Historical perspectives and emerging trends in fentanyl use: Part 1 – Pharmacological profile

Fentanyl, a potent synthetic opioid, is widely used for severe pain management and anesthesia but poses significant risks due to its extreme potency and addictive potential. It acts primarily on μ-opioid receptors, with additional effects on κ- and δ-receptors, producing analgesia and adverse effect...

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Main Authors: Stanila Stoeva-Grigorova, Maya Radeva-Ilieva, Nadezhda Karkkeselyan, Stela Dragomanova, Gabriela Kehayova, Simeonka Dimitrova, Maria Petrova, Snezha Zlateva, Petko Marinov
Format: Article
Language:English
Published: Pensoft Publishers 2025-06-01
Series:Pharmacia
Online Access:https://pharmacia.pensoft.net/article/149206/download/pdf/
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author Stanila Stoeva-Grigorova
Maya Radeva-Ilieva
Nadezhda Karkkeselyan
Stela Dragomanova
Gabriela Kehayova
Simeonka Dimitrova
Maria Petrova
Snezha Zlateva
Petko Marinov
author_facet Stanila Stoeva-Grigorova
Maya Radeva-Ilieva
Nadezhda Karkkeselyan
Stela Dragomanova
Gabriela Kehayova
Simeonka Dimitrova
Maria Petrova
Snezha Zlateva
Petko Marinov
author_sort Stanila Stoeva-Grigorova
collection DOAJ
description Fentanyl, a potent synthetic opioid, is widely used for severe pain management and anesthesia but poses significant risks due to its extreme potency and addictive potential. It acts primarily on μ-opioid receptors, with additional effects on κ- and δ-receptors, producing analgesia and adverse effects, such as respiratory depression, mediated via G-protein and β-arrestin signaling pathways. Fentanyl’s pharmacokinetics include rapid onset and a short duration, with extensive liver metabolism via CYP3A4 enzymes. Its high lipophilicity allows it to cross the blood-brain barrier quickly, contributing to its rapid central nervous system effects and associated risk of respiratory depression. Despite its therapeutic value, fentanyl’s potential to induce tolerance and dependence, coupled with escalating illicit use, underscores the need for enhanced prevention strategies, improved overdose management, and stricter regulatory measures to balance therapeutic utility with abuse prevention.
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institution Kabale University
issn 2603-557X
language English
publishDate 2025-06-01
publisher Pensoft Publishers
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series Pharmacia
spelling doaj-art-822d57fa6e4d42c3ad1d0c75f61fe2d12025-08-20T03:45:30ZengPensoft PublishersPharmacia2603-557X2025-06-01721910.3897/pharmacia.72.e149206149206Historical perspectives and emerging trends in fentanyl use: Part 1 – Pharmacological profileStanila Stoeva-Grigorova0Maya Radeva-Ilieva1Nadezhda Karkkeselyan2Stela Dragomanova3Gabriela Kehayova4Simeonka Dimitrova5Maria Petrova6Snezha Zlateva7Petko Marinov8Medical UniversityMedical UniversityMedical UniversityMedical UniversityMedical UniversityMedical UniversityMedical UniversityMedical UniversityMedical UniversityFentanyl, a potent synthetic opioid, is widely used for severe pain management and anesthesia but poses significant risks due to its extreme potency and addictive potential. It acts primarily on μ-opioid receptors, with additional effects on κ- and δ-receptors, producing analgesia and adverse effects, such as respiratory depression, mediated via G-protein and β-arrestin signaling pathways. Fentanyl’s pharmacokinetics include rapid onset and a short duration, with extensive liver metabolism via CYP3A4 enzymes. Its high lipophilicity allows it to cross the blood-brain barrier quickly, contributing to its rapid central nervous system effects and associated risk of respiratory depression. Despite its therapeutic value, fentanyl’s potential to induce tolerance and dependence, coupled with escalating illicit use, underscores the need for enhanced prevention strategies, improved overdose management, and stricter regulatory measures to balance therapeutic utility with abuse prevention.https://pharmacia.pensoft.net/article/149206/download/pdf/
spellingShingle Stanila Stoeva-Grigorova
Maya Radeva-Ilieva
Nadezhda Karkkeselyan
Stela Dragomanova
Gabriela Kehayova
Simeonka Dimitrova
Maria Petrova
Snezha Zlateva
Petko Marinov
Historical perspectives and emerging trends in fentanyl use: Part 1 – Pharmacological profile
Pharmacia
title Historical perspectives and emerging trends in fentanyl use: Part 1 – Pharmacological profile
title_full Historical perspectives and emerging trends in fentanyl use: Part 1 – Pharmacological profile
title_fullStr Historical perspectives and emerging trends in fentanyl use: Part 1 – Pharmacological profile
title_full_unstemmed Historical perspectives and emerging trends in fentanyl use: Part 1 – Pharmacological profile
title_short Historical perspectives and emerging trends in fentanyl use: Part 1 – Pharmacological profile
title_sort historical perspectives and emerging trends in fentanyl use part 1 pharmacological profile
url https://pharmacia.pensoft.net/article/149206/download/pdf/
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