氟地西泮

化合物

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
临床资料
AHFS/Drugs.com国际药品名称
怀孕分级
  • ?
给药途径Oral
ATC码
法律规范状态
法律规范
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
识别信息
  • 7-chloro-5-(2-fluorophenyl)-1-methyl-1H-benzo[e][1,4]diazepin-2(3H)-one
CAS号3900-31-0  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.292.343 编辑维基数据链接
化学信息
化学式C16H12ClFN2O
摩尔质量302.7
3D模型(JSmol英语JSmol
  • 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 checkY
  • Key:ROYOYTLGDLIGBX-UHFFFAOYSA-N checkY

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

  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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外部链接