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Opioids Ultra low dose naloxone? Not naltraxone

T

tacodude

Bluelighter
Joined
Jan 30, 2014
Messages
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So I need to lower my tolerance and have read great things about ultra low dose naltraxone yet not much on naloxone besides one study that is not clear about whether naloxone works or just naltraxone. Can anybody clear up if naloxone could work for uldn in place of naltraxone being much easier to obtain? I'd really appreciate advice on the topic ASAP
 
I think the problem with naloxone will be the short half life (around an hour I think) instead of 4h and an active metabolite with an even longer HL + the oral bioavailability is like 2% instead of 5-40%, so you'd need to inject it
 
kleinerkiffer said:
I think the problem with naloxone will be the short half life (around an hour I think) instead of 4h and an active metabolite with an even longer HL + the oral bioavailability is like 2% instead of 5-40%, so you'd need to inject it
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Absolutely, you would just be exposing yourself to an hour or 2 of precipitated w/d for nothing, as your tolerance will be more or less the same as soon as it wears off.
 
yeah i think i saw something like this on a DNM while back, someone selling low-dose naloxone nasal sprays, said that it would make the opiate rush better or something? never believed it
 
It will have little to no noticeable effect for most, unless they were to try and use an opiate / oid where you will find that they will not work for the 60 - 90 minutes while the naloxoneis eliminated.

Unless, of course, you have a physical dependence on OPI, where the above will happen, you will go into severe w/d untill the naloxone wears off after which any active OPI's will simply return to the receptor site and unless you are on a long acting drug (i.e an ER version of drugs with a standard duration, or methadone), you will simply return to whatever 'baseline' your body would have been at following any elimination of the drug via usual metabolic processes.

It has no abuse potential whatsoever, as an antagonist it is the last drug on the planet to have any synergy with consecutive OPI use. It's for bringing people round from overdose and nothing else, it will not reduce ones tolerance and, to re - iterate, it is far too short acting for use as 'blocking' agent such as Naltraxone.

After I got sick and tired of watching a friend crank half a gram at a time despite my pleas for him to take it easy, with him constantly falling out on many occasions (usually smashing his head off something as he pitched over) before going blue, I eventually got a product from my DSP called 'Prenoxad' containing a series of IM doses of naloxone 1mg/ml, which I now wave in his face ever time he cooks up, as I'm quite happy to stick him and fall out with him as a result rather than get pissed at his wake. It's just handy to have for myself anyhoo - whenever I IV now I make sure that the Kit and instructions are clearly visible next to my sharps box. Whether anyone would ever have the confidence to use it (it's pretty idiot proof so there is no reason why anyone should not be able to administer it) is in God's hands....

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I tried mixing 8 ug into my shots yesterday and will continue over the next few days. I was thinking the half life would be an issue, but the reason it works is how affects the opiate agonist at the time it binds so it should at least work right? Maybe it should be injected every hour?
 
Honestly fella, your better off trying this by microdosing naltraxone, if what you researched suggests that this will work. You would need a vat of naloxone even using such tiny doses and it just doesn't sound sustainable, especially having to IM 24 x / day + your regular IV use. You will end up holier than the Pope. Save the naloxone in case you really need it, and if you cannot source naltraxone..2 words....

Tolerance break.

It's a good question though and discussion and does provide plenty of food for thought..
 
tacodude said:
I tried mixing 8 ug into my shots yesterday and will continue over the next few days. I was thinking the half life would be an issue, but the reason it works is how affects the opiate agonist at the time it binds so it should at least work right? Maybe it should be injected every hour?
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I don't quite get how this should work.
All I see is you get decreased effects of the opioid you take/get thrown into withdrawal
 
I mean, all that this drug does is displace an OPI agonist from the receptor site, no?

I would have thought that your tolerance is based on more than how much of the drug actually reaches the brain, as this only covers 'behavioural' effects and your overall tolerance to a drug is dependant on other factors, such as metabolism and other pharmacokinetic processes.

I still think it's a good question but after going onto umpteen aspects of this now I'm pretty much back where I started - cannot see why it would work. I know that these robdog 5 day detox clinics use agents such as this to supposedly blast the dependency out of people, but even though I question the use and efficacy of these sorts of detoxes as far as I know it's done using nothing but antagonists.

To think that you can lower your tolerance AND still use without tapering just doesn't make sense, to my feeble brain anyway. You can't have it both ways.
 
I think the idea behind all of this is that opioid tolerance is simply a matter of downregulation of opioid receptors.
Like you start with 100 mu-opioid-receptors take heroin for a few weeks and this leads to internalization of say 50 mu-opioid-receptors.
So you only have 50 mu-opioid-receptors left plus your body decreases the production of endorphines, because you take exogenous opioids.
Now you introduce naloxone to the system -> it kicks off the remaining opioids on the mu-opioid-receptors -> withdrawal and upregulation of mu-opioid-receptors

But internalization of receptors is just one part of the bigger picture
 
kleinerkiffer said:
I think the idea behind all of this is that opioid tolerance is simply a matter of downregulation of opioid receptors.
Like you start with 100 mu-opioid-receptors take heroin for a few weeks and this leads to internalization of say 50 mu-opioid-receptors.
So you only have 50 mu-opioid-receptors left plus your body decreases the production of endorphines, because you take exogenous opioids.
Now you introduce naloxone to the system -> it kicks off the remaining opioids on the mu-opioid-receptors -> withdrawal and upregulation of mu-opioid-receptors

But internalization of receptors is just one part of the bigger picture
Click to expand...

Absolutely, that's the aspect that kind of makes sense but as you said and I intimated, your overall tolerance is a holistic issue and I would assume goes above and beyond the pharmacodydamic's of receptor availability / sensitivity.
 
I will have a gander this very second, but looking at the conclusion it pretty much states what we said above. It looks like a fantastic paper though for me to try and get my head around all the individual ins and outs of the process.
 
Just found this https://www.ncbi.nlm.nih.gov/pubmed/11805221

Opioid agonists such as morphine have been found to exert excitatory and inhibitory receptor-mediated effects at low and high doses, respectively. Ultra-low doses of opioid antagonists (naloxone and naltrexone), which selectively inhibit the excitatory effects, have been reported to augment systemic morphine analgesia and inhibit the development of tolerance/physical dependence. This study investigated the site of action of the paradoxical effects of naltrexone and the generality of this effect. The potential of ultra-low doses of naltrexone to influence morphine-induced analgesia was investigated in tests of nociception. Administration of intrathecal (0.05 and 0.1 ng) or systemic (10 ng/kg i.p.) naltrexone augmented the antinociception produced by an acute submaximal dose of intrathecal (5 microg) or systemic (7.5 mg/kg i.p.) morphine in the tail-flick test. Chronic intrathecal (0.005 and 0.05 ng) or systemic (10 ng/kg) naltrexone combined with morphine (15 microg i.t.; 15 mg/kg i.p.) over a 7-day period inhibited the decline in morphine antinociception and prevented the loss of morphine potency. In animals rendered tolerant to intrathecal (15 microg) or systemic (15 mg/kg) morphine, administration of naltrexone (0.05 ng i.t.; 10 and 50 ng/kg i.p.) significantly restored the antinociceptive effect and potency of morphine. Thus, in ultra-low doses, naltrexone paradoxically enhances morphine analgesia and inhibits or reverses tolerance through a spinal action. The potential of naltrexone to influence morphine-induced reward was also investigated using a place preference paradigm. Systemic administration of ultra-low doses of naltrexone (16.7, 20.0, and 25.0 ng/kg) with morphine (1.0 mg/kg) extended the duration of the morphine-induced conditioned place preference. These effects of naltrexone on morphine-induced reward may have implications for chronic treatment with agonist-antagonist combinations.
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So it's not as crazy as I though
 
Whaaaa I'm still going through the first paper. When it comes to the general standards of our members I know fook all when it comes to psychopharmacology so this will take some time with all the cross referencing I need to get the gist....

They will be read tho klienkiffer so again, thank you for posting. You will just have to bear with a thick slowcoach when it comes to this stuff. While my overall standard of scientific knowledge is generally poor, what reading I do is usually more around physics and cosmology which fascinates me.

As a qualified nurse I always thought that I had a good standard of knowledge of drugs and their effects, but even a nursing degree does bring me anywhere near to the complexity of the discussions on BL.

It's embarrassing, but despite my career background, a 25 year history of polydrug use including 12 years of revolving door heroin dependency and subsequnet methadone maintenance , the first thing I learnt when I was given the privilege of my current role on Bluelight is that I know NOTHING.
 
^No problem :D
I too don't understand everything and I study biology and want to major in drug research or neurosience.


I copied and moved the thread over to N&PD, so hopefully someone more versed will chime in
 
I'll keep an eye kleinerkiffer cheers, even if 90% of the discussion goes over my head, the 10% that I might take on board is 10% more than my sum total at present.
 
https://www.ncbi.nlm.nih.gov/pubmed/16084657

This was the study I looked at, but I had a link with the whole study PDF. I can't find it right now, by the title should explain enough the theory of action.

I'll add no apparent weakening of effect is happening except maybe less pins and needles, which is only a bonus to me. I'm still sleeping in damn nice... Still though I don't dose the narcan when I have to go to work...

Edit: this PDF seems to have a table and discuss uldn with naloxone including a table early on, but is not the one I read. All evidence seems to point to this working, but if it was that easy and already known of wouldn't everyone be doing it?
 
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