This was copied and pasted from the C-3 forum. I found it interesting and thought I would share it.


Myth vs Fact


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NALTREXONE HALF LIFE

This particular question has been one of the most common misconceptions that I have come across, with many varying answers provided about what half life means in practical terms. Its implications are something that I freely admit I am not exactly clear on myself.

Please would you confirm for the readers what Naltrexone’s half life actually is, what this means and why it is important?

Dr E: The plasma half-life of naltrexone is about 4 h, and for its active metabolite 6-β-naltrexol it is 13 h.

Therefore one 50 mg tablet of naltrexone blocks opiates and endorphins for at least 24 hours.

More is not better. For example, to control heart rate by taking the beta blocker propranalol or atenalol in higher doses than the maximum recommended dosage will not block adrenaline any more effectively. So taking 200 mg naltrexone is not more effective than the recommended 50 mg dose.

The half life of Nalmefene is longer, so again more is not better. In fact, in clinical testing the recommended dosage of 18mg per 24 hours was tolerated better than higher doses. Nalmefene binds to receptors more strongly, hence the lower dosage required to achieve the receptor blockage. The research indicates that naltrexone and nalmefene are equally as effective for pharmacological extinction (TSM) in reducing craving and actual drinking levels.



ADDITIONAL OR BOOSTER TABLETS

Dr. Roy Eskapa, author of The Cure for Alcoholism
Dr. Roy Eskapa, author of The Cure for Alcoholism

There are suggestions that an additional dose or half-dose is taken as a booster for prolonged protection.

For the majority of individuals taking the full suggested dose of naltrexone or nalmefene, are there any circumstances in which you would suggest an additional tablet is taken if their drinking exceeds, for example, 5 or 6 hours in length?

Dr E: There is no FDA indication or approval on this topic but it MAY be that if a person starts drinking at say 8 am and finds he or she is drinking at 10 or 11 pm then it MAY be advisable to take another 50 mg tablet. This should be done under the supervision of a medical doctor.

But certainly there is no need after just a few hours of drinking – as explained above a 50mg dose WILL be more than adequate for shorter than 12 hour periods of drinking.

A good example of this would be the analogy of filling your car with gas – once it has been filled to the brim, no matter how hard you try you will not be able to put any more gas into that tank, it is full. Similarly, once the receptors in the brain are blocked by your medication, they remain that way for some time – taking another tablet in the hope of speeding up the TSM process, or taking another tablet too early for fear of the effect wearing off, will be of no benefit whatsoever. The receptors are already fully blocked.

And please remember this: naltrexone and nalmefene are utterly ineffective if taken with abstinence. The medication itself is not curative – it is the combination of drinking while on the medication that produces the desired result – pharmacological extinction!

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MORNING VS EVENING DRINKING

In my own TSM journey, I initially had issues with both morning and evening drinking and precisely at what time it was best to take my naltrexone. I feared that the effects of the drug would wear off by the evening if I took it very early in the morning, or that it would no longer be effective at 4.00am if I took it at 5.00pm the previous evening.

For a short time, I took a tablet at 3.00am then took a few drinks an hour later as usual, went to work and then took another tablet at 5.00pm before my drinking started again in the evening. This worked for me and within a couple of weeks my morning drinking ceased.

In the case of morning and evening drinking with a distinct break of many hours in between, please inform us of the best way to follow TSM.

Dr E: For most people, follow the ONE HOUR BEFORE DRINKING RULE — one hour before drinking in a 24 hour period.

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DOUBLE DOSE

In The Cure For Alcoholism it is shown that Dr Sinclair’s recommended dosage for The Sinclair Method to be effective is one 50 mg tablet of naltrexone, one hour prior to drinking alcohol but that naltrexone is certainly safe up to 300 mgs in a 24 hour period.

Since every drinker is different, are there circumstances that it has been beneficial to increase the dosage, when would this be advisable, and to what level would be the next possible dose?

Dr E: On this one, the doctor should decide. There is no clinical evidence that 100 mg is more effective than 50 mg one hour before drinking but there could be individual differences amongst drinkers and it is possible, though not actually proven, that increasing the dose will be more effective.



LENGTH OF TREATMENT

For those fearing the treatment isn’t working, or their drinking remains unchanged after many months, once any potential compliance issues have been resolved, at what point would you suggest that they may be one of the very small amount of people for which Naltrexone or Nalmefene does not work?

Is there any evidence to suggest a limit at which point the medication should be discontinued and other potential options explored?

Dr E: Probably, if after 10 or 11 months there is absolutely no benefit then the person may not be addicted through the opioid system … and could then try a traditional treatment.

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TYPES OF DRINKERS AND THEIR DRINKS OF CHOICE

I have been reading of many conclusions that TSM works best or quickest on a set type of drinker profile, or the length of time that they have been drinking, or whether they are liquor or beer or wine drinkers.

Are there any truth to these suggestions?

Dr E: No, none whatsoever. What matters is litres of Ethanol per year, units per session or per week, and finally loss of control over drinking even it is it three beers a night.

I had a clinical supervisor who had a plague on the wall that said ‘If you drink beer, you drink’. Ethanol is Ethanol.



THE LAST ONE IS SOMETHING I FOUND INTERESTING, I GUESS I WAS WRONG ABOUT THE TIME FRAME...OOPS!

It is interesting and thanks for sharing, jaba. Newlife

interesting then that going to 75mg is mentioned in Dr Eskapa's book, albeit by Claudia in the introduction

That is interesting.

This is from the options saves lives forum (where I found the link). I found it interesting that they contradict each other with upping the dose.



Joanna the Moderator:

Well done, Liz! This is great to hear.

I do feel I should just give a little caution on CB's post though. Yes, he/she is correct that naltrexone was tested up to 300mg a day and was proven safe.

HOWEVER, I spoke to Dr Eskapa about this very subject a while ago and he says that 50mg per day is (for most people) the optimum dosage needed to provide 100% blockage of the receptors for the purposes of TSM. In fact, when used for heroin addiction, naltrexone is usually given at 100mg every 3 days, so you can see from this that although it is safe, there is absolutely no need to take nal every 4 hours as CB implies. We are not medically trained on this forum, so please DO NOT increase your dosage without checking first with a physician.

Dr Eskapa likened taking additional naltrexone tablets to filling a glass of water. Once the glass is full, then trying to continue to fill it with water is pointless. It is FULL. So, the same is true with naltrexone. Taking more than is required has absolutely no additional benefit whatsoever.

It is true that a FEW people may need to slightly increase their dosage to perhaps 75mg if they are not responding after a few months on TSM but this should be discussed with your prescribing physician.

When I spoke to Dr Eskapa we wrote up the answers to a few basic questions that seem to get those of us not medically trained into some confusion.

Here is the link for that article. cthreeeurope.com/2014/04/20/the-sinclair-method-myth-busting-with-dr-roy-eskapa/

Please read as it also covers an additional point of confusion with regards to the half-life of naltrexone. Specifically, here is a quote from the article about the half life of naltrexone:


Naltrexone Half Life

''This particular question has been one of the most common misconceptions that I have come across, with many varying answers provided about what half life means in practical terms. Its implications are something that I freely admit I am not exactly clear on myself.

Please would you confirm for the readers what Naltrexone’s half life actually is, what this means and why it is important?

Dr E: The plasma half-life of naltrexone is about 4 h, and for its active metabolite 6-β-naltrexol it is 13 h.

Therefore one 50 mg tablet of naltrexone blocks opiates and endorphins for at least 24 hours.

More is not better. For example, to control heart rate by taking the beta blocker propranalol or atenalol in higher doses than the maximum recommended dosage will not block adrenaline any more effectively. So taking 200 mg naltrexone is not more effective than the recommended 50 mg dose.

The half life of Nalmefene is longer, so again more is not better. In fact, in clinical testing the recommended dosage of 18mg per 24 hours was tolerated better than higher doses. Nalmefene binds to receptors more strongly, hence the lower dosage required to achieve the receptor blockage. The research indicates that naltrexone and nalmefene are equally as effective for pharmacological extinction (TSM) in reducing craving and actual drinking levels.''

Well that's cleared all of that up!

Relax, take the pill, drink. That's it.

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