Hi

I started the sinclair method as per instructions here and the Dr Sinclair interview, about 5 weeks ago. I take naltrexone an hour before drinking - which is approximately 4 times per week. I then drink slowly for 3-4 hours. Will the pill keep working for 3-4 hours? How quickly are the molecules displaced or removed from their receptors? My current 'set point' for alcohol tolerance is about 1.5 bottles of wine and even though I promise myself I will not drink any more than one bottle - I always go into the second one. I have not seen a reduction yet in my consumption, or, an increase in control, but I am continuing as I know it takes time.

Thanks to all for the ongoing encouragement.

Camelia

Hi Camelia

I believe we are covered for between 24 and 48 hours, it might be an idea to ask Dr. Eskapa, but you are most definitely covered for 3-4 hours.

Do you find drinking with Naltrexone any different to when you drank without it? I am sure there will be many changes going on- but at present they are under your perception radar, we will have started about the same time. I have noticed quite a lot of changes in my drinking, but I was (am) an everyday drinker- I don't know if maybe that makes a difference.

Well hang on in there, as you say it takes time.

Nice to have you here!

Naltrexone 50 mg will block the effects of opiates and endorphins for 24 hours. Doubling the dose may increase the metabolite half-life to 48 hours ... However, there may be individual differences and some may metabolize it more rapidly than others. Thus if you take the tablet at 8 am and start drinking at 10 pm you may not be covered. There is a reason why we only want you to take the medication 1 hour before drinking not more. There is no benefit from blocking the endorphins before they are released as a result of drinking. Moreover, if you take naltrexone with abstinence for extended periods you will 'upregulate' your opioid receptors - meaning there will be more of them (millions more) in your body. If you drink at this point without coverage (opioid blockade / antagonism) you will receive an especially strong jolt of reinforcement from the endorphins thereby enhancing your craving and drinking levels.

Here is the the information for Medical Professionals from Chapter 17 in the book - hope this is not too technical:

Pharmacokinetics: Naltrexone is a pure opioid receptor antagonist. Although well absorbed orally, naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5% to 40%. The activity of naltrexone is believed to be due to both parent and the 6-f3-naltrexol metabolite. Both parent drug and metabolites are excreted primarily by the kidney (53% to 79% of the dose), however, urinary excretion of unchanged naltrexone accounts for less than 2% of an oral dose and fecal excretion is a minor elimination pathway. The mean elimination half-life (T-1/2) values for naltrexone and 6-f3-naltrexol are 4 hours and 13 hours, respectively. Naltrexone and 6-f3-naltrexol are dose proportional in terms of AUC and Cmax over the range of 50 to 200 mg and do not accumulate after 100 mg daily doses.

Absorption: Following oral administration, naltrexone undergoes rapid and nearly complete absorption with approximately 96% of the dose absorbed from the gastrointestinal tract. Peak plasma levels of both naltrexone and 6-f3-naltrexol occur within one hour of dosing.

Distribution: The volume of distribution for naltrexone following intravenous administration is estimated to be 1350 liters. In vitro tests with human plasma show naltrexone to be 21% bound to plasma proteins over the therapeutic dose range.

Metabolism: The systemic clearance (after intravenous administration) of naltrexone is ~3.5 L/min, which exceeds liver blood flow (~1.2 L/min). This suggests both that naltrexone is a highly extracted drug (>98% metabolized) and that extra-hepatic sites of drug metabolism exist. The major metabolite of naltrexone is 6-f3- naltrexol. Two other minor metabolites are 2-hydroxy-3-methoxy6-f3-naltrexol and 2-hydroxy-3-methyl-naltrexone. Naltrexone and its metabolites are also conjugated to form additional metabolic products.

Elimination: The renal clearance for naltrexone ranges from 30 to 127 mL/min and suggests that renal elimination is primarily by glomerular filtration. In comparison, the renal clearance for 6-β-naltrexol ranges from 230 to 369 mL/min, suggesting an additional renal tubular secretory mechanism. The urinary excretion of unchanged naltrexone accounts for less than 2% of an oral dose; urinary excretion of unchanged and conjugated 6-β-naltrexol accounts for 43% of an oral dose. The pharmacokinetic profile of naltrexone suggests that naltrexone and its metabolites may undergo enterohepatic recycling.

Hi

thank you Dr Escappa and Marbella - I am an Irish citizen who lives in the UK who has ordered but not yet received your book! I am also a neuroscientist and completely understand the logic - hence the question. I hope I am not in the minority who do not respond! if my response is positive I have a bucket load of friends and 100% of my living relatives who will benefit!

Marbella, its great that we are more or less in the same time frame. I do drink most days - but lighter some days than others. I think I have definitely enjoyed the 'license to binge' associated with doing a program which requires you to drink. Can we be 'Sinclair buddies' ? I need all the help and support I can get. Maybe we can support and encourage each other.

We are all participants in an extraordinary experiment!

Cheers

Camelia

Hi again Marbella,

just to answer your specific question as to whether I have noticed 'anything different'. Maybe the fact that I am now absolutely not worried about the prospect of losing complete interest in alcohol, and, open to the possibility of complete abstinence, is a subliminal change. Before now I would have considered this impossible. Now I am looking forward to freedom above the need to remain a social drinker. This period seems a bit like 'a chore' but I would rather do this chore than fight cravings ad nausem. I give in to those cravings so easily I have little faith in my ability to fight them!

Camelia

To Dr Eskappa

sorry - I spelled your name wrong. Please forgive me!

Camelia

and I did it again! I will get it right next time

Hi Camelia

We sure can be buddies- I am from the UK living in Spain, so we are on the same time frame.

ASHL and Q are also at the same stage- I think they are both just a few days ahead of me.

Are you tracking your days? I find this very helpful in noticing how my drinking is changing- even if the unts at the end of the week do not seem much different the pattern is changing.

Maybe you could start a 'Weekly Progress Thread?' The newcomers like to see how the program is doing for others that have been on it a while.

I am not fighting cravings either, I don't think we are meant to- but I am having a little bit of trouble distinguishing a genuine craving from just an alcohol thought- for example when I log on here I will think of alcohol, but it is not a craving.

Well if I get it mixed up, I guess it doesn't matter either- as long as I take the Nal in advance, all will be well

Hi Marbella and all,

I just received the book yesterday and have read most of it. Had also read and listened to the Sinclair Broadcast as well as Dr Roys stuff on here. I have been a bit lax about tracking units and craving but have just produced photocopy of the units and VAS tracking on one page - so im 'off' as far as thats concerned.

as far as distinguishing cravings from thoughts about alcohol - I think I have been a bit lazy about this too - giving in to any thoughts very easily. Thats partly a function of the 'freedom to drink' conferred by this program. I know that I have been in a bit of a 'free fall' drinking habit for the last few weeks and am not feeling the better for it. I now realise I don't have to completely wreck myself for the cure to work

This is week 7 and I am now going to give myself a few days off alcohol (if I can) and see how high the craving levels really are.

Maybe I shall start a new thread - even at this later stage.

Camelia


Week 7

Keep on going on