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A review of the influence of functional group modifications to the core scaffold of synthetic cathinones on drug pharmacokinetics.
- Source :
-
Psychopharmacology [Psychopharmacology (Berl)] 2019 Mar; Vol. 236 (3), pp. 881-890. Date of Electronic Publication: 2018 Aug 01. - Publication Year :
- 2019
-
Abstract
- Rationale: The synthetic cathinones are a class of designer drugs of abuse that share a common core scaffold. The pharmacokinetic profiles of the synthetic cathinones vary based on the substitutions to the core scaffold.<br />Objectives: To provide a summary of the literature regarding the pharmacokinetic characteristics of the synthetic cathinones, with a focus on the impact of the structural modifications to the pharmacokinetics.<br />Results: In many, but not all, instances the pharmacokinetic characteristics of the synthetic cathinones can be reasonably predicted based on the substitutions to the core scaffold. Mephedrone and methylone are chemically alike and have similar T <subscript>max</subscript> and t <subscript>1/2</subscript> in male rats. MDPV, a structurally distinct synthetic cathinone from mephedrone and methylone, has a lower T <subscript>max</subscript> and t <subscript>1/2</subscript> . Increasing the length of the alkyl chain on the α position of methylone, to produce pentylone, results in increased plasma concentrations and longer t <subscript>1/2</subscript> . Metabolism of the synthetic cathinones is reasonably predictable based on the chemical structure, and several phase I metabolites retain pharmacodynamic activity. CYP2D6 is implicated in the metabolism of all of the synthetic cathinones, and other P450s (CYP1A2, CYP2B6, and CYP2C19) are known to contribute variably to the metabolism of specific synthetic cathinones.<br />Conclusions: Continued research will lead to a better understanding of the pharmacokinetic changes associated with structural modifications to the cathinone scaffold, and potentially in the long range, enhanced overdose and addiction therapy. Additionally, the areas of polydrug use and pharmacogenetics have been largely overlooked with regard to synthetic cathinones.
- Subjects :
- Alkaloids adverse effects
Amphetamines adverse effects
Amphetamines chemistry
Amphetamines pharmacokinetics
Animals
Designer Drugs adverse effects
Designer Drugs chemistry
Designer Drugs pharmacokinetics
Humans
Methamphetamine adverse effects
Methamphetamine analogs & derivatives
Methamphetamine chemistry
Methamphetamine pharmacokinetics
Substance-Related Disorders epidemiology
Substance-Related Disorders metabolism
Synthetic Drugs adverse effects
Alkaloids chemistry
Alkaloids pharmacokinetics
Synthetic Drugs chemistry
Synthetic Drugs pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1432-2072
- Volume :
- 236
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Psychopharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 30069588
- Full Text :
- https://doi.org/10.1007/s00213-018-4985-6