Clinical Pharmacology of the Synthetic Cathinone Mephedrone

Papaseit, Esther; Moltó, José; Muga, Roberto; Torrens, Marta; Torre, Rafael de la; Farré, Magı́

doi:10.1007/7854_2016_61

Cited by 31 publications

(18 citation statements)

References 93 publications

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“…Possibly, due to the increased SERT/DAT ratio of S-mephedrone, administration of this drug adequately compensates for deficits in extracellular 5-HT, which are associated with cocaine withdrawal (Parsons et al, 1995(Parsons et al, , 1996. The increased SERT selectivity of S-normephedrone may contribute to the entactogenic effects of mephedrone (Papaseit et al, 2017).…”

Section: Discussionmentioning

confidence: 99%

Stereochemistry of phase-1 metabolites of mephedrone determines their effectiveness as releasers at the serotonin transporter

et al. 2019

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Section: Discussionmentioning

confidence: 99%

Stereochemistry of phase-1 metabolites of mephedrone determines their effectiveness as releasers at the serotonin transporter

et al. 2019

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“…27 Cathinone addicts commonly report re-injecting of the drug with excessive binge use over long periods of time, with shorter half-life and duration of effects leading to more compulsive drug-taking behaviour to maintain euphoria. 28 1.…”

Section: Clinical Neuropharmacological Issuesmentioning

confidence: 99%

“…Up to 30% of mephedrone users may report dependence, with synthetic cathinone users possibly experiencing as well both tolerance and withdrawal symptoms, which include tiredness, insomnia, nasal congestion and impaired concentration . Cathinone addicts commonly report re‐injecting of the drug with excessive binge use over long periods of time, with shorter half‐life and duration of effects leading to more compulsive drug‐taking behaviour to maintain euphoria …”

Section: Introductionmentioning

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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“…MEPH’s effects are rapid and of relatively short duration depending on the administration route (intranasal: ~30 min, oral: ~2–3 h) ( 7 , 8 ), resulting in a tendency for recreational users to re-dose, as is the case with cocaine ( 9 , 10 ). Prolonged and/or poly-drug use [including “slamming”—intravenous injection of MEPH combined with other drugs ( 11 )] may be associated with adverse psychological (e.g., paranoia, depression, panic attacks), cardiovascular, or renal effects ( 12 , 13 ). Furthermore, at least 90 deaths have been documented where MEPH alone (or its combination with other psychoactive compounds) was implicated ( 14 – 17 ).…”

Section: Introductionmentioning

confidence: 99%

Mephedrone (4-Methylmethcathinone): Acute Behavioral Effects, Hyperthermic, and Pharmacokinetic Profile in Rats

et al. 2018

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Mephedrone (MEPH) is a synthetic cathinone derivative with effects that mimic MDMA and/or cocaine. Our study in male Wistar rats provides detailed investigations of MEPH’s and its primary metabolite nor-mephedrone’s (nor-MEPH) pharmacokinetics and bio-distribution to four different substrates (serum, brain, lungs, and liver), as well as comparative analysis of their effects on locomotion [open field test (OFT)] and sensorimotor gating [prepulse inhibition of acoustic startle reaction (PPI ASR)]. Furthermore, in order to mimic the crowded condition where MEPH is typically taken (e.g., clubs), the acute effect of MEPH on thermoregulation in singly- and group-housed rats was evaluated. Pharmacokinetics of MEPH and nor-MEPH after MEPH (5 mg/kg, sc.) were analyzed over 8 h using liquid chromatography with mass spectrometry. MEPH (2.5, 5, or 20 mg/kg, sc.) and nor-MEPH (5 mg/kg, sc.) were administered 5 or 40 min before the behavioral testing in the OFT and PPI ASR; locomotion and its spatial distribution, ASR, habituation and PPI itself were quantified. The effect of MEPH on rectal temperature was measured after 5 and 20 mg/kg, sc. Both MEPH and nor-MEPH were detected in all substrates, with the highest levels detected in lungs. Mean brain: serum ratios were 1:1.19 (MEPH) and 1:1.91 (nor-MEPH), maximum concentrations were observed at 30 min; at 2 and 4 h after administration, nor-MEPH concentrations were higher compared to the parent drug. While neither of the drugs disrupted PPI, both increased locomotion and affected its spatial distribution. The effects of MEPH were dose dependent, rapid, and short-lasting, and the intensity of locomotor stimulant effects was comparable between MEPH and nor-MEPH. Despite the disappearance of behavioral effects within 40 min after administration, MEPH induced rectal temperature elevations that persisted for 3 h even in singly housed rats. To conclude, we observed a robust, short-lasting, and most likely synergistic stimulatory effect of both drugs which corresponded to brain pharmacokinetics. The dissociation between the duration of behavioral and hyperthermic effects is indicative of the possible contribution of nor-MEPH or other biologically active metabolites. This temporal dissociation may be related to the risk of prolonged somatic toxicity when stimulatory effects are no longer present.

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Clinical Pharmacology of the Synthetic Cathinone Mephedrone

Cited by 31 publications

References 93 publications

Stereochemistry of phase-1 metabolites of mephedrone determines their effectiveness as releasers at the serotonin transporter

Stereochemistry of phase-1 metabolites of mephedrone determines their effectiveness as releasers at the serotonin transporter

The clinical challenges of synthetic cathinones

Mephedrone (4-Methylmethcathinone): Acute Behavioral Effects, Hyperthermic, and Pharmacokinetic Profile in Rats

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