Dose-response pharmacological study of mephedrone and its metabolites: pharmacokinetics, serotoninergic effects, and impact of CYP2D6 genetic variation
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- dc.contributor.author Olesti Muñoz, Eulàlia, 1991-
- dc.contributor.author Farré Albaladejo, Magí
- dc.contributor.author Carbó Banús, Marcel·lí
- dc.contributor.author Papaseit Fontanet, Esther
- dc.contributor.author Pérez Mañá, Clara
- dc.contributor.author Torrens, Marta
- dc.contributor.author Yubero Lahoz, Samanta, 1985-
- dc.contributor.author Pujadas Bastardes, Mitona
- dc.contributor.author Pozo Mendoza, Óscar J., 1975-
- dc.contributor.author Torre Fornell, Rafael de la
- dc.date.accessioned 2019-11-28T08:26:41Z
- dc.date.issued 2019
- dc.description.abstract Mephedrone (MEPH), the most widely consumed synthetic cathinone, has been associated with acute toxicity episodes. The aim of this report was to study its metabolic disposition and the impact of genetic variation of CYP2D6 on MEPH metabolism, in a dose range compatible with its recreational use. A randomized, crossover, phase I clinical trial was performed. Subjects received 50 and 100 mg (n = 3) and 150 and 200 mg (n = 6) of mephedrone and were genetically and phenotypically characterized for the CYP2D6 allelic variation. Our results showed a linear kinetics of mephedrone at the dose range assayed: plasma concentrations, cardiovascular and subjective effects, and blood serotonin concentrations all correlated in a dose-dependent manner. Mephedrone metabolic disposition is mediated by CYP2D6. Mephedrone pharmacology presented a linear dose-dependence within the range of doses tested. The metabolism of mephedrone by CYP2D6 implies that recreational users with no or low CYP2D6 functionality are exposed to unwanted acute toxicity episodes.
- dc.format.mimetype application/pdf
- dc.identifier.citation Olesti E, Farré M, Carbó ML, Papaseit E, Perez-Mañá C, Torrens M et al. Dose-response pharmacological study of mephedrone and its metabolites: pharmacokinetics, serotoninergic effects, and impact of CYP2D6 genetic variation. Clin Pharmacol Ther. 2019 Sep;106(3):596-604. DOI: 10.1002/cpt.1417
- dc.identifier.doi http://dx.doi.org/10.1002/cpt.1417
- dc.identifier.issn 0009-9236
- dc.identifier.uri http://hdl.handle.net/10230/43021
- dc.language.iso eng
- dc.publisher Wiley
- dc.relation.ispartof Clinical Pharmacology & Therapeutics. 2019 Sep;106(3):596-604
- dc.rights This is the peer reviewed version of the following article: Olesti E, Farré M, Carbó ML, Papaseit E, Perez-Mañá C, Torrens M. et al. Dose-response pharmacological study of mephedrone and its metabolites: pharmacokinetics, serotoninergic effects, and impact of CYP2D6 genetic variation. Clin Pharmacol Ther. 2019 Sep;106(3):596-604. which has been published in final form at http://dx.doi.org/10.1002/cpt.1417. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions.
- dc.rights.accessRights info:eu-repo/semantics/openAccess
- dc.subject.other Medicaments -- Administració
- dc.subject.other Medicaments -- Toxicologia
- dc.subject.other Mephedrone
- dc.title Dose-response pharmacological study of mephedrone and its metabolites: pharmacokinetics, serotoninergic effects, and impact of CYP2D6 genetic variation
- dc.type info:eu-repo/semantics/article
- dc.type.version info:eu-repo/semantics/acceptedVersion