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Opioid Antagonists |
Credits: 1.25 Post-Assessment Questions: 8
Release Date: 5 Oct 2020
Expiration Date: 27 Jul 2021
Last Reviewed: 27 Jul 2020
Estimated Time To Finish: 75 Minutes
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Opioid receptor antagonists block one or more of the opioid receptors in the central or peripheral nervous system. Opioid receptors are specific transmembrane neurotransmitter receptors that couple G-proteins, which upon stimulation by endogenous or exogenous opioids, leading to the intracellular process of signal transduction. The two most commonly used centrally acting opioid receptor antagonists are naloxone and naltrexone. Naloxone comes in intravenous, intramuscular and intranasal formulations, and is FDA-approved for the use in an opioid overdose, and the reversal of respiratory depression associated with opioid use. Naltrexone is available in both oral and long-acting injectable formulations and is FDA-approved for the treatment of opioid, and/or alcohol maintenance treatment. The most commonly used peripheral opioid receptor antagonist is methylnaltrexone, which is a potent competitive antagonist acting at the digestive tract and is also FDA-approved for the treatment of opioid-induced constipation. This activity outlines the indications, mechanism of action, methods of administration, important adverse effects, contraindications, monitoring, and toxicity of opioid antagonists, so providers can direct patient therapy to optimal outcomes to combat opioid overdose, misuse, or adverse effects.
This activity has been designed to meet the educational needs of physicians.
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Authors: Jonathan Theriot, Sarah Sabir
Editors: Mohammadreza Azadfard
Editors-In-Chief: Gregory PlaugherMark Pellegrini
Chief Medical Reviewer: Mark Pellegrini
Nurse Planner/Reviewer/Editor: Lisa Haddad
Nurse Planner/Reviewer/Editor: Bernadette Makar
Nurse Planner/Reviewer/Editor: Dorothy Caputo
Pharmacy Planner/Reviewer/Editor: Mark Pellegrini
Physician Planner/Reviewer/Editor: Scott Dulebohn
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Quillen College of Medicine, East Tennessee State University designates this activity for a maximum of 1.25 AMA PRA Category 1 CreditsTM. Physicians should only claim credit commensurate with the extent of their participation in the activity.
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