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Review
. 2021 Aug;46(4):861-866.
doi: 10.1111/jcpt.13320. Epub 2021 Apr 28.

Are opioid receptor antagonists adequate for "Opioid" overdose in a changing reality?

John F Peppin  1   2 , Joseph V Pergolizzi Jr  3   4   5 , Albert Dahan  6 , Robert B Raffa  3   4   7   8
Affiliations
Review

Are opioid receptor antagonists adequate for "Opioid" overdose in a changing reality?

John F Peppin et al. J Clin Pharm Ther. 2021 Aug.

Abstract

What is known and objective: Deaths due to opioid-induced respiratory depression (OIRD) continue to rise despite intense regulatory and professional actions. COVID-19 has only worsened this situation.1 An opioid receptor antagonist (ORA) such as naloxone is the most common intervention for OIRD. However, with increasing overdose from highly potent illicit opioids and polysubstance abuse, appraisal of the adequacy of ORA seems warranted and timely.

Comment: OIRD results from the binding of an excess number of agonist molecules to opioid receptors. Mechanistically, it makes sense to reverse this by displacing agonist molecules by administering an ORA. But realistically, the trend to higher-potency agonists and polysubstance abuse diminishes the effectiveness of this approach. We are left facing a crisis without a solution.

What is new and conclusion: For the increasingly common OIRD from highly potent illicit agonists and polysubstance overdose, ORAs are correspondingly less effective. Alternatives are needed-soon.

Keywords: adverse effect; naloxone; opioid antagonist; opioid overdose; polysubstance use.

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References

REFERENCES

    1. Kamp J, Campo-Flores A.The Opioid Crisis, Already Serious, Has Intensified During Coronavirus Pandemic. Wall Street Journal. Accessed October 28, 2020.
    1. Niles JK, Gudin J, Radcliff J, Kaufman HW. The Opioid Epidemic Within the COVID-19 Pandemic: Drug Testing in 2020. Popul Health Manag. 2021;24(S1):S-43.
    1. Azzam AAH, McDonald J, Lambert DG. Hot topics in opioid pharmacology: mixed and biased opioids. Br J Anaesth. 2019;122(6):e136-e145.
    1. Boyer EW. Management of opioid analgesic overdose. N Engl J Med. 2012;367(2):146-155.
    1. Valentino RJ, Volkow ND. Untangling the complexity of opioid receptor function. Neuropsychopharmacology. 2018;43(13):2514-2520.

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