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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| Veröffentlicht in: | Pharmaceuticals (Basel, Switzerland) Switzerland), 2021-01, Vol.14 (2), p.100, Article 100 |
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| creator | Papaseit, Esther Olesti, Eulalia Perez-Mana, Clara Torrens, Marta Fonseca, Francina Grifell, Marc Ventura, Mireia de la Torre, Rafael Farre, Magi |
| 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 (n = 5, 100-200 mg; mean 150 mg) or intranasally (n = 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. |
| doi_str_mv | 10.3390/ph14020100 |
| format | Article |
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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 (n = 5, 100-200 mg; mean 150 mg) or intranasally (n = 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.</description><identifier>ISSN: 1424-8247</identifier><identifier>EISSN: 1424-8247</identifier><identifier>DOI: 10.3390/ph14020100</identifier><identifier>PMID: 33525579</identifier><language>eng</language><publisher>BASEL: Mdpi</publisher><subject>Amphetamines ; cathinones bath salts ; Chemistry, Medicinal ; Drug dosages ; Ecstasy ; Hallucinations ; intranasal administration ; Life Sciences & Biomedicine ; mephedrone (4-methylmethcathinone) ; Metabolites ; novel psychoactive substances (NPS) ; Observational studies ; oral administration ; Pharmacokinetics ; Pharmacology & Pharmacy ; Physiology ; Psychosis ; psychostimulants ; Questionnaires ; Science & Technology ; Urine</subject><ispartof>Pharmaceuticals (Basel, Switzerland), 2021-01, Vol.14 (2), p.100, Article 100</ispartof><rights>2021. This work is licensed under http://creativecommons.org/licenses/by/3.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2021 by the authors. 2021</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>true</woscitedreferencessubscribed><woscitedreferencescount>13</woscitedreferencescount><woscitedreferencesoriginalsourcerecordid>wos000622906000001</woscitedreferencesoriginalsourcerecordid><citedby>FETCH-LOGICAL-c472t-aa92f6f9979f9dc3c72347d8372c66c3cd378434c9174d1ef5f3e1f1224fae0f3</citedby><cites>FETCH-LOGICAL-c472t-aa92f6f9979f9dc3c72347d8372c66c3cd378434c9174d1ef5f3e1f1224fae0f3</cites><orcidid>0000-0001-6222-4761 ; 0000-0002-0779-6545 ; 0000-0001-8338-7543 ; 0000-0002-6765-1866 ; 0000-0001-6343-6918</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7912650/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7912650/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,315,728,781,785,865,886,2103,2115,27929,27930,39263,53796,53798</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33525579$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Papaseit, Esther</creatorcontrib><creatorcontrib>Olesti, Eulalia</creatorcontrib><creatorcontrib>Perez-Mana, Clara</creatorcontrib><creatorcontrib>Torrens, Marta</creatorcontrib><creatorcontrib>Fonseca, Francina</creatorcontrib><creatorcontrib>Grifell, Marc</creatorcontrib><creatorcontrib>Ventura, Mireia</creatorcontrib><creatorcontrib>de la Torre, Rafael</creatorcontrib><creatorcontrib>Farre, Magi</creatorcontrib><title>Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans</title><title>Pharmaceuticals (Basel, Switzerland)</title><addtitle>PHARMACEUTICALS-BASE</addtitle><addtitle>Pharmaceuticals (Basel)</addtitle><description>Mephedrone (4-methylmethcathinone) is a synthetic cathinone with psychostimulant properties which remains one of the most popular new psychoactive substances (NPS). 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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 (n = 5, 100-200 mg; mean 150 mg) or intranasally (n = 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. 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| subjects | Amphetamines cathinones bath salts Chemistry, Medicinal Drug dosages Ecstasy Hallucinations intranasal administration Life Sciences & Biomedicine mephedrone (4-methylmethcathinone) Metabolites novel psychoactive substances (NPS) Observational studies oral administration Pharmacokinetics Pharmacology & Pharmacy Physiology Psychosis psychostimulants Questionnaires Science & Technology Urine |
| title | Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans |
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