Dextromethorphan 3

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Dextromethorphan 3










Dextromethorphan 3

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Dextromethorphan 3

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Dextromethorphan 3

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Dextromethorphan DXM or DM is a medication most often used as a cough suppressant in over-the-counter cold and cough medicines. It is sold in syrup , tablet, spray, and lozenge forms. It is in the morphinan class of medications with sedative , dissociative , and stimulant properties at lower doses , although dextromethorphan is a synthetic combination drug not found in the opium poppy itself directly i. In its pure form, dextromethorphan occurs as a white powder. DXM is also used recreationally. When exceeding approved dosages, dextromethorphan acts as a dissociative hallucinogen. It has multiple mechanisms of action , including actions as a nonselective serotonin reuptake inhibitor \\\\\\[4\\\\\\] and a sigma-1 receptor agonist. It was patented in and approved for medical use in The primary use of dextromethorphan is as a cough suppressant , for the temporary relief of cough caused by minor throat and bronchial irritation such as commonly accompanies the flu and common cold , as well as those resulting from inhaled particle irritants. Dextromethorphan is the actual therapeutic agent in the combination; quinidine merely serves to inhibit the enzymatic degradation of dextromethorphan and thereby increase its circulating concentrations via inhibition of CYP2D6. In , a randomized clinical trial was conducted at Tabriz University of Medical Sciences in Tabriz, Iran, that indicated dextromethorphan may help reduce the overall discomfort and duration of withdrawal symptoms associated with opioid use disorder. When combined with clonidine , dextromethorphan reduced the overall time needed for withdrawal symptoms to peak by 24 hours while also reducing the severity of the symptoms compared to clonidine alone. Because dextromethorphan can trigger a histamine release allergic reaction , atopic children, who are especially susceptible to allergic reactions, should be administered dextromethorphan only if absolutely necessary, and only under the strict supervision of a healthcare professional. Side effects of dextromethorphan at normal therapeutic doses can include: \\\\\\[2\\\\\\] \\\\\\[8\\\\\\] \\\\\\[15\\\\\\]. A rare side effect is respiratory depression. Neurotoxic changes, including vacuolation, have been observed in posterior cingulate and retrosplenial cortices of rats administered other NMDA receptor antagonists such as PCP, but not with dextromethorphan. In many documented cases, dextromethorphan has produced psychological dependence in people who used it recreationally. Additionally, disturbances have been reported in sleep, senses, movement, mood, and thinking. Episodic acute psychosis can occur with high doses of DXM taken for recreational use, and an abundance of psychiatric symptoms can result, including dissociation and other PCP-like symptoms. Dextromethorphan should not be taken with monoamine oxidase inhibitors MAOIs \\\\\\[15\\\\\\] due to the potential for serotonin syndrome , which is a potentially life-threatening condition that can occur rapidly, due to a buildup of an excessive amount of serotonin in the body. Caution should be exercised when taking dextromethorphan when drinking grapefruit juice or eating grapefruit, as compounds in grapefruit affect a number of drugs , including dextromethorphan, through the inhibition of the cytochrome p system in the liver, and can lead to excessive accumulation and prolonged effects. Grapefruit and grapefruit juices especially white grapefruit juice, but also including other citrus fruits such as bergamot and lime , as well as a number of noncitrus fruits \\\\\\[22\\\\\\] generally are recommended to be avoided while using dextromethorphan and numerous other medications. Dextromethorphan is a prodrug of dextrorphan , which is the actual mediator of most of its dissociative effects through acting as a more potent NMDA receptor antagonist than dextromethorphan itself. Following oral administration, dextromethorphan is rapidly absorbed from the gastrointestinal tract , where it enters the bloodstream and crosses the blood—brain barrier. At therapeutic doses, dextromethorphan acts centrally meaning that it acts on the brain as opposed to locally on the respiratory tract. It elevates the threshold for coughing, without inhibiting ciliary activity. Dextromethorphan is rapidly absorbed from the gastrointestinal tract and converted into the active metabolite dextrorphan in the liver by the cytochrome P enzyme CYP2D6. The International Society for the Study of Cough recommends 'an adequate first dose of medication is 60 mg in the adult and repeat dosing should be infrequent rather than the qds recommended. Around one in 10 of the Caucasian population has little or no CYP2D6 enzyme activity, leading to long-lived high drug levels. The first pass through the hepatic portal vein results in some of the drug being metabolized by O-demethylation into an active metabolite of dextromethorphan called dextrorphan DXO. DXO is the 3-hydroxy derivative of dextromethorphan. The therapeutic activity of dextromethorphan is believed to be caused by both the drug and this metabolite. Dextromethorphan also undergoes N-demethylation to 3-methoxymorphinan or MEM , \\\\\\[35\\\\\\] and partial conjugation with glucuronic acid and sulfate ions. A significant portion of the population has a functional deficiency in this enzyme and are known as poor CYP2D6 metabolizers. The distribution of alleles is uneven amongst ethnic groups. A large number of medications are potent inhibitors of CYP2D6. Some types of medications known to inhibit CYP2D6 include certain SSRIs and tricyclic antidepressants , some antipsychotics , and the commonly available antihistamine diphenhydramine. Therefore, the potential of interactions exists between dextromethorphan and medications that inhibit this enzyme, particularly in slow metabolizers. Dextromethorphan is the dextrorotatory enantiomer of levomethorphan , which is the methyl ether of levorphanol , both opioid analgesics. As its pure form, dextromethorphan occurs as an odorless, opalescent white powder. It is freely soluble in chloroform and insoluble in water ; the hydrobromide salt is water-soluble up to 1. The racemic parent compound racemorphan was first described in a Swiss and US patent application from Hoffmann-La Roche in and , respectively; a patent was granted in A resolution of the two isomers of racemorphan with tartaric acid was published in , \\\\\\[39\\\\\\] and DXM was successfully tested in as part of US Navy and CIA -funded research on nonaddictive substitutes for codeine. During the s and s, dextromethorphan became available in an over-the-counter tablet form by the brand name Romilar. In , Romilar was taken off the shelves after a burst in sales because of frequent misuse. A few years later, products with an unpleasant taste were introduced such as Robitussin, Vicks, and Dextrotussion , but later the same manufacturers began producing products with a better taste. Indonesia is the only country in the world that makes single-component dextromethorphan illegal even by prescription \\\\\\[43\\\\\\] and violators may be prosecuted by law. It has been used in counterfeit medications. DXM Pharmaceuticals sells a highly concentrated product called 'RoboCough' which appears to be marketed for recreational use. Over-the-counter preparations containing dextromethorphan have been used in manners inconsistent with their labeling, often as a recreational drug. Some users report stimulant-like euphoria , particularly in response to music. Dextromethorphan usually provides its recreational effects in a non-linear fashion, so that they are experienced in significantly varied stages. These stages are commonly referred to as 'plateaus'. These plateaus are numbered from one to four, with the first having the mildest effects to fourth being the most intense. Each plateau is said to come with different related effects and experiences. From Wikipedia, the free encyclopedia. Not to be confused with Dextrorphan or Dexamethasone. IUPAC name. Interactive image. Main article: Recreational use of dextromethorphan. Journal of Veterinary Pharmacology and Therapeutics. Medscape Reference. Retrieved 15 April Archived from the original on Retrieved Clinical Toxicology. May Neurochemistry International. April British Journal of Pharmacology. Robin Analogue-based Drug Discovery. Australian Medicines Handbook. Retrieved 10 April ISRN Psychiatry. GlobeNewswire News Room. Axsome Therapeutics, Inc. Bibcode : Sci World Health Organization. Psychopharmacology Bulletin. Retrieved 23 August Retrieved 14 August Experimental Neurology. January The Journal of Pharmacology and Experimental Therapeutics. June European Journal of Pharmacology. Bibcode : PLoSO Substance Abuse and Rehabilitation. Brain Research. International Society for the Study of Cough. Food and Chemical Toxicology. Drug Metabolism and Disposition. Clinical Pharmacology and Therapeutics. Journal of Clinical Pharmacology. Drug Testing and Analysis. Archived PDF from the original on An act to add Sections and to the Health and Safety Code, relating to nonprescription drugs. State of California, Legislative Counsel. Archived from the original PDF on Retrieved 13 December Drugs and Chemicals of Concern. Drug Enforcement Administration. August Drugs of abuse 2nd ed. Journal of Dual Diagnosis. Cough and cold preparations R Recreational uses. Recreational drug use. Calea zacatechichi Silene capensis. Coffee break Coffeehouse Latte art Tea house. Abuse Date rape drug Impaired driving Drug harmfulness Effects of cannabis Addiction Dependence Prevention Opioid replacement therapy Rehabilitation Responsible use Drug-related crime Fetal alcohol spectrum disorder Long-term effects of cannabis Neurotoxicity Overdose Passive smoking of tobacco or other substances. Alcohol legality Alcohol consumption Anabolic steroid legality Cannabis legality Annual use Lifetime use Cigarette consumption Cocaine legality Cocaine use Methamphetamine legality Opiates use Psilocybin mushrooms legality Salvia legality. Diphenidine Ephenidine Fluorolintane Methoxphenidine. Dextrallorphan Dextromethorphan Dextrorphan Racemethorphan Racemorphan. Apomorphine Aporphine Bromocriptine Cabergoline Lisuride Memantine Nuciferine Pergolide Phenethylamine Piribedil Pramipexole Ropinirole Rotigotine Salvinorin A Also indirect D 2 agonists, such as dopamine reuptake inhibitors cocaine , methylphenidate , releasing agents amphetamine , methamphetamine , and precursors levodopa. Glaucine Isoaminile Noscapine Pukateine. Ionotropic glutamate receptor modulators. Monoamine reuptake inhibitors. Others: Antihistamines e. Others: A Amoxapine Antihistamines e. Amiodarone Amphetamines e. Nicotinic acetylcholine receptor modulators. Opioid receptor modulators. Sigma receptor modulators. Hidden categories: Wikipedia articles needing page number citations from April Webarchive template wayback links All articles with incomplete citations Articles with incomplete citations from April CS1 Indonesian-language sources id All articles with dead external links Articles with dead external links from March Wikipedia articles needing page number citations from March Articles with short description Template:drugs. Namespaces Article Talk. Views Read Edit View history. In other projects Wikimedia Commons. By using this site, you agree to the Terms of Use and Privacy Policy. Values are K i nM , unless otherwise noted. The smaller the value, the more strongly the drug binds to the site. Wikimedia Commons has media related to Dextromethorphan.

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