GC–MS Quantification Method for Mephedrone in Plasma and Urine: Application to Human Pharmacokinetics
Eulàlia Olesti, Mitona Pujadas, Esther Papaseit, Clara Pérez‐mañá, Óscar J. Pozo, Magı́ Farré, Rafael de la Torre
Journal of Analytical Toxicology October 3, 2016 DOI: 10.1093/jat/bkw120 via OpenAlex
Summary
Mephedrone, a synthetic cathinone increasingly used by young people and linked to acute intoxication and fatalities, was studied in a controlled clinical trial. A gas chromatography-mass spectrometry method was developed to measure mephedrone in human plasma and urine. Six healthy men received 150 mg of mephedrone orally. Peak plasma concentration averaged 122.6 ng/mL, reached within 0.5–2 hours, and the drug was eliminated rapidly with a half-life of 2.2 hours. Less than 15% of the dose appeared unchanged in urine, and concentrations varied widely among individuals.
Study at a glance
| Characteristics | Randomized controlled trial Double-blind Peer reviewed |
|---|---|
| Sample size | 6 |
| Population | Healthy males |
| Intervention | Mephedrone |
| Dose | 150 mg |
| Keywords | Mephedrone Pharmacokinetics Urine Cmax Derivatization |
| Citations | 41 |
| Key finding | Mephedrone reaches peak plasma concentration within 1 hour, has a rapid elimination half-life of 2.2 hours, and less than 15% is excreted unchanged in urine, with high inter-subject variability. |
Abstract
Increasing consumption has been observed among young people of new psychoactive substances, including synthetic cathinone derivatives. The most well known of these is mephedrone whose use has been related to acute intoxication and fatality. Several methods able to detect mephedrone have been reported, although to date, none have been applied to human pharmacokinetic studies in a controlled setting. We developed a gas chromatography-mass spectrometry technique for mephedrone quantification in human plasma and urine. Plasma after deproteinization and urine were submitted to a liquid-liquid extraction and derivatization of the extract with MSTFA prior to analysis. Calibration curves covered concentration ranges in plasma between 5 and 300 ng/mL and in urine between 20 and 1,500 ng/mL. The method has been successfully applied to biological samples obtained from a pilot clinical trial intended to evaluate the human pharmacology of mephedrone and its relative bioavailability and pharmacokinetics. Six healthy males were administered 150 mg of mephedrone by the oral route in a randomized, double-blind, cross-over controlled trial. Peak plasma concentration (Cmax = 122.6 ± 32.9 ng/mL) was reached at 1 hour (0.5-2 h) post-drug administration. Mephedrone showed a rapid elimination half-life (t1/2 = 2.2 h) compared to other psychostimulants. Less than 15% of the dose was excreted in urine as a free-form. Mephedrone concentrations displayed a relevant inter-subject variability.