Antitussives and substance abuse

Burns, Jarrett M.; Boyer, Edward W.

doi:10.2147/sar.s36761

Cited by 25 publications

(42 citation statements)

References 39 publications

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“…Dextromethorphan is metabolized by cytochrome P450 2D6 and converted into dextrorphan. Individuals who are rapid metabolizers of dextromethorphan can get a more intense euphoric effect and are predisposed to addictive behavior (Burns and Boyer, 2013).…”

Section: Discussionmentioning

confidence: 99%

“…DXM, as an over-the-counter medicine, is often rationalized by its users as being safer, easier to obtain, widely accessible, and undetected on routine drug screen; furthermore, confirmed dextromethorphan dependence is rarely reported in the literature (Burns and Boyer, 2013).…”

mentioning

confidence: 99%

“…There are 4 stages of dextromethorphan intoxication, based on the amount of the substance that is used (Burns and Boyer, 2013). The first stage is a stimulant effect.…”

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confidence: 99%

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Dextromethorphan Addiction Mediated Through the NMDA System

Roy

Hsieh

Crapanzano

2015

Journal of Addiction Medicine

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Dextromethorphan, an antitussive (cough suppressant) drug of the morphinan class with sedative and dissociative properties found in cough syrup and other over-the-counter products, is also a substance of abuse, seen primarily in young adults all over the world. A case of dextromethorphan use disorder is presented in a 45-year-old women. Her repeated attempts at abstinence were unsuccessful secondary to continued intense cravings. Treatment with topiramate resulted in complete resolution of her cravings. Topiramate was chosen empirically because of a common action with dextromethorphan in the NMDA system. Genetic testing was obtained and the patient was found to be a carrier of the GRIK1 rs2832407(C:C) allele. The (C:C) allele has been associated with an increased risk of alcohol use disorder and a treatment response of patients with heavy drinking to topiramate. This case provides an opportunity to discuss personalized medicine (treatment options aided by the use of genetic testing) and the possible shared genetic susceptibility for dependence in 2 substances of abuse.

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Section: Discussionmentioning

confidence: 99%

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confidence: 99%

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Dextromethorphan Addiction Mediated Through the NMDA System

Roy

Hsieh

Crapanzano

2015

Journal of Addiction Medicine

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“…Dextromethorphan is a noncompetitive NMDA receptor antagonist and σ 1 -receptor agonist, commonly used antitussive compound [113,114] (for σ 1 -receptors in depression, see references [115,116]). Quinidine is a CYP2D6 enzyme inhibitor, which serves to increase plasma concentrations of dextromethorphan and prolong its plasma half-life [78,79].…”

Section: Compounds In Recent Phase II Clinical Trialsmentioning

confidence: 99%

Investigational drugs in recent clinical trials for treatment-resistant depression

Garay

Zarate

Charpeaud³

et al. 2017

Expert Review of Neurotherapeutics

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Introduction The authors describe the medications for treatment-resistant depression (TRD) in phase II/III of clinical development in the EU and USA and provide an opinion on how current treatment can be improved in the near future. Areas covered Sixty-two trials were identified in US and EU clinical trial registries that included six investigational compounds in recent phase III development and 12 others in recent phase II clinical trials. Glutamatergic agents have been the focus of many studies. A single intravenous dose of the glutamatergic modulator ketamine produces a robust and rapid antidepressant effect in persons with TRD; this effect continues to remain significant for 1 week. This observation was a turning point that opened the way for other, more selective glutamatergic modulators (intranasal esketamine, AVP-786, AVP-923, AV-101, and rapastinel). Of the remaining compounds, monoclonal antibodies open highly innovative therapeutic options, based on new pathophysiological approaches to depression. Expert commentary Promising new agents are emerging for TRD treatment. Glutamatergic modulators likely represent a very promising alternative to monoaminergic antidepressant monotherapy. We could see the arrival of the first robust and rapid acting antidepressant drug in the near future, which would strongly facilitate the ultimate goal of recovery in persons with TRD.

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“…This especially concerns the opioid drugs that tend to be omitted from such reviews. Out of four of the most extensive works investigated by the authors, only two discuss codeine, and none discuss either dihydrocodeine or loperamide [ 6 , 7 , 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

Pharmacological Aspects of Over-the-Counter Opioid Drugs Misuse

Sobczak

Goryński

2020

Molecules

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Several over-the-counter (OTC) drugs are known to be misused. Among them are opioids such as codeine, dihydrocodeine, and loperamide. This work elucidates their pharmacology, interactions, safety profiles, and how pharmacology is being manipulated to misuse these common medications, with the aim to expand on the subject outlined by the authors focusing on abuse prevention and prevalence rates. The reviewed literature was identified in several online databases through searches conducted with phrases created by combining the international non-proprietary names of the drugs with terms related to drug misuse. The results show that OTC opioids are misused as an alternative for illicit narcotics, or prescription-only opioids. The potency of codeine and loperamide is strongly dependent on the individual enzymatic activity of CYP2D6 and CYP3A4, as well as P-glycoprotein function. Codeine can also be utilized as a substrate for clandestine syntheses of more potent drugs of abuse, namely desomorphine (“Krokodil”), and morphine. The dangerous methods used to prepare these substances can result in poisoning from toxic chemicals and impurities originating from the synthesis procedure. OTC opioids are generally safe when consumed in accordance with medical guidelines. However, the intake of supratherapeutic amounts of these substances may reveal surprising traits of common medications.

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Antitussives and substance abuse

Cited by 25 publications

References 39 publications

Dextromethorphan Addiction Mediated Through the NMDA System

Dextromethorphan Addiction Mediated Through the NMDA System

Investigational drugs in recent clinical trials for treatment-resistant depression

Pharmacological Aspects of Over-the-Counter Opioid Drugs Misuse

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