Moguisteine
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Formula | C16H21NO5S |
Molar mass | 339.41g·mol−1 |
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Moguisteineis a non-narcotic, peripherally actingantitussive.[1]In a small double-blind, randomized controlled trial, 200 mg of moguisteine suspension taken 3 times daily significantly reduced the frequency of coughing in patients withCOPD,compared to placebo.[2]It has also been studied in small trials in comparison to codeine[3]and dextromethorphan,[4]and has similar efficacy to both. It has not been approved for use in the United States.[5]
It was discovered by searching forexpectorantsof thethiazolidineclass, when compounds with a cough suppressant effect were accidentally found and moguisteine was selected as the most effective and safest representative of the class.[6]Its mechanism of action may be the activation ofATP-sensitive potassium channels.[7]
References
[edit]- ^Gallico L, Borghi A, Dalla Rosa C, Ceserani R, Tognella S (July 1994)."Moguisteine: a novel peripheral non-narcotic antitussive drug".British Journal of Pharmacology.112(3): 795–800.doi:10.1111/j.1476-5381.1994.tb13149.x.PMC1910192.PMID7921605.
- ^Aversa C, Cazzola M, Clini V, Dal Negro R, Maiorano V, Tana F, Allegra L (1993). "Clinical trial of the efficacy and safety of moguisteine in patients with cough associated with chronic respiratory diseases".Drugs Under Experimental and Clinical Research.19(6): 273–9.PMID8013271.
- ^Barnabè R, Berni F, Clini V, Pirrelli M, Pisani Ceretti A, Robuschi M, et al. (April 1995). "The efficacy and safety of moguisteine in comparison with codeine phosphate in patients with chronic cough".Monaldi Archives for Chest Disease = Archivio Monaldi per le Malattie del Torace.50(2): 93–7.PMID7613554.
- ^Del Donno M, Aversa C, Corsico R, Foresi A, Grassi V, Malerba M, et al. (1994). "Efficacy and Safety of Moguisteine in Comparison with Dextromethorphan in Patients with Persistent Cough".Drug Investigation.7(2): 93–100.doi:10.1007/BF03257404.S2CID72285850.
- ^Bolser DC (January 2006)."Cough suppressant and pharmacologic protussive therapy: ACCP evidence-based clinical practice guidelines".Chest.129(1 Suppl): 238S–249S.doi:10.1378/chest.129.1_suppl.238S.PMC3127247.PMID16428717.
- ^Gandolfi CA, Di Domenico R, Spinelli S, Gallico L, Fiocchi L, Lotto A, et al. (February 1995). "N-acyl-2-substituted-1,3-thiazolidines, a new class of non-narcotic antitussive agents: studies leading to the discovery of ethyl 2-[(2-methoxyphenoxy)methyl]-beta-oxothiazolidine-3-propanoate".Journal of Medicinal Chemistry.38(3): 508–25.doi:10.1021/jm00003a014.PMID7853344.
- ^Morita K, Kamei J (April 2000). "Involvement of ATP-sensitive K(+) channels in the anti-tussive effect of moguisteine".European Journal of Pharmacology.395(2): 161–4.doi:10.1016/s0014-2999(00)00197-7.PMID10794823.