ULDN - The magic weapon to reduce and keep tolerance to Opioids low

[Hexenstahl]

Further update:
the receptor reset seems to be somewhat unreliable, but not in terms of tolerance reduction (this will always happen when doing ULDN), but in terms of euphoria. For those who haven't followed this thread: back in January I accidentally found out that a normal naltrexone dose (50mg) brings back the honeymoon phase of opioids. I repeated the same procedure last sunday (of course after I tapered off), waited 72h and then took heroin again expecting that I will experience euphoria again. Unfortunately that didn't happen. I was fully sedated but I felt none of that warm, fuzzy, rose colored glasses feeling, which was extremely disappointing. So either I have done something wrong, or this method is somewhat unreliable. I will repeat the same procedure next month and report back.

 

[cdin]

I have had fantastic long term results with ULDN paired with black seed oil. I don't try to get high though, i just manage pain.

 

[SpiralusSancti]

What about ultra-high doses for a month? That would lower my mild tolerance to 0?
That’s experience from most people I know (and some dead I heard about) but it gets up soon and I would try to prevent that with ULDN.

 

[Rosee26]

I have had fantastic long term results with ULDN paired with black seed oil. I don't try to get high though, i just manage pain.

Can you use the black seed oil with an opiate? For example while tapering... Also does the uldn and bso help manage withdrawals for you? Im about to make the jump and I have chronic pain.

 

[cdin]

Can you use the black seed oil with an opiate? For example while tapering... Also does the uldn and bso help manage withdrawals for you? Im about to make the jump and I have chronic pain.

yes and yes

 

[Hexenstahl]

What about ultra-high doses for a month? That would lower my mild tolerance to 0?
That’s experience from most people I know (and some dead I heard about) but it gets up soon and I would try to prevent that with ULDN.

Not necessary. If you just want to lower your tolerance take ULDN as described. If you want to reset your µ-opioid receptors to feel euphoria again, then you should taper down and jump off, take a normal 50mg naltrexone pill and wait at least 72h, better yet 96h and most importantly: do NOT under any circumstance take any opioid while the full dose of naltrexone is still working on your receptors. Not because you won't feel anything, but rather because the opioid, for some reason, interferes with the naltrexone properly resetting your receptors, so that you won't feel euphoric like you're supposed to as soon as the naltrexone wears off and you start taking opioids again. This is something I learned through experience.

 

[Jabberwocky]

Has anyone tried this for kratom?

I'm getting a script for Naltrexone soon

Kratom pharmacology is atypical though, and is an antagonist itself

 

[Hexenstahl]

Has anyone tried this for kratom?

I'm getting a script for Naltrexone soon

Kratom pharmacology is atypical though, and is an antagonist itself

I'd be interested in knowing that too, even though I don't use Kratom.

 

[Rosee26]

Not necessary. If you just want to lower your tolerance take ULDN as described. If you want to reset your µ-opioid receptors to feel euphoria again, then you should taper down and jump off, take a normal 50mg naltrexone pill and wait at least 72h, better yet 96h and most importantly: do NOT under any circumstance take any opioid while the full dose of naltrexone is still working on your receptors. Not because you won't feel anything, but rather because the opioid, for some reason, interferes with the naltrexone properly resetting your receptors, so that you won't feel euphoric like you're supposed to as soon as the naltrexone wears off and you start taking opioids again. This is something I learned through experience.

It sounds like you have quite a bit of experience with LDN. Im curious if you could answer for me, how long after using opiates after being super dependent would you be able to use LDN without it putting you into precipitated withdrawal? Should I start with ULDN either way?

 

[jambabomba]

Exactly, and this is what made me skeptical. Even if you know that you have overdosed the moment you take another pill, and then swallow a naltrexone pill, it takes way too long to save you from dying. You'd need to get the injectable naltrexone in order for that to work.


Yes of course, that's what the whole post is about. Reducing tolerance and keeping it low. I went from 200mg (which is a high dose in the area where I live) to 70mg.
And yes, it does also work for Kratom since it binds to the opioid receptors just like the "real" opioids.

No, that is not how it works. I agree with the original poster you replied to about this issue of overdosing. It is one thing with injectable opioids when you do not have time but if you are eating opioids they will usually take at least 30-60min to get their full effects. And by eating your body has time to adjust so you will not pass out instantly but slowly fade away. And if you have become accustomed to a certain dose/feeling and feel lets say after 20 minutes of eating your opioids (say codein or moprhine) that now you have taken maybe too much and are in possible dangerzone of passing out then you definately have time to put one 1,5mg naltrexone tab under your tongue and within 5 minutes most of your danger will be gone.

So it is definately possible to prevent opioid overdose by putting naltrexone into your mouth and let it dissolve there as you only need 500-1000ug to prevent fatal overdose or atleast to markedly reduce the effects. So the naltrexone put under your tongue will reduce the effects enough before the opiod has even achieved its maximum peak plasma levels. Then you can keep putting more naltrexone into your mouth put you don't actually need much unless overdose is very severe. I guess few milligrams would be enough in most cases to reduce your high enough out from danger zone and that can be done within time window of under 5mins and when eating opioids time window of 5minutes is certainly enough.

 

[jambabomba]

No, that is not how it works. I agree with the original poster you replied to about this issue of overdosing. It is one thing with injectable opioids when you do not have time but if you are eating opioids they will usually take at least 30-60min to get their full effects. And by eating your body has time to adjust so you will not pass out instantly but slowly fade away. And if you have become accustomed to a certain dose/feeling and feel lets say after 20 minutes of eating your opioids (say codein or moprhine) that now you have taken maybe too much and are in possible dangerzone of passing out then you definately have time to put one 1,5mg naltrexone tab under your tongue and within 5 minutes most of your danger will be gone.

So it is definately possible to prevent opioid overdose by putting naltrexone into your mouth and let it dissolve there as you only need 500-1000ug to prevent fatal overdose or atleast to markedly reduce the effects. So the naltrexone put under your tongue will reduce the effects enough before the opiod has even achieved its maximum peak plasma levels. Then you can keep putting more naltrexone into your mouth put you don't actually need much unless overdose is very severe. I guess few milligrams would be enough in most cases to reduce your high enough out from danger zone and that can be done within time window of under 5mins and when eating opioids time window of 5minutes is certainly enough.

And btw, I actually know this from experience as I have allso took ULDN many years and long time ago to boost my opioids. And I used to to use microgram doses and sometimes when I sensed that I had took either too much opioids or reduced my sensitivity too much with microdoses of naltrexone and started to feel too much shortening of breath or similar I just put more naltrexone under my tongue in those situations (meaning milli- instead of micrograms) and the effects of opioids were allmost instantly reduced. It takes very little time to absorp from mouth. But I never used intravenously so that is a different thing.

 

[jambabomba]

Can someone with knowledge in pharmacology please explain why naloxone is unable to sensitize the opioid receptors as opposed to naltrexone? As far as I know they bind to the same receptors and have the same mode of action, right? Why then is naltrexone so incredibly effective in μ-opioid receptor sensitization? Is it because of the long duration? Help would be much appreciated.

I am not a professional, but I believe the short action of naloxone is the key like you said. Naltrexone's half-life is 4h and its metabolite's has 12h and its also active but naloxone has only 1,5h. By analogy, you will not get tolerance to short acting ex. Sleep medicines like Zolpidem either but can use them quite a long time without desensitazing your gaba system. Or if you use codeine only once daily you will not get much addicted to it or will not desensitize your opioid receptors much and those two has also half lives in similar range as naloxone.

Also, Naltrexone is an inverse agonist unlike Naloxone which is more pure antagonist. That might explain something also. On the other hand not sure how much that plays as also Flumazenil is working similarly with benzos/benzotolerance as Naltrexone with opioids but it isn't inverse agonist either. I am planning to use Flumazenil at some point to reverse my benzo tolerance. There are multiple studies showing it actually does it like naltrexone does to opioid tolerance. I guess Naloxone would work tolerance too but you would just need to use it more often maybe at least 3-4 times per day.

 

[Curious one]

Further update:
the receptor reset seems to be somewhat unreliable, but not in terms of tolerance reduction (this will always happen when doing ULDN), but in terms of euphoria. For those who haven't followed this thread: back in January I accidentally found out that a normal naltrexone dose (50mg) brings back the honeymoon phase of opioids. I repeated the same procedure last sunday (of course after I tapered off), waited 72h and then took heroin again expecting that I will experience euphoria again. Unfortunately that didn't happen. I was fully sedated but I felt none of that warm, fuzzy, rose colored glasses feeling, which was extremely disappointing. So either I have done something wrong, or this method is somewhat unreliable. I will repeat the same procedure next month and report b

 

[blxnc]

Hate to be a bother but if anyone has any research similar to this on benzo tolerance, would be an interesting read

 

[Curious one]

Mr. Hexenstahl, have you heard of or tried naloxone for resetting the receptors?
I have the nasal spray.
I have been prescribed oxy's for 4 years after spinal injury's from car accident. This medication barely works anymore.
After reading your original post I was able to procure a Rx of 3mg LDN, 15 capsules.
Per your recipe I took a 3 mg capsule and mixed thoroughly with 120 ml of water.
Purchased a 1ml dropper and proceeded to try the tolerance reducing recipe.
Unfortunately the neltrexone did not seem to dissolve. It just sits at the bottom of the jar. Apparently there is a non water soluble naltrexone product. If you were me would you take the remaining 42mg's of non water soluble naltrexone after tapering off and try to do the reset?
Thank you for all your work and info.

 

[Juicewrldfan]

Mr. Hexenstahl, have you heard of or tried naloxone for resetting the receptors?
I have the nasal spray.
I have been prescribed oxy's for 4 years after spinal injury's from car accident. This medication barely works anymore.
After reading your original post I was able to procure a Rx of 3mg LDN, 15 capsules.
Per your recipe I took a 3 mg capsule and mixed thoroughly with 120 ml of water.
Purchased a 1ml dropper and proceeded to try the tolerance reducing recipe.
Unfortunately the neltrexone did not seem to dissolve. It just sits at the bottom of the jar. Apparently there is a non water soluble naltrexone product. If you were me would you take the remaining 42mg's of non water soluble naltrexone after tapering off and try to do the reset?
Thank you for all your work and info.

As far as naloxone, I have only seen studies that show it slows tolerance but nothing that says it decreases it. I don’t think it would work. I can’t answer your other question though.

Edit: I take that back. I have found some studies that show that it does have the same effect as naltrexone. Yet maybe they weren’t measuring euphoria effects. So there is an increase in analgesia and such but analgesia increase doesn’t mean always the recreational effects increase as well.

And how would you take a small dose when it’s a nasal device?

Ultra-low dose naloxone restores the antinociceptive effect of morphine in pertussis toxin-treated rats by reversing the coupling of mu-opioid receptors from Gs-protein to coupling to Gi-protein - PubMed

Pertussis toxin (PTX) treatment results in ADP-ribosylation of Gi-protein and thus in disruption of mu-opioid receptor signal transduction and loss of the antinociceptive effect of morphine. We have previously demonstrated that pretreatment with ultra-low dose naloxone preserves the...

pubmed.ncbi.nlm.nih.gov

 

[jambabomba]

Hate to be a bother but if anyone has any research similar to this on benzo tolerance, would be an interesting read

Yes, they use Flumazenil in Italy and some other countries on some clinics and it has been a wonder drug for benzo withdrawals and resetting benzo tolerance.

Intravenous flumazenil following prolonged exposure to lormetazepam in humans: lack of precipitated withdrawal - PubMed

The capacity of flumazenil to reverse benzodiazepine agonist effects has been widely demonstrated. In contrast, the role of flumazenil in precipitating withdrawal symptoms is unclear in humans: the inability of RO 15-1788 to induce benzodiazepine withdrawal seems to be related to the duration of...

pubmed.ncbi.nlm.nih.gov

Benzodiazepine dependence and its treatment with low dose flumazenil - PubMed

Globally benzodiazepines remain one of the most prescribed medication groups, especially in the primary care setting. With such high levels of prescribing it is not surprising that benzodiazepine dependence is common, cutting across all socioeconomic levels. Despite recognition of the potential...

pubmed.ncbi.nlm.nih.gov

The role of flumazenil in the treatment of benzodiazepine dependence: physiological and psychological profiles - PubMed

Two-related studies are presented here, detailing our early experience with benzodiazepine-dependent patients treated with a four-day flumazenil infusion using a novel delivery technique. Patients with long-term benzodiazepine dependence who attended the Australian Medical Procedures Research...

pubmed.ncbi.nlm.nih.gov

Low risk of seizures with slow flumazenil infusion and routine anticonvulsant prophylaxis for high-dose benzodiazepine dependence - PubMed

High-dose benzodiazepine (BZD) dependence represents an emerging and under-reported addiction phenomenon and is associated with reduced quality of life. To date there are no guidelines for the treatment of high-dose BZD withdrawal. Low-dose slow flumazenil infusion was reported to be effective...

pubmed.ncbi.nlm.nih.gov

Intravenous flumazenil versus oxazepam tapering in the treatment of benzodiazepine withdrawal: a randomized, placebo-controlled study - PubMed

Flumazenil (FLU), a benzodiazepine (BZD) partial agonist with a weak intrinsic activity, was previously found unable to precipitate withdrawal in tolerant subjects submitted to long-lasting BZD treatment. The potential use of FLU to treat BZD withdrawal symptoms has also been evaluated...

pubmed.ncbi.nlm.nih.gov

Slow subcutaneous infusion of flumazenil for the treatment of long-term, high-dose benzodiazepine users: a review of 214 cases - PubMed

Despite the first reports concerning benzodiazepine dependence being published in the early 1960s literature, the risk of benzodiazepine addiction is still greatly debated. The severe discomfort and life threatening complications usually experienced by long-term benzodiazepine users who suddenly...

pubmed.ncbi.nlm.nih.gov

Flumazenil reverses the tolerance to anticonvulsant effect of clonazepam

Feasibility of reversing benzodiazepine tolerance with flumazenil - PubMed

To examine whether the benzodiazepine antagonist flumazenil can reverse tolerance to benzodiazepines but without precipitating withdrawal seizures, the antiepileptic effect of flumazenil itself and its ability to reverse tolerance at a dose that would leave sufficient receptors free for the...

pubmed.ncbi.nlm.nih.gov

Clinics in Italy use Flunazepam in practise with great succes

https://onlinelibrary.wiley.com/doi/10.1111/j.1360-0443.2012.03851.x

I am planning to use Flumazenil myself at some point but not sure where to get it from. Maybe ordering from China or something. As it seems allmost impossible to get it from a doctor where I live.. Also I would be interested to use Saclofen for the same purposes of resetting my dysfunctional gaba-b system.

 

[MeDieViL]

Hey dude thats some interesting research, any succesfull anecdotes?

 

[AlsoTapered]

While I can see that ULDN might have benefits for people who use opioids on occasion, it's use in combination opioids (buprenorphine and naloxone) seem mixed - and that's quite a large study.

I know people who will IV the mixture and put up with being sick for 20 minutes to get high for 24 hours. I think it's important to make it clear that while it might help to reduce dependence, it doesn't seem to alter dependence. I mean, people who can control their opioid use impress me, but so often people drift from one place to the other,

It's most certainly of interest, but it's limits should be made clear. It won't (seemingly) prevent addiction. That doesn't make it useless and possibly of great benefit to people using opioids for medical reasons.

 

[Juicewrldfan]

While I can see that ULDN might have benefits for people who use opioids on occasion, it's use in combination opioids (buprenorphine and naloxone) seem mixed - and that's quite a large study.

I know people who will IV the mixture and put up with being sick for 20 minutes to get high for 24 hours. I think it's important to make it clear that while it might help to reduce dependence, it doesn't seem to alter dependence. I mean, people who can control their opioid use impress me, but so often people drift from one place to the other,

It's most certainly of interest, but it's limits should be made clear. It won't (seemingly) prevent addiction. That doesn't make it useless and possibly of great benefit to people using opioids for medical reasons.

Yeah. I don’t think there’s a magic bullet.