Literature DB >> 3533370

Prolonged blockade of opioid effect with oral nalmefene.

T J Gal, C A DiFazio, R Dixon.   

Abstract

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 micrograms/kg fentanyl). Fentanyl-induced respiratory depression (CO2 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 t1/2 11.1 hours). These findings suggest that nalmefene could provide prolonged effectiveness in limiting emergence of opioid effects during addiction therapy.

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Year:  1986        PMID: 3533370     DOI: 10.1038/clpt.1986.220

Source DB:  PubMed          Journal:  Clin Pharmacol Ther        ISSN: 0009-9236            Impact factor:   6.875


  5 in total

1.  Who Receives Nalmefene and How Does It Work in the Real World? A Single-Arm, Phase IV Study of Nalmefene in Alcohol Dependent Outpatients: Baseline and 1-Month Results.

Authors:  Pablo Barrio; Lluisa Ortega; Josep Guardia; Carlos Roncero; Lara Yuguero; Antoni Gual
Journal:  Clin Drug Investig       Date:  2018-02       Impact factor: 2.859

Review 2.  [Nalmefene: a novel pharmacotherapeutic option for alcoholism].

Authors:  M Soyka
Journal:  Nervenarzt       Date:  2014-05       Impact factor: 1.214

3.  Effects of opioid receptor gene variation on targeted nalmefene treatment in heavy drinkers.

Authors:  Albert J Arias; Stephen Armeli; Joel Gelernter; Jonathan Covault; Antero Kallio; Sakari Karhuvaara; Tiina Koivisto; Rauno Mäkelä; Henry R Kranzler
Journal:  Alcohol Clin Exp Res       Date:  2008-07       Impact factor: 3.455

4.  Opioid peptides and primary biliary cirrhosis.

Authors:  J R Thornton; M S Losowsky
Journal:  BMJ       Date:  1988-12-10

Review 5.  Opioid antagonists in the treatment of alcohol dependence.

Authors:  G O'Leary; J Borrow; R D Weiss
Journal:  Curr Psychiatry Rep       Date:  2001-12       Impact factor: 8.081

  5 in total

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