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

[tacodude]

As the title states does it work to use narcan before using bupebupe and hopes to prevent precipitated withdrawals. My thoughts are that the narcan would rip off any full agonist and replacing with a full antagonist so when the bupe enters the system it rips off anatagonist for a partial agonist vs a full agonist being ripped off for a partial agonist. I am assuming it doesn't work like that and the precipitated WD comes from the bupe knocking off whatever was bound and not just from going to a full agonist to a partial agonist/antagonist as if it did work then it would become a standard for bupe induction. Then again it might me a method no one has ever attempted. If anyone has any thoughts or experiences I would love to hear them.

 

[CfZrx]

Hi Taco, I read a study where they used a butrans patch in between the subjects last opiate of choice and daily buprenorphine films. It worked perfectly to avoid precip wd.

 

[tacodude]

That has nothing to do with what I asked and a user Homer suggested that using bupe with a full agonist allows one to stop bupe for the full agonist while being able to resume bupe without precipitated w/d

(Edit: thank you though for a fast response)

I am suggesting knocking the agonist off with narcan and using bupe right after to rip the narcan off for the bupe in hopes to go from antagonist effect to partial agonist/antagonist vs going from full agonist to partial agonist/antagonist.

 

[d1ahp]

I'm eager to hear the answer on this. Given my minuscule level of knowledge, your logic sounds reasonable to me.

 

[Soulgasm]

I don't understand your logic. Naloxone causes precipitated wd's itself.

 

[RDP89]

I don't understand your logic. Naloxone causes precipitated wd's itself.

Exactly. The same way the bupe causes precipitated w.d.'s is the way naloxone will, by pulling the opioids off your receptors.

 

[Mad Dash]

oops losing mt mind today.

 

[SixBuckets]

NARCAN is naloxone, not naltrexone.

 

[Mad Dash]

NARCAN is naloxone, not naltrexone.

Duh, sorry my dumbass is having a bad day.

 

[JessFR]

It's an interesting idea.

I assume your logic is that while the naloxone will put you into precipitated withdrawal, the buprenorphine will then take you out of it again.

The logic sounds sound to me too. As buprenorphine does indeed have a higher affinity than naloxone despite common belief to the contrary. Will it work? I don't know. I know I wouldn't go first.

 

[tacodude]

JessFR got it and I'm with him I wouldn't go first..... Not without being inpatient medical care to make sure I'm as comfortable through it as possible if it doesn't work. Does bupe withdrawal happen from ripping whatever's bound to the opiate receptor be it an agonist or antagonist? Or is it possible to cause precipitated withdrawals with narcan that can be immediately undone with an injection or sublingual (≈5 minutes vs immediate) dose of bupe to make sure one isn't thrown into a half hour or more of unreversable precipitated withdrawals accidentally using bupe to soon after your last dose especially possible if using "bth" that turns out to be produced cut with methadone making the time needed in between the last dose that much longer without knowledge.

Plus waiting 24+ hours going into withdrawals likely 12-18 hours of those 24 hours being at there worst is just a nightmare and being able to just rip off the agonists all at once and replacing it with bupe would be awesome although honestly I still think one needs to wait until they are starting to feel withdrawals as before that point the medication is active and even using narcan and then bupe would not relieve it as quickly as even though all the agonist is ripped off the pathways will still have to go from active to inactive specifically in the kappa region while the Mu would go from a strong activation to weaker possibly.....

Essentially it would be used as insurance that bupe won't throw someone into precipitated withdrawals if dosed and not to go from being on a full agonist to bupe without withdrawals as it will happen.

 

[Hodor]

As the title states does it work to use narcan before using bupebupe and hopes to prevent precipitated withdrawals. My thoughts are that the narcan would rip off any full agonist and replacing with a full antagonist so when the bupe enters the system it rips off anatagonist for a partial agonist vs a full agonist being ripped off for a partial agonist. I am assuming it doesn't work like that and the precipitated WD comes from the bupe knocking off whatever was bound and not just from going to a full agonist to a partial agonist/antagonist as if it did work then it would become a standard for bupe induction. Then again it might me a method no one has ever attempted. If anyone has any thoughts or experiences I would love to hear them.

This would only "work" in the sense that the Naloxone would induce such an extremely unpleasant form of precipitated withdrawal that the moderately unpleasant precipitated withdrawal induced by the buprenorphine would seem like an upgrade by comparison.

 

[tacodude]

Are you positive hodor that it would go from extreme precipitated withdrawals to less extreme? Even if one waits until they feel things wearing off and beginning to enter withdrawals in hopes one doesn't have to withdraw for 12+ hours before going into bupe? Do you have any evidence to back up your statement or are you just pulling that opinion out of your ass? If so I'm not interested in that and hope if there has never been an attempt to do something like this that some research actually be done legitimately if not than even if just one member gave it a shot and reported back I'd be pretty satisfied. As I said bullshit responses pulled out of your ass with no reasoning and presented as fact is the last thing needed in this thread I created and ask you please keep those opinions to yourself and take that attitude elsewhere as I don't need this thread becoming cluttered pages and pages of assumptions vs statements backed by actual evidence

 

[kleinerkiffer]

You may find reading this interesting http://www.ncbi.nlm.nih.gov/books/NBK64236/#A72334

Precipitated withdrawal also occurs in individuals who are physically dependent on mu agonist opioids. Precipitated withdrawal usually occurs when an individual physically dependent on opioids is administered an opioid antagonist. In an individual who is not physically dependent upon opioids, the acute administration of an antagonist typically produces no effects. In an individual who is physically dependent on opioids, however, an antagonist produces a syndrome of withdrawal that is qualitatively similar to that seen with spontaneous withdrawal (although the onset is faster and the syndrome is shorter, depending on the half‐life of the antagonist). One way to conceptualize precipitated withdrawal is that the antagonist displaces agonists from receptors, but because the antagonist does not activate the receptor, there is a net decrease in agonist effect, resulting in withdrawal.

It is also possible for partial agonists to precipitate withdrawal. If an individual who is physically dependent on opioids receives an acute dose of a partial agonist, the partial agonist can displace the full agonist from the receptors yet not activate the receptors as much as the full agonist had. The net effect would be a decrease in agonist effect and a precipitated withdrawal syndrome. Precipitated withdrawal with a partial agonist is more likely to occur in an individual who has a high level of physical dependence (e.g., high use of opioids each day), who takes the partial agonist soon after a dose of full agonist, and/or who takes a high dose of the partial agonist.

Buprenorphine is a partial agonist that exerts significant actions at the mu opioid receptor. As reviewed in the previous section, however, its maximal opioid effects are less than that of full agonists

Administration of buprenorphine can precipitate an opioid withdrawal syndrome. Although there is much

variability in response to buprenorphine, precipitated withdrawal symptoms tend to be milder than those produced by antagonist‐precipitated withdrawal, and intervention is rarely required. In controlled studies in which buprenorphine was given to individuals who were physically dependent on opioids, the precipitated withdrawal syndrome was both mild in intensity and easily tolerated (Strain et al. 1995). However, at least one open‐label small‐sample trial of low‐dose buprenorphine caused a patient to experience pronounced, precipitated, and poorly tolerated withdrawal of severe intensity (Banys et al. 1994). The probability of precipitating a withdrawal syndrome is minimized by reducing the dose of mu agonist before buprenorphine treatment is initiated, by allowing a longer elapsed interval between last agonist dose and first buprenorphine dose, and by starting treatment with a lower buprenorphine dose.

If you want to, I can elaborate my theory, based on this paper/book. I'm pretty sure Hodor is right.

 

[Cliffy78]

I don't understand your logic. Naloxone causes precipitated wd's itself.

Exactly and napa one is only active for about 20min ime/IMO and then the opiates reattach to the receptors. The Bupe would still rip the opiates off after that. This is why people who get narcaned need to be observed because they can of again when the naltrexone wears off. Subs have pulled me outta od but it can right back once the naltrexone in the sub wears off. I honestly don't see this working for most people and don't think it should be attempted unless one wants to suffer badly... Just my .02 cents

 

[tacodude]

I don't think you understand me completely.... I understand what that says completely and already understand it. My thoughts are not to cause precipitated withdrawals and undo them with bupe, but instead to use the narcan something like 8-12 hours after the last dose of whatever with a half life no greater than 4 hours as by that point most should be unbound and one should already be pretty much in withdrawals so when the narcan is administered it doesn't precipitate WD as it's already happening. Although it makes 100% sure the full agonist opiates are ripped off the receptors most likely making the already occurring withdrawals worse although hopefully not nearly as severe as using narcan while there is an active dose of the full agonist bind to the receptors. That way when the partial agonist is applied it goes from having little to no activation even with the full agonist still bound here and there to full antagonist (again only to rip off the last of the agonist that are clinging on yet not activating enough to give relief allowing withdrawals to begin) to having the partial antagonist move in and bind and activate it hopefully moreso than it was with the full agonist bound here and there while it never will come close due to the antagonist effect at the kappa that until the norbupe metabolite forms, which has the ability to agonize the kappa if I'm not mistaken from a couple opinions I've read from posts on this board.

No matter what bupe has that period of not giving full relief at first due to the norbupe not forming until the body metabolizes enough bupe to produce enough norbup (again if I understand the metabolite piece that allows less to be more, which seems only true after stabilizing and not during induction), but the hopes is to speed up the transition from the full agonist to partial agonist as quickly as possible without creating the lasting discomfort that one has to go through if they wait 24+ hours and at worst causing it for five or ten minutes before it starts getting better granted probably gradually over ten-thirty minutes rather than taking thirty minutes before the precipitated WD starts wearing off, which could take more than the half hour before it starts getting better as precipitated WD don't just stop in an instant, but gradually after lasting at least a half hour at a stable worst state.

Again I'm hypothesising here, but I see no evidence that confirms one way or another. Just a general understand that explains it can really go either way after it initiates the precipitated WD from the full antagonist... To say the least I doubt it will go from severe antagonist WD to less severe partial agonist WD as I've gone through both (used narcan while on scripted morphine just to know what I'm putting someone I'd be rescuing through) and really they were both pretty severe where honestly the bupe was more severe 6 out 8 hours after doses of oxycodone I had vs the narcan while I was on a sustained released morphine prescription.

 

[Cliffy78]

Some people like myself don't get the precip wds at all, I've taken subs to come outta wd 20min after dosing heroin and was just fine, and this was on multiple occasions. I think were all different with how we react to Bupe and naltrexone. I usually try to wait about 6hrs from my last dose of h or oxy just in case and I've always been fine.
Now I'm in no way saying anyone else should try this but I'm just using myself as an example that there's no hard rules for how Bupe affects everyone the same cause we all react differently.

 

[kleinerkiffer]

Let me try to explain by giving an example.
Lets say you have 100 mu-opioid recepors. You take some morphine and 100 morphine molecules bind to your 100 mu-opioid recepors, morphine has an Intrinsic Activity of lets say 100% so all of your receptors are saturated and opend 100 %.
Now you wait and more and more morphine molecules dissociate from your receptors. You go into withdrawal.
Now you introduce naloxone. Naloxone has a higher affinity as morphine, so it kicks off all of the morphine molecules left on your receptores. You go into full blown withdrawal as all of your 100 mu-opioid recepors are bound to naloxone.
Now you take some bupe. Bupe has an even higher affinity as naloxone, so it kicks off the naloxone on your receptors.
All of your 100 mu-opioid recepors are now saturated with bupe, but bupe only being a partial agonist the Intrinsic Activity is lower than the one of morphine.
So you end up with 100 bupe molecules bound to your 100 mu-opioid recepors but bupe has an Intrinsic Activity of lets say 50 % so you have only 50% of the activity you had with morphine, thus you will still experience withdrawal.
I hope you get what I'm trying to say.

 

[d1ahp]

People who have a hard time getting this.

I think Taco means:

1. Get Narcan into your body, go into withdrawal right away. No waiting 12-48 hours for the appropriate point in order to dose Buprenorphine without risk of precipitated withdrawal. Read on to understand why not just dose Bupe since it cause PWDs too.
2. Go through precipitated withdrawal long enough to knock any and all opiates from receptor sites. Something tells me, precipitated withdrawal from Naloxone will be less severe than the precipitated withdrawal from way more powerful Buprenorphine.
3. Dose Buprenorphine, since its affinity is higher than Naloxone, it'll knock it off. Since Naloxone is an antagonist, Bupe should work as if you're taking it after the proper waiting period or the first time. Everyone knows that if you take Buprenorphine after 3-4 days of withdrawal, you don't need a ridiculous dose and it actually works right away without the need for a couple of days adjustment period most people need in order to feel normal again.

Dosing Bupe too early, doesn't cause PWDs for me. But, I will need 4 days to for it to completely work, as in, feel completely normal. BUT, if you wait until you're slightly past the severe withdrawal point, and then dose Bupe at 2-3MG(to reap more of its full agonist properties, info is available via search function), it feels Bupe works right away. You even get a nice warm buzz.

Bupe is extremely powerful, those people dosing 16-24MG daily simply didn't do their intake right. Of course its creators wouldn't want to market it as "wait tll your WD is pretty much done, then dose" type of drug, but that's how Bupe works the best. If you take it too early, you end up needing 8-24MG of it to try and feel better.

The sad part is that doctors are completely clueless about the shit they're peddling. It makes my blood boil.

 

[kleinerkiffer]

I really hope that sekio will shed some light on this question