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• Nalmefene abstract "Nalmefene (trade name Selincro), originally known as nalmetrene, is an opioid receptor antagonist developed in the early 1970s, and used primarily in the management of alcohol dependence, and also has been investigated for the treatment of other addictions such as pathological gambling and addiction to shopping.Nalmefene is an opiate derivative similar in both structure and activity to the opiate antagonist naltrexone. Advantages of nalmefene relative to naltrexone include longer half-life, greater oral bioavailability and no observed dose-dependent liver toxicity. As with other drugs of this type, nalmefene can precipitate acute withdrawal symptoms in patients who are dependent on opioid drugs, or more rarely when used post-operatively to counteract the effects of strong opioids used in surgery.Nalmefene differs from naltrexone by substitution of the ketone group at the 6-position of naltrexone with a methylene group (CH2), which considerably increases binding affinity to the μ-opioid receptor. Nalmefene also has high affinity for the other opioid receptors, and is known as a "universal antagonist" for its ability to block all three.In clinical trials using this drug, doses used for treating alcoholism were in the range of 20–80 mg per day, orally.The doses tested for treating pathological gambling were between 25–100 mg per day.In both trials, there was little difference in efficacy between the lower and higher dosage regimes, and the lower dose (20 and 25 mg, respectively) was the best tolerated, with similar therapeutic efficacy to the higher doses and less side effects. Nalmefene is thus around twice as potent as naltrexone when used for the treatment of addictions.Intravenous doses of nalmefene at between 0.5 to 1 milligram have been shown effective at counteracting the respiratory depression produced by opiate overdose, although this is not the usual application for this drug as naloxone is less expensive.Doses of nalmefene greater than 1.5 mg do not appear to give any greater benefit in this application. Nalmefene's longer half-life might however make it useful for treating overdose involving longer acting opioids such as methadone, as it would require less frequent dosing and hence reduce the likelihood of renarcotization as the antagonist wears off.Nalmefene is extensively metabolised in the liver, mainly by conjugation with glucuronic acid and also by N-dealkylation. Less than 5% of the dose is excreted unchanged. The glucuronide metabolite is entirely inactive, while the N-dealkylated metabolite has minimal pharmacological activity.Lundbeck has licensed the drug from Biotie Therapies and performed clinical trials with nalmefene for treatment of alcohol-dependence.In 2011 they submitted an application for their drug termed Selincro to the European Medicines Agency.It has not been available on the US market since at least August 2008.[citation needed]".
• Nalmefene atcPrefix "N07".
• Nalmefene atcSuffix "BB05".
• Nalmefene casNumber "55096-26-9".
• Nalmefene casSupplemental "(HCl)".
• Nalmefene fdaUniiCode "TOV02TDP9I".
• Nalmefene iupacName "17-cyclopropylmethyl-4,5α-epoxy-6-methylenemorphinan-3,14-diol".
• Nalmefene pubchem "5284594".
• Nalmefene thumbnail Nalmefene_sceletal.svg?width=300.
• Nalmefene wikiPageID "8311052".
• Nalmefene wikiPageRevisionID "592611271".
• Nalmefene atcPrefix "N07".
• Nalmefene atcSuffix "BB05".
• Nalmefene c "21".
• Nalmefene casNumber "55096".
• Nalmefene chembl "982".
• Nalmefene chemspiderid "4447642".
• Nalmefene eliminationHalfLife "18720.0".
• Nalmefene excretion "renal".
• Nalmefene h "25".
• Nalmefene hasPhotoCollection Nalmefene.
• Nalmefene inchi "1".
• Nalmefene inchikey "WJBLNOPPDWQMCH-MBPVOVBZBG".
• Nalmefene iupacName "17".
• Nalmefene legalStatus "Prescription Only Medicine".
• Nalmefene medlineplus "a605043".
• Nalmefene metabolism "hepatic".
• Nalmefene molecularWeight "375.9".
• Nalmefene n "1".
• Nalmefene o "3".
• Nalmefene proteinBound "45.0".
• Nalmefene pubchem "5284594".
• Nalmefene routesOfAdministration "Oral, Intravenous".
• Nalmefene smiles "OC=CC=C2C[C@@H][C@]3CCC5=C".
• Nalmefene stdinchi "1".
• Nalmefene stdinchikey "WJBLNOPPDWQMCH-MBPVOVBZSA-N".
• Nalmefene tradename "Selincro".
• Nalmefene unii "TOV02TDP9I".
• Nalmefene verifiedfields "changed".
• Nalmefene verifiedrevid "462258343".
• Nalmefene watchedfields "changed".
• Nalmefene width "240".
• Nalmefene subject Category:Alcohols.
• Nalmefene subject Category:Alkenes.
• Nalmefene subject Category:Morphinans.
• Nalmefene subject Category:Phenols.
• Nalmefene subject Category:Semisynthetic_opioids.
• Nalmefene type Abstraction100002137.
• Nalmefene type Agent114778436.
• Nalmefene type Alcohol107884567.
• Nalmefene type Alcohols.
• Nalmefene type AliphaticCompound114601294.
• Nalmefene type Alkene114713120.
• Nalmefene type Alkenes.
• Nalmefene type Beverage107881800.
• Nalmefene type CausalAgent100007347.
• Nalmefene type Chemical114806838.
• Nalmefene type Compound114818238.
• Nalmefene type Drug103247620.
• Nalmefene type DrugOfAbuse103248958.
• Nalmefene type Fluid114939900.
• Nalmefene type Food100021265.
• Nalmefene type Liquid114940386.
• Nalmefene type Material114580897.
• Nalmefene type Matter100020827.
• Nalmefene type OrganicCompound114727670.
• Nalmefene type Part113809207.
• Nalmefene type Phenol114989545.
• Nalmefene type Phenols.
• Nalmefene type PhysicalEntity100001930.
• Nalmefene type Relation100031921.
• Nalmefene type Substance100019613.
• Nalmefene type Substance100020090.
• Nalmefene type Drug.
• Nalmefene type DrugProduct.
• Nalmefene type FunctionalSubstance.
• Nalmefene comment "Nalmefene (trade name Selincro), originally known as nalmetrene, is an opioid receptor antagonist developed in the early 1970s, and used primarily in the management of alcohol dependence, and also has been investigated for the treatment of other addictions such as pathological gambling and addiction to shopping.Nalmefene is an opiate derivative similar in both structure and activity to the opiate antagonist naltrexone.".
• Nalmefene label "Nalmefen".
• Nalmefene label "Nalmefen".
• Nalmefene label "Nalmefene".
• Nalmefene label "Nalméfène".
• Nalmefene sameAs Nalmefen.
• Nalmefene sameAs Nalmefen.
• Nalmefene sameAs Nalméfène.
• Nalmefene sameAs Nalmefen.
• Nalmefene sameAs m.026zykt.
• Nalmefene sameAs Q4353252.
• Nalmefene sameAs Q4353252.
• Nalmefene sameAs nalmefene.
• Nalmefene sameAs Nalmefene.
• Nalmefene wasDerivedFrom Nalmefene?oldid=592611271.
• Nalmefene depiction Nalmefene_sceletal.svg.
• Nalmefene isPrimaryTopicOf Nalmefene.