Opioid Reversal Agents and Their Effectiveness
Explore the different opioid reversal agents available, such as Naloxone, Naltrexone, and Nalmefene, and understand their mechanisms of action, effectiveness, and implications for overdose management. Learn about the differences between Naloxone and Nalmefene in terms of bioavailability, half-life, and observation time to make informed decisions in emergency situations. Gain insights into the preferred treatment options for Alcohol Use Disorder (AUD) based on effectiveness. Additionally, discover key references and studies providing valuable information on opioid overdose reversal strategies.
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Presentation Transcript
Click to edit Master title style Opioid Reversal Agents James B. Shuler, DO, MS, FACOEP, FAWM, FASAM 1
Click to edit Master title style For opioid overdose, there is only one goal of opioid reversal: Return of spontaneous respirations 2 2
Click to edit Master title style Available Agents Naloxone IV, IM, Long-acting IM, Intranasal spray Naltrexone Oral NOT used acutely/for overdose Nalmefene IM, IV, SQ, Oral, Intranasal spray 3 3
Click to edit Master title style Naloxone vs. Nalmefene Intranasal Naloxone Mu-antagonist, also other opioid receptors 4 and 8mg single-dose devices About 45% bioavailable, half-life, ~2 hours Shorter observation time, less resources Nalmefene Mu-antagonist, also other opioid receptors 2.7mg single-dose device About 40% bioavailable, half-life, ~12.5 hours Longer observation time, more resources 4 4
Click to edit Master title style Naloxone vs. Nalmefene Intranasal NEITHER is more effective than the other, Nalmefene just lasts ~6X longer If some is good, more is not better In studies, the higher dose (naltrexone) is not associated with better outcomes, it is associated with more agitation, combativeness and rage Precipitated withdrawal is strongly associated with leaving the ED/medical care AMA/without treatment 5 5
Click to edit Master title style With respect to AUD treatment effectiveness: Injectable naltrexone>oral nalmefene>oral naltrexone 6 6
Click to edit Master title style Questions? References available 7
Click to edit Master title style REFERENCES Ther Adv Drug Saf. 2018 Jan; 9(1): 63 88. Published online 2017 Dec 13. doi: 10.1177/2042098617744161 Medscape Medical News Fulton, R. Higher Dose of Naloxone Has No Impact on Overdose Survival; Increases Withdrawal Symptoms. February 12, 2024, reporting on NY State CDC Morbidity and Mortality Report. Int J of Drug Policy. Parkin et. Al., Overdose reversals using naloxone in New York City by people who use opioids: Implications for public health and overdose harm reduction approaches from a qualitative study, May 2020 8 8
