Nalmefene is a modulator of the endogenic opioid system acting as competitive antagonist at receptors and partial agonist at receptors with predominant affinity to the receptors. It belongs to agents suppressing well-documented changes in the brain opioid system associated with repeated effects of alcohol.
This review provides an overview of both preclinical and clinical evidence suggesting: a) an important role of the brain opioid system in development of alcoholism; b) a prospective use of nalmefene suppressing craving to reduce alcohol consumption and thus in pharmacotherapy of alcoholism.