Naloxone for the Reversal of Opioid Adverse Effects

Marcia L. Buck, PharmD, FCCP


Pediatr Pharm. 2002;8(8) 

In This Article

Mechanism of Action

Naloxone is a pure opioid antagonist. It prevents or reverses the effects of opioids, including respiratory depression, sedation, and hypotension, by direct competition at mu, kappa, and sigma opioid receptor binding sites. Naloxone reverses both exogenous and endogenous opioids (endorphins, enkephalins, and dynorphins). It has no agonist properties; and, in the absence of opioids, naloxone exhibits little significant pharmacologic activity.[1,2,3]


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