氟地西泮

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氟地西泮
Fludiazepam.svg
Fludiazepam3d.png
系统(IUPAC)命名名称
7-chloro-5-(2-fluorophenyl)-1-methyl-1H-benzo[e][1,4]diazepin-2(3H)-one
临床数据
Drugs.com 国际药品名称
妊娠分级
  •  ?
给药途径 Oral
合法狀態
合法状态
药代动力学数据
生物利用度 ?
代谢 肝臟
生物半衰期 ?
排泄
识别信息
CAS注册号 3900-31-0 ✓
ATC代码 N05BA17
PubChem CID 3369
DrugBank DB01567 ✓
ChemSpider 3252 ✓
UNII 7F64A2K16Z ✓
KEGG D01354 ✓
ChEBI CHEBI:31618 ✓
ChEMBL英语ChEMBL CHEMBL13291 ✓
化学信息
化学式 C16H12ClFN2O
摩尔质量 302.7
  (verify)

氟地西泮Fludiazepam)是由羅氏藥廠(Hoffman-LaRoche)在20世紀60年代所開發的一種苯二氮平類藥物之衍生藥物,和地西泮有密切關聯[1][2]。在日本商品名(Erispan)、在台灣商品名 「癒利舒盼錠」(Erispan)、福安源錠(Flupine),用0.25毫克的片劑裝來銷售[3][4]

氟地西泮通過增強GABA的抑制性來發揮其藥理特性[5],且氟地西泮對苯二氮卓受體(benzodiazepine receptor)比起對地西泮來有四倍多的結合親和力[6]。它具有抗焦慮[7][8][9]抗驚厥鎮靜催眠骨骼肌鬆弛等特性[10]。不過,氟地西泮有藥物濫用的潛在趨勢[11],在多個國家列為管制藥品

參見[编辑]

註釋[编辑]

  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. 

外部連結[编辑]