Systematic (IUPAC) name | |
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7-chloro-5-(2-fluorophenyl)-1-methyl-1H-benzo[e][1,4]diazepin-2(3H)-one
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Clinical data | |
AHFS/Drugs.com | International Drug Names |
Pregnancy category |
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Legal status |
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Routes of administration |
Oral |
Pharmacokinetic data | |
Bioavailability | ? |
Metabolism | Hepatic |
Biological half-life | ? |
Excretion | Renal |
Identifiers | |
CAS Registry 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 |
Molecular mass | 302.7 |
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Fludiazepam, marketed under the brand name Erispan[1][2] is a potent benzodiazepine and 2'-fluoro derivative of diazepam,[3] originally developed by Hoffman-La Roche in the 1960s.[4] It is marketed in Japan and Taiwan in the form of 0.25 mg tablets, making it around 40x more potent than diazepam. 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]
As with all benzodiazepines, fludiazepam is used recreationally.[11]
See also
- Benzodiazepine
- Diazepam
- Diclazepam (the 2'-chloro-analogue).
- Flunitrazepam (the 7-nitro-analogue).
References
- ^ 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.
- ^ US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES
- ^ 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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