氟地西泮

氟地西泮
临床资料
AHFS/Drugs.com	国际药品名称
怀孕分级	?;
给药途径	Oral
ATC码	N05BA17 (WHO) ;
法律规范状态
法律规范	加：Schedule IV; 德：Anlage III; 台：第四级管制药品; 美：附表IV; Schedule IV(US);
药物动力学数据
生物利用度	?
药物代谢	肝脏
生物半衰期	?
排泄途径	肾
识别信息
	IUPAC命名法 7-chloro-5-(2-fluorophenyl)-1-methyl-1H-benzo[e][1,4]diazepin-2(3H)-one; ;
CAS号	3900-31-0
PubChem CID	3369;
DrugBank	DB01567 ;
ChemSpider	3252 ;
UNII	7F64A2K16Z;
KEGG	D01354 ;
ChEBI	CHEBI:31618 ;
ChEMBL	ChEMBL13291 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID00192277 ;
ECHA InfoCard	100.292.343
化学信息
化学式	C16H12ClFN2O
摩尔质量	302.7
3D模型（JSmol（英语：JSmol））	交互式图像;
	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 ;

氟地西泮（Fludiazepam）是由罗氏药厂（Hoffman-LaRoche）在20世纪60年代所开发的一种苯二氮平类药物之衍生药物，和地西泮有密切关联^[1]^[2]。在日本商品名（Erispan）、在台湾商品名 “愈利舒盼锭”（Erispan）、福安源锭（Flupine），用0.25毫克的片剂装来销售^[3]^[4]。

氟地西泮通过增强GABA的抑制性来发挥其药理特性^[5]，且氟地西泮对苯二氮卓受体（benzodiazepine receptor）比起对地西泮来有四倍多的结合亲和力^[6]。它具有抗焦虑^[7]^[8]^[9]、抗惊厥、镇静、催眠及骨骼肌松弛等特性^[10]。不过，氟地西泮有药物滥用的潜在趋势^[11]，在多个国家列为管制药品。

注释

^ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
^ Neville, GA.; Beckstead, HD.; Shurvell, HF. A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam.. J Pharm Sci. Feb 1994, 83 (2): 143–51. PMID 7909552. doi:10.1002/jps.2600830207.
^ 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 (Taipei). Aug 2002, 65 (8): 378–91. PMID 12455808.
^ Benzodiazepine Names. non-benzodiazepines.org.uk. [2008-12-29]. （原始内容存档于2008-12-08）.
^ Tsuchiya, T.; Fukushima, H. Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons.. Eur J Pharmacol. Apr 1978, 48 (4): 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 Sci. Jan 1985, 36 (2): 113–9. PMID 2857046. doi:10.1016/0024-3205(85)90089-X.
^ Okada, S.; Ichiki, K.; Tanokuchi, S.; Ishii, K.; Hamada, H.; Ota, Z. Effect of an anxiolytic on lipid profile in non-insulin-dependent diabetes mellitus.. J Int Med Res. 1994, 22 (6): 338–42. PMID 7895897.
^ Okada, S.; Ichiki, K.; Tanokuchi, S.; Ishii, K.; Hamada, H.; Ota, Z. Improvement of stress reduces glycosylated haemoglobin levels in patients with type 2 diabetes.. J Int Med Res. 1995, 23 (2): 119–22. PMID 7601294.
^ Okada, S.; Ichiki, K.; Tanokuchi, S.; Ishii, K.; Hamada, H.; Ota, Z. How blood pressure in patients with non-insulin-dependent diabetes mellitus is influenced by stress.. J Int Med Res. 1995, 23 (5): 377–80. PMID 8529781.
^ 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 Sci Int. Sep 2000, 113 (1-3): 367–73. PMID 10978650. doi:10.1016/S0379-0738(00)00226-7.
^ Shimamine, M.; Masunari, T.; Nakahara, Y. [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. 1993, (111): 47–56. PMID 7920567.

参见

苯二氮平类药物

外部链接

（日语） Erispan フルジアゼパム锭，细粒^{[永久失效链接]} (PDF) Dainippon Sumitomo Pharma. November 2005.
（日语） Official Dainippon Sumitomo Pharma Website （页面存档备份，存于互联网档案馆）

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

[2] Neville, GA.; Beckstead, HD.; Shurvell, HF. A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam.. J Pharm Sci. Feb 1994, 83 (2): 143–51. PMID 7909552. doi:10.1002/jps.2600830207.

[3] 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 (Taipei). Aug 2002, 65 (8): 378–91. PMID 12455808.

[4] Benzodiazepine Names. non-benzodiazepines.org.uk. [2008-12-29]. （原始内容存档于2008-12-08）.

[5] Tsuchiya, T.; Fukushima, H. Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons.. Eur J Pharmacol. Apr 1978, 48 (4): 421–4. PMID 648585. doi:10.1016/0014-2999(78)90169-3.

[6] 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 Sci. Jan 1985, 36 (2): 113–9. PMID 2857046. doi:10.1016/0024-3205(85)90089-X.

[7] Okada, S.; Ichiki, K.; Tanokuchi, S.; Ishii, K.; Hamada, H.; Ota, Z. Effect of an anxiolytic on lipid profile in non-insulin-dependent diabetes mellitus.. J Int Med Res. 1994, 22 (6): 338–42. PMID 7895897.

[8] Okada, S.; Ichiki, K.; Tanokuchi, S.; Ishii, K.; Hamada, H.; Ota, Z. Improvement of stress reduces glycosylated haemoglobin levels in patients with type 2 diabetes.. J Int Med Res. 1995, 23 (2): 119–22. PMID 7601294.

[9] Okada, S.; Ichiki, K.; Tanokuchi, S.; Ishii, K.; Hamada, H.; Ota, Z. How blood pressure in patients with non-insulin-dependent diabetes mellitus is influenced by stress.. J Int Med Res. 1995, 23 (5): 377–80. PMID 8529781.

[10] 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 Sci Int. Sep 2000, 113 (1-3): 367–73. PMID 10978650. doi:10.1016/S0379-0738(00)00226-7.

[11] Shimamine, M.; Masunari, T.; Nakahara, Y. [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. 1993, (111): 47–56. PMID 7920567.

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