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 Post subject: Opioid Receptor Queston?
PostPosted: Thu Mar 20, 2008 10:41 pm 
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I have looked extensively online to find the answer to these questions but to no avail. It may just be that I need to talk to a Neurologist to get the answer; however, I am hoping that someone out there with some knowledge in this area can help me or point me in the right direction to find the answers.

Before I start I want to make a distinction here. In this post, I am only referring to the physical dependence (changes in the brain) of opiates (pain meds) not the emotional mental addiction to opiates.

I have done a lot of reading on the effects of long term opiate use on the brain and nervous system. Basically when opiates are taken chronically our brains produce more and more opioid receptors. This creates the need to take more and more opiates (tolerance). These are physiological changes that happen in the brain. It is true also that when the opiates are stopped the physical withdrawal symptoms increase depending on the amount of opiates taken and the amount of opioid receptors produced.

I have also done a significant amount of research on Suboxone and how it works in the brain. I did this prior to my induction onto Suboxone so that I could make the most informed decision possible. Therefore, before answering my questions below please know that I do have this knowledge.

Now for my first question:

1. If one stops taking opiates, will these physiological changes in the brain (the increase of Opioid receptors) reverse itself?

2. If one starts taking Suboxone, does the brain still continue to produce more opioid receptors or is this process halted?

To me the answers to both of these questions are extremely important and yet they seem to be extremely elusive.

I would like to believe that now that I am on Suboxone, these changes in my brain will stop and not get any worse. I would also like to believe that once I am off the Suboxone, there is hope that the changes that have already occurred in my brain will reverse itself over time to ultimately bring my brain back into my pre-opiate use condition and or to a normal state.

Is there someone out there that knows the answer to these two questions?


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PostPosted: Fri Mar 21, 2008 10:57 am 
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I don't know the answer to your questions, but have you read " A New Presciption for Addiction" by Dr. Richard I. Gracer?
This might help. Good questions. I hope someone will respond.


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 Post subject: Just a suggestion
PostPosted: Fri Mar 21, 2008 12:18 pm 
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You have a lot of good questions, I wish I knew the answers, but pretty sure the Sub doc does, Please e mail him under memberlist or PM him also as a favor to me, ask that he answer on the forum, because I'm interested in the answers to your questions as well. :idea:

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PostPosted: Fri Mar 21, 2008 6:47 pm 
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It is important to understand that we have models to describe things, so that our brains can make sense of what is going on... but in reality the model is a simplification of what is going on. For example, I present receptors during lectures as locks, and neurotransmitters as keys. We get an image of a transmitter fitting into the receptor and turning something, or maybe just sitting there and blocking the site like a key broken off in a lock. In reality, unless the brain is sitting in a freezer at absolute zero (something like minus 300 degrees C-- I can't remember exactly, but it is the coldest state there is, where molecules and atoms stop moving entirely) where was I... unless it is THAT cold, atoms and molecules are always moving. At the receptor, the transmitters are associating and dissociating millions of times per second. The 'affinity' of a drug for a receptor is the 'tightness' that the drug binds, and is most accurately thought of as probability-- the probability that at any one time it is bound, vs the probability that it is unbound. Also remember that those models we had in 6th grade of atoms and molecules, made of stick-toys, are not even close to reality, where electrons exist not as 'things' but as clouds, or waves, or forces.

This issue with tolerance and withdrawal is not so much the number of opiate receptors in the brain. The issue is what the receptors are allowing to happen, and what pathways are being blocked or activated. For future research look up the terms 'up regulation' and 'down regulation'-- those are the processes where large amounts of a 'ligand' (the term for the 'key') induce change in the receptors. These changes then alter the effect of the drug on the neuron. For example, say we have one neuron that can fire and send a signal down the spinal cord, which will block all pain input at the spinal level. This neuron has 'dendrites'-- thousands of branches, and each branch has thousands of smaller branches, and each smaller branch has thousands of receptors for dozens of transmitters. Some receptors, when activated, dampen the effect of other receptors (say by allowing chloride to flow into the neuron, making it more negative inside so that it is less likely to become 'positive enough' to fire and 'action potential'). There is an intricate interplay of all of these receptor systems, and the neuron is like a micro-processor, weighing all of the input, and eventually 'deciding' whether or not to fire that precious signal down its axon to the spinal cord. But it is even more complicated-- the dendrite branches have shapes that change, and changes in shape effect the impact of the receptors on that particular little one in a million dendrite branch. The dendrite branch may have a narrow little neck at one point that snuffs out the signal from receptors on that branch. And all of these shapes are constantly changing-- that is one way that memories are formed, as the pattern of use of certain branches causes changes in shapes that affect firing patterns. Are you bored yet?

Opiate receptors are just one tiny part of the equation. In the presence of a lot of molecules to activate the opiate receptor, the receptor 'down regulates'-- I like to think of it as becoming less sensitive. It takes more and more molecules, then, to activate the receptors, which become less and less sensitive. We want this little neuron to fire, but it is taking more and more drug to get it to fire. Then we remove the drug... and we have all these insensitive receptors, and even our own opiates now have no effect at all on them. THat, my friends, is withdrawal. The neuron now is not firing at all-- not for anything. We have to just wait-- all parts of all cells are constantly being recycled and turned over, including the receptors in the cell membrane. They will be pinched off, destroyed, and replaced with fresh, new, sensitive receptors. And eventually things will go back to normal.

I used to study receptors-- my PhD in Neurochemistry involved grinding up the brains of 60 rats per week over 4 years (I hope heaven isn't run by rats) and studying binding properties of radioactive chemicals. This is an educated guess, this next part-- but with 'agonists' like oxy or methadone, everything is always in flux-- receptors are always being changed one way or the other. With suboxone, the agonist property of buprenorphine pushes one way, and the antagonist property pushes the other way, and my image is of things being more 'static' (not changing, but holding constant). So to answer the question finally, I think that on suboxone, the brain reaches a level of tolerance, but then stays there. I think that the cravings come from change-- from receptors becoming less sensitive and needing more stimulation. With suboxone the receptors stop changing, and become 'content' with the degree of stimulation.

As an aside, there are people searching for a way to prevent the change of receptors that causes tolerance. It appears that the transmitter glutamate acts at receptors and that if that doesn't happen, the receptors cannot change. Imagine a day when a person can take a percocet over and over, and no matter how many times it is taken, it always has the same effect. It never loses potency. There is no withdrawal, because the receptors never change. Imagine that-- it would be wonderful for people in pain, but what about those of us who just love the feeling of an opiate? The whole thing is in some ways very exciting, and in other ways very frightening.


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PostPosted: Fri Mar 21, 2008 7:16 pm 
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Thank you so much kilby5.0, Masuka & especially Suboxdoc!!!

Finally, I have received the info that I have been searching for! I really do appreciate the detailed explanation. It's funny because after I left my post yesterday, I found a site "Drugs on The Brain" and after I read it I was very discouraged because in a nutshell it said that the changes that occur in the brain after long term use of cocain and or opiates are permanent. Your explanation on the other hand has left me feeling encouraged.


I can't thank you enough!


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PostPosted: Thu Jun 04, 2009 8:49 am 
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When I was using herion my habit got very severe, I was using a large amount close to two to three bundles of street bought heroin a day. Been on the suboxone for a while now and like it but was hoping that the receptors in my brain were changing was hoping that I was somehow reducing the number that I created during my years of heroin abuse hoping that once I decided to come off the suboxone that I would not experience the intense cravings that I had back before getting the sub. So now after reading the posts here...am I now to believe that by not taking the full agonists all this time and by just taking the suboxone that i have not changed anything and all is as it was? So when I do eventually stop taking the suboxone I am to start feeling all the cravings I had back then? That is I hope not the case...I am hoping that by not taking any of the full agonists that I am somehow reducing the number of receptors in my brain and in turn reverting back to an earlier state where my life isnt spent thinking of when I will relapse and how long can I hold off till it happens again. I am hoping that this post being from 2008 is a little more understood now and maybe there is another answer that more accurately describes the changes occuring as a result of the use of suboxone. Thanks for any help u guys can provide.


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 Post subject: Perry68414 Concerns
PostPosted: Thu Jun 04, 2009 4:47 pm 
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Hello Perry68414!

I'm pretty sure that you are correct in that when you stop taking Suboxone you will feel some withdrawal (physically) due to your receptors being less sensitive. During the time that you've been on Suboxone your receptors have been in a state of "Limbo" or they, as the Suboxdoc said, are "content"; therefore, after you are off of Suboxone it will probably take some time for the old receptors to be replaced naturally with new sensitive ones, but it does happen if you abstain long enough. This is actually good news and a whole lot better than the prospect of your receptors being permanently screwed up.

The good news is that since you have been on Suboxone you probably have gotten over some of the psychological dependence that you had when using heroin, such as the highs and lows and the clock watching for your next dose etc... This in itself makes taking Suboxone worthwhile because you have learned to live a "normal" life with a "normal" mood etc. If you had not gotten off the Heroin and onto Suboxone, you would have done more damage to your receptors, your body and you may have even died. I've been on Suboxone for a little over one year now and I feel much more stable now. Therefore, if I taper slow enough for my body to adjust naturally to less and less of the Suboxone, I am hoping that the withdrawal won't be too horribly bad. When I decide to do this (I'm in no hurry), I will work with my prescribing doctor (my psychiatrist) and ask for help if I need it for regulating my mood etc...

My psychiatrist has given me some further insight into why I may have chosen to "self medicate" myself with opiates. I was a functional addict and never took so much that I was out of control. It was almost like I took them to feel normal or to feel what others feel is a normal or good mood. My psychiatrist thinks that I have a mood disorder and that I was trying to feel better by taking the drugs. I wonder if other people who choose to take opiates have the same problem? I've taken many types of antidepressant drugs and none of them worked for me because they made me feel "dull or zombie like hindering me from feeling my emotions", Suboxone on the other hand seems to regulate my mood perfectly (except I have no libido). My psychiatrist is from the Ukraine and she doesn't have the mind set of American doctors or American people regarding drug addiction and the blame/shame game that goes along with it. It seems that here in America there is a contradiction going on. On the one hand drug addiction is supposed to be a "disease"; however, the person with the "disease" is blamed and judged as being "weak" or even "criminal" depending on the drug they are taking. If addiction is a "disease" like "diabetes" why do we blame the person instead of the disease?

Anyway--I digress. I hope you are doing well and that when you do decide to taper off Suboxone you will do it very, very slowly and that you will be kind to yourself and keep in touch here at this blog.

Take Care


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 Post subject:
PostPosted: Mon Jun 08, 2009 11:41 am 
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When one takes any opiate, including sub, the number of opiate receptors that need to be satisfied does increase. Suboxone maintenance will typically maintain or increase your level of opiate tolerance (as anyone who has had a relapse shortly after taking sub can attest), but once you are off all opiates (including sub) your opiate tolerance will tend to decrease back to normal levels, though probably not quite to the sensitivity that you had before abusing opiates.

As mbra mentioned, a lot of people started using opiates to "self-medicate", so once you are opiate-free (if that is your desire) you may very well need to take an antidepressent or other drug to feel "normal".


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PostPosted: Sat Jun 13, 2009 12:14 am 
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did you guys not read the docs reply, it is not about how many opiate receptors their are, rather how sensitive they are. When on suboxone you receptors do not change as they used to, therefore maintaining a consistent sensitivity. As you slowly taper off, and i do mean slowly, gradually your receptors become attuned to the amount of suboxone being taken. This is different than methadone where it is a full agonist and therefor there is not that balance of agonist and antagonist. Suboxone is a very stabilizing medication.


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 Post subject: Suboxone Tolerance
PostPosted: Wed Sep 23, 2009 4:33 pm 
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I have been taking Suboxone now for over 1.5 years and I have developed a tolerance to it, it just took longer for it to happen on Suboxone. I think if you take Suboxone long enough, you will develop a tolerance to it and you will need to increase your dose. I'm going to begin a very slow taper on October 1st. because I do not want to start increasing my dose!! I hope I will be successful!!


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 Post subject:
PostPosted: Thu Sep 24, 2009 8:12 am 
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How would you describe your tolerance? What symptoms?

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 Post subject: Tolerance
PostPosted: Thu Sep 24, 2009 2:22 pm 
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I started to feel depressed, achy, unmotivated and my legs were feeling like they were "waking up" into that horrible state of restless leg syndrome that I have had during withdrawal. I told my psychiatrist this and she upped my dose 2mg and these symptoms went away. I don't want this to be the beginning of me continually upping my dose so I am going to start a very slow taper soon. Plus, I have read some very disturbing information about people who have been on Suboxone for extended periods of time. I've been on it over a year and people who have been on Sub for this long or longer find themselves in PAWS (Post Acute Withdrawal Syndrome) when they try to quit. Here is one post I found from the following link: http://www.withdrawal-ease.com/suboxone ... m-looming/

"Here’s essentially what I have noticed with Sub patients. Those that have been on it for a year or longer are usually able to taper down to about 1-2mg’s per day but once they try and “jump” to zero, they have a really hard time and often experience what is called PAWS (Post Acute Withdrawal Syndrome). PAWS is basically an extended withdrawal process that some people suffer from for months and months. The people that I have encountered with PAWS seem to have a lot of psychological symptoms such as ongoing lethargy and depression but there’s no doubt about it, it’s opiate withdrawal. Of course I have to mention again that Suboxone has a much longer half-life than hydrocodone so it makes sense that it would have an extended withdrawal period. Having said that, I’m really surprised at the acuity and the duration of the symptoms that people who are trying to get off Suboxone after long term use. It’s a bit alarming. And it must be downright scary for those people who thought that they were getting clean and sober by using Suboxone only to find out they they are sort of stuck with a worse “cellmate” than their original drug of choice. "

This is very scary!

Why do you ask?


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