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==Overview==
==Overview==
'''Fludiazepam''', marketed under the brand name '''Erispan'''<ref>{{Cite journal | last1 = Su | first1 = TP. | last2 = Chen | first2 = TJ. | last3 = Hwang | first3 = SJ. | last4 = Chou | first4 = LF. | last5 = Fan | first5 = AP. | last6 = Chen | first6 = YC. | title = Utilization of psychotropic drugs in Taiwan: an overview of outpatient sector in 2000. | journal = Zhonghua Yi Xue Za Zhi (Taipei) | volume = 65 | issue = 8 | pages = 378–91 |date=Aug 2002 | PMID = 12455808 }}</ref><ref>{{cite web| url= http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html| title=Benzodiazepine Names| accessdate=2008-12-29| publisher=non-benzodiazepines.org.uk}}</ref> is a potent [[benzodiazepine]] and 2'-fluoro derivative of [[diazepam]],<ref>{{Cite journal | last1 = Neville | first1 = GA. | last2 = Beckstead | first2 = HD. | last3 = Shurvell | first3 = HF. | title = A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam. | journal = J Pharm Sci | volume = 83 | issue = 2 | pages = 143–51 |date=Feb 1994 | PMID = 7909552 | doi=10.1002/jps.2600830207}}</ref> originally developed by [[Hoffman-La Roche]] in the 1960s.<ref>US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES</ref> It is marketed in [[Japan]] and [[Taiwan]] in the form of 0.25&nbsp;mg tablets, making it around 40x more potent than diazepam. It exerts its pharmacological properties via enhancement of GABAergic inhibition.<ref>{{Cite journal | last1 = Tsuchiya | first1 = T. | last2 = Fukushima | first2 = H. | title = Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons. | journal = Eur J Pharmacol | volume = 48 | issue = 4 | pages = 421–4 |date=Apr 1978 | PMID = 648585 | doi=10.1016/0014-2999(78)90169-3}}</ref> Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than [[diazepam]].<ref>{{Cite journal | last1 = Nakatsuka | first1 = I. | last2 = Shimizu | first2 = H. | last3 = Asami | first3 = Y. | last4 = Katoh | first4 = T. | last5 = Hirose | first5 = A. | last6 = Yoshitake | first6 = A. | title = Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. | journal = Life Sci | volume = 36 | issue = 2 | pages = 113–9 |date=Jan 1985 | pmid = 2857046 | doi=10.1016/0024-3205(85)90089-X}}</ref> It possesses [[anxiolytic]],<ref>{{Cite journal | last1 = Okada | first1 = S. | last2 = Ichiki | first2 = K. | last3 = Tanokuchi | first3 = S. | last4 = Ishii | first4 = K. | last5 = Hamada | first5 = H. | last6 = Ota | first6 = Z. | title = Effect of an anxiolytic on lipid profile in non-insulin-dependent diabetes mellitus. | journal = J Int Med Res | volume = 22 | issue = 6 | pages = 338–42 | PMID = 7895897 | year=1994}}</ref><ref>{{Cite journal | last1 = Okada | first1 = S. | last2 = Ichiki | first2 = K. | last3 = Tanokuchi | first3 = S. | last4 = Ishii | first4 = K. | last5 = Hamada | first5 = H. | last6 = Ota | first6 = Z. | title = Improvement of stress reduces glycosylated haemoglobin levels in patients with type 2 diabetes. | journal = J Int Med Res | volume = 23 | issue = 2 | pages = 119–22 | PMID = 7601294 | year=1995}}</ref><ref>{{Cite journal | last1 = Okada | first1 = S. | last2 = Ichiki | first2 = K. | last3 = Tanokuchi | first3 = S. | last4 = Ishii | first4 = K. | last5 = Hamada | first5 = H. | last6 = Ota | first6 = Z. | title = How blood pressure in patients with non-insulin-dependent diabetes mellitus is influenced by stress. | journal = J Int Med Res | volume = 23 | issue = 5 | pages = 377–80 | PMID = 8529781 | year=1995}}</ref> [[anticonvulsant]], [[sedative]], [[hypnotic]] and [[skeletal muscle relaxant]] properties.<ref>{{Cite journal | last1 = Inoue | first1 = H. | last2 = Maeno | first2 = Y. | last3 = Iwasa | first3 = M. | last4 = Matoba | first4 = R. | last5 = Nagao | first5 = M. | title = Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry. | journal = Forensic Sci Int | volume = 113 | issue = 1-3 | pages = 367–73 |date=Sep 2000 | pmid = 10978650 | doi=10.1016/S0379-0738(00)00226-7}}</ref>
'''Fludiazepam''', marketed under the brand name '''Erispan'''<ref>{{Cite journal | last1 = Su | first1 = TP. | last2 = Chen | first2 = TJ. | last3 = Hwang | first3 = SJ. | last4 = Chou | first4 = LF. | last5 = Fan | first5 = AP. | last6 = Chen | first6 = YC. | title = Utilization of psychotropic drugs in Taiwan: an overview of outpatient sector in 2000. | journal = Zhonghua Yi Xue Za Zhi (Taipei) | volume = 65 | issue = 8 | pages = 378–91 |date=Aug 2002 | PMID = 12455808 }}</ref><ref>{{cite web| url= http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html| title=Benzodiazepine Names| accessdate=2008-12-29| publisher=non-benzodiazepines.org.uk}}</ref> is a potent [[benzodiazepine]] and 2'-fluoro derivative of [[diazepam]],<ref>{{Cite journal | last1 = Neville | first1 = GA. | last2 = Beckstead | first2 = HD. | last3 = Shurvell | first3 = HF. | title = A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam. | journal = J Pharm Sci | volume = 83 | issue = 2 | pages = 143–51 |date=Feb 1994 | PMID = 7909552 | doi=10.1002/jps.2600830207}}</ref> originally developed by [[Hoffman-La Roche]] in the 1960s.<ref>US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES</ref> It is marketed in [[Japan]] and [[Taiwan]] in the form of 0.25&nbsp;mg tablets, making it around 40x more potent than diazepam. It exerts its pharmacological properties via enhancement of GABAergic inhibition.<ref>{{Cite journal | last1 = Tsuchiya | first1 = T. | last2 = Fukushima | first2 = H. | title = Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons. | journal = Eur J Pharmacol | volume = 48 | issue = 4 | pages = 421–4 |date=Apr 1978 | PMID = 648585 | doi=10.1016/0014-2999(78)90169-3}}</ref> Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than [[diazepam]].<ref>{{Cite journal | last1 = Nakatsuka | first1 = I. | last2 = Shimizu | first2 = H. | last3 = Asami | first3 = Y. | last4 = Katoh | first4 = T. | last5 = Hirose | first5 = A. | last6 = Yoshitake | first6 = A. | title = Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. | journal = Life Sci | volume = 36 | issue = 2 | pages = 113–9 |date=Jan 1985 | pmid = 2857046 | doi=10.1016/0024-3205(85)90089-X}}</ref> It possesses [[anxiolytic]],<ref>{{Cite journal | last1 = Okada | first1 = S. | last2 = Ichiki | first2 = K. | last3 = Tanokuchi | first3 = S. | last4 = Ishii | first4 = K. | last5 = Hamada | first5 = H. | last6 = Ota | first6 = Z. | title = Effect of an anxiolytic on lipid profile in non-insulin-dependent diabetes mellitus. | journal = J Int Med Res | volume = 22 | issue = 6 | pages = 338–42 | PMID = 7895897 | year=1994}}</ref><ref>{{Cite journal | last1 = Okada | first1 = S. | last2 = Ichiki | first2 = K. | last3 = Tanokuchi | first3 = S. | last4 = Ishii | first4 = K. | last5 = Hamada | first5 = H. | last6 = Ota | first6 = Z. | title = Improvement of stress reduces glycosylated haemoglobin levels in patients with type 2 diabetes. | journal = J Int Med Res | volume = 23 | issue = 2 | pages = 119–22 | PMID = 7601294 | year=1995}}</ref><ref>{{Cite journal | last1 = Okada | first1 = S. | last2 = Ichiki | first2 = K. | last3 = Tanokuchi | first3 = S. | last4 = Ishii | first4 = K. | last5 = Hamada | first5 = H. | last6 = Ota | first6 = Z. | title = How blood pressure in patients with non-insulin-dependent diabetes mellitus is influenced by stress. | journal = J Int Med Res | volume = 23 | issue = 5 | pages = 377–80 | PMID = 8529781 | year=1995}}</ref> [[anticonvulsant]], [[sedative]], [[hypnotic]] and [[skeletal muscle relaxant]] properties.<ref>{{Cite journal | last1 = Inoue | first1 = H. | last2 = Maeno | first2 = Y. | last3 = Iwasa | first3 = M. | last4 = Matoba | first4 = R. | last5 = Nagao | first5 = M. | title = Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry. | journal = Forensic Sci Int | volume = 113 | issue = 1-3 | pages = 367–73 |date=Sep 2000 | pmid = 10978650 | doi=10.1016/S0379-0738(00)00226-7}}</ref>


Revision as of 19:29, 9 April 2015

Fludiazepam
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E number{{#property:P628}}
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FormulaC16H12ClFN2O
Molar mass302.7
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Fludiazepam, marketed under the brand name Erispan[1][2] is a potent benzodiazepine and 2'-fluoro derivative of diazepam,[3] originally developed by Hoffman-La Roche in the 1960s.[4] It is marketed in Japan and Taiwan in the form of 0.25 mg tablets, making it around 40x more potent than diazepam. It exerts its pharmacological properties via enhancement of GABAergic inhibition.[5] Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam.[6] It possesses anxiolytic,[7][8][9] anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.[10]

As with all benzodiazepines, fludiazepam is used recreationally.[11]

References

  1. ↑ Su, TP.; Chen, TJ.; Hwang, SJ.; Chou, LF.; Fan, AP.; Chen, YC. (Aug 2002). "Utilization of psychotropic drugs in Taiwan: an overview of outpatient sector in 2000". Zhonghua Yi Xue Za Zhi (Taipei). 65 (8): 378–91. PMID 12455808.
  2. ↑ "Benzodiazepine Names". non-benzodiazepines.org.uk. Retrieved 2008-12-29.
  3. ↑ Neville, GA.; Beckstead, HD.; Shurvell, HF. (Feb 1994). "A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam". J Pharm Sci. 83 (2): 143–51. doi:10.1002/jps.2600830207. PMID 7909552.
  4. ↑ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
  5. ↑ Tsuchiya, T.; Fukushima, H. (Apr 1978). "Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons". Eur J Pharmacol. 48 (4): 421–4. doi:10.1016/0014-2999(78)90169-3. PMID 648585.
  6. ↑ Nakatsuka, I.; Shimizu, H.; Asami, Y.; Katoh, T.; Hirose, A.; Yoshitake, A. (Jan 1985). "Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity". Life Sci. 36 (2): 113–9. doi:10.1016/0024-3205(85)90089-X. PMID 2857046.
  7. ↑ 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". J Int Med Res. 22 (6): 338–42. PMID 7895897.
  8. ↑ 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". J Int Med Res. 23 (2): 119–22. PMID 7601294.
  9. ↑ 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". J Int Med Res. 23 (5): 377–80. PMID 8529781.
  10. ↑ Inoue, H.; Maeno, Y.; Iwasa, M.; Matoba, R.; Nagao, M. (Sep 2000). "Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry". Forensic Sci Int. 113 (1–3): 367–73. doi:10.1016/S0379-0738(00)00226-7. PMID 10978650.
  11. ↑ 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 (111): 47–56. PMID 7920567.

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