Dimemorfan
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| Clinical data | |
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| Trade names | Astomin, Datosin, Gentus |
| AHFS/Drugs.com | International Drug Names |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.048.134 |
| Chemical and physical data | |
| Formula | C18H25N |
| Molar mass | 255.405g·mol−1 |
| 3D model (JSmol) | |
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Dimemorfan(INN) (ordimemorphan) (brand namesAstomin,Dastosirr,Tusben), ordimemorfan phosphate(JAN), also known as3,17-dimethylmorphinan,is anantitussive(cough suppressant) of themorphinanfamily that is widely used inJapanand is also marketed inSpainandItaly.[1][2][3][4]It was developed byYamanouchi Pharmaceutical(nowAstellas Pharma) and introduced in Japan in 1975.[3]It was later introduced in Spain in 1981 and Japan in 1985.[5]
Side effects
[edit]Adverse effects include nausea, somnolence, dry mouth, and decreased appetite.[5]
Pharmacology
[edit]Dimemorfan is ananalogueofdextromethorphan(DXM) and itsactive metabolitedextrorphan(DXO), and similarly to them, acts as a potentagonistof theσ1receptor(Ki= 151 nM).[6][7]However, unlike DXM and DXO, it does not act significantly as anNMDA receptor antagonist(Ki= 16,978 nM), and for this reason, lacksdissociativeeffects, thereby having reducedside effectsandabuse potentialin comparison.[8][9]Similarly to DXM and DXO, dimemorfan has only relatively lowaffinityfor theσ2receptor(Ki= 4,421 nM).[7]
See also
[edit]- Cough syrup
- Noscapine
- Codeine;Pholcodine
- Dextromethorphan
- Racemorphan;Dextrorphan;Levorphanol
- Butamirate
- Pentoxyverine
- Tipepidine
- Cloperastine
- Levocloperastine
References
[edit]- ^Elks J (14 November 2014).The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies.Springer. pp. 427–.ISBN978-1-4757-2085-3.
- ^Bruera E, Higginson I, von Gunten CF, Morita T (15 January 2015).Textbook of Palliative Medicine and Supportive Care, Second Edition.CRC Press. pp. 677–.ISBN978-1-4441-3526-8.
- ^abIda H (1997). "The nonnarcotic antitussive drug dimemorfan: a review".Clinical Therapeutics.19(2): 215–231.doi:10.1016/S0149-2918(97)80111-7.PMID9152562.
- ^Armstrong LL, Goldman MP (1 January 2005).Lexi-Comp's Drug Information Handbook International: With Canadian and International Drug Monographs.Lexi-Comp.ISBN978-1-59195-110-0.
- ^abSchlesser JL (1991).Drugs Available Abroad, 1st Edition.Derwent Publications Ltd. p. 66.ISBN0-8103-7177-4.
- ^Maurice T, Su TP (November 2009)."The pharmacology of sigma-1 receptors".Pharmacology & Therapeutics.124(2): 195–206.doi:10.1016/j.pharmthera.2009.07.001.PMC2785038.PMID19619582.
- ^abBotana LM, Loza M (20 April 2012).Therapeutic Targets: Modulation, Inhibition, and Activation.John Wiley & Sons. pp. 234–.ISBN978-1-118-18552-0.
- ^Chou YC, Liao JF, Chang WY, Lin MF, Chen CF (March 1999). "Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan".Brain Research.821(2): 516–519.doi:10.1016/S0006-8993(99)01125-7.PMID10064839.S2CID22762264.
- ^Shin EJ, Nah SY, Kim WK, Ko KH, Jhoo WK, Lim YK, et al. (April 2005)."The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan".British Journal of Pharmacology.144(7): 908–918.doi:10.1038/sj.bjp.0705998.PMC1576070.PMID15723099.
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