Bupe using narcan before bupe in hopes to avoid precipitated withdrawals... does it work?

[d1ahp]

To add to my point number 3:

If you dose Bupe too early and don't go into precipitated withdrawal, you're still not "winning" because you're going from your full agonist to a partial agonist. This is what causes the discomfort and that adjustment period. Suboxone has attached itself, but isn't releasing all that you need at this point to feel normal.

If you were to go from a full antagonist(Naloxone), which has knocked off any full agonist opiates, attached itself and put you into a full on withdrawal, to a partial agonist like Buprenorphine which will over power our antagonist friend. This, theoretically, should provide a full on relief from WDs like Suboxone/Subutex is intended to provide if it is used correctly.

You'd basically go from a full on agonist which makes you *happy*. On to a full on antagonist which will put you into day 3 agony of withdrawal. Then finally, onto a partial agonist, which is very reminiscent of your full agonist action.

Bypassing the process of going straight from full agonist to a very powerful partial agonist would avoid that awful transition period of not feeling good on Suboxone but not being able to do your DOC in order to feel better.

If you're anything like me, then waiting the proper amount of time to correctly do Suboxone intake is anything but easy and 90% of the time I end up going back to my DOC. Though, I do have experience with waiting the proper amount of time and then taking Sub. The latter provides a full on WD relief within minutes while the former requires days of adjustment.

 

[crzydiamond]

Having had wd due to narcan, and also precip wd due to bupe, I can say neither is comfortable. Both hit you like a ton of bricks. The only advantage to narcan(naloxone) is that unlike bupe it is short lived and the agony wear off quickly.

But as a poster above stated--narcan (naloxone) wears off quickly and those full agonists are still in your body. As soon as the naloxone wears off the full agonist re-fills the receptors and you're back to square one.

Now, could it possibly work if you were to take the narcan (naloxone) and go into withdrawal and then soon after take the bupe? I'm not sure on that. But I think you would still be in such agony that the bupe wouldn't be likely to help. Because either way you are going from a filled receptor to an empty or partially filled receptor.

You *might* feel slightly better from the bupe if you took it while in the worst of the narcan wd. But overall would it put you to "normal"? That I doubt, because your receptors are still used to full agonists and now will be with a partial agonist at best

It would be nice if there were a magic simple transition...but I don't see this one being it. Still, the concept is interesting

 

[d1ahp]

Having had wd due to narcan, and also precip wd due to bupe, I can say neither is comfortable. Both hit you like a ton of bricks. The only advantage to narcan(naloxone) is that unlike bupe it is short lived and the agony wear off quickly.

But as a poster above stated--narcan (naloxone) wears off quickly and those full agonists are still in your body. As soon as the naloxone wears off the full agonist re-fills the receptors and you're back to square one.

Now, could it possibly work if you were to take the narcan (naloxone) and go into withdrawal and then soon after take the bupe? I'm not sure on that. But I think you would still be in such agony that the bupe wouldn't be likely to help. Because either way you are going from a filled receptor to an empty or partially filled receptor.

You *might* feel slightly better from the bupe if you took it while in the worst of the narcan wd. But overall would it put you to "normal"? That I doubt, because your receptors are still used to full agonists and now will be with a partial agonist at best

It would be nice if there were a magic simple transition...but I don't see this one being it. Still, the concept is interesting

For sure, there's no magic in WDs and transitions. That's a given.

Heroin/DOC would still be bioactive, but how much of it is attached at the site would depend on how much Naloxone is administered. I'm not too knowledgeable on Naloxone, but I would guess that body stress issues would arise from doses of Naloxone high enough to completely take all of the heroin off the receptors.

While Naloxone is active, receptors i what's important here. It doesn't matter that there's still your DOC in your system. Once Bupe gets in, it'll rip Naloxone off the receptors unless you wait long enough for Naloxone to lose its action. Then, obviously, it'll be Heroin/your DOC that Bupe is violently knocking off to attach itself.

Obviously, this is all just theoretical babbling, but you can't deny that this has some potential or is at least a very interesting thought.

 

[speedballs_over]

This doesn't require so much debate.

Full agonists that are generally available, ex. maybe fent & it's analogs, are weaker binders than either naloxone or bupe.

Either will probably cause precip. w/ds, if you don't allow natural withdrawal to begin.

Why would anyone do this? If you can't handle the time b/w last use of agonist to sufficient w/ds for bupe induction you need to re-evaluate your situation and consider methadone therapy / taper instead. A 28 day methadone taper isn't that difficult, though access is a bitch.

Ride it out, and take the bupe in due time. Trying to accelerate the process like this is similar to rapid withdrawl "treatments" popular in the mid-2000s but without being sedated and unconscious, hell on earth for most. Only diff., is that you end up on bupe, not something terrible like naltrexone or nothing.

Only advantage, maybe quicker to get to bupe, but is it worth the worst type of w/ds that may last longer than you anticipate? If you can't handle normal w/ds what makes you think you won't be trying to get someone to bring you dope or going to the ER in a panic?

Just let the agonist metabolize and be eliminated b/f loading in a partial antagonist like bupe. I just don't get the advantage.

Just my opionion, not arguing.

 

[Hodor]

While Naloxone is active, receptors i what's important here. It doesn't matter that there's still your DOC in your system. Once Bupe gets in, it'll rip Naloxone off the receptors unless you wait long enough for Naloxone to lose its action. Then, obviously, it'll be Heroin/your DOC that Bupe is violently knocking off to attach itself.

Obviously, this is all just theoretical babbling, but you can't deny that this has some potential or is at least a very interesting thought.

I still don't see the "potential" - like, what does it matter if the thing the bupe is displacing happens to be Naloxone or a full agonist? Receptors don't feel pain, as if "violently knocking off" a full agonist is like ripping off a band-aid.

The problem is that your nervous system has been spoiled rotten (i.e. your receptors have downregulated) by constantly being supplied with a decent amount of full agonists. It's going to take a while for your brain to adjust to the fact that it's no longer riding the opioid gravy train, and that Bupe is going to be as good as it gets. You can't "shock some sense" into it by dosing yourself with Narcan for a few minutes.

 

[d1ahp]

I still don't see the "potential" - like, what does it matter if the thing the bupe is displacing happens to be Naloxone or a full agonist? Receptors don't feel pain, as if "violently knocking off" a full agonist is like ripping off a band-aid.

The problem is that your nervous system has been spoiled rotten (i.e. your receptors have downregulated) by constantly being supplied with a decent amount of full agonists. It's going to take a while for your brain to adjust to the fact that it's no longer riding the opioid gravy train, and that Bupe is going to be as good as it gets. You can't "shock some sense" into it by dosing yourself with Narcan for a few minutes.

It matters a lot. Because the Bupe is either knocking off an agonist to make go into a precipitated withdrawal or an unsuccessful intake or, theoretically, an antagonist to avoid the unsuccessful intake. Maybe you don't understand the point I'm trying to make

Another point where you misunderstood me is receptors. I'm aware that receptors don't feel pain when Bupe "violently" replaces whatever is present with itself. You're the one who feels pain because of the violent exchange that happens at the receptor side.

My point is that this adjustment that you're talking about can potentially be greatly improved. Down regulation needs to happen in order for the brain to be satisfied with Bupe. Throwing yourself into a withdrawal with Naloxone instead of Subs just might improve this process.

 

[tacodude]

People don't seem to get partial agonist. That doesn't mean it binds to Mu partially, but that it agonises the Mu and Delta sigma(one receptor that is unique action in bupe other opiates don't bind to) while antagonizing the kappa region. I'm shocked at how hard it is for some people I've seen make posts on the subject of bupe who not only get the fact above, but who don't understand my theory. I am on my way to induce bupe in patient now (my choice to a degree as I would prefer a full agonist fit pain management, but fuck that CA doctor getting charged with manslaughter changing the whole fucking system) and while of course I can't test this theory it is the reason I started thinking about it. Anyways I will not have much access so I'll check back in later to clear things up hopefully after this weekend I'll make it clear barely anyone understands my idea. It's not too skip the wait, but to make sure that after 6, 8, 12, or etc. nothing will be on the receptor to cause precipitated withdrawal that will last and can't be undone even if it does cause a precipitated withdrawal to a degree as one at that point should already be in withdrawal symptoms therefore it can't be precipitated as it already exists only made worse. Then before the narcan wears off allowing whatever's left of the full agonist to rebind bupe is used to replace the nalaxone, which is then bound is powerfully and long enough the full agonist can't rebind and floats in the synapse until it is metabolized fully. If you can't understand that you just won't understand my concept and no reason to try only to confuse anyone who wants to try and understand.

 

[fractiousrabbit]

6 months ago, I did this with 1 mg naloxone via MAD (mucosal atomization) device. I waited an hour before the bupi, no particular reason for the timing, was just winging it. The buprenex was administered SQ and I basically felt simply "level" but lacking some motivation. This was 8 hours past the last full agonist. The hour between naloxone and bupi wasn't horrific withdrawal, to th

 

[fractiousrabbit]

Sorry for the incomplete, I must have got click happy...Anyways it was just back to the orthopedic pain but probably more severe as it had been getting blunted for 2 years.

 

[Hodor]

People don't seem to get partial agonist. That doesn't mean it binds to Mu partially, but that it agonises the Mu and Delta sigma(one receptor that is unique action in bupe other opiates don't bind to) while antagonizing the kappa region.

No, what you are describing (agonist at some subtypes, antagonist at others) is a mixed agonist-antagonist.

A partial agonist is an agonist that, once bound, has an efficacy that is significantly lower than the endogenous ligand but also significantly higher than 0.

Bupe is both of the above, but the reason you're feeling precipitated withdrawal is the partial agonism.

 

[tacodude]

My bad thanks for correcting me hordor. In case anyone is wondering my bupe is going well.... Only my sciatic right leg pain out of three pain areas get difficult and not that bad. Going to maintain with 8/4 or 4/8 dosing, whichever works best as far as not causing sedation in daytime and allowing nighttime sleep. Also met someone who was in bupe trials before they started using it given extremely high doses where now they stabilize with 10 mg oc ER 2x a day told me she ended up nodding on those high doses of bupe.... I was surprised.

 

[ferinox]

I don't think it would work. The beta arrestins and other mechanisms that are keeping the opiates receptors resistant to the effects of a partial agonist wouldn't magically dissipate because the receptors were briefly touched by nalaxone. Depletion of full agonist plasma levels is part of it but time to resensize to a lower levels of stimulation probably is too. Spending enough time in naloxone precipitated withdrawal doesn't sound worth it.