Pharmacokinetic properties of the synthetic cannabinoid JWH-018 and of its metabolites in serum after inhalation

Stefan W. Toennes, Anna Geraths, Werner Pogoda, Alexander Paulke, Cora Wunder, Eef L Theunissen, Johannes G Ramaekers

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

Each year, synthetic cannabinoids are occurring in high numbers in the illicit drug market, but data on their pharmacology and toxicology are scarcely available. Therefore, a pilot study was performed to assess adverse effects of JWH-018, which is one of the oldest and best known synthetic cannabinoids. Six subjects inhaled smoke from 2 and 3mg JWH-018. The drug and nine of its metabolites were analyzed in their blood samples taken during the following 12h by liquid chromatography-mass spectrometry (LC-MSMS). The maximum concentration of JWH-018 reached 2.9-9.9ng/ml after inhalation and markedly decreased during the next 1.5h, followed by a multiexponential decline (t1/2 in median 1.3h and 5.7h). The concentration of the pentanoic acid metabolite was slightly higher than that of the 3-, 4- and 5-hydroxypentyl metabolites and of the 6-hydroxyindol metabolite. The data also suggest a multiexponential decline and slow terminal elimination of JWH-018 and all metabolites. The detection of JWH-018 and of its metabolites in serum requires high analytical sensitivity. The pharmacokinetic properties of inhaled JWH-018 are similar to that of THC. A slow terminal elimination of drug and metabolites may lead to accumulation in chronic users.

Original languageEnglish
Pages (from-to)215-222
Number of pages8
JournalJournal of Pharmaceutical and Biomedical Analysis
Volume140
DOIs
Publication statusPublished - 5 Jun 2017

Keywords

  • Pharmacokinetics
  • Synthetic cannabinoids
  • JWH-018
  • Metabolites
  • Liquid chromatography-mass spectrometry
  • TANDEM MASS-SPECTROMETRY
  • HUMAN URINE
  • QUANTITATIVE MEASUREMENT
  • WHOLE-BLOOD
  • QUANTIFICATION
  • IDENTIFICATION
  • VALIDATION
  • EXTRACTION
  • MS/MS
  • OMEGA

Cite this

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title = "Pharmacokinetic properties of the synthetic cannabinoid JWH-018 and of its metabolites in serum after inhalation",
abstract = "Each year, synthetic cannabinoids are occurring in high numbers in the illicit drug market, but data on their pharmacology and toxicology are scarcely available. Therefore, a pilot study was performed to assess adverse effects of JWH-018, which is one of the oldest and best known synthetic cannabinoids. Six subjects inhaled smoke from 2 and 3mg JWH-018. The drug and nine of its metabolites were analyzed in their blood samples taken during the following 12h by liquid chromatography-mass spectrometry (LC-MSMS). The maximum concentration of JWH-018 reached 2.9-9.9ng/ml after inhalation and markedly decreased during the next 1.5h, followed by a multiexponential decline (t1/2 in median 1.3h and 5.7h). The concentration of the pentanoic acid metabolite was slightly higher than that of the 3-, 4- and 5-hydroxypentyl metabolites and of the 6-hydroxyindol metabolite. The data also suggest a multiexponential decline and slow terminal elimination of JWH-018 and all metabolites. The detection of JWH-018 and of its metabolites in serum requires high analytical sensitivity. The pharmacokinetic properties of inhaled JWH-018 are similar to that of THC. A slow terminal elimination of drug and metabolites may lead to accumulation in chronic users.",
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author = "Toennes, {Stefan W.} and Anna Geraths and Werner Pogoda and Alexander Paulke and Cora Wunder and Theunissen, {Eef L} and Ramaekers, {Johannes G}",
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month = "6",
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language = "English",
volume = "140",
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Pharmacokinetic properties of the synthetic cannabinoid JWH-018 and of its metabolites in serum after inhalation. / Toennes, Stefan W.; Geraths, Anna; Pogoda, Werner; Paulke, Alexander; Wunder, Cora; Theunissen, Eef L; Ramaekers, Johannes G.

In: Journal of Pharmaceutical and Biomedical Analysis, Vol. 140, 05.06.2017, p. 215-222.

Research output: Contribution to journalArticleAcademicpeer-review

TY - JOUR

T1 - Pharmacokinetic properties of the synthetic cannabinoid JWH-018 and of its metabolites in serum after inhalation

AU - Toennes, Stefan W.

AU - Geraths, Anna

AU - Pogoda, Werner

AU - Paulke, Alexander

AU - Wunder, Cora

AU - Theunissen, Eef L

AU - Ramaekers, Johannes G

N1 - Copyright © 2017 Elsevier B.V. All rights reserved.

PY - 2017/6/5

Y1 - 2017/6/5

N2 - Each year, synthetic cannabinoids are occurring in high numbers in the illicit drug market, but data on their pharmacology and toxicology are scarcely available. Therefore, a pilot study was performed to assess adverse effects of JWH-018, which is one of the oldest and best known synthetic cannabinoids. Six subjects inhaled smoke from 2 and 3mg JWH-018. The drug and nine of its metabolites were analyzed in their blood samples taken during the following 12h by liquid chromatography-mass spectrometry (LC-MSMS). The maximum concentration of JWH-018 reached 2.9-9.9ng/ml after inhalation and markedly decreased during the next 1.5h, followed by a multiexponential decline (t1/2 in median 1.3h and 5.7h). The concentration of the pentanoic acid metabolite was slightly higher than that of the 3-, 4- and 5-hydroxypentyl metabolites and of the 6-hydroxyindol metabolite. The data also suggest a multiexponential decline and slow terminal elimination of JWH-018 and all metabolites. The detection of JWH-018 and of its metabolites in serum requires high analytical sensitivity. The pharmacokinetic properties of inhaled JWH-018 are similar to that of THC. A slow terminal elimination of drug and metabolites may lead to accumulation in chronic users.

AB - Each year, synthetic cannabinoids are occurring in high numbers in the illicit drug market, but data on their pharmacology and toxicology are scarcely available. Therefore, a pilot study was performed to assess adverse effects of JWH-018, which is one of the oldest and best known synthetic cannabinoids. Six subjects inhaled smoke from 2 and 3mg JWH-018. The drug and nine of its metabolites were analyzed in their blood samples taken during the following 12h by liquid chromatography-mass spectrometry (LC-MSMS). The maximum concentration of JWH-018 reached 2.9-9.9ng/ml after inhalation and markedly decreased during the next 1.5h, followed by a multiexponential decline (t1/2 in median 1.3h and 5.7h). The concentration of the pentanoic acid metabolite was slightly higher than that of the 3-, 4- and 5-hydroxypentyl metabolites and of the 6-hydroxyindol metabolite. The data also suggest a multiexponential decline and slow terminal elimination of JWH-018 and all metabolites. The detection of JWH-018 and of its metabolites in serum requires high analytical sensitivity. The pharmacokinetic properties of inhaled JWH-018 are similar to that of THC. A slow terminal elimination of drug and metabolites may lead to accumulation in chronic users.

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KW - HUMAN URINE

KW - QUANTITATIVE MEASUREMENT

KW - WHOLE-BLOOD

KW - QUANTIFICATION

KW - IDENTIFICATION

KW - VALIDATION

KW - EXTRACTION

KW - MS/MS

KW - OMEGA

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DO - 10.1016/j.jpba.2017.03.043

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VL - 140

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EP - 222

JO - Journal of Pharmaceutical and Biomedical Analysis

JF - Journal of Pharmaceutical and Biomedical Analysis

SN - 0731-7085

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