Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans

Mephedrone (4-methylmethcathinone) is a synthetic cathinone with psychostimulant properties which remains one of the most popular new psychoactive substances (NPS). It is frequently used orally and/or intranasally. To date, no studies have evaluated the acute effects and pharmacokinetics after self-...

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Main Authors: Esther Papaseit, Eulalia Olesti, Clara Pérez-Mañá, Marta Torrens, Francina Fonseca, Marc Grifell, Mireia Ventura, Rafael de la Torre, Magí Farré
Format: Article
Language:English
Published: MDPI AG 2021-01-01
Series:Pharmaceuticals
Subjects:
Online Access:https://www.mdpi.com/1424-8247/14/2/100
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author Esther Papaseit
Eulalia Olesti
Clara Pérez-Mañá
Marta Torrens
Francina Fonseca
Marc Grifell
Mireia Ventura
Rafael de la Torre
Magí Farré
author_facet Esther Papaseit
Eulalia Olesti
Clara Pérez-Mañá
Marta Torrens
Francina Fonseca
Marc Grifell
Mireia Ventura
Rafael de la Torre
Magí Farré
author_sort Esther Papaseit
collection DOAJ
description Mephedrone (4-methylmethcathinone) is a synthetic cathinone with psychostimulant properties which remains one of the most popular new psychoactive substances (NPS). It is frequently used orally and/or intranasally. To date, no studies have evaluated the acute effects and pharmacokinetics after self-administration of mephedrone orally (ingestion) and intranasally (insufflation) in naturalistic conditions. An observational study was conducted to assess and compare the acute pharmacological effects, as well as the oral fluid (saliva) concentrations of mephedrone self-administered orally and intranasally. Ten healthy experienced drug users (4 females and 6 males) self-administered a single dose of mephedrone, orally (<i>n</i> = 5, 100–200 mg; mean 150 mg) or intranasally (<i>n</i> = 5, 50–100 mg, mean 70 mg). Vital signs (blood pressure, heart rate, and cutaneous temperature) were measured at baseline (0), 1, 2, and 4 h after self-administration. Each participant completed subjective effects questionnaires: A set of Visual Analogue Scales (VAS), the 49-item Addiction Research Centre Inventory (ARCI), and Evaluation of the Subjective Effects of Substances with Abuse Potential (VESSPA-SSE) at baseline, 1, 2, and 4 h after self-administration. Oral fluid and urine were collected during 4 h. Both routes of mephedrone self-administration enhanced ratings of euphoria and well-being effects and increased cardiovascular effects in humans. Although it was at times assessed that the oral route produced greater and larger effects than the intranasal one, concentrations of mephedrone in oral fluid and also the total amount of mephedrone and metabolites in urine showed that concentrations of mephedrone are considerably higher when self-administered intranasally in comparison to orally. Controlled clinical trials are needed to confirm our observational results.
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spelling doaj.art-23f0f597701143f89257827378f1e0082023-12-03T15:05:55ZengMDPI AGPharmaceuticals1424-82472021-01-0114210010.3390/ph14020100Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in HumansEsther Papaseit0Eulalia Olesti1Clara Pérez-Mañá2Marta Torrens3Francina Fonseca4Marc Grifell5Mireia Ventura6Rafael de la Torre7Magí Farré8Clinical Pharmacology Unit, Hospital Universitari Germans Trias i Pujol (HUGTP-IGTP), 08916 Badalona, SpainIntegrative Pharmacology and Systems Neuroscience Research Group, Neurosciences Research Program, Hospital del Mar Medical Research Institute (IMIM) and Universitat Pompeu Fabra (CEXS-UPF), 08003 Barcelona, SpainClinical Pharmacology Unit, Hospital Universitari Germans Trias i Pujol (HUGTP-IGTP), 08916 Badalona, SpainDepartment of Psychiatry and Forensic Medicine, Institut de Neuropsiquiatria i Adiccions (INAD), Universitat Autònoma de Barcelona (UAB), 08003 Barcelona, SpainDepartment of Psychiatry and Forensic Medicine, Institut de Neuropsiquiatria i Adiccions (INAD), Universitat Autònoma de Barcelona (UAB), 08003 Barcelona, SpainDepartment of Psychiatry and Forensic Medicine, Institut de Neuropsiquiatria i Adiccions (INAD), Universitat Autònoma de Barcelona (UAB), 08003 Barcelona, SpainEnergy Control, Associació Benestar i Desenvolupament, 08041 Barcelona, SpainIntegrative Pharmacology and Systems Neuroscience Research Group, Neurosciences Research Program, Hospital del Mar Medical Research Institute (IMIM) and Universitat Pompeu Fabra (CEXS-UPF), 08003 Barcelona, SpainClinical Pharmacology Unit, Hospital Universitari Germans Trias i Pujol (HUGTP-IGTP), 08916 Badalona, SpainMephedrone (4-methylmethcathinone) is a synthetic cathinone with psychostimulant properties which remains one of the most popular new psychoactive substances (NPS). It is frequently used orally and/or intranasally. To date, no studies have evaluated the acute effects and pharmacokinetics after self-administration of mephedrone orally (ingestion) and intranasally (insufflation) in naturalistic conditions. An observational study was conducted to assess and compare the acute pharmacological effects, as well as the oral fluid (saliva) concentrations of mephedrone self-administered orally and intranasally. Ten healthy experienced drug users (4 females and 6 males) self-administered a single dose of mephedrone, orally (<i>n</i> = 5, 100–200 mg; mean 150 mg) or intranasally (<i>n</i> = 5, 50–100 mg, mean 70 mg). Vital signs (blood pressure, heart rate, and cutaneous temperature) were measured at baseline (0), 1, 2, and 4 h after self-administration. Each participant completed subjective effects questionnaires: A set of Visual Analogue Scales (VAS), the 49-item Addiction Research Centre Inventory (ARCI), and Evaluation of the Subjective Effects of Substances with Abuse Potential (VESSPA-SSE) at baseline, 1, 2, and 4 h after self-administration. Oral fluid and urine were collected during 4 h. Both routes of mephedrone self-administration enhanced ratings of euphoria and well-being effects and increased cardiovascular effects in humans. Although it was at times assessed that the oral route produced greater and larger effects than the intranasal one, concentrations of mephedrone in oral fluid and also the total amount of mephedrone and metabolites in urine showed that concentrations of mephedrone are considerably higher when self-administered intranasally in comparison to orally. Controlled clinical trials are needed to confirm our observational results.https://www.mdpi.com/1424-8247/14/2/100mephedrone (4-methylmethcathinone)novel psychoactive substances (NPS)psychostimulantscathinones bath saltsoral administrationintranasal administration
spellingShingle Esther Papaseit
Eulalia Olesti
Clara Pérez-Mañá
Marta Torrens
Francina Fonseca
Marc Grifell
Mireia Ventura
Rafael de la Torre
Magí Farré
Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans
Pharmaceuticals
mephedrone (4-methylmethcathinone)
novel psychoactive substances (NPS)
psychostimulants
cathinones bath salts
oral administration
intranasal administration
title Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans
title_full Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans
title_fullStr Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans
title_full_unstemmed Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans
title_short Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans
title_sort acute pharmacological effects of oral and intranasal mephedrone an observational study in humans
topic mephedrone (4-methylmethcathinone)
novel psychoactive substances (NPS)
psychostimulants
cathinones bath salts
oral administration
intranasal administration
url https://www.mdpi.com/1424-8247/14/2/100
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