| pubmed-article:15956985 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:15956985 | lifeskim:mentions | umls-concept:C0066908 | lld:lifeskim |
| pubmed-article:15956985 | lifeskim:mentions | umls-concept:C0205341 | lld:lifeskim |
| pubmed-article:15956985 | lifeskim:mentions | umls-concept:C0068377 | lld:lifeskim |
| pubmed-article:15956985 | lifeskim:mentions | umls-concept:C0439590 | lld:lifeskim |
| pubmed-article:15956985 | lifeskim:mentions | umls-concept:C0205099 | lld:lifeskim |
| pubmed-article:15956985 | lifeskim:mentions | umls-concept:C0205171 | lld:lifeskim |
| pubmed-article:15956985 | lifeskim:mentions | umls-concept:C2827063 | lld:lifeskim |
| pubmed-article:15956985 | pubmed:issue | 12 | lld:pubmed |
| pubmed-article:15956985 | pubmed:dateCreated | 2005-11-18 | lld:pubmed |
| pubmed-article:15956985 | pubmed:abstractText | 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, orally). Pharmacokinetics and mu-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 dosings, and pharmacokinetic parameters for nalmefene and main metabolites were determined. Central mu-opioid receptor occupancy of nalmefene was measured with positron emission tomography (PET) and [(11)C]carfentanil at four time points (3, 26, 50, 74 h) after both dosings. Nalmefene was rapidly absorbed in all subjects. The mean t(1/2) of nalmefene was 13.4 h after single and repeated dosing. The accumulation of nalmefene and its main metabolites in plasma during the repeated dosing period was as expected for a drug with linear pharmacokinetics, and steady-state was reached for all analytes. Both nalmefene dosings resulted in a very high occupancy at mu-opioid receptors (87-100%), and the decline in the occupancy was similar after both dosings but clearly slower than the decline in the plasma concentration of nalmefene or metabolites. High nalmefene occupancy (83-100%) persisted at 26 h after the dosings. The prolonged mu-opioid receptor occupancy by nalmefene indicates slow dissociation of the drug from mu-opioid receptors. These results support the rational of administering nalmefene when needed before alcohol drinking, and they additionally suggest that a high mu-opioid receptor occupancy can be maintained when nalmefene is taken once daily. | lld:pubmed |
| pubmed-article:15956985 | pubmed:language | eng | lld:pubmed |
| pubmed-article:15956985 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15956985 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:15956985 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15956985 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15956985 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15956985 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15956985 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15956985 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15956985 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15956985 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15956985 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:15956985 | pubmed:month | Dec | lld:pubmed |
| pubmed-article:15956985 | pubmed:issn | 0893-133X | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:HietalaJarmoJ | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:ScheininHarry... | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:NågrenKjellK | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:HagelbergNora... | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:OikonenVesaV | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:AaltoSargoS | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:IngmanKimmoK | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:KallioAnteroA | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:KarhuvaaraSak... | lld:pubmed |
| pubmed-article:15956985 | pubmed:author | pubmed-author:JuhakoskiAuni... | lld:pubmed |
| pubmed-article:15956985 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:15956985 | pubmed:volume | 30 | lld:pubmed |
| pubmed-article:15956985 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:15956985 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:15956985 | pubmed:pagination | 2245-53 | lld:pubmed |
| pubmed-article:15956985 | pubmed:dateRevised | 2011-5-18 | lld:pubmed |
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| pubmed-article:15956985 | pubmed:meshHeading | pubmed-meshheading:15956985... | lld:pubmed |
| pubmed-article:15956985 | pubmed:year | 2005 | lld:pubmed |
| pubmed-article:15956985 | pubmed:articleTitle | Prolonged central mu-opioid receptor occupancy after single and repeated nalmefene dosing. | lld:pubmed |
| pubmed-article:15956985 | pubmed:affiliation | Clinical Research Services Turku (CRST), University of Turku, FIN-20521 Turku, Finland. | lld:pubmed |
| pubmed-article:15956985 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:15956985 | pubmed:publicationType | Clinical Trial | lld:pubmed |
| pubmed-article:15956985 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:15956985 | lld:pubmed |
