sarmazenil SH-053-R-CH3-2′F
Oxazolobenzodiazepinas	Cloxazolam Flutazolam Haloxazolam Mexazolam Oxazolam
Tienodiazepinas	Bentazepam Clotiazepam
Tienotriazolodiazepinas	Brotizolam Ciclotizolam Descloroetizolam Etizolam Fluclotizolam Israpafante* JQ1* Metizolam
Tienobenzodiazepinas*	Olanzapina Telenzapina
Piridodiazepinas	Lopirazepam
Piridotriazolodiazepinas	Zapizolam
Pirazolodiazepinas	Razobazam* Ripazepam Zolazepam Zomebazam Zometapina*
Pirrolodiazepinas	Premazepam
Tetrahidroisoquinobenzodiazepinas	Clazolam
Pirrolobenzodiazepinas*	Antramicina
Pró-fármacos benzodiazepínicos	Alprazolam triazolobenzofenona Avizafona Rilmazafona
* perfil de atividade atípica (não ligantes do receptor GABA_A)