Frontiers in Pharmacology
March 13, 2018
Esther Papaseit, Marta Torrens, Mireia Ventura et al.
61 citations
2C-B, a psychedelic similar to mescaline, acts on serotonin receptors and produces mild psychedelic and stimulant-like effects. In an observational study, 16 healthy experienced users took 10–20 mg orally. The drug increased blood pressure and heart rate, elevated scores on scales for euphoria, liking, and stimulation, and altered perceptions of distances, colors, shapes, and lights. Five participants reported mild hallucinations. Peak 2C-B levels in saliva occurred at 1 hour, and peak cortisol at 3 hours. The effects resemble those of other serotonin-acting drugs.
Journal of Analytical Toxicology
October 3, 2016
Eulàlia Olesti, Mitona Pujadas, Esther Papaseit et al.
41 citations
Mephedrone, a synthetic cathinone increasingly used by young people and linked to acute intoxication and fatalities, was studied in a controlled clinical trial. A gas chromatography-mass spectrometry method was developed to measure mephedrone in human plasma and urine. Six healthy men received 150 mg of mephedrone orally. Peak plasma concentration averaged 122.6 ng/mL, reached within 0.5–2 hours, and the drug was eliminated rapidly with a half-life of 2.2 hours. Less than 15% of the dose appeared unchanged in urine, and concentrations varied widely among individuals.
Expert Opinion on Drug Metabolism & Toxicology
March 31, 2020
Esther Papaseit, Clara Pérez‐mañá, Marta Torrens et al.
34 citations
MDMA (ecstasy) is a widely used recreational stimulant. Users often combine it with other drugs to enhance effects, reduce toxicity, or manage comedowns, which increases the risk of severe toxicity. This review covers known interactions between MDMA and other pharmaceuticals or drugs of abuse, offering clinical recommendations. The authors note that few published studies exist and documented clinically significant interactions are scarce. Experimental evidence shows that interactions are especially relevant when MDMA is taken with drugs metabolized by the CYP2D6 enzyme, due to MDMA's inhibitory effect, and during repeated MDMA use.
Pharmaceuticals
January 28, 2021
Esther Papaseit, Eulàlia Olesti, Clara Pérez‐mañá et al.
30 citations
Mephedrone, a synthetic cathinone and popular new psychoactive substance, produces euphoria and well-being and increases cardiovascular effects when self-administered orally or intranasally by healthy experienced drug users. In this observational study, ten participants took a single dose orally (100–200 mg, mean 150 mg) or intranasally (50–100 mg, mean 70 mg). Although the oral route sometimes produced greater subjective effects, concentrations of mephedrone in oral fluid and total amounts in urine were considerably higher after intranasal administration. Controlled clinical trials are needed to confirm these results.
Frontiers in Pharmacology
January 28, 2020
Esther Papaseit, Clara Pérez-mañá, Elizabeth B. de Sousa Fernandes Perna et al.
27 citations
Combining mephedrone with alcohol amplifies cardiovascular effects and intensifies euphoria and well-being compared to either drug alone, while mephedrone reduces the sedative effects of alcohol. In a double-blind, placebo-controlled trial with 11 male volunteers, the combination increased blood pressure, heart rate, and subjective feelings of euphoria. Mephedrone alone and alcohol alone were also tested. The results suggest that the abuse liability of mephedrone is greater when taken with alcohol, similar to other psychostimulants like amphetamines and MDMA.
Frontiers in Pharmacology
February 17, 2023
Lourdes Poyatos, Clara Pérez‐mañá, Olga Hladun et al.
26 citations
Methylone, a common synthetic cathinone used as a substitute for MDMA, produces similar acute effects in humans. In a controlled trial with 17 experienced psychostimulant users, a single 200 mg oral dose of methylone increased blood pressure and heart rate and induced pleasurable effects including stimulation, euphoria, wellbeing, enhanced empathy, and altered perception. Methylone's effect profile resembled MDMA's but with a faster onset and earlier disappearance of subjective effects. The findings suggest methylone's abuse potential is comparable to that of MDMA in humans.
Journal of Clinical Medicine
February 15, 2022
Lourdes Poyatos, A Acuna Torres, Esther Papaseit et al.
26 citations
Cathinone, mephedrone, methylone, and diethylpropion produce stimulant and euphorigenic effects similar to amphetamines and MDMA, with varying intensities that may correspond to different levels of abuse potential. This systematic review of 18 studies (5 on cathinone, 7 on mephedrone, 1 on methylone, 5 on diethylpropion) found that all four substances induce desirable and reinforcing effects that could lead to misuse and addiction. The authors conclude that further investigation is needed to minimize and prevent their impact on society and public health.
Biology
August 17, 2021
Lourdes Poyatos, Esther Papaseit, Eulàlia Olesti et al.
26 citations
Methylone, a synthetic cathinone and beta-keto analogue of MDMA, produces acute subjective and physiological effects similar to MDMA but less intense. In an observational-naturalistic study of 14 healthy poly-drug users who self-administered oral doses (methylone 100-300 mg, mean 187.5 mg; MDMA 75-100 mg, mean 87.5 mg), methylone showed a prototypical psychostimulant and empathogenic profile. Oral fluid concentrations of both substances peaked at 2 hours, with MDMA levels matching those from controlled studies. The findings indicate that methylone's abuse potential is comparable to MDMA's in recreational users.
Journal of Psychopharmacology
August 25, 2016
EB de Sousa Fernandes Perna, Esther Papaseit, Clara Pérez‐mañá et al.
26 citations
Mephedrone, a recreational drug similar to MDMA, impairs short-term spatial memory one hour after intake but improves critical tracking performance four hours later. When combined with alcohol, mephedrone reduces reaction time compared to alcohol alone, but does not counteract alcohol's impairing effects on divided attention or spatial memory. Alcohol alone impairs both short- and long-term spatial memory and divided attention. The findings suggest mephedrone enhances psychomotor performance while harming memory, and its stimulatory effects are insufficient to offset alcohol-induced deficits on most cognitive tasks.
International Journal of Molecular Sciences
November 23, 2022
Lourdes Poyatos, Alfredo Fabrizio Lo Faro, Diletta Berardinelli et al.
22 citations
After controlled oral doses of 50–200 mg methylone given to 12 male volunteers, plasma concentrations increased in proportion to dose. Maximum concentrations ranged from 153 ng/mL at the lowest dose to 604 ng/mL at the highest dose. The drug was absorbed rapidly, reaching peak levels in 1.5–2 hours, and had a half-life of about 6 hours. Its metabolite HMMC reached peak concentrations 10–14 times lower than methylone. Unlike MDMA, methylone showed linear pharmacokinetics across the dose range. A validated LC-MS/MS method was used to measure methylone, MDMA, and their metabolites in plasma.
Frontiers in Pharmacology
March 18, 2020
Esther Papaseit, Marta Torrens, Mireia Ventura et al.
20 citations
2C-E, a psychedelic phenylethylamine similar to mescaline, acts as a partial agonist at serotonin 2A, 2B, and 2C receptors and inhibits norepinephrine and serotonin uptake. In an observational study, ten recreational psychedelic users self-administered single oral doses of 2C-E (6.5–25 mg). The drug induced alterations in perception, hallucinations, and euphoric mood, with saliva concentrations peaking 2 hours after administration. The effects resembled those of 2C-B and other serotonin-acting drugs.
Expert Opinion on Drug Metabolism & Toxicology
January 5, 2018
Esther Papaseit, Marta Torrens, Clara Pérez‐mañá et al.
20 citations
MDMA (ecstasy) produces amphetamine-like euphoria and well-being, increases empathy, and induces pro-social effects that drive recreational use and suggest therapeutic potential. This review examines interindividual differences in MDMA's pharmacodynamics, focusing on sex-gender, race-ethnicity, genetic differences, interactions, acute toxicity, and therapeutic use. Acute MDMA effects are more pronounced in women than men. Very limited data exist on race-ethnicity effects. MDMA metabolism involves polymorphic enzymes that slightly alter plasma concentrations and effects. The small number of subjects in acute-effect trials limits evaluation of interindividual factors and prevents clear conclusions about their influence, which should be considered in therapeutic studies.
Journal of pharmaceutical and biomedical analysis
January 20, 2024
Alfredo Fabrizio Lo Faro, Giorgia Sprega, Diletta Beradinelli et al.
14 citations
Enantioselective high-performance liquid chromatography-tandem mass spectrometry methods were developed to quantify MDMA and its phase-1 metabolites HMA, HMMA, and MDA in human plasma, sweat, oral fluid, and urine. Two polysaccharide-based chiral columns achieved baseline separation of most enantiomer pairs: the Lux AMP column separated MDMA, HMA, and HMMA enantiomers but not MDA; the Lux i-Amylose-3 column separated MDMA, HMMA, and MDA enantiomers but not HMA. Analysis took under 4 minutes with one column and under 6 minutes with the other. Both methods were validated and applied to biological fluids, confirming enantioselective metabolism of MDMA.
Biology
March 24, 2021
Nunzia la Maida, Esther Papaseit, Lucía Martínez de Soto et al.
14 citations
Synthetic cannabinoid UR-144, monitored by the EU Early Warning System since 2012 for severe adverse effects, shows a similar cardiovascular profile to delta-9-tetrahydrocannabinol (THC) but with less intense subjective effects. In an observational study, 16 volunteers smoked joints containing either UR-144 (1 or 1.5 mg) or cannabis (10 or 20 mg THC). Both substances significantly increased systolic and diastolic blood pressure and heart rate. UR-144 produced lower scores on visual analog scales for stimulant-like and high effects compared to cannabis, and no hallucinogenic effects were observed. UR-144 was detectable in oral fluid, peaking at 20 minutes after smoking, offering a non-invasive biomarker of consumption. These preliminary findings require confirmation in larger samples.
Frontiers in pharmacology
January 1, 2025
Georgina De la Rosa, Esther Papaseit, Olga Hladun et al.
7 citations
Alpha-pyrrolidinopentiophenone (α-PVP), a synthetic cathinone similar to MDPV and cocaine, produces rapid-onset psychostimulant and empathogenic effects after a single intranasal dose. In nine participants with prior psychostimulant use, 10 mg or 20 mg of α-PVP caused an acute increase in blood pressure and heart rate that peaked 40 minutes after administration. Subjective effects appeared quickly and resolved within 3 to 5 hours. The drug's psychostimulant properties resembled those of cocaine, and its empathogenic effects were similar to those of MDMA and other cathinones like methylone.
Handbook of Substance Misuse and Addictions
January 1, 2022
Esther Papaseit, Magí Farré, Clara Pérez-mañá
Public health efforts must balance preventing illicit drug use with ensuring access to medicines that have abuse potential. Drug interactions for drugs of abuse, unlike those for medicines, are largely underexplored and not part of clinical routine. MDMA (ecstasy, molly) exemplifies this: it is a popular recreational psychostimulant and is being evaluated for treating post-traumatic stress disorder. Understanding inter- and intraindividual factors, modulation factors, and potential interactions is crucial to assess intoxication risk for both recreational users and patients in future MDMA-assisted therapy.