Dextromethorphan (DXM) is a cough suppressant used in many cough and cold medicines.[6] It affects serotonin, norepinephrine, NMDA, and sigma-1 receptors in the brain, all of which have been implicated in the pathophysiology of depression. In 2022, the FDA approved the combination dextromethorphan/bupropion to serve as a rapid acting antidepressant in patients with major depressive disorder.[7]
It is in the morphinan class of medications with sedative, dissociative, and stimulant properties (at lower doses). Dextromethorphan does not have a significant affinity for the mu-opioid receptor activity typical of morphinan compounds and exerts its therapeutic effects through several other receptors.[8] In its pure form, dextromethorphan occurs as a white powder.[9]
When exceeding approved dosages, dextromethorphan acts as a dissociative hallucinogen. It has multiple mechanisms of action, including actions as a nonselective serotonin reuptake inhibitor[10] and a sigma-1 receptor agonist.[11][12] Dextromethorphan and its major metabolite, dextrorphan, also block the NMDA receptor at high doses, which produces effects similar to other dissociative anesthetics such as ketamine, nitrous oxide, and phencyclidine.
It was patented in 1949 and approved for medical use in 1953.[13]
^"Dextromethorphan Monograph for Professionals". Drugs.com.
^Windhab LG, Gastberger S, Hulka LM, Baumgartner MR, Soyka M, Müller TJ, et al. (2020). "Dextromethorphan Abuse Among Opioid-Dependent Patients". Clinical Neuropharmacology. 43 (5): 127–133. doi:10.1097/WNF.0000000000000403. PMID 32947422. S2CID 221798401.
^McCarthy B (2023-11-30). "Dextromethorphan-bupropion (Auvelity) for the Treatment of Major Depressive Disorder". Clinical Psychopharmacology and Neuroscience. 21 (4): 609–616. PMID 37859435.
^Kukanich B, Papich MG (October 2004). "Plasma profile and pharmacokinetics of dextromethorphan after intravenous and oral administration in healthy dogs". Journal of Veterinary Pharmacology and Therapeutics. 27 (5): 337–341. doi:10.1111/j.1365-2885.2004.00608.x. PMID 15500572.
^"Balminil DM, Benylin DM (dextromethorphan) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 15 April 2014.
^Dicpinigaitis P (2022-09-12). "The Current and Emerging Treatment Landscape for Chronic Cough". The American Journal of Managed Care. Uncovering the Economic Burden of Chronic Cough and the Promising Role of Emerging Targeted Therapies. 28 (9): S159–S165. doi:10.37765/ajmc.2022.89244. PMID 36198074. S2CID 252736111. By sales, dextromethorphan is the most widely used OTC antitussive drug in the United States, and approximately 85% to 90% of OTC cough medicines contain dextromethorphan
^Majeed A, Xiong J, Teopiz KM, Ng J, Ho R, Rosenblat JD, et al. (March 2021). "Efficacy of dextromethorphan for the treatment of depression: a systematic review of preclinical and clinical trials". Expert Opinion on Emerging Drugs. 26 (1): 63–74. doi:10.1080/14728214.2021.1898588. PMID 33682569. S2CID 232141396.
^Taylor CP, Traynelis SF, Siffert J, Pope LE, Matsumoto RR (August 2016). "Pharmacology of dextromethorphan: Relevance to dextromethorphan/quinidine (Nuedexta®) clinical use". Pharmacology & Therapeutics. 164: 170–182. doi:10.1016/j.pharmthera.2016.04.010. PMID 27139517.
^"Reference Tables: Description and Solubility - D". Archived from the original on 2017-07-04. Retrieved 2011-05-06.
^Shin EJ, Nah SY, Chae JS, Bing G, Shin SW, Yen TP, et al. (May 2007). "Dextromethorphan attenuates trimethyltin-induced neurotoxicity via sigma1 receptor activation in rats". Neurochemistry International. 50 (6): 791–799. doi:10.1016/j.neuint.2007.01.008. PMID 17386960. S2CID 43230896.
^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. PMC 1576070. PMID 15723099.
^Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 527. ISBN 9783527607495.
Dextromethorphan (DXM) is a cough suppressant used in many cough and cold medicines. It affects serotonin, norepinephrine, NMDA, and sigma-1 receptors...
Dextromethorphan, or DXM, a common active ingredient found in many over-the-counter cough suppressant cold medicines, is used as a recreational drug and...
Flukit; with dextromethorphan as Axcel Dextrozine and Hosedyl DM; with dextromethorphan and ephedrine as Methorsedyl; with dextromethorphan and pseudoephedrine...
O-demethylation of dextromethorphan by CYP2D6. Dextrorphan is an NMDA antagonist and contributes to the psychoactive effects of dextromethorphan. The pharmacology...
resolution outcomes versus no treatment. Abuse and recreational use of dextromethorphan have been reported with over-the-counter preparations and can cause...
and is sometimes combined with the antitussive (cough suppressant) dextromethorphan, such as in Mucinex DM or Robitussin DM. It is also combined with ephedrine...
levels of dextromethorphan by competitively inhibiting cytochrome P450 2D6, which catalyzes a major biotransformation pathway for dextromethorphan," enabling...
suppressants, are substances which suppress the coughing itself. Examples are dextromethorphan, benzonatate, codeine, pholcodine, noscapine, cloperastine, and butamirate...
is the name of an over-the-counter cough and cold drug containing dextromethorphan (a cough suppressant) and chlorpheniramine maleate (an antihistamine)...
pectin as an oral demulcent. Several brands of throat lozenges contain dextromethorphan. Other varieties such as Halls contain menthol, peppermint oil and/or...
and ketobemidone. Some NMDA receptor antagonists, such as ketamine, dextromethorphan (DXM), phencyclidine (PCP), methoxetamine (MXE), and nitrous oxide...
approach utilizing dextromethorphan and quinidine sulfate. Nuedexta is an FDA approved medication for pseudobulbar affect. Dextromethorphan, an N-methyl-D-aspartate...
1948 and came into medical use in 1955. In 2021, the combination with dextromethorphan and pseudoephedrine was the 294th most commonly prescribed medication...
Additionally, some clinically used drugs such as chlorpheniramine, dextromethorphan, and methadone possess SRI properties secondarily to their primary...
Typical examples include compounds such as morphine, codeine, and dextromethorphan (DXM). Despite related molecular structures, the pharmacological profiles...
marketed in several countries as Benylin DM, for its active ingredient, dextromethorphan. However, the range of products available in both solid dosage and...
sometimes used reluctantly. Certain morphinan dissociatives such as dextromethorphan are also used in sub-psychoactive dosages to suppress coughing. Ketamine...
(contains acetaminophen, doxylamine succinate 6.25 to 12.5 mg, and dextromethorphan hydrobromide), where it serves as the sedating component. The fetal...
Dexing may refer to: Recreational use of dextromethorphan Dexing, Tibet, village in the Tibet Autonomous Region of China Dexing, Jiangxi, city in Jiangxi...
somnolence, dry mouth, and decreased appetite. Dimemorfan is an analogue of dextromethorphan (DXM) and its active metabolite dextrorphan (DXO), and similarly to...
additional active ingredients such as antihistamines, guaifenesin, dextromethorphan, paracetamol (acetaminophen), or an NSAID (such as aspirin or ibuprofen)...
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