Fludiazepam

Fludiazepam
Systematic (IUPAC) name
	7-chloro-5-(2-fluorophenyl)-1-methyl-3H-1,4-benzodiazepin-2-one
Clinical data
Trade names	Erispan (JP, TW)
AHFS/Drugs.com	International Drug Names
Legal status	CA: Schedule IV; DE: Anlage III; US: Schedule IV;
Routes of; administration	Oral (tablets)
Pharmacokinetic data
Metabolism	Hepatic
Excretion	Renal
Identifiers
CAS Number	3900-31-0
ATC code	N05BA17
PubChem	CID 3369
DrugBank	DB01567
ChemSpider	3252
UNII	7F64A2K16Z
KEGG	D01354
ChEBI	CHEBI:31618
ChEMBL	CHEMBL13291
Chemical data
Formula	C16H12ClFN2O
Molar mass	302.7
	SMILES O=C1CN=C(C2=CC=CC=C2F)C3=CC(Cl)=CC=C3N1C ;
	InChI 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 ; Key:ROYOYTLGDLIGBX-UHFFFAOYSA-N ;
(verify)

Fludiazepam, marketed under the brand name Erispan (エリスパン)^[1]^[2] is a potent benzodiazepine and 2ʹ-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[edit]

^ 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.
^ "Benzodiazepine Names". non-benzodiazepines.org.uk. Retrieved 2008-12-29.
^ 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.
^ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.

External links[edit]

(Japanese) "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." (PDF). Sumitomo Dainippon Pharma.
(Japanese) Official Dainippon Sumitomo Pharma Website

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[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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Jan	FEB	Mar
	24
2015	2016	2017

Fludiazepam

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