Opioid Antagonists

In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan.


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, lead 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 use in 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 to treat opioid and/or alcohol maintenance treatment. The most commonly used peripheral opioid receptor antagonist is methylnaltrexone, which is a potent competitive antagonist acting in 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.

Publication types

  • Study Guide