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Core Topics => Other Non-Drug Addictions => Topic started by: Chip on May 05, 2019, 07:48:33 AM
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Source:
https://en.m.wikipedia.org/wiki/Nalmefene
Nalmefene (originally known as nalmetrene; trade name Selincro) is an opioid antagonist used primarily in the management of alcohol dependence. It has also been investigated for the treatment of other addictions such as pathological gambling.
Edit: Perfect for a pub or club gaming lounge brewing problematic gambler !
Pharmacokinetic data of this prescription drug:
Protein binding is 45%
Metabolism is Hepatic (liver)
Elimination half-life is 10.8 ± 5.2 hours
Excretion is Renal (kidneys)
Chemical and physical data:
Formula is C21H25NO3
Molar mass is 339.435 g·mol−1
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.
Like other drugs of this type, nalmefene may 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.
Medical uses :
Opioid overdose
Intravenous doses of nalmefene have been shown effective at counteracting the respiratory depression produced by opioid overdose.
This is not the usual application for this drug, for two reasons:
The half-life of nalmefene is longer than that of naloxone. One might have thought this would make it useful for treating overdose involving long-acting opioids: it would require less frequent dosing, and hence reduce the likelihood of renarcotization as the antagonist wears off.
But, in fact, the use of nalmefene is not recommended in such situations. Unfortunately, opioid-dependent patients may go home and use excessive doses of opioids in order to overcome nalmefene's opioid blockade and to relieve the discomfort of opioid withdrawal. Such large doses of opioids may be fatal. This is why naloxone (a shorter-acting drug) is normally a better choice for overdose reversal.[4]
In addition, injectable nalmefene is no longer available on the market.
When nalmefene is used to treat an opioid overdose, doses of nalmefene greater than 1.5 mg do not appear to give any greater benefit than doses of only 1.5 mg.
Alcohol dependence
Nalmefene is used in Europe to reduce alcohol dependence and NICE recommends the use of nalmefene to reduce alcohol consumption in combination with psychological support for people who drink heavily.[6]
Based on a meta analysis, the usefulness of nalmefene for alcohol dependence is unclear.
Nalmefene, in combination with psychosocial management, may decrease the amount of alcohol drunk by people who are alcohol dependent.
The medication may also be taken "as needed", when a person feels the urge to consume alcohol.