Fludiazepam

Fludiazepam Alerta sobre risco à saúde


Nome IUPAC	7-chloro-5-(2-fluorophenyl)-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
Identificadores
Número CAS	3900-31-0
PubChem	3369
DrugBank	DB01567
ChemSpider	3252
ChEBI	31618
Código ATC	N05BA17
SMILES	`O=C1CN=C(C2=CC=CC=C2F)C3=CC(Cl)=CC=C3N1C`
Primeiro nome comercial ou de referência	Erispan (Japão, Taiwan)
Propriedades
Fórmula química	C₁₆H₁₂ClFN₂O
Massa molar	302.73 g mol^-1
Farmacologia
Metabolismo	Hepático
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.

Fludiazepam,^[1] comercializado sob o nome de Erispan (エリスパン)^[2]^[3] é uma benzodiazepina potente derivada do 2ʹ-fluoro do diazepam,^[4] originalmente desenvolvido por Hoffman-La Roche na década de 1960.^[5] É comercializado no Japão e em Taiwan. Ele exerce suas propriedades farmacológicas através do aumento da inibição GABAérgica.^[6] O fludiazepam tem 4 vezes mais afinidade de ligação com os receptores GABA que o diazepam.^[7] Possui propriedades ansiolíticas,^[8]^[9]^[10] anticonvulsivantes, sedativas, hipnóticas e relaxantes musculoesqueléticas.^[11] O fludiazepam tem sido usado recreacionalmente.^[12]

Ver também

Diazepam
Diclazepam (o análogo 2ʹ-cloro)
Difludiazepam (o derivado 2',6'-difluoro)
Flunitrazepam (o análogo 7-nitro)
Flualprazolam (o derivado de triazolo)
Lista de benzodiazepinas

Referências

↑ US Patent 3371085 5-aryl-3h-1,4-benzodiazepin-2(1h)-ones
↑ Su TP, Chen TJ, Hwang SJ, Chou LF, Fan AP, Chen YC. «Utilization of psychotropic drugs in Taiwan: an overview of outpatient sector in 2000». Zhonghua Yi Xue Za Zhi (Chinese Medical Journal; Free China ed). 65: 378–91. PMID 12455808
↑ «Benzodiazepine Names». non-benzodiazepines.org.uk. Consultado em 29 de dezembro de 2008. Cópia arquivada em 8 de dezembro de 2008
↑ Neville GA, Beckstead HD, Shurvell HF. «A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam». Journal of Pharmaceutical Sciences. 83: 143–51. PMID 7909552. doi:10.1002/jps.2600830207
↑ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
↑ Tsuchiya T, Fukushima H. «Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons». European Journal of Pharmacology. 48: 421–4. PMID 648585. doi:10.1016/0014-2999(78)90169-3
↑ Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A. «Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity». Life Sciences. 36: 113–9. PMID 2857046. doi:10.1016/0024-3205(85)90089-X
↑ Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z (1994). «Effect of an anxiolytic on lipid profile in non-insulin-dependent diabetes mellitus». The Journal of International Medical Research. 22: 338–42. PMID 7895897. doi:10.1177/030006059402200605
↑ Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z (1995). «Improvement of stress reduces glycosylated haemoglobin levels in patients with type 2 diabetes». The Journal of International Medical Research. 23: 119–22. PMID 7601294. doi:10.1177/030006059502300205
↑ Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z (1995). «How blood pressure in patients with non-insulin-dependent diabetes mellitus is influenced by stress». The Journal of International Medical Research. 23: 377–80. PMID 8529781. doi:10.1177/030006059502300508
↑ Inoue H, Maeno Y, Iwasa M, Matoba R, Nagao M. «Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry». Forensic Science International. 113: 367–73. PMID 10978650. doi:10.1016/S0379-0738(00)00226-7
↑ Shimamine M, Masunari T, Nakahara Y (1993). «[Studies on identification of drugs of abuse by diode array detection. I. Screening-test and identification of benzodiazepines by HPLC-DAD with ICOS software system]». Eisei Shikenjo Hokoku. Bulletin of National Institute of Hygienic Sciences: 47–56. PMID 7920567

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[1] US Patent 3371085 5-aryl-3h-1,4-benzodiazepin-2(1h)-ones

[2] Su TP, Chen TJ, Hwang SJ, Chou LF, Fan AP, Chen YC. «Utilization of psychotropic drugs in Taiwan: an overview of outpatient sector in 2000». Zhonghua Yi Xue Za Zhi (Chinese Medical Journal; Free China ed). 65: 378–91. PMID 12455808

[3] «Benzodiazepine Names». non-benzodiazepines.org.uk. Consultado em 29 de dezembro de 2008. Cópia arquivada em 8 de dezembro de 2008

[4] Neville GA, Beckstead HD, Shurvell HF. «A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam». Journal of Pharmaceutical Sciences. 83: 143–51. PMID 7909552. doi:10.1002/jps.2600830207

[5] US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES

[6] Tsuchiya T, Fukushima H. «Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons». European Journal of Pharmacology. 48: 421–4. PMID 648585. doi:10.1016/0014-2999(78)90169-3

[7] Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A. «Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity». Life Sciences. 36: 113–9. PMID 2857046. doi:10.1016/0024-3205(85)90089-X

[8] Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z (1994). «Effect of an anxiolytic on lipid profile in non-insulin-dependent diabetes mellitus». The Journal of International Medical Research. 22: 338–42. PMID 7895897. doi:10.1177/030006059402200605

[9] Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z (1995). «Improvement of stress reduces glycosylated haemoglobin levels in patients with type 2 diabetes». The Journal of International Medical Research. 23: 119–22. PMID 7601294. doi:10.1177/030006059502300205

[10] Okada S, Ichiki K, Tanokuchi S, Ishii K, Hamada H, Ota Z (1995). «How blood pressure in patients with non-insulin-dependent diabetes mellitus is influenced by stress». The Journal of International Medical Research. 23: 377–80. PMID 8529781. doi:10.1177/030006059502300508

[11] Inoue H, Maeno Y, Iwasa M, Matoba R, Nagao M. «Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry». Forensic Science International. 113: 367–73. PMID 10978650. doi:10.1016/S0379-0738(00)00226-7

[12] Shimamine M, Masunari T, Nakahara Y (1993). «[Studies on identification of drugs of abuse by diode array detection. I. Screening-test and identification of benzodiazepines by HPLC-DAD with ICOS software system]». Eisei Shikenjo Hokoku. Bulletin of National Institute of Hygienic Sciences: 47–56. PMID 7920567

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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)