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Wikipedia

Fludiazepam

February 06, 2023

Fludiazepam,[1] marketed under the brand name Erispan (エリスパン)[2][3] is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam,[4] originally developed by Hoffman-La Roche in the 1960s.[5] It is marketed in Japan and Taiwan.[citation needed] It exerts its pharmacological properties via enhancement of GABAergic inhibition.[6] Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam.[7] It possesses anxiolytic,[8][9][10] anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.[11] Fludiazepam has been used recreationally.[12]

Fludiazepam
Clinical data
Trade namesErispan (JP, TW)
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral (tablets)
ATC code
Legal status
Legal status
Pharmacokinetic data
MetabolismHepatic
ExcretionRenal
Identifiers
  • 7-chloro-5-(2-fluorophenyl)-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
CAS Number
  • 3900-31-0 Y
PubChem CID
  • 3369
DrugBank
  • DB01567 Y
ChemSpider
  • 3252 Y
UNII
  • 7F64A2K16Z
KEGG
  • D01354 Y
ChEBI
  • CHEBI:31618 Y
ChEMBL
  • ChEMBL13291 Y
CompTox Dashboard (EPA)
  • DTXSID00192277
ECHA InfoCard100.292.343
Chemical and physical data
FormulaC16H12ClFN2O
Molar mass302.7 g·mol−1
3D model (JSmol)
  • Interactive image
  • O=C1CN=C(C2=CC=CC=C2F)C3=CC(Cl)=CC=C3N1C
  • InChI=1S/C16H12ClFN2O/c1-20-14-7-6-10(17)8-12(14)16(19-9-15(20)21)11-4-2-3-5-13(11)18/h2-8H,9H2,1H3 Y
  • Key:ROYOYTLGDLIGBX-UHFFFAOYSA-N Y
  (verify)

See also

References

  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 (August 2002). "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 (8): 378–91. PMID 12455808.
  3. ^ . non-benzodiazepines.org.uk. Archived from the original on 2008-12-08. Retrieved 2008-12-29.
  4. ^ Neville GA, Beckstead HD, Shurvell HF (February 1994). "A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam". Journal of Pharmaceutical Sciences. 83 (2): 143–51. doi:10.1002/jps.2600830207. PMID 7909552.
  5. ^ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
  6. ^ Tsuchiya T, Fukushima H (April 1978). "Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons". European Journal of Pharmacology. 48 (4): 421–4. doi:10.1016/0014-2999(78)90169-3. PMID 648585.
  7. ^ Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A (January 1985). "Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity". Life Sciences. 36 (2): 113–9. doi:10.1016/0024-3205(85)90089-X. PMID 2857046.
  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 (6): 338–42. doi:10.1177/030006059402200605. PMID 7895897. S2CID 9591519.
  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 (2): 119–22. doi:10.1177/030006059502300205. PMID 7601294. S2CID 12865838.
  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 (5): 377–80. doi:10.1177/030006059502300508. PMID 8529781. S2CID 42485678.
  11. ^ Inoue H, Maeno Y, Iwasa M, Matoba R, Nagao M (September 2000). "Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry". Forensic Science International. 113 (1–3): 367–73. doi:10.1016/S0379-0738(00)00226-7. PMID 10978650.
  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 (111): 47–56. PMID 7920567.

External links

  • "エリスパンフルジアゼパム錠0.25mg，細粒0.1% Erispan (fludiazepam tablets 0.25 mg, fine granules 0.1%) Prescribing Information" (in Japanese). Sumitomo Dainippon Pharma.
  • (in Japanese) Official Dainippon Sumitomo Pharma Website
 

This drug article relating to the musculoskeletal system is a stub. You can help Wikipedia by expanding it.

 

This article about an anxiolytic is a stub. You can help Wikipedia by expanding it.

February 06, 2023
fludiazepam, marketed, under, brand, name, erispan, エリスパン, potent, benzodiazepine, fluoro, derivative, diazepam, originally, developed, hoffman, roche, 1960s, marketed, japan, taiwan, citation, needed, exerts, pharmacological, properties, enhancement, gabaergi. Fludiazepam 1 marketed under the brand name Erispan エリスパン 2 3 is a potent benzodiazepine and 2ʹ fluoro derivative of diazepam 4 originally developed by Hoffman La Roche in the 1960s 5 It is marketed in Japan and Taiwan citation needed It exerts its pharmacological properties via enhancement of GABAergic inhibition 6 Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam 7 It possesses anxiolytic 8 9 10 anticonvulsant sedative hypnotic and skeletal muscle relaxant properties 11 Fludiazepam has been used recreationally 12 FludiazepamClinical dataTrade namesErispan JP TW AHFS Drugs comInternational Drug NamesRoutes ofadministrationOral tablets ATC codeN05BA17 WHO Legal statusLegal statusCA Schedule IV DE Anlage III Special prescription form required US Schedule IVPharmacokinetic dataMetabolismHepaticExcretionRenalIdentifiersIUPAC name 7 chloro 5 2 fluorophenyl 1 methyl 1 3 dihydro 2H 1 4 benzodiazepin 2 oneCAS Number3900 31 0 YPubChem CID3369DrugBankDB01567 YChemSpider3252 YUNII7F64A2K16ZKEGGD01354 YChEBICHEBI 31618 YChEMBLChEMBL13291 YCompTox Dashboard EPA DTXSID00192277ECHA InfoCard100 292 343Chemical and physical dataFormulaC 16H 12Cl F N 2OMolar mass302 7 g mol 13D model JSmol Interactive imageSMILES O C1CN C C2 CC CC C2F C3 CC Cl CC C3N1CInChI InChI 1S C16H12ClFN2O c1 20 14 7 6 10 17 8 12 14 16 19 9 15 20 21 11 4 2 3 5 13 11 18 h2 8H 9H2 1H3 YKey ROYOYTLGDLIGBX UHFFFAOYSA N Y verify See also EditDiazepam Diclazepam the 2ʹ chloro analog Difludiazepam the 2 6 difluoro derivative Flunitrazepam the 7 nitro analog Flualprazolam the triazolo derivative Ro20 8552References Edit US Patent 3371085 5 aryl 3h 1 4 benzodiazepin 2 1h ones Su TP Chen TJ Hwang SJ Chou LF Fan AP Chen YC August 2002 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 8 378 91 PMID 12455808 Benzodiazepine Names non benzodiazepines org uk Archived from the original on 2008 12 08 Retrieved 2008 12 29 Neville GA Beckstead HD Shurvell HF February 1994 A Fourier transform Raman and infrared vibrational study of delorazepam fludiazepam flurazepam and tetrazepam Journal of Pharmaceutical Sciences 83 2 143 51 doi 10 1002 jps 2600830207 PMID 7909552 US Patent 3299053 ARYL JH L X BENZODIAZEPIN Z LH ONES Tsuchiya T Fukushima H April 1978 Effects of benzodiazepines and pentobarbitone on the gaba ergic recurrent inhibition of hippocampal neurons European Journal of Pharmacology 48 4 421 4 doi 10 1016 0014 2999 78 90169 3 PMID 648585 Nakatsuka I Shimizu H Asami Y Katoh T Hirose A Yoshitake A January 1985 Benzodiazepines and their metabolites relationship between binding affinity to the benzodiazepine receptor and pharmacological activity Life Sciences 36 2 113 9 doi 10 1016 0024 3205 85 90089 X PMID 2857046 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 6 338 42 doi 10 1177 030006059402200605 PMID 7895897 S2CID 9591519 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 2 119 22 doi 10 1177 030006059502300205 PMID 7601294 S2CID 12865838 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 5 377 80 doi 10 1177 030006059502300508 PMID 8529781 S2CID 42485678 Inoue H Maeno Y Iwasa M Matoba R Nagao M September 2000 Screening and determination of benzodiazepines in whole blood using solid phase extraction and gas chromatography mass spectrometry Forensic Science International 113 1 3 367 73 doi 10 1016 S0379 0738 00 00226 7 PMID 10978650 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 111 47 56 PMID 7920567 External links Edit エリスパンフルジアゼパム錠0 25mg 細粒0 1 Erispan fludiazepam tablets 0 25 mg fine granules 0 1 Prescribing Information in Japanese Sumitomo Dainippon Pharma in Japanese Official Dainippon Sumitomo Pharma Website This drug article relating to the musculoskeletal system is a stub You can help Wikipedia by expanding it vte This article about an anxiolytic is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Fludiazepam amp oldid 1084239286, wikipedia, wiki, book, books, library,

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