Overdoses due to fentanyl and its analogues (F/FAs) push naloxone to the limit.

Abstract

WHAT IS KNOWN AND OBJECTIVE:

Food and Drug Administration (FDA) risk evaluation and mitigation strategies (REMs) encourage emergency responders, paramedics, law enforcement agents, and even laypeople to be trained in the administration of naloxone with the intent of rescuing individuals from a known or suspected opioid overdose.

COMMENT:

Although naloxone is generally safe and effective at reversing respiratory depression caused by a conventional opioid such as morphine or heroin by competing with the opioid and displacing it from the μ-opioid receptor, questions increasingly are arising as to whether naloxone can adequately reverse opioid overdoses that may involve the potent opioids fentanyl and its analogues (F/FAs). In other words, as more and more opioid overdoses involve F/FAs, can naloxone keep up?

WHAT IS NEW AND CONCLUSION:

As a competitive antagonist at μ-opioid receptors, naloxone is often a life-saving agent in cases of overdose caused by conventional opioids, but it may not be versatile or powerful enough to combat the rising tide of overdoses due to fentanyl and its illicit analogues, or in cases of overdose involving combinations of opioids and non-opioids.

• Authors: Joseph V Pergolizzi Jr, Albert Dahan, Jo Ann LeQuang, Robert B Raffa
• Journal: Journal of clinical pharmacy and therapeutics (J Clin Pharm Ther) Vol. 46 Issue 6 Pg. 1501-1504 (Dec 2021) ISSN: 1365-2710 [Electronic] England
• PMID: 34111307 (Publication Type: Journal Article, Review)
• Copyright: © 2021 John Wiley & Sons Ltd.

Chemical References

• Narcotic Antagonists
• Receptors, Opioid, mu
• Naloxone
• Heroin
• Fentanyl

Topics

• Diaphragm (drug effects)
• Dose-Response Relationship, Drug
• Fentanyl (pharmacology, toxicity)
• Heroin (toxicity)
• Humans
• Laryngismus (chemically induced)
• Muscle Rigidity (chemically induced)
• Naloxone (pharmacology, therapeutic use)
• Narcotic Antagonists (pharmacology, therapeutic use)
• Opiate Overdose (drug therapy)
• Receptors, Opioid, mu (drug effects)
• Thoracic Wall (drug effects)