Prolonged Central μ-Opioid Receptor Occupancy after Single and Repeated Nalmefene Dosing

• Published in: Neuropsychopharmacology (New York, N.Y.) Vol. 30; no. 12; pp. 2245 - 2253
• Main Authors: Ingman, Kimmo, Hagelberg, Nora, Aalto, Sargo, Någren, Kjell, Juhakoski, Auni, Karhuvaara, Sakari, Kallio, Antero, Oikonen, Vesa, Hietala, Jarmo, Scheinin, Harry
• Format: Journal Article
• Language: English
• Published: New York, NY Nature Publishing 01.12.2005
• Subjects: Adolescent; Adult; Alcoholism and acute alcohol poisoning; Analgesics, Opioid - pharmacokinetics; Area Under Curve; Biological and medical sciences; Caudate Nucleus - metabolism; Electrocardiography - drug effects; Fentanyl - analogs & derivatives; Fentanyl - pharmacokinetics; Glucuronides - metabolism; Humans; Male; Medical sciences; Naltrexone - analogs & derivatives; Naltrexone - pharmacokinetics; Narcotic Antagonists - pharmacokinetics; Positron-Emission Tomography; Prefrontal Cortex - metabolism; Receptors, Opioid, mu - drug effects; Thalamus - metabolism; Toxicology; Morphinan derivatives; Alcoholism; μ Opioid receptor; Opiates; Neuroprotective agent; Antagonist; Nalmefene; Opioid peptide; opioid antagonists; μ-opioid receptor; Prolonged

The opioid antagonist nalmefene offers an alternative to traditional pharmacological treatments for alcoholism. The present study was designed to investigate the relationship between nalmefene plasma concentration and central mu-opioid receptor occupancy after a clinically effective dose (20 mg, ora...