Loperamide misuse to avoid opioid withdrawal and to achieve a euphoric effect: high doses and high risk

Lee, Vincent R.; Vera, Ariel; Alexander, Andreia B.; Ruck, Bruce; Nelson, Lewis S.; Wax, Paul M.; Campleman, Sharan L.; Brent, Jeffrey; Calello, Diane P.

doi:10.1080/15563650.2018.1510128

Cited by 20 publications

(17 citation statements)

References 31 publications

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“…As a result, the acute DXM intoxication has been linked to a serotonin syndrome, especially if used together with remaining serotonergic agents (Linn et al, 2014) (Table 1). Recently, the anti-diarrhoeal opiatergic compound loperamide has been reported for its euphoric effects (Lee et al, 2019;). At therapeutic dosages (2-16mg/day), due to both rapid metabolism and poor blood-brain barrier penetration, it is considered safe.…”

Section: Otc Drugsmentioning

confidence: 99%

New/emerging psychoactive substances and associated psychopathological consequences

et al. 2019

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Background The present paper provides an updated review of both the large number of new/novel/emerging psychoactive substances (NPS) and their associated psychopathological consequences. Focus was here given on identification of those NPS being commented in specialised online sources and the related short-/long-term psychopathological and medical ill-health effects. Methods NPS have been identified through an innovative crawling/navigating software, called the ‘NPS.Finder®’, created in order to facilitate the process of early recognition of NPS online. A range of information regarding NPS, including chemical and street names; chemical formula; three-dimensional image and anecdotally reported clinical/psychoactive effects, were here made available. Results Using the ‘NPS.Finder®’ approach, a few thousand NPS were here preliminarily identified, a number which is about 4-fold higher than those figures suggested by European and international drug agencies. NPS most commonly associated with the onset of psychopathological consequences included here synthetic cannabinoids/cannabimimetics; new synthetic opioids; ketamine-like dissociatives; novel stimulants; novel psychedelics and several prescription and over-the-counter medicines. Conclusions The ever-increasing changes in terms of recreational psychotropics' availability represent a relatively new challenge for psychiatry, as the pharmacodynamics and pharmacokinetics of many NPS have not been thoroughly understood. Health/mental health professionals should be informed about the range of NPS; their intake modalities; their psychoactive sought-after effects; the idiosyncratic psychotropics' combinations and finally, their medical and psychopathological risks.

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Section: Otc Drugsmentioning

confidence: 99%

New/emerging psychoactive substances and associated psychopathological consequences

et al. 2019

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“…For dextromethorphan intentional abuse, the NPDS received 3,472 calls (11.4 mean rate per million population) for the period (2000–2015) [ 30 ]. Among loperamide-related cases being reported to the European Medicines Agency's (EMA) from 2005 to 2017, the rate of intentional misuse was 14.9%, 0.2% for abuse and 0.4% for dependence, while the rate of misuse/abuse in the USA was 67% of cases with known intent (n = 26) according to data registered on The ToxIC registry from November 2011 to December 2016 [ 31 , 32 ].…”

Section: Resultsmentioning

confidence: 99%

“…Cough mixtures containing promethazine, ephedrine, pseudoephedrine, codeine, hydrocodone were reported to cause psychotic disorder, schizophrenia, depressive disorder, and dysthymia in abusers admitted for treatment in specialised abuse clinics in Hong Kong [ 45 ]. Cardiovascular events such as QTC-prolongation, ventricular dysrhythmias were distinctive of loperamide abuse and dependence in patients presented in hospital with toxicity symptoms [ 32 ]. Harms related to dextromethorphan abuse included balance disorders, psychomotor retardation and agitation in individuals admitted to hospital for DXM poising [ 30 , 42 ].…”

Section: Resultsmentioning

confidence: 99%

A mixed-methods systematic review of the prevalence, reasons, associated harms and risk-reduction interventions of over-the-counter (OTC) medicines misuse, abuse and dependence in adults

Algarni

Hadi

Yahyouche

et al. 2021

J of Pharm Policy and Pract

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Background Over-the-counter (OTC) medicines are typically safe. However, there is evidence that OTC medicines can sometimes cause harm as a result of their misuse, abuse and dependence. Aim of the review To review the literature on OTC medicines misuse, abuse and dependence in adults and identify the implicated medicines, contributing factors, associated harms and risk-mitigating interventions. Methods Following PRISMA guidelines, electronic databases including Cumulative Index to Nursing and Allied Health Literature (CINAHL), EMBASE, MEDLINE, PsycINFO Web of Science and Google Scholar were searched for peer-reviewed journal articles published in English between January 2011 and March 2019. Quantitative, qualitative and mixed-methods studies assessing aspects of misuse, abuse and dependence of OTC medicines in individuals aged 18 years or more were included. Studies that solely focused on adolescents only, doping in sports or abuse of OTC medicines in people who are substance abusers were excluded. The random effect meta-analysis model was used to pool the prevalence among the population-based studies. Results Of 2355 peer-reviewed studies initially identified, 53 were included in this review. According to the study design, the prevalence varied, but the overall pooled prevalence in the population-based studies was: 16.2% for misuse, 2.0% for abuse, and 7.2% for dependence. The common OTC medicines groups involved in the problematic use were analgesics (with or without codeine), sedative antihistamines, cough mixtures containing dextromethorphan. Physical, psychological, social and financial harms were associated with problematic use of OTC medicines in addition to hospitalisation and death. Interventions for the affected individuals were provided mainly through the community pharmacies, general practices and specialised addiction centres. Conclusion The problematic use of OTC medicines is quite prevalent in adults, necessitating raising public awareness about their safe use. In addition, innovative harm minimisation models need to be developed, evaluated and implemented across health care settings.

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“…The first reports of loperamide misuse surfaced in 2015 with restricted availability of scheduled opioid drugs that forced users to manage opioid withdrawal symptoms with high doses of unscheduled opioids such as loperamide 117 . The therapeutic dose for treatment of acute diarrhea or diarrhea‐predominant irritable bowel syndrome is 2‐4 mg, whereas abuse doses frequently reach more than 200 mg per day, with even higher acute doses leading to fatalities primarily because of cardiac arrhythmias and arrest 118–120 . Tolerance and dependence with physical withdrawal symptoms can develop with loperamide, and reversal of respiratory depression and other adverse effects with naloxone is possible 121,122 .…”

Section: Other Opioidsmentioning

confidence: 99%

Clinical Pharmacology, Toxicity, and Abuse Potential of Opioids

Vearrier

Grundmann

2021

The Journal of Clinical Pharma

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Opioids were the most common drug class resulting in overdose deaths in the United States in 2019. Widespread clinical use of prescription opioids for moderate to severe pain contributed to the ongoing opioid epidemic with the subsequent emergence of fentanyl‐laced heroin. More potent analogues of fentanyl and structurally diverse opioid receptor agonists such as AH‐7921 and MT‐45 are fueling an increasingly diverse illicit opioid supply. Overdose from synthetic opioids with high binding affinities may not respond to a typical naloxone dose, thereby rendering autoinjectors less effective, requiring higher antagonist doses or resulting in a confusing clinical picture for health care providers. Nonscheduled opioid drugs such as loperamide and dextromethorphan are associated with dependence and risk of overdose as easier access makes them attractive to opioid users. Despite a common opioid‐mediated pathway, several opioids present with unique pharmacodynamic properties leading to acute toxicity and dependence development. Pharmacokinetic considerations involve half‐life of the parent opioid and its metabolites as well as resulting toxicity, as is established for tramadol, codeine, and oxycodone. Pharmacokinetic considerations, toxicities, and treatment approaches for notable opioids are reviewed.

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Loperamide misuse to avoid opioid withdrawal and to achieve a euphoric effect: high doses and high risk

Cited by 20 publications

References 31 publications

New/emerging psychoactive substances and associated psychopathological consequences

New/emerging psychoactive substances and associated psychopathological consequences

A mixed-methods systematic review of the prevalence, reasons, associated harms and risk-reduction interventions of over-the-counter (OTC) medicines misuse, abuse and dependence in adults

Clinical Pharmacology, Toxicity, and Abuse Potential of Opioids

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