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New Psychoactive Substances: Chemistry, Pharmacology, Metabolism, and Detectability of Amphetamine Derivatives With Modified Ring Systems.
- Source :
-
Therapeutic drug monitoring [Ther Drug Monit] 2016 Feb; Vol. 38 (1), pp. 4-11. - Publication Year :
- 2016
-
Abstract
- In recent years, new amphetamine derivatives with modified ring systems were sold and consumed as new drugs of abuse. They belong together with other new drugs of abuse classes to the so-called new psychoactive substances (NPS). The chemistry, pharmacology, toxicology, metabolism, and toxicokinetics are shortly discussed of camfetamine, 3 methylphenyl-amphetamines (2-MA, 3-MA, and 4-MA), 2-methiopropamine (2-MPA), and 5-(2-aminopropyl)benzofuran (5-APB), 6-(2-aminopropyl)benzofuran (6-APB, so-called "benzofury") and their N-methyl derivatives 5-MAPB and 6-MAPB. Only a rough assessment of the pharmacology and toxicology NPS can be performed in most cases using published data of analogs, trip reports, and described clinical cases. Accordingly, they all act more or less as central nervous stimulants mainly by increasing the concentration of the neurotransmitters noradrenaline, dopamine, and serotonin (5-HT) by inducing their release and reuptake inhibition. Thus, the acute toxicity is associated with the sympathomimetic effects, such as mydriasis, hyperthermia, hypertension, tachycardia, insomnia, and anxiety. With the exception of 5- and 6-APB, these NPS were extensively metabolized by N-demethylation and/or aromatic hydroxylation catalyzed by various cytochrome P450 isoenzymes followed by partial glucuronidation and/or sulfation. For urinalysis, the unchanged drugs and/or the nor-metabolites are the main targets.
- Subjects :
- Amphetamines pharmacokinetics
Amphetamines pharmacology
Central Nervous System Stimulants pharmacokinetics
Central Nervous System Stimulants pharmacology
Humans
Substance Abuse Detection methods
Amphetamine-Related Disorders diagnosis
Amphetamines chemistry
Central Nervous System Stimulants chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1536-3694
- Volume :
- 38
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Therapeutic drug monitoring
- Publication Type :
- Academic Journal
- Accession number :
- 26327309
- Full Text :
- https://doi.org/10.1097/FTD.0000000000000240