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

[Xorkoth]

Naltrexone, at normal dosages, blocks all opioid effects, in fact if you are on a daily dose of naltrexone in the normal doses they prescribe, 5-50mg, you will be utterly unable to feel opiates, because they will be blocked. And if you're dependent on opiates, it will send you into precipitated withdrawal. And if you overdosed, if you somehow managed to get the naltrexone into your bloodstream fast enough (ie, injected), it would prevent overdose.

However, ultra low dose naltrexone is hundreds to thousands of times less of a dose than any dose a doctor typically prescribes. At that dose, it does not block opioids, instead, the antagonism (at least I assume this is how it works) serves to upregulate your opioid receptors, and thus, reduce tolerance.

I have heard way too many stories of this working for people to dismiss it, despite never having tried it myself. I've read the studies, too.

 

[StickToYourGuns]

Will this reduce your tolerance to opioids if you already have one — or does it just prevent you from obtaining a tolerance if you don't already have one?

Also... would it work for Kratom?

 

[Hexenstahl]

And if you overdosed, if you somehow managed to get the naltrexone into your bloodstream fast enough (ie, injected), it would prevent overdose.

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.

Will this reduce your tolerance to opioids if you already have one — or does it just prevent you from obtaining a tolerance if you don't already have one?

Also... would it work for Kratom?

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.

 

[StickToYourGuns]

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.

Excellent - that's good to know. Because I have been using Kratom daily for the past 2.5 years to manage my chronic pain, so the tolerance I have to that plant is ridiculous — I have to take extremely high amounts to just find the adequate relief that I used to find in mild to moderate doses. I may give this a try sometime. Thanks!

 

[bookshelf1]

i want to try uldn...did anyone here try naltrexone orally?on the article which hexanstal has placed it on his first post of this thread

Ultra-Low Dose Oral Naltrexone Decreases Side Effects and Potentiates the Effect of Methadone

The use of N-methyl-D-aspartate (NMDA) receptor antagonists to decrease opioid side effects, potentiate opioid actions, and decrease the development of tolerance has been a topic of substantial interest over the last decade. The pioneering work by Trujillo and Akil suggested that tolerance to...

www.jpsmjournal.com

,they say naltrexone works by mouth for tolerance reduction.injecting pills is a little dangerous i think.especially when you do this daily. im a bit anxious about overdosing on uldn.because i take oxycodone couple times in a day.and they say we shouldn't take our normal dosage after using naltrexone.

 

[Hexenstahl]

i want to try uldn...did anyone here try naltrexone orally?on the article which hexanstal has placed it on his first post of this thread

Ultra-Low Dose Oral Naltrexone Decreases Side Effects and Potentiates the Effect of Methadone

The use of N-methyl-D-aspartate (NMDA) receptor antagonists to decrease opioid side effects, potentiate opioid actions, and decrease the development of tolerance has been a topic of substantial interest over the last decade. The pioneering work by Trujillo and Akil suggested that tolerance to...

www.jpsmjournal.com

,they say naltrexone works by mouth for tolerance reduction.injecting pills is a little dangerous i think.especially when you do this daily. im a bit anxious about overdosing on uldn.because i take oxycodone couple times in a day.and they say we shouldn't take our normal dosage after using naltrexone.

Look, it's very simple. You do NOT take ULDN intravenously. You prepare the ORAL solution the way I described, then start with 5µg, wait half an hour and take a low dose of your opioid of choice. If your tolerance is still high, wait until the naltrexone is out of your system until you redose ULDN. Increase in 5µg increments. Repeat this until you have found the right dose that resets your tolerance. From there on you'll increase your ULDN dosage only if your tolerance to naltrexone has increased.

 

[bookshelf1]

i have naltrexone capsules now,i am just waiting for the right moment to take it.
i have a question.if you had a high tolerance and then use ULDN for couple days.what happens?is your tolerance lower than before even when you're not using naltrexone?what if you just use ULDN for one day.does your actual tolerance come down?or its just a temporary tolerance reduction?

 

[Keif' Richards]

I am definitely not as educated as some of you guys regarding the neuroscience and all of that jazz, but I have an opinion here. This strikes me as something that is theoretically possible, but that in practice will likely be extremely difficult to make work for the average person. My reasoning is that, sure, by doing the math, running the experiments, conducting good research over an extended period of time and under different conditions, could arrive at something resembling a proper protocol that your average person could then adapt for themselves, but again, this seems a little unrealistic.

I'm not raining on anyone's parade here. I enjoy discussing things like this myself just because pharmacology and HR are a love of mine. I think this is useful information that could one day lead to progressive approach to handling Opioid tolerance, but that is probably years away. I'd like to move this over to the neuroscience sub-forum. If anyone feels this is a mistake, let me know and we can talk about it.

 

[Hexenstahl]

I'd like to move this over to the neuroscience sub-forum. If anyone feels this is a mistake, let me know and we can talk about it.

That's perfectly fine with me. I often put my threads into the wrong sub

 

[fastandbulbous]

Facts.

A lot aren't that big on pharmacology either (that from a friend, who's a pathologist, but did a biochem degrre before the medical one).

 

[Hexenstahl]

Addendum:
this stuff is truly a wonder drug. I have noticed an interesting and unintentional side-effect of Naltrexone. I recently tried a full dose (50mg) with the intention to kill off craving for a day. 96h later I took 100mg of Tilidine and was amazed that I felt euphoria. Not that half-assed euphoria that you get when you abstain from opioids for a while, but a good portion of the old warm blanket euphoria during my newbie times came back. 200mg and I was nodding complete with that lovey-dovey rose colored glasses feeling! It took me by total surprise as I did not expect such an effect. It seems that a normal dose of Naltrexone kind of sensitizes the opioid receptors and resets them to an earlier state. For a long time I accepted the fact that as a long-term opioid user I'll never feel that euphoria again and was simply content with the occasional sedation, but this is truly a game changer. This makes it all the more impossible to achieve an opioid free life for me lol.

If anyone here has access to Naltrexone and has currently no opioid tolerance: please try it out and report here if it worked the same way it did for me. There are no reports online about such a side-effect, but I can't believe that this is a coincidence that works only for me. Just to clarify again, ULDN merely reduces tolerance but doesn't make opioids feel like in the past. It merely economizes your use. A normal dose of Naltrexone, however, seems to reset the opioid receptors of addicts to a much earlier state. While it doesn't feel like the first few times, it certainly brings back the honeymoon phase which I find amazing. Wish you Bluelighters all the best

 

[Fertile]

Editorial note: "Ultra-low-dose naloxone suppresses opioid tolerance, dependence, associated changes in mu opioid receptor-G protein coupling, Gβγ signalling" [Neuroscience 135(1)(2005)247-261] - PubMed

Editorial note: "Ultra-low-dose naloxone suppresses opioid tolerance, dependence, associated changes in mu opioid receptor-G protein coupling, Gβγ signalling" [Neuroscience 135(1)(2005)247-261]

pubmed.ncbi.nlm.nih.gov

Ultra-low-dose naloxone suppresses opioid tolerance, dependence and associated changes in mu opioid receptor-G protein coupling and Gbetagamma signaling - PubMed

Opiates produce analgesia by activating mu opioid receptor-linked inhibitory G protein signaling cascades and related ion channel interactions that suppress cellular activities by hyperpolarization. After chronic opiate exposure, an excitatory effect emerges contributing to analgesic tolerance...

pubmed.ncbi.nlm.nih.gov

It's well researched BUT it does not deal with addiction which can be much harder to deal with.

 

[Hexenstahl]

Editorial note: "Ultra-low-dose naloxone suppresses opioid tolerance, dependence, associated changes in mu opioid receptor-G protein coupling, Gβγ signalling" [Neuroscience 135(1)(2005)247-261] - PubMed

Editorial note: "Ultra-low-dose naloxone suppresses opioid tolerance, dependence, associated changes in mu opioid receptor-G protein coupling, Gβγ signalling" [Neuroscience 135(1)(2005)247-261]

pubmed.ncbi.nlm.nih.gov

Ultra-low-dose naloxone suppresses opioid tolerance, dependence and associated changes in mu opioid receptor-G protein coupling and Gbetagamma signaling - PubMed

Opiates produce analgesia by activating mu opioid receptor-linked inhibitory G protein signaling cascades and related ion channel interactions that suppress cellular activities by hyperpolarization. After chronic opiate exposure, an excitatory effect emerges contributing to analgesic tolerance...

pubmed.ncbi.nlm.nih.gov

It's well researched BUT it does not deal with addiction which can be much harder to deal with.

I just found it incredible to feel that old euphoria again, but yeah it'll be even more hard to quit.

 

[bigmeechLH]

Can you do the OP's ULDN recipe with capsules? I can get some, but am unsure if I'd be able to properly dissolve in the distilled water. Any input here would be great! Thanks

 

[plumbus-nine]

Can you do the OP's ULDN recipe with capsules? I can get some, but am unsure if I'd be able to properly dissolve in the distilled water. Any input here would be great! Thanks

You would need to cut a single pill into hundreds of fractions, this is the reason why volumetric dosing is used.

Welcome to bluelight btw!

 

[bigmeechLH]

I'm fairly experienced with volumetric dosing.

I'm just not sure what's in a naltrexone capsule. The guides I've seen have always referenced pills. Like perhaps the naltrexone capsules have little coated beads inside or something. Does anyone know about that?

Hopefully it's just a powder/something that lends itself to dissolution in distilled water.

Thanks

 

[Hexenstahl]

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.

 

[plumbus-nine]

I imagine that naloxone's duration will be too short, yeah, like why memantine is much more effective at alleviating opioid dependence than ketamine is but I'm by no means sure.

 

[Snafu in the Void]

Does anyone suppose this may work with kratom as well?

 

[plumbus-nine]

Does anyone suppose this may work with kratom as well?

I think it should, not completely but for the opioid part of mitragynine. See no reason why it shouldn't.

Wonder whether ULN when taken without an opioid was still worthwile and sensitizing the receptors to endorphins?