Subacute Toxicity and Pharmacokinetic Evaluation of the Synthetic Cannabinoid 4F-MDMB-BUTINACA in Rats: A Forensic and Toxicological Perspective

<b>Background</b>: 4-MDMB-BUTINACA, a next-generation synthetic cannabinoid, presents significant public health and forensic challenges due to its evolving nature and potential toxicity. <b>Methods</b>: This study evaluates the subacute toxic effects and pharmacokinetics of 4...

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Main Authors: Elkhatim Hassan Abdelgadir, Jihad Al-Qudsi, Elham S. Abu-Nukhaa, Dimah A. Alsidrani
Format: Article
Language:English
Published: MDPI AG 2024-10-01
Series:Future Pharmacology
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Online Access:https://www.mdpi.com/2673-9879/4/4/36
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author Elkhatim Hassan Abdelgadir
Jihad Al-Qudsi
Elham S. Abu-Nukhaa
Dimah A. Alsidrani
author_facet Elkhatim Hassan Abdelgadir
Jihad Al-Qudsi
Elham S. Abu-Nukhaa
Dimah A. Alsidrani
author_sort Elkhatim Hassan Abdelgadir
collection DOAJ
description <b>Background</b>: 4-MDMB-BUTINACA, a next-generation synthetic cannabinoid, presents significant public health and forensic challenges due to its evolving nature and potential toxicity. <b>Methods</b>: This study evaluates the subacute toxic effects and pharmacokinetics of 4−Fluoro MDMB−BUTINACA (4F-MDMB-BUTINACA) in adult male albino rats, administered orally for seven days at doses of 1 mg/kg, 5 mg/kg, and 15 mg/kg. The hematological, biochemical, and histopathological parameters were assessed and compared to controls. <b>Results</b>: The pharmacokinetics were determined using GC–MS/MS with a positive chemical ionization and granisetron as an internal standard. A histological analysis revealed inflammatory cell aggregation, congestion, hemorrhage, edema, and fibrosis in various tissues, with renal examinations showing tubule degradation, glomerular atrophy, Bowman’s space expansion, edema, and hemorrhage. The liver exhibited cellular infiltration, while cardiac muscle fibers showed myocardial fiber degradation and inflammatory cell aggregation. Biochemical assays indicated significant alterations (<i>p</i> < 0.05) in the serum levels of AST, ALT, ALP, GGT, total protein, albumin, triglycerides, urea, MCHC, MCV, RDW, platelets, neutrophils, eosinophils, and basophils compared to the controls. <b>Conclusions</b>: The validated bioanalytical method revealed rapid absorption of 4F-MDMB-BUTINACA, with a plasma half-life of 2.371 h, a volume of distribution of 2272.85 L, and a plasma clearance rate of 664.241 L/h. In conclusion, 4F-MDMB-BUTINACA is a highly toxic synthetic cannabinoid, particularly affecting the liver, kidneys, and heart.
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spelling doaj-art-eca0155a1a3e4a44a112e2f3d6d2fa202024-12-27T14:27:25ZengMDPI AGFuture Pharmacology2673-98792024-10-014467669910.3390/futurepharmacol4040036Subacute Toxicity and Pharmacokinetic Evaluation of the Synthetic Cannabinoid 4F-MDMB-BUTINACA in Rats: A Forensic and Toxicological PerspectiveElkhatim Hassan Abdelgadir0Jihad Al-Qudsi1Elham S. Abu-Nukhaa2Dimah A. Alsidrani3Department of Forensic Sciences, College of Criminal Justice, Naif Arab University for Security Sciences, Riyadh 14812, Saudi ArabiaDepartment of Forensic Sciences, College of Criminal Justice, Naif Arab University for Security Sciences, Riyadh 14812, Saudi ArabiaDepartment of Forensic Sciences, College of Criminal Justice, Naif Arab University for Security Sciences, Riyadh 14812, Saudi ArabiaDepartment of Forensic Sciences, College of Criminal Justice, Naif Arab University for Security Sciences, Riyadh 14812, Saudi Arabia<b>Background</b>: 4-MDMB-BUTINACA, a next-generation synthetic cannabinoid, presents significant public health and forensic challenges due to its evolving nature and potential toxicity. <b>Methods</b>: This study evaluates the subacute toxic effects and pharmacokinetics of 4−Fluoro MDMB−BUTINACA (4F-MDMB-BUTINACA) in adult male albino rats, administered orally for seven days at doses of 1 mg/kg, 5 mg/kg, and 15 mg/kg. The hematological, biochemical, and histopathological parameters were assessed and compared to controls. <b>Results</b>: The pharmacokinetics were determined using GC–MS/MS with a positive chemical ionization and granisetron as an internal standard. A histological analysis revealed inflammatory cell aggregation, congestion, hemorrhage, edema, and fibrosis in various tissues, with renal examinations showing tubule degradation, glomerular atrophy, Bowman’s space expansion, edema, and hemorrhage. The liver exhibited cellular infiltration, while cardiac muscle fibers showed myocardial fiber degradation and inflammatory cell aggregation. Biochemical assays indicated significant alterations (<i>p</i> < 0.05) in the serum levels of AST, ALT, ALP, GGT, total protein, albumin, triglycerides, urea, MCHC, MCV, RDW, platelets, neutrophils, eosinophils, and basophils compared to the controls. <b>Conclusions</b>: The validated bioanalytical method revealed rapid absorption of 4F-MDMB-BUTINACA, with a plasma half-life of 2.371 h, a volume of distribution of 2272.85 L, and a plasma clearance rate of 664.241 L/h. In conclusion, 4F-MDMB-BUTINACA is a highly toxic synthetic cannabinoid, particularly affecting the liver, kidneys, and heart.https://www.mdpi.com/2673-9879/4/4/364F-MDMB-BUTINACA toxicitysynthetic cannabinoid pharmacokineticsrat model drug studyGC–MS/MS analysishematological and biochemical changeshistopathological examination
spellingShingle Elkhatim Hassan Abdelgadir
Jihad Al-Qudsi
Elham S. Abu-Nukhaa
Dimah A. Alsidrani
Subacute Toxicity and Pharmacokinetic Evaluation of the Synthetic Cannabinoid 4F-MDMB-BUTINACA in Rats: A Forensic and Toxicological Perspective
Future Pharmacology
4F-MDMB-BUTINACA toxicity
synthetic cannabinoid pharmacokinetics
rat model drug study
GC–MS/MS analysis
hematological and biochemical changes
histopathological examination
title Subacute Toxicity and Pharmacokinetic Evaluation of the Synthetic Cannabinoid 4F-MDMB-BUTINACA in Rats: A Forensic and Toxicological Perspective
title_full Subacute Toxicity and Pharmacokinetic Evaluation of the Synthetic Cannabinoid 4F-MDMB-BUTINACA in Rats: A Forensic and Toxicological Perspective
title_fullStr Subacute Toxicity and Pharmacokinetic Evaluation of the Synthetic Cannabinoid 4F-MDMB-BUTINACA in Rats: A Forensic and Toxicological Perspective
title_full_unstemmed Subacute Toxicity and Pharmacokinetic Evaluation of the Synthetic Cannabinoid 4F-MDMB-BUTINACA in Rats: A Forensic and Toxicological Perspective
title_short Subacute Toxicity and Pharmacokinetic Evaluation of the Synthetic Cannabinoid 4F-MDMB-BUTINACA in Rats: A Forensic and Toxicological Perspective
title_sort subacute toxicity and pharmacokinetic evaluation of the synthetic cannabinoid 4f mdmb butinaca in rats a forensic and toxicological perspective
topic 4F-MDMB-BUTINACA toxicity
synthetic cannabinoid pharmacokinetics
rat model drug study
GC–MS/MS analysis
hematological and biochemical changes
histopathological examination
url https://www.mdpi.com/2673-9879/4/4/36
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