A Comparison of Acute Pharmacological Effects of Methylone and MDMA Administration in Humans and Oral Fluid Concentrations as Biomarkers of Exposure
Lourdes Poyatos, Esther Papaseit, Eulàlia Olesti, Clara Pérez‐mañá, Mireia Ventura, Xoán Carbón, M. Grifell, Francina Fonseca, Marta Torrens, Rafael de la Torre, Magı́ Farré
Biology August 17, 2021 DOI: 10.3390/biology10080788 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Observational-naturalistic study Peer reviewed |
|---|---|
| Sample size | 14 |
| Population | Healthy poly-drug users |
| Interventions | Methylone MDMA |
| Dose | 100 to 300 mg (methylone), 75 to 100 mg (MDMA) |
| Duration | 4 hours |
| Topics | MDMA |
| Keywords | Cathinone Pharmacology Mephedrone Hallucinogen Methamphetamine Toxicology Anesthesia Drug |
| Citations | 26 |
| Key findings | Methylone produces acute psychostimulant and empathogenic effects similar to MDMA but less intense, with comparable abuse potential. |
Abstract
Considered the β-keto analogue of 3,4-methylenedioxymethamphetamine (MDMA, ecstasy), 3,4-Methylenedioxymethcathinone (methylone) is a synthetic cathinone. Over the years, methylone has been used as a substitute for conventional psychostimulants, such as MDMA. To date, little is known about the human pharmacology of methylone; the only available information has been provided by surveys or published intoxication reports. In the present observational–naturalistic study, we evaluate the acute subjective and physiological effects of methylone after oral self-administration in comparison to MDMA in healthy poly-drug users. Fourteen participants (10 males, 4 females) selected their single oral doses of methylone from 100 to 300 mg (n = 8, mean dose 187.5 mg) or MDMA from 75 to 100 mg (n = 6, mean dose 87.5 mg) based on their experience. Study variables were assessed at 0, 1, 2, and 4 h (h) and included vital signs (non-invasive blood pressure, heart rate, cutaneous temperature) and subjective effects using visual analogue scales (VAS), the 49-item Addiction Research Centre Inventory (ARCI) short form, and the Evaluation of the Subjective Effects of Substances with Abuse Potential (VESSPA-SSE) questionnaire. Additionally, oral fluid concentrations of methylone and MDMA were determined. Acute pharmacological effects produced by methylone followed the prototypical psychostimulant and empathogenic profile associated with MDMA, although they were less intense. Methylone concentrations in oral fluid can be considered a useful biomarker to detect acute exposure in oral fluid. Oral fluid concentrations of MDMA and methylone peaked at 2 h and concentrations of MDMA were in the range of those previously described in controlled studies. Our results demonstrate that the potential abuse liability of methylone is similar to that of MDMA in recreational subjects.
Comparable studies
Other observational and cohort studies on MDMA, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Subjective Reports of the Effects of MDMA in a Clinical Setting Individuals who took MDMA in a clinical setting | 1986 | Observational study | |
| Memory impairment in abstinent MDMA ("Ecstasy") users Abstinent MDMA users | 1998 | Observational cohort | |
| Impaired cognitive performance in drug free users of recreational ecstasy (MDMA) Otherwise healthy young people | 2000 | Observational | |
| The Psychological and Physiological Effects of MDMA on Normal Volunteers Older, more educated, drug-experienced individuals | 1986 | Observational cohort | |
| Cognitive performance in recreational users of MDMA or 'ecstasy': evidence for memory deficits Young people who were regular or novice MDMA users, or non-users | 1998 | Observational cohort | n = 30 |
Citations in the library
Cited by 12
- Pharmacological effects of methylone and MDMA in humans Frontiers in Pharmacology February 17, 2023
- Abuse Potential of Cathinones in Humans: A Systematic Review Journal of Clinical Medicine February 15, 2022
- Methylone and MDMA Pharmacokinetics Following Controlled Administration in Humans International Journal of Molecular Sciences November 23, 2022
- Synthetic cathinones in drug-facilitated sexual assault: A case report involving the novel generation substituted cathinone N-ethylpentedrone and a review of the literature. Forensic Science International June 1, 2024
- Methylone, a rapid acting entactogen with robust anxiolytic and antidepressant-like activity Frontiers in Psychiatry January 10, 2023
and 7 more in the library
Cites 15
- Distinct acute effects of LSD, MDMA, and d-amphetamine in healthy subjects Neuropsychopharmacology November 16, 2019
- Pattern of use and subjective effects of Salvia divinorum among recreational users. Drug and Alcohol Dependence November 8, 2006
- Effects of Acute MDMA Intoxication on Mood and Impulsivity: Role of the 5-HT2 and 5-HT1 Receptors PLoS One July 10, 2012
- Multifaceted empathy of healthy volunteers after single doses of MDMA: A pooled sample of placebo-controlled studies Journal of Psychopharmacology April 3, 2017
- Pharmacokinetic, Ambulatory, and Hyperthermic Effects of 3,4-Methylenedioxy-N-Methylcathinone (Methylone) in Rats Frontiers in Psychiatry November 17, 2017
and 10 more in the library