Citation

Cannaert A, Ambach L, Blanckaert P, Stove CP. Front. Pharmacol. 2018; 9(MAY).

Copyright

(Copyright © 2018, Frontiers Media)

DOI

10.3389/fphar.2018.00486

PMID

unavailable

Abstract

Carfentanil, one of the most potent opioids known, has recently been reported as a contaminant in street heroin in the United States and Europe, and is associated with an increased number of life-threatening emergency department admissions and deaths. Here, we report on the application of a novel in vitro opioid activity reporter assay and a sensitive bioanalytical assay in the context of a fatal carfentanil intoxication, revealing the highest carfentanil concentrations reported until now. A 21-year-old male was found dead at home with a note stating that he had taken carfentanil with suicidal intentions. A foil bag and plastic bag labeled "C.50" were found at the scene. These bags were similar to a sample obtained by the Belgian Early Warning System on Drugs from a German darknet shop and to those found in the context of a fatality in Norway. Blood, urine and vitreous, obtained during autopsy, were screened with a newly developed in vitro opioid activity reporter assay able to detect compounds based on their μ-opioid receptor activity rather than their chemical structure. All extracts showed strong opioid activity.

RESULTS were confirmed by a bioanalytical assay, which revealed extremely high concentrations for carfentanil and norcarfentanil. It should be noted that carfentanil concentrations are typically in pg/mL, but here they were 92 ng/mL in blood, 2.8 ng/mL in urine, and 23 ng/mL in vitreous. The blood and vitreous contained 0.532 and 0.300 ng/mL norcarfentanil, respectively. No norcarfentanil was detected in urine. This is the first report where a novel activity-based opioid screening assay was successfully deployed in a forensic case. Confirmation and quantification using a validated bioanalytical procedure revealed the, to our knowledge, highest carfentanil concentrations reported in humans so far. © 2018 Cannaert, Ambach, Blanckaert and Stove.

Language: en

Keywords

adult; human; male; autopsy; case report; suicide attempt; LC-MS/MS; toxicology; blood sampling; clinical article; drug intoxication; drug fatality; drug monitoring; drug potency; chemical structure; quantitative analysis; mass fragmentography; Article; in vitro study; tandem mass spectrometry; mu opiate receptor; enzyme linked immunosorbent assay; vitreous body; young adult; bioassay; enzyme multiplied immunoassay technique; Activity-based; beta arrestin 2; Bioassay; carfentanil; Carfentanil; liquid chromatography-mass spectrometry; Synthetic opioids; Untargeted screening; urine sampling