Fludiazepam
Fludiazepam[1], marketed under the brand name Erispan (エリスパン)[2][3] is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam,[4] originally developed by Hoffman-La Roche in the 1960s.[5] It is marketed in Japan and Taiwan. It exerts its pharmacological properties via enhancement of GABAergic inhibition.[6] Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam.[7] It possesses anxiolytic,[8][9][10] anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.[11] Fludiazepam has been used recreationally.[12]
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Trade names | Erispan (JP, TW) |
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Routes of administration | Oral (tablets) |
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Metabolism | Hepatic |
Excretion | Renal |
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Formula | C16H12ClFN2O |
Molar mass | 302.7 g·mol−1 |
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See also
- Diazepam
- Diclazepam (the 2ʹ-chloro analog)
- Difludiazepam (the 2',6'-difluoro derivative)
- Flunitrazepam (the 7-nitro analog)
- Flualprazolam (the triazolo derivative)
References
- US Patent 3371085 5-aryl-3h-1,4-benzodiazepin-2(1h)-ones
- 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. Archived from the original on 2008-12-08. 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
- "エリスパンフルジアゼパム錠0.25mg,細粒0.1% Erispan (fludiazepam tablets 0.25 mg, fine granules 0.1%) Prescribing Information" (in Japanese). Sumitomo Dainippon Pharma.
- (in Japanese) Official Dainippon Sumitomo Pharma Website
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