11 analytically confirmed cases of mexedrone use among polydrug users

Roberts, Liam; Ford, Loretta; Patel, Nandesh; Vale, J Allister; Bradberry, Sally

doi:10.1080/15563650.2016.1271424

Cited by 15 publications

(13 citation statements)

References 8 publications

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“…[40][41][42] Like amphetamine, synthetic cathinones result in medical sideeffects consistent with sympathomimetic toxicity. [43][44][45] Hence, acute intoxication issues include hypertension, tachycardia, cardiac, kidney and liver failure, rhabdomyolysis, electrolyte imbalance, metabolic toxicity, paradoxical hypoglycaemia, 46 and cerebral oedema. [47][48][49] Flushing, sweating, chills, restlessness, shortness of breath, dry mouth, abdominal pain, anorexia, vomiting, erectile dysfunction and discolouration of the skin have also been reported.…”

Section: Nomenclature Of Targets and Ligandsmentioning

confidence: 99%

The clinical challenges of synthetic cathinones

Schifano

Napoletano

Arillotta

et al. 2020

Brit J Clinical Pharma

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Aims Within the new psychoactive substances (NPS) scenario, several hundred different molecules, mostly including synthetic cannabinoids and cathinones, have been identified so far. The aims of the paper were to: (i) identify the number of synthetic cathinones mentioned in a range of psychonaut, NPS‐related, online sources; and (ii) describe the associated acute/long term clinical scenario and the related treatment/management plan. Methods After about 18 months of operation and exclusion of false positives/duplicates, some 4204 unique NPS molecules were included in the NPSfinder® crawling/navigating software database. Most popular NPS included: 1265 psychedelic phenethylamines (30.1%; confidence interval [CI] 95%: 28.7–31.5%); 1253 synthetic cannabinoids (29.8%; CI 95%: 28.4–31.2%); 429 synthetic opioids (10.2%; CI 95%: 9.3–10.2%); and 171 synthetic cathinones (4.1%; CI 95% 3.5–4.7%). Conversely, the United Nations Office on Drugs and Crime and the European Monitoring Centre for Drugs and Drug Addiction databases respectively included 169 and 140 cathinones. Overall, the 3 databases reported some 222 synthetic cathinones, and 41 were uniquely identified by the NPSfinder®. Results In terms of clinical scenarios, synthetic cathinone ingestion is initially associated with stimulant effects; however, psychopathological disturbances, violence, suicidal behaviour, hyperthermia, coma and death have also been described. Conclusion The proportion of cathinones commented on by psychonaut fora appeared to be relatively small, and similar to those reported by both the United Nations Office on Drugs and Crime and European Monitoring Centre for Drugs and Drug Addiction. This may be associated with a recent significant decline in both cathinone‐related consumption and acute medical presentation. Due to their complex behavioural and medical toxicity issues, healthcare professionals should be, however, be educated to recognise the signs and symptoms of NPS, including synthetic cathinone, ingestion.

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Section: Nomenclature Of Targets and Ligandsmentioning

confidence: 99%

The clinical challenges of synthetic cathinones

Schifano

Napoletano

Arillotta

et al. 2020

Brit J Clinical Pharma

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“…Accepted manuscript. Book chapter (https://doi.org/10.1007/978-3-030-33188-7_6) published in Violence and Mental Disorders (https://doi.org/10.1007/978-3-030-33188-7), Springer, 01/12/2019 Toxicity of synthetic cathinones includes significant sympathomimetic effects similar to amphetamines, related to both a dose-dependent inhibition on the re-uptake of serotonin and dopamine and their affinity for serotonin 5-HT2 and dopamine D2 membrane transporters and receptors (Roberts et al, 2017). This stimulation could lead to psychotic episodes, agitation, aggression, and sometimes violent and bizarre behaviours (Capriola, 2013).…”

Section: New Psychoactive Substances (Nps): Synthetic Cannabinoids Anmentioning

confidence: 99%

“…Finally, mexedrone, a mephedrone derivative, was found in 11 of 305 patients who presented to an emergency department. All of them presented with agitation and 6 patients required sedation and/or physical restraint (Roberts et al, 2017).…”

Section: New Psychoactive Substances (Nps): Synthetic Cannabinoids Anmentioning

confidence: 99%

Substance-Use Disorders and Violence

Schifano

Zangani

Chiappini

et al. 2019

Comprehensive Approach to Psychiatry

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Substance use seems to be associated with increased prevalence levels of violent behaviour in both general population and psychiatric patients, with 'dual diagnosis' clients showing high rates of risky and criminal behaviour and worse therapy compliance. Cases of drug-related aggressiveness mostly involve a number of molecules, e.g. ethanol, stimulants, cannabinoids, opiates, benzodiazepines, synthetic cannabinoids and synthetic cathinones. Consumers of the virtually few hundreds, and up to a few thousands substances currently available may present to the emergency departments without providing information about the substances(s) ingested and it is likely that standard drug tests will show negative results. An appropriate treatment/management plan to cope with the related acute behavioural and psychopathological disturbances is here discussed. Because of the complex behavioural and medical toxicity issues associated with drug intake, raising awareness and education of health care professionals on drugs' health harms, interventions, harm reduction techniques, and referral pathways are here deemed of particular relevance.

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“…Novel stimulants, a class of new psychoactive substances which includes amphetaminerelated compounds, substituted cathinones and benzofurans, are being detected in "street drug" combinations (bath salts), in blood and/or tissue of emergency room patients, and in stimulant-abuse related deaths (King and Corkery 2018;Krotulski et al 2018;Tettey et al 2018;Simmler and Liechti 2018). The reported use or detection of new compounds includes mexedrone, PV9 (αPOP) and 2-MAPB (Roberts et al 2017;Uchiyama et al 2014;Staeheli et al 2017). In vitro pharmacological assays are valuable for determining the initial sites of action of new compounds, and can aid in predicting abuse potential and possible toxicity by comparison with well characterized compounds (Simmler and Liechti 2017).…”

Section: Introductionmentioning

confidence: 99%

Structure-activity relationships of bath salt components: substituted cathinones and benzofurans at biogenic amine transporters

et al. 2018

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Rationale-New psychoactive substances (NPS), including substituted cathinones and other stimulants, are synthesized, sold on the Internet, and ingested without knowledge of their pharmacological activity and/or toxicity. In vitro pharmacology plays a role in therapeutic drug development, drug-protein in silico interaction modeling, and drug scheduling. Objectives-The goal of this research was to determine mechanisms of action that may indicate NPS abuse liability.Methods-Affinities to displace the radioligand [ 125 I]RTI-55 and potencies to inhibit [ 3 H]neurotransmitter uptake for 22 cathinones, 6 benzofurans and another stimulant were characterized using human embryonic kidney cells stably expressing recombinant human transporters for dopamine, norepinephrine or serotonin (hDAT, hNET, or hSERT, respectively). Selected compounds were tested for potencies and efficacies at inducing [ 3 H]neurotransmitter release via the transporters. Computational modeling was conducted to explain plausible molecular interactions established by NPS and transporters.Results-Most α-pyrrolidinophenones had high hDAT potencies and selectivities in uptake assays, with hDAT/hSERT uptake selectivity ratios of 83 −360. Other substituted cathinones varied in their potencies and selectivities, with N-ethyl-hexedrone and N-ethyl-pentylone having highest hDAT potencies and N-propyl-pentedrone having highest hDAT selectivity. 4-Cl-

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11 analytically confirmed cases of mexedrone use among polydrug users

Cited by 15 publications

References 8 publications

The clinical challenges of synthetic cathinones

The clinical challenges of synthetic cathinones

Substance-Use Disorders and Violence

Structure-activity relationships of bath salt components: substituted cathinones and benzofurans at biogenic amine transporters

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