Naloxone + Naltrexone

Naloxone + naltrexone is a combination of two opioid receptor antagonists, both of which act primarily at the μ-opioid receptor. Naloxone is used for the rapid reversal of opioid overdose by displacing opioids from their receptors and reversing life-threatening central nervous system and respiratory depression. It has a short half-life, often necessitating repeated dosing in cases of long-lasting opioids. Naltrexone is also a pure opioid antagonist with high affinity for μ-opioid receptors and some activity at κ and δ receptors; it blocks the effects of endogenous and exogenous opioids, reducing euphoria, cravings, and other subjective effects associated with opioid or alcohol use. When combined, these agents may extend the window for effective intervention after an overdose by providing both immediate (naloxone) and sustained (naltrexone) antagonism[1][2][3][5][6]. This combination has been studied in phase 1 trials to assess pharmacokinetics when administered intranasally[1].

Brand names

Evzio

Other names

none