In Vitro Neurochemical Assessment of Methylphenidate and Its “Legal High†Analogs 3,4-CTMP and Ethylphenidate in Rat Nucleus Accumbens and Bed Nucleus of the Stria Terminalis 3,4-dichloromethylphenidate (3,4-CTMP) and ethylphenidate are new psychoactive substances and analogs of the attention deficit medication methylphenidate. Both drugs have been reported on online user fora to induce effects similar to cocaine. In the UK, 3,4-CTMP appeared on the drug market in 2013 and ethylphenidate has been sold since 2010. We aimed to explore the neurochemical effects of these drugs on brain dopamine and noradrenaline efflux. 3,4-CTMP and ethylphenidate, purchased from online vendors, were analyzed using gas chromatography and mass spectroscopy to confirm their identity. Drugs were then tested
Assessing the impact of a temporary class drug order on ethylphenidate-related infections among people who inject drugs in Lothian, Scotland: an interrupted time-series analysis. In April 2015, the UK government enacted a temporary class drug order (TCDO) on ethylphenidate in response to reported harms associated with its use, in particular an outbreak of infections among people who inject drugs with NPS use for a specific strain, S. pyogenes emm76.0, against the risk of infection with NPS use for S. pyogenes (emm types other than emm76.0) (RR = 3.49, 95% CI = 1.32-9.21). The UK government's 2015 temporary class drug order on ethylphenidate was effective in reducing infections among people who inject drugs during an outbreak situation in Lothian, Scotland.
in trials of brief interventions. In contrast, the effectiveness of MI on use of illicit substances (and by extension NPS) is understudied in these settings.Are drug treatment services ready and waiting for NPS referrals from health services?Injecting Novel Psychoactive SubstancesNovel Psychoactive Substances pose additional behavioural risks. Some stimulant NPS (e.g. ethylphenidate) have been reported to dissolve drugs, where none was needed), and injection site damage due to a loss of motor control as a result of intoxication. Such risk factors may underlie the association between injection of the NPS alpha-pyrrolidinovalerophenone (α-PVP) and HIV infections among homeless PWID in Dublin, and Staphylococcus aureus and Streptococcus pyogenes infections in people who injected ethylphenidate
pulse of d-MPH Cmax for dl-MPH by 35% (P < 0.01) and the partial area under the plasma concentration curve from 4 to 8 hours by 25% (P < 0.05). The respective values for enantiopure d-MPH were 27% (P = 0.001) and 20% (P < 0.01). The carboxylesterase 1-mediated transesterification metabolite ethylphenidate served as a biomarker for coexposure. Ethanol significantly potentiated stimulant responses
environment with a high level of confidence is enabled. In this study we report the use of a SRI-ToF-MS instrument to investigate the reactions of HO, O, NO and Kr with 10 readily available (at the time of purchase) new psychoactive substances, namely 4-fluoroamphetamine, methiopropamine, ethcathinone, 4-methylethcathinone, N-ethylbuphedrone, ethylphenidate, 5-MeO-DALT, dimethocaine, 5-(2-aminopropyl
with ethanol results in elevated d-MPH plasma concentrations accompanied by CES1-mediated enantioselective transesterification of l-MPH to l-ethylphenidate (EPH). The present study tested the hypothesis that administration of the pure isomer dexmethylphenidate (d-MPH) will overcome the influence of ethanol on d-MPH absorption by eliminating competitive CES1-mediated presystemic metabolism of l-MPH to l-EPH
Influence of ethanol and gender on methylphenidate pharmacokinetics and pharmacodynamics. This study explores the hypotheses that: (1) ethanol will interact with dl-Methylphenidate (MPH) to enantioselectively elevate plasma d-MPH, and primarily yield l-ethylphenidate as a transesterification metabolite; (2) women will exhibit lower relative bioavailability of MPH than men; and (3) sex-dependent was present in plasma only at 1-3% of the concentration of d-MPH, except in the poor metabolizer where l-MPH exceeded that of d-MPH. The metabolite l-ethylphenidate frequently exceeded 1 ng/ml in plasma, whereas d-ethylphenidate was detected only in low pg/ml concentrations. Women reported a significantly greater stimulant effect than men when questioned "Do you feel any drug effect?" (P<0.05), in spite
Transdermal and Oral dl-Methylphenidate–Ethanol Interactions in C57BL/6J Mice: Transesterification to Ethylphenidate and Elevation of d-Methylphenidate Concentrations We tested the hypothesis that C57BL/6J mice will model human metabolic interactions between dl-methylphenidate (MPH) and ethanol, placing an emphasis on the MPH transdermal system (MTS). Specifically, we asked: (1) will ethanol increase d-MPH biological concentrations, (2) will MTS facilitate the systemic bioavailability of l-MPH, and (3) will l-MPH enantioselectively interact with ethanol to yield l-ethylphenidate (l-EPH)? Mice were dosed with MTS (¼ of a 12.5 cm(2) patch on shaved skin) or a comparable oral dl-MPH dose (7.5 mg/kg), with or without ethanol (3.0 g/kg), and then placed in metabolic cages for 3 h. MPH and EPH