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The synthetic cathinone α-pyrrolidinovalerophenone (α-PVP): pharmacokinetic and pharmacodynamic clinical and forensic aspects.
Drug Metab Rev. 2018 05; 50(2):125-139.DM

Abstract

New psychoactive substances (NPS), often referred as 'legal highs' or 'designer drugs', are derivatives and analogs of existing psychoactive drugs that are introduced in the recreational market to circumvent existing legislation on drugs of abuse. This work aims to review the state-of-the-art regarding chemical, molecular pharmacology, and in vitro and in vivo data on toxicokinetics of the potent synthetic cathinone α-pyrrolidinovalerophenone (α-PVP or flakka or zombie drug). Chemical, pharmacological, toxicological, and clinical effects of α-PVP were searched in PubMed (U.S. National Library of Medicine) and governmental websites without limitation of the period. α-PVP is a wide spread and easy to get special type of synthetic cathinone with seemingly powerful cocaine-like stimulant effects, high brain penetration, high liability for abuse and with increased risk of adverse effects such as tachycardia, agitation, hypertension, hallucinations, delirium, mydriasis, self-injury, aggressive behavior, and suicidal ideations. α-PVP undergoes extensive metabolism via different pathways and the α-PVP itself or its metabolites β-hydroxy-α-PVP and α-PVP lactam represent the main targets for toxicological analysis in urine. There is a limited knowledge regarding the short- and long-term effects of α-PVP and metabolites, and pharmacogenetic influence, hence further clinical and forensic toxicological studies are required. Moreover, since α-PVP cannot be detected with classic routine analysis procedures, statements on the frequency of their consumption cannot be made.

Authors+Show Affiliations

a Department of Public Health, Forensic Sciences, and Medical Education, Faculty of Medicine , University of Porto , Porto , Portugal.a Department of Public Health, Forensic Sciences, and Medical Education, Faculty of Medicine , University of Porto , Porto , Portugal. b UCIBIO, REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy , University of Porto , Porto , Portugal. c Department of Sciences, IINFACTS - Institute of Research and Advanced Training in Health Sciences and Technologies , University Institute of Health Sciences (IUCS), CESPU, CRL , Gandra , Portugal.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

29540067

Citation

Nóbrega, Leandro, and Ricardo Jorge Dinis-Oliveira. "The Synthetic Cathinone Α-pyrrolidinovalerophenone (α-PVP): Pharmacokinetic and Pharmacodynamic Clinical and Forensic Aspects." Drug Metabolism Reviews, vol. 50, no. 2, 2018, pp. 125-139.
Nóbrega L, Dinis-Oliveira RJ. The synthetic cathinone α-pyrrolidinovalerophenone (α-PVP): pharmacokinetic and pharmacodynamic clinical and forensic aspects. Drug Metab Rev. 2018;50(2):125-139.
Nóbrega, L., & Dinis-Oliveira, R. J. (2018). The synthetic cathinone α-pyrrolidinovalerophenone (α-PVP): pharmacokinetic and pharmacodynamic clinical and forensic aspects. Drug Metabolism Reviews, 50(2), 125-139. https://doi.org/10.1080/03602532.2018.1448867
Nóbrega L, Dinis-Oliveira RJ. The Synthetic Cathinone Α-pyrrolidinovalerophenone (α-PVP): Pharmacokinetic and Pharmacodynamic Clinical and Forensic Aspects. Drug Metab Rev. 2018;50(2):125-139. PubMed PMID: 29540067.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The synthetic cathinone α-pyrrolidinovalerophenone (α-PVP): pharmacokinetic and pharmacodynamic clinical and forensic aspects. AU - Nóbrega,Leandro, AU - Dinis-Oliveira,Ricardo Jorge, Y1 - 2018/03/14/ PY - 2018/3/16/pubmed PY - 2018/8/24/medline PY - 2018/3/16/entrez KW - New psychoactive substances KW - pharmacodynamics KW - pharmacokinetics KW - synthetic cathinones KW - α-pyrrolidinovalerophenone SP - 125 EP - 139 JF - Drug metabolism reviews JO - Drug Metab Rev VL - 50 IS - 2 N2 - New psychoactive substances (NPS), often referred as 'legal highs' or 'designer drugs', are derivatives and analogs of existing psychoactive drugs that are introduced in the recreational market to circumvent existing legislation on drugs of abuse. This work aims to review the state-of-the-art regarding chemical, molecular pharmacology, and in vitro and in vivo data on toxicokinetics of the potent synthetic cathinone α-pyrrolidinovalerophenone (α-PVP or flakka or zombie drug). Chemical, pharmacological, toxicological, and clinical effects of α-PVP were searched in PubMed (U.S. National Library of Medicine) and governmental websites without limitation of the period. α-PVP is a wide spread and easy to get special type of synthetic cathinone with seemingly powerful cocaine-like stimulant effects, high brain penetration, high liability for abuse and with increased risk of adverse effects such as tachycardia, agitation, hypertension, hallucinations, delirium, mydriasis, self-injury, aggressive behavior, and suicidal ideations. α-PVP undergoes extensive metabolism via different pathways and the α-PVP itself or its metabolites β-hydroxy-α-PVP and α-PVP lactam represent the main targets for toxicological analysis in urine. There is a limited knowledge regarding the short- and long-term effects of α-PVP and metabolites, and pharmacogenetic influence, hence further clinical and forensic toxicological studies are required. Moreover, since α-PVP cannot be detected with classic routine analysis procedures, statements on the frequency of their consumption cannot be made. SN - 1097-9883 UR - https://www.unboundmedicine.com/medline/citation/29540067/The_synthetic_cathinone_α_pyrrolidinovalerophenone__α_PVP_:_pharmacokinetic_and_pharmacodynamic_clinical_and_forensic_aspects_ L2 - https://www.tandfonline.com/doi/full/10.1080/03602532.2018.1448867 DB - PRIME DP - Unbound Medicine ER -