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PostPosted: Sun Sep 23, 2012 12:16 am 
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Can't believe I just found out about this drug.

Nalmefene is an antagonist structurally similar to naltrexone. The main difference that's relevant to us is that nalmefene has a stronger binding affinity to all known opioids, including buprenorphine. In a nutshell, Nalmefene (unlike Naltrexone) can displace buprenorphine from ALL opioid receptor subtypes (mu, kappa and delta) thus kicking buprenorphine completely off the brain.

First obvious application would be buprenorphine overdose. Instead of needing incredibly high doses of naltrexone in an infusion and only getting a partial effect, nalmefene could reverse the effect and precipitate withdrawal from buprenorphine, and only need one dose because of its long half life.

The other (more controversial) application could be its ability to induce a rapid-detox off buprenorphine. We may start to see rapid-detox facilities start to target people trying to get off Suboxone. Traditionally they've only been able to service people on agonists... Nalmafene may change that.

At the moment Lundbeck have put in a new drug application targeting alcoholism. It's main benefit for that indication over Naltrexone is that there's no evidence of hepatoxicity. This is just the beginning though. We may see them create a depot formulation in the future similar to Vivitrol.

Also, like buprenorphine, we may see some doctors prescribe it off-label for opioid dependence. Conservative politicians of the anti-maintenance lobby are particularly fond of the antagonist "solutions" to opioid addiction, as (unlike Sub and methadone) antagonists don't maintain a state of dependence.

http://investor.lundbeck.com/pipeline.cfm

http://en.wikipedia.org/wiki/Nalmefene


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PostPosted: Sun Sep 23, 2012 1:14 am 
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eep. Turns out even nalmefene can't fully reverse buprenorphine's effects. Bupe must be a darn sticky little molecule!!


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Fond Du Lac Psychiatry
Dr. Jeffrey Junig, M.D., Ph.D.

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