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Heroin Naloxone in Heroin withdrawl?

Zopiclone bandit

Zopiclone bandit

Temporary Ban
Joined
Jan 25, 2018
Messages
14,237
What would happen if someone took a I.M. shot of one of the Naloxone Epi-pen looking things if in Heroin withdrawl?
Would it stop you being dopesick?
 
Delam said:
It wouldn't effect anything. There are already no opiates on the receptors which is why they are crying out in pain and longing. Never met anyone who has tried it however so curious to hear any first hand accounts.
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I'm not so sure, I.V. use of buprenorphine subutex was a big thing in Finland, who would have known shooting that stuff had the same kind of effect as Heroin.
 
Yeah all i imagine that would happen is it would very quickly displace whatever opiates still clung on to your receptors, producing horrible agony. If there were no opiates on your receptors to start with, and you were in a detox state, the naloxone would bind to the receptors, but since it does not activate them there would be no relief or euphoric effect from it. Theoretically it would just make future use (Until the naloxone metabolizes) of opiates more difficult/require more for the same effect.
 
Zopiclone bandit said:
I'm not so sure, I.V. use of buprenorphine subutex was a big thing in Finland, who would have known shooting that stuff had the same kind of effect as Heroin.
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Buprenorphine is a partial agonist, and it is much more potent (higher affinity) than naloxone (naloxone in suboxone is, frankly, a marketing move).

Naloxone is a pure antagonist of the mu opioid receptors. This adds nothing, while blocking any endorphin or enkephalin signaling.

Though I’ve always wondered if naloxone could be microdosed and used like ultra low dose naltrexone, to reverse the inflammatory effects of using opioids long term (via blocking the toll-like receptor 4 signaling that opioid agonists tend to drive).
 
Skorpio said:
Buprenorphine is a partial agonist, and it is much more potent (higher affinity) than naloxone (naloxone in suboxone is, frankly, a marketing move).

Naloxone is a pure antagonist of the mu opioid receptors. This adds nothing, while blocking any endorphin or enkephalin signaling.

Though I’ve always wondered if naloxone could be microdosed and used like ultra low dose naltrexone, to reverse the inflammatory effects of using opioids long term (via blocking the toll-like receptor 4 signaling that opioid agonists tend to drive).
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"inflammatory effects".. can you elaborate?
 
evo4ever said:
"inflammatory effects".. can you elaborate?
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Opioids act as agonists at this receptor called toll like receptor 4 (TLR4)(and I’m generalizing with morphine/fentanyl scaffolds in mind). These receptors are on immune cells and normally sense molecules that tend to be part of pathogens (double stranded RNA, lipopolysaccharide, single stranded DNA). Activating these receptors causes the production of inflammatory cytokines, which make immune cells more active.

In the case of opioids, this immune involvement is likely to be a significant contributor to long term opioid issues, like how they can worsen chronic pain. This is likely to be involved in opioid tolerance to some degree.
 
Skorpio said:
Opioids act as agonists at this receptor called toll like receptor 4 (TLR4)(and I’m generalizing with morphine/fentanyl scaffolds in mind). These receptors are on immune cells and normally sense molecules that tend to be part of pathogens (double stranded RNA, lipopolysaccharide, single stranded DNA). Activating these receptors causes the production of inflammatory cytokines, which make immune cells more active.

In the case of opioids, this immune involvement is likely to be a significant contributor to long term opioid issues, like how they can worsen chronic pain. This is likely to be involved in opioid tolerance to some degree.
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Can this phenomenon be counter-acted by Corticosteroids? I've been taking Oxycodone for nearly 10 years and I've never experienced this issue.
 
evo4ever said:
Can this phenomenon be counter-acted by Corticosteroids? I've been taking Oxycodone for nearly 10 years and I've never experienced this issue.
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Possibly, but it would certainly not be worth all the other effect of corticosteroids. Corticosteroids both activate and inhibit a whole host of processes that tend to tamp down inflammation.

Inflammation is a super shitty term because it encompasses a whole host of similar processes which have different outcomes and are generally not synonymous to one another.

Here is a review (open access) if you are interested in the fine details of opioid/inflammatory crosstalk.
 
Skorpio said:
Possibly, but it would certainly not be worth all the other effect of corticosteroids. Corticosteroids both activate and inhibit a whole host of processes that tend to tamp down inflammation.

Inflammation is a super shitty term because it encompasses a whole host of similar processes which have different outcomes and are generally not synonymous to one another.

Here is a review (open access) if you are interested in the fine details of opioid/inflammatory crosstalk.
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There's always a catch to everything lol.
 
Skorpio said:
Buprenorphine is a partial agonist, and it is much more potent (higher affinity) than naloxone (naloxone in suboxone is, frankly, a marketing move).

Naloxone is a pure antagonist of the mu opioid receptors. This adds nothing, while blocking any endorphin or enkephalin signaling.

Though I’ve always wondered if naloxone could be microdosed and used like ultra low dose naltrexone, to reverse the inflammatory effects of using opioids long term (via blocking the toll-like receptor 4 signaling that opioid agonists tend to drive).
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Maybe something you wanna watch, this is an amazing film.

"The documentary follows several young drug abusers, but focuses on Jani Raappana. Jani is a drug addict, whose drug of choice is Subutex taken intravenously."

Documentary Film makers & Film Productions. Watch Documentaries Online

Documentary on Without moralizing, the film shows the real life of a group of friends in the Arctic Circle, dabbling in petty crime and hard drugs. Disturbing,...
www.cultureunplugged.com www.cultureunplugged.com

Thanks for the reply btw, I live & learn each day.
 
Skorpio said:
Opioids act as agonists at this receptor called toll like receptor 4 (TLR4)(and I’m generalizing with morphine/fentanyl scaffolds in mind). These receptors are on immune cells and normally sense molecules that tend to be part of pathogens (double stranded RNA, lipopolysaccharide, single stranded DNA). Activating these receptors causes the production of inflammatory cytokines, which make immune cells more active.

In the case of opioids, this immune involvement is likely to be a significant contributor to long term opioid issues, like how they can worsen chronic pain. This is likely to be involved in opioid tolerance to some degree.
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Can this be the explanation why i suffer leukocytosis since and ONLY since i started taking opioids ? 15 years ago and 14 years of leukocytosis.
 
Skorpio said:
In the case of opioids, this immune involvement is likely to be a significant contributor to long term opioid issues, like how they can worsen chronic pain.
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Sorry but I am kinda stupid & I am not sure I follow you here, please forgive my stupidity here.

What you are saying in simple words is if you have used Heroin (for 1 example) for ages, say 24 years in my experience that will make pain worse?
 
Zopiclone bandit said:
Sorry but I am kinda stupid & I am not sure I follow you here, please forgive my stupidity here.

What you are saying in simple words is if you have used Heroin (for 1 example) for ages, say 24 years in my experience that will make pain worse?
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Depending on the type of pain, it might. This effect seems to be worse in cases of neuropathic pain.
 
evo4ever said:
Can this phenomenon be counter-acted by Corticosteroids? I've been taking Oxycodone for nearly 10 years and I've never experienced this issue.
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The ideal option would be things that block TLR4 directly & indirectly. Cortisol is not appropriate for this imo. There's a few options on this thread.

...structurally diverse opioids (including the clinically relevant agonists morphine, fentanyl, remifentanil, methadone, oxycodone, buprenorphine, meperidine and antagonists naloxone and naltrexone) interact with TLR4
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Drugs like opioids, alcohol and psychostimulants activate TLR4 signaling and subsequently induce proinflammatory responses, which in turn contributes to the development of drug addiction. Inhibition of TLR4 or its downstream effectors attenuated the reinforcing effects of opioids, alcohol and psychostimulants, and this effect is also involved in the withdrawal and relapse-like behaviors of different drug classes.
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You certainly wouldn’t stop being dopesick. If it was that simple everyone would be doing it. I think it would depend on how dopesick you are. If you are just beginning to be sick it will probably throw you into precipitated withdrawal but if you were deep into withdrawal like at the peak then it probably wouldn’t do anything.
 
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