Naltrexone - Mechanism of Action

Mechanism of Action

Naltrexone and its active metabolite 6-β-naltrexol are competitive antagonists at μ- and κ-opioid receptors, and to a lesser extent at δ-opioid receptors. The plasma half-life of naltrexone is about 4 h, for 6-β-naltrexol 13 h. The blockade of opioid receptors is the basis behind its action in the management of opioid dependence—it reversibly blocks or attenuates the effects of opioids.

Its use in alcohol (ethanol) dependence has been studied and has been shown to be effective. Its mechanism of action in this indication is not fully understood, but as an opioid-receptor antagonist is likely to be due to the modulation of the dopaminergic mesolimbic pathway which is hypothesized to be a major center of the reward associated with addiction (being one of the primary centers for risk-reward analysis in the brain, and a tertiary "pleasure center") that all major drugs of abuse are believed to activate.

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