title: Treatment of cocaine craving with as-needed nalmefene, a partial κ opioid receptor agonist: first clinical experience.
abstract: The treatment of cocaine dependence is difficult as no approved pharmacotherapy is available as yet. However, in preclinical and clinical trials, a variety of compounds were tested for suitability as inhibitors of craving for and relapse into the use of cocaine, among these antidepressants, antiepileptics, dopamine agonists, disulfiram, and naltrexone. Nalmefene, a structural derivative of naltrexone, shares with its parent compound approval (granted by the European Medical Agency in 2013) as a medication for the treatment of alcohol addiction in the European Union. It differs from naltrexone by a higher affinity for the δ opioid-receptors and a partial agonistic affinity to the κ opioid-receptors. It should be noted that patients addicted to cocaine show a considerable increase in κ receptors in the nucleus accumbens. This report describes the case of an abstinent cocaine-addicted patient regularly afflicted with cravings for cocaine. The patient took as-needed nalmefene for 5 months whenever she developed a craving for cocaine. For most of these interventions, the patient reported an abatement of craving and could avoid relapsing into cocaine consumption. This effect may be accounted for by nalmefene acting, other than naltrexone, as a partial agonist of the κ opioid-receptors. Therefore, nalmefene might be a promising new option in the pharmacological repertoire for the treatment of cocaine addiction.
authors: aDepartment of Addictive Behavior and Addiction Medicine, Central Institute of Mental Health, University of Heidelberg/Medical Faculty Mannheim, Mannheim, Germany bDepartment of Psychiatry, Psychotherapy, and Psychosomatics, Zürich University Hospital for Psychiatry, Zürich, Switzerland.
authors: Martin
authors: M
authors: Grosshans
authors: Jochen
authors: J
authors: Mutschler
authors: Falk
authors: F
authors: Kiefer
mesh_terms: D000328:Adult; D016739:Behavior, Addictive / Q000175:diagnosis / Q000188:drug therapy* / Q000378:metabolism / Q000523:psychology; D019970:Cocaine-Related Disorders / Q000175:diagnosis / Q000188:drug therapy* / Q000378:metabolism / Q000523:psychology; D066249:Craving / Q000187:drug effects*; D054333:Drug Partial Agonism; D005260:Female; D006801:Humans; D009271:Naltrexone / Q000008:administration & dosage / Q000031:analogs & derivatives*; D009292:Narcotic Antagonists / Q000008:administration & dosage*; D017473:Receptors, Opioid, kappa / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012008:Recurrence; D013997:Time Factors; D016896:Treatment Outcome
chemical_list: D009292:Narcotic Antagonists; D017473:Receptors, Opioid, kappa; D009271:Naltrexone; C038981:nalmefene