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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/07/03 09:41:44」(JST)

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Fludiazepam was developed by Hoffman-LaRoche in the 1960s^[1] and is marketed in Japan and Taiwan in 0.25mg tablets under the brand name Erispan^[2]^[3] is a drug which is a benzodiazepine derivative and is closely related to diazepam.^[4] 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]

Fludiazepam has drug abuse potential.^[11]

References

^ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
^ 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.
^ 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

(Japanese) Erispan フルジアゼパム錠，細粒 (PDF) Dainippon Sumitomo Pharma. November 2005.
(Japanese) Official Dainippon Sumitomo Pharma Website

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English Journal

Development and validation of an EI-GC-MS method for the determination of benzodiazepine drugs and their metabolites in blood: applications in clinical and forensic toxicology.

Papoutsis II, Athanaselis SA, Nikolaou PD, Pistos CM, Spiliopoulou CA, Maravelias CP.Author information Department of Forensic Medicine and Toxicology, School of Medicine, National and Kapodistrian University of Athens, Mikras Asias 75, Athens 11527, Greece. jopamal@hotmail.comAbstractBenzodiazepines are used widely in daily clinical practice, due to their multiple pharmacological actions. The frequent problems associated with the wide use of benzodiazepines, as well as the multiple incidents of poisonings, led to the necessity for the development of a precise, sensitive and rapid method for the simultaneous determination of the 23 most commonly used benzodiazepines (diazepam, nordiazepam, oxazepam, bromazepam, alprazolam, lorazepam, medazepam, flurazepam, fludiazepam, tetrazepam, chlordiazepoxide, clobazam, midazolam, flunitrazepam, 7-amino-flunitrazepam, triazolam, prazepam, nimetazepam, nitrazepam, temazepam, lormetazepam, clonazepam, camazepam) in blood. A gas chromatographic method combined with mass spectrometric detection was developed, optimized and validated for the determination of the above substances. This method includes liquid-liquid extraction with chloroform at pH 9 and two stages of derivatization using tetramethylammonium hydroxide and propyliodide (propylation), as well as a mixture of triethylamine:propionic anhydride (propionylation). The recoveries were higher than 74% for all the benzodiazepines. The calibration curves were linear within the dynamic range of each benzodiazepine with a correlation coefficient higher than 0.9981. The limits of detection and quantification for each analyte were statistically calculated from the relative calibration curves. Accuracy and precision were also calculated and were found to be less than 8.5% and 11.1%, respectively. The developed method was successfully applied for the investigation of both forensic and clinical toxicological cases of accidental and suicidal poisoning.
Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2010 Aug 1;52(4):609-14. doi: 10.1016/j.jpba.2010.01.027. Epub 2010 Feb 1.
Benzodiazepines are used widely in daily clinical practice, due to their multiple pharmacological actions. The frequent problems associated with the wide use of benzodiazepines, as well as the multiple incidents of poisonings, led to the necessity for the development of a precise, sensitive and rapi
PMID 20172681

Simultaneous determination of benzodiazepines and their metabolites in human serum by liquid chromatography-tandem mass spectrometry using a high-resolution octadecyl silica column compatible with aqueous compounds.

Nakamura M, Ohmori T, Itoh Y, Terashita M, Hirano K.Author information Laboratory of Drug Informatics, Gifu Pharmaceutical University, 5-6-1 Mitahora-higashi, Gifu 502-8585, Japan. mnakamura@gifu-pu.ac.jpAbstractA liquid chromatography-tandem mass spectrometry (LC-MS/MS) method using a high-resolution octadecyl silica column compatible with aqueous compounds was developed for the simultaneous determination of benzodiazepines and their metabolites in human serum. This method enabled us to determine multiple benzodiazepines, including flurazepam, bromazepam, chlordiazepoxide, nitrazepam, clonazepam, flunitrazepam, estazolam, clobazam, lorazepam, alprazolam, triazolam, brotizolam, fludiazepam, diazepam, quazepam, prazepam and their metabolites such as 7-aminonitrazepam, 7-aminoclonazepam, 7-acetamidonitrazepam, N-desmethylclobazam and N-desmethyldiazepam. The analytes spiked into human serum were subjected to solid-phase extraction followed by liquid chromatography coupled with electrospray ionization tandem mass spectrometry. The running time was within 25 min for the measurement of 22 benzodiazepines and their metabolites. The recovery rates exceeded 58.1% for those compounds except for quazepam, which showed a recovery of 45.8%. The limit of detection ranged from 0.3 to 11.4 ng/mL. Linearity was satisfactory for all compounds. These data suggest that the present method can be applicable to routine assay for benzodiazepines in the clinical setting.
Biomedical chromatography : BMC.Biomed Chromatogr.2009 Apr;23(4):357-64. doi: 10.1002/bmc.1122.
A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method using a high-resolution octadecyl silica column compatible with aqueous compounds was developed for the simultaneous determination of benzodiazepines and their metabolites in human serum. This method enabled us to determine multiple
PMID 18937304

Non-life-threatening leukopenia in a renal transplant recipient with acute overdose of mycophenolate mofetil.

Wu SW, Chang HR, Lai YR, Lian JD.Author information Division of Nephrology, Department of Internal Medicine, Chung Shan Medical University Hospital, Taichung, Taiwan.AbstractMycophenolate mofetil (MMF) is increasingly used as an immunosuppressant for organ transplantation and for treatment of autoimmune diseases. As yet, the experience with acute overdose of MMF in humans is limited. Herein we have reported a 40-year-old female kidney recipient with moderate leukopenia and lack of gastrointestinal toxicity following ingestion of 25 g MMF, which was confirmed by serum drug levels. We treated the patient with charcoal decontamination and oral cholestyramine. She recovered completely without sequelae.
Transplantation proceedings.Transplant Proc.2008 Dec;40(10):3770-1. doi: 10.1016/j.transproceed.2008.06.100.
Mycophenolate mofetil (MMF) is increasingly used as an immunosuppressant for organ transplantation and for treatment of autoimmune diseases. As yet, the experience with acute overdose of MMF in humans is limited. Herein we have reported a 40-year-old female kidney recipient with moderate leukopenia
PMID 19100486

Japanese Journal

DETECTION OF BENZODIAZEPINES IN HUMAN URINE BY DIRECT IMMERSION SOLID PHASE MICRO EXTRACTION AND GAS CHROMATOGRAPHY

Seno Hiroshi,Kumazawa Takeshi,Ishii Akira,Watanabe Kanako,Hattori Hideki,Suzuki Osamu
1997-01-31
… Medazepam, fludiazepam, diazepam, midazolam, flunitrazepam, prazepam, nimetazepam and flurazepam could be extracted under the present DI-SPME conditions, and their recoveries were 1.55-17.0%. … those for medazepam, fludiazepam, diazepam, midazolam, flunitrazepam, prazepam and flurazepam were 10-20 ng/ml.rights:日本法中毒学会rights:本文データは日本法中毒学会の許諾のもと掲載しています。 …
NAID 120005314025

Clinical Effect of Fludiazepam on Tinnitus. Comparison with the Result of Lidocaine Test.:-Comparison with the Result of Lidocaine Test-

清田隆二,今給黎泰二郎,渡辺荘郁,岩淵康雄,鰺坂孝二,大山勝
耳鼻咽喉科臨床 86(10), 1387-1395, 1993
… The therapeutic effect of fludiazepam was studied in 72 patients with tinnitus. … Subjects were given oral fludiazepam 0.75mg daily, and the severity of tinnitus was recorded before and two or four weeks after the start of administration.The medication was effective in 65.3% of the patients. … However, the efficacy of fludiazepam did not correlate with findings of a psychological test (TMI test: Toho-medical index test).A side effect, sleepiness was detected in 15.3% of 72 patients. …
NAID 130001812497

Comparison of the effects of benzodiazepine and nonbenzodiazepine anxiolytics on mouse-killing behavior in rats.

TAKAOKA Nobuyuki,YOSHIMURA Hiroyuki,OGAWA Nobuya
The Japanese Journal of Pharmacology 46(3), 315-318, 1988
… The following drugs were administered 1ntraperitonea Ily: chlord 1azepoxide, diazepam, ethyl loflazepate, fludiazepam, zopiclone, suriclone, and CL 218, 872. … Among these drugs, suriclone (ED50=1.3 mg/kg) and fludiazepam (ED50=5.9 mg/kg) showed potent suppressive effects. …
NAID 130000832126

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★リンクテーブル★

リンク元

「フルジアゼパム」

Fludiazepam
Systematic (IUPAC) name
	7-chloro-5-(2-fluorophenyl)-1-methyl-1H-benzo[e][1,4]diazepin-2(3H)-one
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	?
Legal status	Schedule IV(US)
Routes	Oral
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Half-life	?
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
Mol. 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 ;
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　　[★]

英: fludiazepam
商: エリスパン

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

[2] 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.

[3] "Benzodiazepine Names". non-benzodiazepines.org.uk. Retrieved 2008-12-29.

[4] 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.

[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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fludiazepam