Continuing Education Activity
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.
- Identify the mechanism of action of various opioid antagonist medications.
- Summarize the different indications for the various opioid antagonist agents.
- Review the adverse event profile of opioid antagonists.
- Outline the importance of collaboration and communication among interprofessional team members to improve outcomes and treatment efficacy for patients who might benefit from therapy with opioid antagonists, especially in light of the ongoing opioid crisis.