Pharmacokinetic properties of 4-fluoroamphetamine in serum and oral fluid after oral ingestion

Stefan W Toennes, David Schneider, Werner Pogoda, Alexander Paulke, Cora Wunder, Eef L Theunissen, Kim P C Kuypers, Eliza de Sousa Fernandes Perna, Johannes G Ramaekers

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

INTRODUCTION: Each year, synthetic drugs are occurring in high numbers in the illicit drug market. But data on their pharmacology and toxicology are scarcely available. Therefore, a controlled study was performed to evaluate pharmacokinetic parameters of 4-fluoroamphetamine (4FA) in humans and to compare it with its effects.

METHODS: Twelve subjects ingested 100 mg and 5 subjects also received 150 mg 4-FA in a bitter lemon drink. Blood and oral fluid samples were taken during the following 12 hours and analyzed for 4-FA and traces of amphetamine as impurity by liquid chromatography-mass spectrometry (LC-MSMS).

RESULTS: During 12 hours after ingestion the concentration-time course of 4-FA was similar to that of amphetamine with maximal concentrations appearing in serum after about 2 hours (in median 195 ng/ml after the 100 mg dose, range 155-316 ng/ml). The elimination half-life was approximately 8-9 hours and shorter than that of amphetamine but exhibited a marked variation (5.5 - 16.8 hours). In oral fluid 4-FA could also be detected for 12 hours and concentrations were higher than in serum. During the first 3 hours after ingestion concentrations were higher most probably due to oral contamination. Serum concentrations in forensic cases were in the range of those observed in the present study suggesting dosages in recreational use in the range of those tested here.

CONCLUSIONS: The pharmacokinetic properties of 4-FA are similar to that of amphetamine including a marked variation in elimination. However, recreational dosages may already exhibit prominent adverse effects and may even have life-threatening consequences.

Original languageEnglish
Pages (from-to)1028-1034
Number of pages7
JournalDrug Testing and Analysis
Volume11
Issue number7
Early online date25 Mar 2019
DOIs
Publication statusPublished - Jul 2019

Keywords

  • 4-fluoroamphetamine
  • AMPHETAMINE
  • PLASMA
  • SYNTHETIC CANNABINOID JWH-018
  • URINE
  • new psychoactive substances (NPS)
  • oral fluid
  • pharmacokinetics
  • serum

Cite this

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title = "Pharmacokinetic properties of 4-fluoroamphetamine in serum and oral fluid after oral ingestion",
abstract = "INTRODUCTION: Each year, synthetic drugs are occurring in high numbers in the illicit drug market. But data on their pharmacology and toxicology are scarcely available. Therefore, a controlled study was performed to evaluate pharmacokinetic parameters of 4-fluoroamphetamine (4FA) in humans and to compare it with its effects.METHODS: Twelve subjects ingested 100 mg and 5 subjects also received 150 mg 4-FA in a bitter lemon drink. Blood and oral fluid samples were taken during the following 12 hours and analyzed for 4-FA and traces of amphetamine as impurity by liquid chromatography-mass spectrometry (LC-MSMS).RESULTS: During 12 hours after ingestion the concentration-time course of 4-FA was similar to that of amphetamine with maximal concentrations appearing in serum after about 2 hours (in median 195 ng/ml after the 100 mg dose, range 155-316 ng/ml). The elimination half-life was approximately 8-9 hours and shorter than that of amphetamine but exhibited a marked variation (5.5 - 16.8 hours). In oral fluid 4-FA could also be detected for 12 hours and concentrations were higher than in serum. During the first 3 hours after ingestion concentrations were higher most probably due to oral contamination. Serum concentrations in forensic cases were in the range of those observed in the present study suggesting dosages in recreational use in the range of those tested here.CONCLUSIONS: The pharmacokinetic properties of 4-FA are similar to that of amphetamine including a marked variation in elimination. However, recreational dosages may already exhibit prominent adverse effects and may even have life-threatening consequences.",
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author = "Toennes, {Stefan W} and David Schneider and Werner Pogoda and Alexander Paulke and Cora Wunder and Theunissen, {Eef L} and Kuypers, {Kim P C} and {de Sousa Fernandes Perna}, Eliza and Ramaekers, {Johannes G}",
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year = "2019",
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language = "English",
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Pharmacokinetic properties of 4-fluoroamphetamine in serum and oral fluid after oral ingestion. / Toennes, Stefan W; Schneider, David; Pogoda, Werner; Paulke, Alexander; Wunder, Cora; Theunissen, Eef L; Kuypers, Kim P C; de Sousa Fernandes Perna, Eliza; Ramaekers, Johannes G.

In: Drug Testing and Analysis, Vol. 11, No. 7, 07.2019, p. 1028-1034.

Research output: Contribution to journalArticleAcademicpeer-review

TY - JOUR

T1 - Pharmacokinetic properties of 4-fluoroamphetamine in serum and oral fluid after oral ingestion

AU - Toennes, Stefan W

AU - Schneider, David

AU - Pogoda, Werner

AU - Paulke, Alexander

AU - Wunder, Cora

AU - Theunissen, Eef L

AU - Kuypers, Kim P C

AU - de Sousa Fernandes Perna, Eliza

AU - Ramaekers, Johannes G

N1 - This article is protected by copyright. All rights reserved.

PY - 2019/7

Y1 - 2019/7

N2 - INTRODUCTION: Each year, synthetic drugs are occurring in high numbers in the illicit drug market. But data on their pharmacology and toxicology are scarcely available. Therefore, a controlled study was performed to evaluate pharmacokinetic parameters of 4-fluoroamphetamine (4FA) in humans and to compare it with its effects.METHODS: Twelve subjects ingested 100 mg and 5 subjects also received 150 mg 4-FA in a bitter lemon drink. Blood and oral fluid samples were taken during the following 12 hours and analyzed for 4-FA and traces of amphetamine as impurity by liquid chromatography-mass spectrometry (LC-MSMS).RESULTS: During 12 hours after ingestion the concentration-time course of 4-FA was similar to that of amphetamine with maximal concentrations appearing in serum after about 2 hours (in median 195 ng/ml after the 100 mg dose, range 155-316 ng/ml). The elimination half-life was approximately 8-9 hours and shorter than that of amphetamine but exhibited a marked variation (5.5 - 16.8 hours). In oral fluid 4-FA could also be detected for 12 hours and concentrations were higher than in serum. During the first 3 hours after ingestion concentrations were higher most probably due to oral contamination. Serum concentrations in forensic cases were in the range of those observed in the present study suggesting dosages in recreational use in the range of those tested here.CONCLUSIONS: The pharmacokinetic properties of 4-FA are similar to that of amphetamine including a marked variation in elimination. However, recreational dosages may already exhibit prominent adverse effects and may even have life-threatening consequences.

AB - INTRODUCTION: Each year, synthetic drugs are occurring in high numbers in the illicit drug market. But data on their pharmacology and toxicology are scarcely available. Therefore, a controlled study was performed to evaluate pharmacokinetic parameters of 4-fluoroamphetamine (4FA) in humans and to compare it with its effects.METHODS: Twelve subjects ingested 100 mg and 5 subjects also received 150 mg 4-FA in a bitter lemon drink. Blood and oral fluid samples were taken during the following 12 hours and analyzed for 4-FA and traces of amphetamine as impurity by liquid chromatography-mass spectrometry (LC-MSMS).RESULTS: During 12 hours after ingestion the concentration-time course of 4-FA was similar to that of amphetamine with maximal concentrations appearing in serum after about 2 hours (in median 195 ng/ml after the 100 mg dose, range 155-316 ng/ml). The elimination half-life was approximately 8-9 hours and shorter than that of amphetamine but exhibited a marked variation (5.5 - 16.8 hours). In oral fluid 4-FA could also be detected for 12 hours and concentrations were higher than in serum. During the first 3 hours after ingestion concentrations were higher most probably due to oral contamination. Serum concentrations in forensic cases were in the range of those observed in the present study suggesting dosages in recreational use in the range of those tested here.CONCLUSIONS: The pharmacokinetic properties of 4-FA are similar to that of amphetamine including a marked variation in elimination. However, recreational dosages may already exhibit prominent adverse effects and may even have life-threatening consequences.

KW - 4-fluoroamphetamine

KW - AMPHETAMINE

KW - PLASMA

KW - SYNTHETIC CANNABINOID JWH-018

KW - URINE

KW - new psychoactive substances (NPS)

KW - oral fluid

KW - pharmacokinetics

KW - serum

U2 - 10.1002/dta.2595

DO - 10.1002/dta.2595

M3 - Article

C2 - 30912312

VL - 11

SP - 1028

EP - 1034

JO - Drug Testing and Analysis

JF - Drug Testing and Analysis

SN - 1942-7603

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ER -