Dr. Eskapa,

Many thanks for your input and time.

I am approaching my 3rd week with Naltrexone and I am finding that the most difficult side effect is that it makes me extremely tired, especially after having a few drinks of alchohol. Some nights I have a hard time keeping my eyes open much past 8pm -- I typically go to bed between 10pm-11pm.

Is this a side effect that I can expect to pass or is this something you just didn't see in your research?

Thank you.

Q

I once asked David Sinclair about this. Alcohol - a 'dirty drug' - exerts many effects on the brain, nervous system, organs, and metabolism - in fact the whole biology of the body is effected. Most addicted drinkers learn the addiction primarily through the opioid (endorphin) system which has become strengthened over many months and years and many drinking sessions especially if one has inherited the genetic predisposition for learned addiction.

Naltrexone only blocks the effects of opiates and endorphins released by alcohol in the brain, but not the other effects it might have on other systems (e.g. GABA, cortisol, serotonin, etc). (Alcohol may substitute or temporarily raise GABA - the neurotransmitter that benzodiadepines like diazepam/valium artificially raise and make one 'feel relaxed' or sleepy.) Alcohol at low doses may have 'stimulatory effects' - think of a cocktail party where people start talking louder and feel awakened. This is probably coming from endorphin release in the brain. At higher doses it is a depressant. It tends to accentuate whatever the individual is feeling at the time - a sort of amplifier of moods and feelings currently present.

Since naltrexone blocks the endorphins it may also block the 'first drink effects' - the stimulatory effects - in some people and therefore one might feel more subjectively tired. Sinclair also mentioned that because of this naltrexone effects 'divided attention' - this one should be especially careful of driving or operating machinery while drinking on the medication presumably because the so-called stimulatory effects coming from endorphin release are blocked.

I'll quote this from the book and hope it helps (see below).

Best wishes with your continued progress:

"A couple of cautions are in order. You must be particularly careful not to drink and drive or use machinery. Naltrexone not only does not block intoxication, it actually can increase some aspects of impairment. Sinclair found that an opioid antagonist could increase the motor impairment from alcohol in rats. Later research showed that in humans naltrexone can increase problems from alcohol that are related to the divided attention needed in driving.

What Should You Expect to Happen?
The answer is that no two people are alike. Some people respond to treatment more quickly than others. Generally, naltrexone side effects are rare and include symptoms like mild itchiness or transient nausea. Compared with the side effects of addictive drinking, most patients report they are both minor and temporary—well worth the effort. The majority of patients taking naltrexone report few or no side effects.
Be alert that, even very early in your treatment, you may occasionally experience a surprising ability to stop after only a couple drinks. However, this decrease in drinking and craving is merely an artifact of the treatment. The naltrexone is blocking some of the effects from the first drink and from stimuli that have become conditioned to release endorphins; this helps block the “first-drink effect.” It is a beneficial but weak effect. The powerful effects from

(* Sinclair reports in a large Finnish trial these effects–zero or no more than nine units per week–were still in effect three years after the end of treatment.)

pharmacological extinction develop much more slowly and cannot cure you in a week or two. It took you a long time to reach your current craving and drinking levels, and it will take at least three to four months to reverse the addiction. Some people take longer before the neurological scaffolding—the addictive wiring in the brain—is brought down, reduced, and restored to its normal, healthy, pre-addicted state.
Of course, each of you will be progressing through treatment at your own pace. But everyone has to follow the formula: Naltrexone + Drinking = Cure to be successful. You should expect success—like the seventy-five patients in Figure 8 who showed reduced craving over three to four months.
You can also expect your actual drinking to go down to about fifteen drinks per week within three to four months and eventually down to nine drinks per week, as shown in Figure 9.
You set your own treatment goals. Only 3 percent of the patients originally treated by Sinclair’s group chose total abstinence as their original goal, but about a quarter of them were abstinent after three months of treatment. Before treatment, it may be difficult to imagine a life without alcohol, but by the end of treatment, your craving will have decreased so noticeably and dramatically that total abstinence becomes a matter of personal choice. You will no longer fear alcohol. You will not be in its vise; you will not be its servant or puppet. You will find that you no longer obsess or think about it and it will become more or less irrelevant in your life. However, the ultimate goal is to break the addiction so that you control your drinking instead of it controlling you.
Some people may wish to drink two or three times a year—for instance, at Christmas or on New Year’s Eve. This is fine as long as you always take your medication before you do so. The point is that the Sinclair Method allows you to cut back or stop altogether without the nagging feelings of deprivation and threat of relapse associated with traditional abstinence-based treatments. You will not have to attend regular support groups—unless you choose to do so.
If you choose to continue drinking, the treatment will result in a massive decrease in your desire for alcohol and also the actual amounts you drink when you do. You will find yourself simply losing interest in alcohol without losing interest in the party.* Because de-addiction occurs at the microscopic level of opioid (endorphin) receptors and synapses in the brain, you will not know why the voice in your head suggesting “I could do with a drink” or “I need a drink” simply seems to have disappeared. Your rescue from the bottle happens as if by magic. It is not magic, of course, but the fruits of the Sinclair Method are astonishing indeed.
Most likely, others will also notice positive changes—you no longer get drunk, depressed, hung over, out of hand, or aggressive, and you don’t lose your judgment and control. Drinking + Naltrexone produces a state of permanent physiological de-addiction.

I forgot to address your question about whether the 'sleepy' side-effect you are experiencing will pass. My guess is that it probably will as you adjust to drinking on naltrexone. Naltrexone itself has no soporific, hypnotic, sleep-inducing effects. It is not a 'mood altering' drug - which is why it is on a low schedule. The tiredness or sleepiness is almost certainly coming from the other things that alcohol does to the brain ... not the naltrexone itself. In other words, if you took naltrexone without drinking (not part of the Sinclair Method and not advised) it would most likely not have any noticeable effects other than the reported transient side-effects reported in the literature.

Best,

Roy Eskapa, PhD

Dr. Eskapa, I was wondering if the nine alcohol units of/per week, for the individuals that Dr. Sinclair was tracking after three years, was a reference to the UK system of alcohol unit measurement.

thankfully,

francophone

The first time I took Naltrexone, it was prescribed as part of an abstinence regime, and I couldn't take it until after I had been abstinent for 5 days. I vividly remember my first experience with Naltrexone in that setting -- it almost resulted in my running my car off the road on the highway on my way back from the clinic appointment because I couldn't keep my eyes open! Fortunately, I had the sense (and opportunity) to pull over at a truck stop and sleep for two hours before proceeding to drive home. My scariest "sleepy-time" episode with Naltrexone was taking it when I was sober.

Now, when I take the Naltrexone prior to drinking, I still get sleepy, but nothing like the first time that made me question my decision to take that first pill! I noticed my prescription bottle does state "may cause drowsiness" -- so the claim that Naltrexone has no soporific effect on the nervous system seems suspect -- in my opinion. I do think the effect is transient, but it does exist, and from personal experience -- I think that particular quality intensifies the effect of alcohol (not the endorphin part -- the motor skills/slurring your speech part). Perhaps that's why lots of us experience the drastic reduction in alcohol consumption during the first week -- the body can't take the heightened "drunk" feeling without the endorphin rush to balance it out -- it's just not fun!. After a little while, the body adjusts to the Naltrexone so it doesn't compound alcohol's negative effect, and so alcohol consumption escalates until the long-term, hard-won extinction protocol eventually wins.

My first post, I admit that I have been intimidated and overwhelmed by the level of intelligence on this message board. Everyone and every post is well thought out and presented very well. I am G4M SO and have had a problem with being tired or sleepy. Every evening at 2100 hrs or around that time, it is like someone flips a switch and I become so sleepy it is almost impossible for me to keep my eyes open, I get extremely tired and can hardly remain awake.
G4M says that it is the crazy hours I keep, but after all these years I sill have my superman cape and refuse to part with it. I get the tired feeling with or without the Nalrexone, so I can say from personal experience that it is not the Naltrexone.
Good Luck to everyone on their journey

Superman, here, gets up every day at 4 a.m. I'd be tired by 9 p.m. too if I kept those crazy hours!

Hi Jake!

How nice to see you here too- I wish I had someone who I could talk to about this, my SO doesn't even know I am on it:o

More about that another time

My tiredness on Nal is getting a bit better now (Week 6 underway) but I have been quite surprised that the few nights I have not drunk or taken Nal, that the tiredness has hit almost as hard.

I think I agree with G4M on this one- I too would be knackered anyway if I got up at 4am!

I actually found in one of the Journal References listed in Dr. Eskapa's book that Fatigue is one of the 4 main side effects of taking Nal, affecting 10%-20% of users: http://content.karger.com/ProdukteDB/pr ... 104882.pdf

Look on about page 4, top of the page.

Fatigue used to hit me like a ton of bricks after taking Nal. Drinking even a small amount after taking Nal was like taking a moderately powered sedative -- I could barely keep my eyes open. This side effect has gotten better for me. I still get a little fatigued (tired), but not nearly as bad as it used to be.

Q

Thanks for the references, and encouragement, Q!