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Prolonged blockade of opioid effect with oral nalmefene
Author(s) -
Gal Thomas J,
DiFazio Cosmo A,
Dixon Ross
Publication year - 1986
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1986.220
Subject(s) - nalmefene , medicine , opioid , anesthesia , placebo , fentanyl , clinical pharmacology , pharmacology , alprazolam , bioavailability , terbutaline , naltrexone , asthma , receptor , anxiety , alternative medicine , pathology , psychiatry
In a placebo‐controlled, double‐blind study we evaluated the ability of a single 50 mg oral dose of nalmefene to block the effects of intravenous opioid challenge (2 µg/kg fentanyl). Fentanyl‐induced respiratory depression (CO 2 responsiveness), analgesia (tourniquet ischemia), and subjective effects were totally blocked for 48 hours and showed only minimal breakthrough 72 hours after nalmefene. Plasma concentration‐time data for nalmefene indicate good oral bioavailability and a prolonged terminal elimination phase (mean t 1/2 11.1 hours). These findings suggest that nalmefene could provide prolonged effectiveness in limiting emergence of opioid effects during addiction therapy. Clinical Pharmacology and Therapeutics (1986) 40, 537–542; doi: 10.1038/clpt.1986.220