氟地西泮

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氟地西泮
IUPAC命名
7-chloro-5-(2-fluorophenyl)-1-methyl-1H-benzo[e][1,4]diazepin-2(3H)-one
識別
CAS號 3900-31-0 ✓
ATC編碼 N05BA17
PubChem CID 3369
DrugBank DB01567
ChemSpider 3252 ✓
UNII 7F64A2K16Z ✓
KEGG D01354 ✓
ChEBI CHEBI:31618 ✓
ChEMBL CHEMBL13291 ✓
化學性質
化學式 C16H12ClFN2O 
分子量 302.7
SMILES 搜尋Jmol 3D模型eMoleculesPubChem
药代动力学性質
生物利用度  ?
代謝 肝臟
半衰期  ?
排泄
治療考量
懷孕分級  ?
合法狀態 Schedule IV(US)
途徑 Oral

氟地西泮(Fludiazepam)是由"霍夫曼-拉羅什"(Hoffman-LaRoche)在20世紀60年代、[1]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。[2] 氟地西泮在日本台灣是以藥品名稱<Erispan>、且用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"(GABAergic inhibition)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( anxiolytic),[7][8][9] 抗驚厥(Anticonvulsant),鎮靜(sedative),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]

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. doi:10.1002/jps.2600830207. PMID 7909552. 
  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]. 
  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. doi:10.1016/0014-2999(78)90169-3. PMID 648585. 
  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. doi:10.1016/0024-3205(85)90089-X. PMID 2857046. 
  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. doi:10.1016/S0379-0738(00)00226-7. PMID 10978650. 
  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. 

外部鏈接[编辑]