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

@article{Ingman2005ProlongedC,
  title={Prolonged Central $\mu$-Opioid Receptor Occupancy after Single and Repeated Nalmefene Dosing},
  author={Kimmo Ingman and Nora Hagelberg and Sargo Aalto and Kjell N{\aa}gren and Auni Juhakoski and Sakari Karhuvaara and Antero Kallio and Vesa Oikonen and Jarmo Hietala and Harry Scheinin},
  journal={Neuropsychopharmacology},
  year={2005},
  volume={30},
  pages={2245-2253}
}
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 μ-opioid receptor occupancy after a clinically effective dose (20 mg, orally). Pharmacokinetics and μ-opioid receptor occupancy of nalmefene after single and repeated dosing over 7 days was studied in 12 healthy subjects. Serial blood samples were obtained after both… 
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Continuous delivery of naltrexone and nalmefene leads to tolerance in reducing alcohol drinking and to supersensitivity of brain opioid receptors
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TLDR
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Pharmacologic and Clinical Considerations of Nalmefene, a Long Duration Opioid Antagonist, in Opioid Overdose
TLDR
Nalmefene is a pure opioid antagonist structurally similar to naltrexone that can serve as an alternative antidote for reversing respiratory depression associated with acute opioid overdose and can be pivotal in reducing healthcare costs, increasing patient satisfaction, and redistributing the time that healthcare staff spend monitoring opioid overdose patients given naloxone.
Population pharmacokinetics of nalmefene in healthy subjects and its relation to μ-opioid receptor occupancy.
TLDR
A robust population PK model for nalmefene was developed and based on the concentration-occupancy model the μ-opioid receptor occupancy after a single 20 mg dose of nalmfene is predicted to be above the target therapeutic occupancy for about 24 h in about 95% of the target population.
Targeted Opioid Receptor Antagonists in the Treatment of Alcohol Use Disorders
TLDR
The targeted or ‘as-needed’ approach to treatment with opioid antagonists is an efficacious harm-reduction strategy for problem drinking and alcohol dependence.
Comparing Nalmefene and Naltrexone in Alcohol Dependence: Are there any Differences? Results from an Indirect Meta-Analysis.
TLDR
An indirect meta-analysis of randomized controlled studies on the treatment of alcohol dependence indicates an advantage of nalmefene over naltrexone, an effective and well-tolerated medication for the reduction of alcohol consumption.
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