Nalmefene for treatment of alcohol dependence.

IMPORTANCE OF THE FIELD: Alcohol use and dependence are frequent disorders. Despite numerous established psychosocial approaches, relapse to heavy drinking is common in alcohol-dependent patients after detoxification and relapse prevention remains a significant medical challenge. AREAS COVERED IN THIS REVIEW: The opioidergic system plays a crucial role in mediating the rewarding effects of alcohol, in part by modulating dopaminergic neurotransmission in mesolimbic brain areas. This review will discuss the neurochemical basis of alcoholism with respect to the opiodergic system. Nalmefene is an alternate opioid receptor that also targets the kappa opioid receptors and thus offers a different treatment approach. The treatment studies conducted so far are discussed. WHAT THE READER WILL GAIN: We present a comprehensive overview of the implication of the opioidergic system in mediating the rewarding effects of alcoholism and the preclinical and clinical studies conducted so far with nalmefene. TAKE HOME MESSAGE: Although the number of clinical studies conducted with naltrexone by far exceeds the number conducted with nalmefene, the four studies on nalmefene published so far may indicate a role of this opioid antagonist in the treatment of alcoholism. Results of some ongoing studies on nalmefene will provide additional data on its use for this indication.