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Multiple Choice

Which medication reverses opioid receptor agonism in overdose?

Reversing opioid overdose relies on a drug that can displace opioids from the receptors they’re binding to. Naloxone acts as a competitive antagonist at mu receptors (also interacts with kappa and delta to a lesser extent), so it binds the receptors with higher affinity and frees them from the opioid. This rapid displacement stops the opioid-induced CNS and respiratory depression, producing quick improvement in consciousness and breathing. Its effects come on quickly after IV dosing, but because many opioids last longer than naloxone, symptoms can return, so patients need to be monitored and may need additional doses. Other options don’t counteract opioid receptor activity: epinephrine can support blood pressure and heart rate but doesn’t block opioid receptors; glucose treats hypoglycemia; oxygen helps with hypoxia but doesn’t reverse receptor binding.

Reversing opioid overdose relies on a drug that can displace opioids from the receptors they’re binding to. Naloxone acts as a competitive antagonist at mu receptors (also interacts with kappa and delta to a lesser extent), so it binds the receptors with higher affinity and frees them from the opioid. This rapid displacement stops the opioid-induced CNS and respiratory depression, producing quick improvement in consciousness and breathing. Its effects come on quickly after IV dosing, but because many opioids last longer than naloxone, symptoms can return, so patients need to be monitored and may need additional doses. Other options don’t counteract opioid receptor activity: epinephrine can support blood pressure and heart rate but doesn’t block opioid receptors; glucose treats hypoglycemia; oxygen helps with hypoxia but doesn’t reverse receptor binding.