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naltrexone (Revia)

University of North Carolina, Chapel Hill · FDA-approved active Small molecule

Naltrexone is an opioid receptor antagonist that blocks the effects of opioids and endogenous opioid peptides in the central nervous system.

Naltrexone is an opioid receptor antagonist that blocks the effects of opioids and endogenous opioid peptides in the central nervous system. Used for Opioid use disorder, Alcohol use disorder.

At a glance

Generic namenaltrexone (Revia)
SponsorUniversity of North Carolina, Chapel Hill
Drug classOpioid receptor antagonist
TargetOpioid receptors (mu, delta, kappa)
ModalitySmall molecule
Therapeutic areaPsychiatry / Addiction Medicine
PhaseFDA-approved

Mechanism of action

Naltrexone competitively binds to opioid receptors (mu, delta, and kappa) with highest affinity for mu receptors, preventing opioid agonists from activating these receptors. This mechanism is used to treat opioid use disorder by reducing cravings and blocking the rewarding effects of opioids, and also for alcohol use disorder where the exact mechanism involves modulation of endogenous opioid signaling related to reward and reinforcement.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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