Opioid antagonism in humans: a primer on optimal dose and timing for central mu-opioid receptor blockade.

ABSTRACT: Non-human animal studies outline precise mechanisms of central mu-opioid regulation of pain, stress, affiliation and reward processing. In humans, pharmacological blockade with non-selective opioid antagonists such as naloxone and naltrexone is typically used to assess involvement of the mu-opioid system in such processing. However, robust estimates of the opioid receptor blockade achieved by opioid antagonists are missing. Dose and timing schedules are highly variable and often based on single studies. Here, we provide a detailed analysis of central opioid receptor blockade after opioid antagonism based on existing positron emission tomography data. We also create models for estimating opioid receptor blockade with intravenous naloxone and oral naltrexone. We find that common doses of int

SUBMITTER: Trostheim M 

PROVIDER: S-EPMC7613944 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature