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‘In and Out of the Hole’
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Since its discovery, research focused on such peculiar properties in order to reduce associated toxicity: a great variety of PCP derivatives have been investigated, both as pharmaceutical compounds and, in recent years, as designer drugs available on the grey market, as part of the vast novel psychoactive substances panorama (Morris & Wallach, 2014). In our chapter, we investigate two of the main PCP derivatives, ketamine, and methoxetamine, providing some highlights on their medical and recreational use, effects, and related risks and exploring their potential in new clinical settings. Finally, we will provide an overview of other novel dissociative compounds which recently appeared on the drug market.
Organic Chemicals
Published in William J. Rea, Kalpana D. Patel, Reversibility of Chronic Disease and Hypersensitivity, Volume 4, 2017
William J. Rea, Kalpana D. Patel
Common NMDA receptor antagonists include amantadine,27 ketamine, methoxetamine, phencyclidine (PCP), nitrous oxide, dextromethorphan and dextrorphan, memantine, ethanol, riluzole (used in ALS),28 xenon, HU-211 (also a cannabinoid), lead (Pb2+),29 conantokins, and huperzine A. Dual opioid and NMDA receptor antagonists include ketobemidone, methadone, dextropropoxyphene, tramadol, kratom alkaloids, and ibogaines.
Prevalence of Stimulant, Hallucinogen, and Dissociative Substances Detected in Biological Samples of NPS-Intoxicated Patients in Italy
Published in Journal of Psychoactive Drugs, 2021
Pietro Papa, Antonella Valli, Marcello Di Tuccio, Eleonora Buscaglia, Elena Brambilla, Giulia Scaravaggi, Mariapina Gallo, Carlo Alessandro Locatelli
Eleven different dissociative substances (Table 4) were identified in 115 patients (7.9% of total cases, 46.7% of positives). The 73% of users were male and the age of the patients ranged from 14 to 62 years (mean = 24.6). Intoxication by the illegal use of ketamine was diagnosed in 105 patients throughout the considered period. Forty-one times ketamine was the only detected NPS, while in 7 cases methoxetamine, an analogue of ketamine, was present. During the period 2012–2014 methoxetamine was identified in 13 other cases. Methoxyphencyclidine (MeO-PCP) and ethylketamine, analogues of ketamine, were detected in 2 cases, one positive for both substances, the other for MeO-PCP and methoxetamine. From 2013, diphenidine (2 cases) and methoxyphenidine (2 cases) appeared in our casuistry. Indeed, data literature (Wallach et al. 2016) report the presence of these substances as chemical research has been available on the internet since 2013 as a legal replacement for the ketamine analogues banned in some European countries. In 2019, 2 cases of phencyclidine and fluoroketamine, respectively, were observed. With regard to the association with different NPS, ketamine was associate with cathinones, atropine, PMMA, and DOC. The designer benzodiazepine flubromazepam was identified in an intoxication involving methoxphenidine (Valli et al. 2017). GHB was involved in an intoxication case with ketamine. Conventional drugs of abuse were detected in 53 of the ketamine-positive cases (50.1%), distributed as follow: 25.5% phytocannabinoids, 17.3% cocaine, 11.2% amphetamines, and 18.4% ecstasy.
Uses, Effects and Toxicity of Synthetic Cannabinoids from the Perspective of People with Lived Experiences
Published in Journal of Psychoactive Drugs, 2020
Sulaf Assi, Danielle Marshall, Francesco Saverio Bersani, Ornella Corazza
Users experienced the combination of SCs with other drugs: antipsychotics, opioid analgesics, hallucinogens, stimulants and depressants. These combinations ranged from two to five substances, although the exact doses and effects of such combinations were note provided in detail. Users sought caffeine (n = 2), tobacco (n = 13), cannabis (n = 4), unspecified NPSs (n = 2) or other SCs (n = 40) in order to intensify the psychedelic effects, increase the duration of effects or resist the urgency to re-dose. Only one combination with antipsychotics was reported and involved mixing a SC (ABFUBINACA) with aripiprazole and chlorprothixene. Four users reported mixing SCs with opioids: one user did not specify the opioid and three reported codeine (with dextromethorphan in two cases). In addition to dextromethorphan, four users combined SCs with psychedelics: 4-acetoxy-N,N-dimethyltryptamine, ketamine, methoxetamine and an unspecified psychedelic. Additional combinations of SCs included alcohol (n = 17) or benzodiazepines (n = 5), mainly in order to mask the SC effects, to counteract SC-induced panic attacks, and to increase depressant effects.
Dorsolateral Prefrontal Cortex Impairment in Methoxetamine-Induced Psychosis: An 18F-FDG PET/CT Case Study
Published in Journal of Psychoactive Drugs, 2019
Lorenzo Moccia, Anna Tofani, Marianna Mazza, Marcello Covino, Giovanni Martinotti, Fabrizio Schifano, Luigi Janiri, Marco Di Nicola
Methoxetamine [2-(3-methoxyphenyl)-2-(ethylamino) cyclohexanone, MXE] is an arylcyclohexylamine derivative of ketamine (KET), which differs from the latter for the insertion, on the phenyl ring, of 3-methoxy and N-ethylamino groups in place of 2-chloro and N-methylamino groups, respectively. The N-ethylamino group accounts for MXE’s increased potency and duration of action as compared to KET, whereas the 3-methoxy group is responsible for decreased analgesic and anesthetic properties (Zanda et al. 2016). MXE is available in the form of white powder, and it is taken through different routes of administration, including nasal insufflation, oral consumption, sublingual or rectal administration, and intramuscular (IM) or intravenous (IV) injections. Dosages can range from 20 to 100 mg for oral administration and from 10 up to 100 mg for IV and IM administrations (Corazza, Assi, and Schifano 2013). MXE’s mechanism of action and effects are thought to be mediated through a combination of N-methyl-D aspartate (NMDA) receptors antagonism, dopamine reuptake inhibition, and muscarinic cholinergic and serotonin (5-HT2) receptors agonism. Human cytochrome CYP2B6 and CYP3A4 are believed to be involved in an initial metabolic pathway, which ultimately leads to N-desethyl(nor)methoxetamine, the MXE main biologically active metabolite (Botanas et al. 2017).