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 Post subject: half-life confusion
PostPosted: Sat Mar 09, 2013 12:53 pm 
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Joined: Sun Mar 03, 2013 2:02 pm
Posts: 8
Hi Dr. Eskapa,

I have been trying to understand the difference between the half-lives of naltrexone and nalmefene. Many sources say nalmefene is superior because of its longer half-life. There are 2 things about this statement that are really confusing me:

1. Why would someone using TSM want a longer half-life? I haven't started TSM yet (I am waiting for my naltrexone order to arrive from India), but I envision taking naltrexone in the evening, an hour before I have a drink, and then having 1-3 drinks and going to sleep. I want to wake up with all of my opioid receptors working again, so I can have a normal response to normal activities the next day. A longer half-life seems like it could be a bad thing!

2. When you consider naltrexone's active metabolite, does nalmefene really have a longer half-life? Several sources I looked at said that naltrexone's half-life is about four hours and nalmefene's averages around 11, but naltrexone apparently has an active metabolite with a half-life around 13 hours. The metabolite is a weaker antagonist, so is it safe to assume the clinical effects of naltrexone don't last as long as nalmefene's?

Thanks!


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 Post subject: Re: half-life confusion
PostPosted: Sun Mar 10, 2013 11:22 am 
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Joined: Fri May 13, 2011 6:52 am
Posts: 1003
Location: England
cirque wrote:
Hi Dr. Eskapa,

I have been trying to understand the difference between the half-lives of naltrexone and nalmefene. Many sources say nalmefene is superior because of its longer half-life. There are 2 things about this statement that are really confusing me:

1. Why would someone using TSM want a longer half-life? I haven't started TSM yet (I am waiting for my naltrexone order to arrive from India), but I envision taking naltrexone in the evening, an hour before I have a drink, and then having 1-3 drinks and going to sleep. I want to wake up with all of my opioid receptors working again, so I can have a normal response to normal activities the next day. A longer half-life seems like it could be a bad thing!

2. When you consider naltrexone's active metabolite, does nalmefene really have a longer half-life? Several sources I looked at said that naltrexone's half-life is about four hours and nalmefene's averages around 11, but naltrexone apparently has an active metabolite with a half-life around 13 hours. The metabolite is a weaker antagonist, so is it safe to assume the clinical effects of naltrexone don't last as long as nalmefene's?

Thanks!


Receptors are not clear of Naltrexone for 48 hours.

_________________
Naltrexone Started 20th April 2011

Cravings eliminated Sept 2011
Now fully in control, alcohol no longer bothers me. Chose to go AF from 22nd July 2013.
TSM set me free


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 Post subject: Re: half-life confusion
PostPosted: Mon Mar 11, 2013 7:55 pm 
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Joined: Sun Mar 03, 2013 2:02 pm
Posts: 8
Yes, but generally a half-life is a better estimation of how long a drug will have a noticeable effect. If naltrexone continued to have a significant effect for 48 hours, the Sinclair Method theoretically wouldn't work very well.


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 Post subject: Re: half-life confusion
PostPosted: Tue Mar 12, 2013 3:22 am 
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Joined: Fri May 13, 2011 6:52 am
Posts: 1003
Location: England
cirque wrote:
Yes, but generally a half-life is a better estimation of how long a drug will have a noticeable effect. If naltrexone continued to have a significant effect for 48 hours, the Sinclair Method theoretically wouldn't work very well.


That depends, it would mean that endorphins were continuously blocked, not desireable state but you'd become deaddicted to alcohol plus a lot of other things!

The new drug is supposed to have less side effects, and the longer half life might suit those who drink for long periods at a time.

_________________
Naltrexone Started 20th April 2011

Cravings eliminated Sept 2011
Now fully in control, alcohol no longer bothers me. Chose to go AF from 22nd July 2013.
TSM set me free


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 Post subject: Re: half-life confusion
PostPosted: Tue Dec 04, 2018 4:44 am 
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