Naltrexone and using heroin

[polo792]

I have been on the naltrexzone for sometime now but I have been using heroin as well, I don't feel stone after using it but just a taste, I was wondering if I will go through withdrawals. I been using heroin on top of my naltrezone pill for a few months. Any advice or info would be helpful.

 

[antman25]

hey polo792 you wont go through any with drawl as you probably already found out. I'm currently on the naltrexone pellet/implant in my arm and am trying to figure out how long until I can feel the effects of opiates again? can anyone tell me from experience?

 

[chugs]

you need a fuck load of heroin (so much that you would probably OD yourself - like a few grams - so don't do it) to override the naltrexzone so if you didn't go into withdrawals then its unlikely that you will.

re Antman25@ the pellets last anywhere between 3-6 months. You can feel it under your skin so I suppose if you can feel it then its still there. Re the effect it takes 48-72 hours after your last dose of Naltrexzone before heroin will be effective

 

[vision conquest]

I would think the best chance of getting over a naltrexone implant would be with buprenorphine.

I have no direct experience it's just a theory, but with bup's greater binding affinity it would probably get over the naltrexone.

Surely have more chance than h.
I have heard of people taking 25mg oral naltrexone daily and still getting effects from oral bup.

Kind of defeats the purpose of being on naltrexone but it's just an idea.

 

[polo792]

Just to clarify my question.. what I mean is would I have any heroin withdrawals, as if I would need to use heroin to feel normal. I didn't mean would I go through rapid detox. My concern is that on the day I don't use heroin on top on taking the naltrexzone tablet would I hang out for heroin.
Would anyone know if that will happen or has anyone experience this??

 

[spacejunk]

If you're using heroin regularly (ie daily) then yeah, from what you've told us, i would expect to experience some sort of withdrawals.
I'm assuming you previously had a habit? If so, it's a lot easier to re-ignite your physical dependency to opiates.
A taper would be advisable.

 

[vision conquest]

Just to clarify my question.. what I mean is would I have any heroin withdrawals, as if I would need to use heroin to feel normal. I didn't mean would I go through rapid detox. My concern is that on the day I don't use heroin on top on taking the naltrexzone tablet would I hang out for heroin.
Would anyone know if that will happen or has anyone experience this??

Hey polo792 sorry I guess I was a bit vague but I wasn't trying to say anything about going into precipitated wd.

What I was saying is that instead of using heroin that you don't feel you could use bup instead which you probably would feel, the bup should get over the naltrexone due to it's high binding affinity.

As for whether or not you would hang out, under normal conditions after using h for a couple of months daily you definitely would, however I wonder, since ther heroin is unable to bind to your receptors due to the naltrexone I wonder if you would experience withdrawl.

As I mentioned I have no direct experience in this regard, the first response in this thread from Antman25 seemd to suggest you would not, sounds like he is speaking from experience as he has a naltrexone implant.

I would be interested to know if you did experience withdrawl or not.

 

[polo792]

Well tomo will be the day I won't be using smack after taking the naltrexzone tablet. Hopefully I won't feel like I'm hanging out and need to use, I am hoping that it will be mentally if anything.

Will let you know how it goes and I'm feeling.

 

[spacejunk]

Please let us know how you go - wishing you all the best.

 

[polo792]

Starting on Sunday....

 

[chugs]

Withdrawals from opiates are actually caused by the activation of TLR family by a metabolite of the opiate. So for example heroin metabolises into M3G and M6G.

M6G binds to the mu receptors and M3G binds to the TLR4 receptor which floods your body with proinflammatory cytokines. These things create resetless leg, nasua, aches and pains - basically withdrawals. But when you think about it its not the absence of the heroin that is causing it but rather the absence of the M6G which was covering up the pain and agony of the proinflammatory cytokines caused by M3G.

THink if heroin didn't have any M6G but only M3G it wouldn't be a nice drug. It would make you feel like you're in instant withdrawals whenever you shoot it up.

Intriguingly, TLR4 is activated by morphine-3-glucoronide (M3G), a morphine metabolite that is inactive at classical opioid receptors, but not by morphine-6-glucoronide (M6G), the opioid receptor active metabolite45,46. Along with nonstereoselectivity, the TLR4 signaling activation by M3G, but not M6G, points to a major difference from the structure activity relationship of the opioid receptor with the reliance of 4,5-epoxymorphinans on the 3’OH for classical opioid receptor activity but not for TLR4 activity. M3G action at TLR4 predicts that intrathecal M3G would induce pain enhancement mediated by TLR4, microglia (given their predominance in TLR4 expression), and proinflammatory cytokines (a downstream product of TLR4 activation). Indeed, this is the case46. TLR4 activation by opioids is now implicated in opposing acute and chronic opioid analgesia, and contributing to opioid-induced hyperalgesia, dependence and reward45,46.

Incidentally improper activation of TLR4 is thought to cause MS. So basically heroin withdrawal syndrome is actually the same thing a MS patient is going through (but never stops) but without any of the analgesic affects of the heroin.

So anyway. back to Polo792. It won't matter if you're on Naltrexone, heroin or whatever. Anything that activates the Toll Like Receptor family, like the metabolite M3G, or B3G (bbuprenorphine-3-glucuronide) is gonna mean that once the pain reliving effect is gone that your gonna feel dope sick.

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1. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2783351/ for more reading.

2. http://www.huffingtonpost.com.au/entry/meth-addiction-cure-ucla-ibudilast_n_2863126

 

[vision conquest]

Withdrawals from opiates are actually caused by the activation of TLR family by a metabolite of the opiate. So for example heroin metabolises into M3G and M6G.

M6G binds to the mu receptors and M3G binds to the TLR4 receptor which floods your body with proinflammatory cytokines. These things create resetless leg, nasua, aches and pains - basically withdrawals. But when you think about it its not the absence of the heroin that is causing it but rather the absence of the M6G which was covering up the pain and agony of the proinflammatory cytokines caused by M3G.

THink if heroin didn't have any M6G but only M3G it wouldn't be a nice drug. It would make you feel like you're in instant withdrawals whenever you shoot it up.




Incidentally improper activation of TLR4 is thought to cause MS. So basically heroin withdrawal syndrome is actually the same thing a MS patient is going through (but never stops) but without any of the analgesic affects of the heroin.

So anyway. back to Polo792. It won't matter if you're on Naltrexone, heroin or whatever. Anything that activates the Toll Like Receptor family, like the metabolite M3G, or B3G (bbuprenorphine-3-glucuronide) is gonna mean that once the pain reliving effect is gone that your gonna feel dope sick.

-----

1. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2783351/ for more reading.

2. http://www.huffingtonpost.com.au/entry/meth-addiction-cure-ucla-ibudilast_n_2863126

This is very interesting information, I have read it in some of your posts previously.

I have a question, maybe it's stupid, maybe I just don't understand the information you are presenting.

But if what you are saying here is true wouldn't someone on naltrexone be feeling terrible as soon as they used heroin, since there would be no pain relief, due to the heroin being unable to bind to opiate receptors to cover the effect of m3g.

I am not saying what you have posted is wrong or trying to start an argument, just trying to understand it.
I would have thought that the naltrexone would prevent the m6g from binding to receptors, therefor there would be no pain relief to cover the effect of m3g.

I will read the links you have provided and hopefully this will help me understand.

 

[madmick19]

there are other risks involved here worth knowing about, take the time to read Amy Gibson
and Louisa Degenhardt Mortality related to naltrexone in the treatment of opioid dependence:A comparative analysis NDARC Technical Report No. 229 even if its just the executine summary of the information. there is a lot of changes to tolerence which is obscured by the blocking effects of natrexone preparations- eg risk of OD on resumption of use is heightened. oh look more information here

Aivl have some good info on Natrexone in one of their pages
be cautious and have a back up plan with friends incase you misjudge your intoxication level.

seriously though if you are struggling this much its time to talk to the person/org treating you or a tertiary level addiction treatment centre.
you are probably one of those people who needs a full agonist opioid like methadone to keep you both happy and safe.
iof you were in canberra thats what i would definitely be recommending.

 

[mianxgp]

Ohh my sweet foreign friend, you and your international quality 10% pure heroin tickle my funny bone.
Sigh. I'm from somewhere where our street heroin is 80% pure and sells for 3$ a gram.
I've been consuming 3 grams a day for the last 2 weeks; via foiling. Don't know what you guys call it but basically you put the H on a piece of foil and light a flame under it so it melts and you inhale the fumes.
Right so I've been on naltraxone for about 3 years, been having H off and on during that time. But this last 2 weeks its been a regular 3 grams a day taken via foil and Im starting to feel withdrawals. There is no high just the taste but I feel physical pain.
Whats going on with my body someone please explain