Opioids Buprenorphine as an Endorphine Inhibitor

[narcoticon]

Greetings Bluelighters!

Opiate users know the pain of withdrawal, both acutely and post-acutely. It's the latter of these two that I would like to discuss.

I am aware that opiates work because they mimic endorphines. I am also aware that the body produces some pretty badass ones, such as beta-endorphine, which is believed to be roughly 80 times more potent than morphine†. It is my understanding that the brain reacts to chronic opiate use in several ways that are harmful, including:

• Ceasing to produce endogenous endorphines
• Down-regulating receptors to said opiate when production limitation fails to lower syrum levels‡

I have been attempting to recover from these effects using a combination of low-dose buprenorphine, nutrition, exercise, and spirituality. My question is this: will the presence of buprenorphine in my system continue to cause my body to down-regulate my µ receptor level? If so, won't I be desensitized to my own endogenous endorphines, even if I manage to return to the homeostatic level at which they are produced at normal levels?

I would appreciate insight into this matter from those who are more educated about the pharmacological and physiological chemistry involved here.

Sources:
† - http://en.wikipedia.org/wiki/Beta-endorphin
‡ - http://www.ncbi.nlm.nih.gov/pubmed/8097244

 

[mrflowers00]

yeah i will make your brain/body produce less endorphins

 

[Cane2theLeft]

Compared to full agonists, it will help you recover some and begin to produce more endorphins than when you were on full agonists but with it you won't go all the way back to baseline.

If the choice is between using buprenorphine and not producing quite as many endorphins (that the bupe would block/reduce the effects of anyway) or not taking bupe, being miserable with craving and relapsing with full agonists and greatly exacerbating the whole situation physically and psychologically, then does it really matter how many you're producing? If you're stable on bupe then you're getting the positive effects exogenously and allowing yourself stability physically and mentally that you'd likely lose if you stopped.

When you are in a place where you no longer need the bupe and get off it there are ways to stimulate endorphin production naturally such as with spicy food.



______________
Sorry that I am anal but 'endogenous endorphin' is redundant. Endorphin is a portmanteau of 'endogenous' and 'morphine' because when it was discovered they realized that it was something your body produces that works like morphine.

 

[sekio]

Yes, it will inhibit endorphin production and keep your receptors downregulated.

Though buprenorphine is not a particularly strong agonist, its primary metabolite norbuprenorphine is usually produced in enough quantity (especially at low doses) to act as a fairly strong agonist.

 

[cire113]

f the choice is between using buprenorphine and not producing quite as many endorphins (that the bupe would block/reduce the effects of anyway) or not taking bupe, being miserable with craving and relapsing with full agonists and greatly exacerbating the whole situation physically and psychologically,

this is exactly why i have enough of sub when armageddon comes lol

I'm not sure if it matters how strong an agonist it is honestly...
When it starts binding to those receptors the body stops producing natural ones..?

I mean doesnt withdrawal happen because of the de-regulation?

Sub withdrawal is pure evil....The definition of opiate withdrawal lol.. If it didnt shut down the natural system wouldnt there be no w/ds?

 

[Cane2theLeft]

^ deregulation means the government has less control over industry

Withdrawal happens when, due to receptor down-regulation, you have too many receptor sites and not enough endorphins (in the case of opioids, otherwise whatever neurotransmitter) to attach to them.

If you abstain long enough you'll eventually up-regulate but this takes time.

The natural system isn't shut down; your body just adapts to the presence of the buprenorphine (or whatever drug) and so since it's used to having it and then all of the sudden doesn't, those adaptations body made to try to achieve homeostasis WITH the drug, work against you by producing the opposite effect that the drug did.

 

[narcoticon]

Endorphin is a portmanteau of 'endogenous' and 'morphine'

Super-cool to know.

I know endorphines are, by definition, endogenous, but I wanted to be specifically clear about the source of any molecule able to bind to a receptor. Thanks for the nifty knowledge!

 

[ONandOFF777]

Do drugs like naloxone, naltrexone and buprenorphine (partially) block endorphins?

I guess I am asking if there are endorphins that have a stronger affinity or by taking Suboxone or other antagonist drugs (such as people with implants or who dose daily to prevent opiate use) are people effectively shutting out their own endorphins?

I hear about the “runners high” all of the time. Let’s say one is a long distance runner and regularly runs to the point of experiencing runners high but then one day take Suboxone or even naltrexone would they then not experience the “runners high” or at least not the part related to endorphins?

On the other hand lets say someone who is not opiate tolerant takes something like naltrexone on a daily basis for 2 or 3 months and then stops. Would their body react by producing more endorphins to try and reach homeostasis? Upon stopping the daily regiment of naltrexone would they possibly feel a period of increased well being/euphoria while the body is adjusting to not having an antagonist blocking the endorphins?

I could go on and on about this but ill stop and see if this goes anywhere.

This is a very very interesting subject. Thanks to the OP

 

[NeighborhoodThreat]

Yes, it will inhibit endorphin production and keep your receptors downregulated.

Though buprenorphine is not a particularly strong agonist, its primary metabolite norbuprenorphine is usually produced in enough quantity (especially at low doses) to act as a fairly strong agonist.

This is exactly true. When I do buprenorphine, I try my best to keep the doses low so less of the norbuprenorphine is blocked by the buprenorphine, so it feels more like a full-agonist. I guess "mixed-agonist" should be the term, not sure, however.