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StatPearls, LLC

  • Analgesics, Opioid
  • Naloxone
  • Naltrexone
  • Narcotic Antagonists
  • Opioid-Related Disorders

Opioid Antagonists

Opioid antagonists act by competitively binding to opioid receptors in the central and peripheral nervous systems without activating them, effectively blocking the effects of opioid agonists. These agents, including naloxone, naltrexone, methylnaltrexone, and nalmefene, target mu ( ), kappa ( ), and delta ( ) receptors to reverse opioid effects, manage opioid and alcohol use disorders, and alleviate opioid-induced constipation. This course reviews opioid antagonists, focusing on their pharmacology, clinical applications, administration protocols, and safety considerations. Participants will gain insight into the mechanisms of key agents like naloxone, naltrexone, and methylnaltrexone, and their vital roles in reversing opioid overdose, managing opioid use disorder, and mitigating opioid-induced adverse effects. Advances in molecular pharmacology that inform the design of next-generation antagonists with improved safety and efficacy are also discussed. Peripherally acting -opioid receptor antagonists (PAMORAs) have also been discussed for the treatment of opioid induced constipation. This course explores precipitated withdrawal, adverse effects, and current federal policies impacting opioid addiction treatment, as well as the selection of appropriate antagonists, optimizing dosing and monitoring strategies, and implementation of patient-centered protocols to prevent overdose and manage withdrawal safely. Community naloxone distribution efforts, legislative protections, and the implications of the Mainstreaming Addiction Treatment Act, which broadens access to buprenorphine for opioid use disorder treatment, are also emphasized. This activity for healthcare professionals is designed to enhance the learner’s competence in integrating opioid antagonists into clinical management, adhering to current opioid guidelines, and implementing an appropriate interprofessional approach in patients receiving opioid antagonist therapy to address the opioid crisis effectively…

Credit & MOC Details

Credit information is provided by the course provider. We recommend confirming credit eligibility with the provider or your licensing board before starting the activity.

Credit types

AAPA Category 1 Credit™Up to 2 creditsAMA PRA Category 1 Credit™Up to 2 creditsNursingUp to 2 creditsPharmacyUp to 2 credits

MOC types

ABS — Accredited CMEUp to 2 pointsABOS — Accredited CMEUp to 2 pointsABPATH — Lifelong LearningUp to 2 pointsABA — Lifelong LearningUp to 2 pointsABTS — Accredited CMEUp to 2 pointsABIM — Medical KnowledgeUp to 2 pointsABS — Self-AssessmentUp to 2 pointsABP — Lifelong Learning and Self-AssessmentUp to 2 pointsABOHNS — Self-AssessmentUp to 2 pointsABTS — Self-AssessmentUp to 2 pointsABIM — Patient SafetyUp to 2 pointsABOHNS — Patient SafetyUp to 2 pointsABA — Patient SafetyUp to 2 pointsABTS — Patient SafetyUp to 2 points

FDA REMS

No

Qualifies for MIPS

No

Target Specialties

Cross-Specialty

Relevant across 11 specialties.

Pricing

Fee varies

This provider typically $49–98

See fees on statpearls.com

Listed by the provider

  • Article / monograph / reference
  • Credit · Up to 2 credits
  • MOC · Up to 2 points
  • Fee varies · this provider typically $49–98
  • Released
    Sep 1, 2026
  • Last day to claim credit
    Sep 1, 2029 3 years left

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