Nalmefene
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| Clinical data | |
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| Trade names | Selincro |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605043 |
| Routes of administration |
Oral, Intravenous |
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| Pharmacokinetic data | |
| Protein binding | 45% |
| Metabolism | hepatic |
| Biological half-life | 10.8 ± 5.2 hours |
| Excretion | renal |
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| ChEMBL | |
| ECHA InfoCard | 100.164.948 |
| Chemical and physical data | |
| Formula | C21H25NO3 |
| Molar mass | 339.43 g/mol |
| 3D model (Jmol) | |
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Nalmefene (trade name Selincro), originally known as nalmetrene, is an opioid antagonist developed in the early 1970s, used primarily in the management of alcohol dependence. It has also been investigated for the treatment of other addictions such as pathological gambling.
Nalmefene is an opiate derivative similar in both structure and activity to the opioid 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.
Intravenous doses of nalmefene 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 greater than 1.5 mg do not appear to give any greater benefit in this application. The half-life of nalmefene is longer than that of naloxone, which might make it useful for treating overdose involving longer acting opioids such as methadone, in that it would require less frequent dosing and hence reduce the likelihood of renarcotization as the antagonist wears off.
The usefulness of nalmefene is unclear for alcoholism. Nalmefene, in combination with psychosocial management, may decrease the amount of alcohol drank in people who are alcohol dependent. The medication can also be taken "as needed", when a person feels the urge to consume alcohol.
There is a case report of nalmefene being effective as an "as-needed" long-term therapy for cravings in a female patient with cocaine addiction. Nalmefene may possess unique potential in the application of cocaine addiction relative to other opioid antagonists such as naltrexone due to its activity as a partial agonist of the κ-opioid receptor.
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Wikipedia