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Opioids Using naloxone to counter tolerance

theebaheeen

Greenlighter
Joined
Oct 7, 2010
Messages
26
Location
SF Bay Area, Caliiii
So today I decided to eat 30mg of crushed oxycodone (roxys/blues w/e), and I didnt get the desired high I normally get, so I decided to look up on methods to reverse opiate tolerance.

In most threads I have seen, people mention using NMDA antagonists to prevent tolerance from forming, with some even reversing tolerance, but then I found something appealing and in immediate reach.

My father was an anesthesiologist before he passed, and he kept many IV ampules in his home office. Now upon reading about reversing tolerance, many people mentioned using small doses of naloxone to reverse tolerance. Because this is one of the drugs I have access to, I decided this would be my best bet.

Now I dont particularly find needles desirable, so if naloxone has a decent bio availability via other ROA's, that would be prime.


Now, how would I go about doing this? I understand if I do this incorrectly, I can throw myself into precipitated withdrawls, even when i'm not on anything (I use once a week on average). I am just looking for the correct dosage amounts, dose regimen, and best ROA (even if it means I have to IV, these ampules are completely sealed, I'm not worried about fucking up my veins with USP grade liquid). I am assuming I will need to set aside a month or more of not using. That's cool, but it would be amazing if it would lower my tolerance in less time.

I know this tolerance is not big compared to many users, but I feel that having to use more then one roxy 30 is unacceptable in terms of cost effectiveness.
 
If you only need to use more "more than one 30" to get you where you want, you in no way shape or form need to be undertaking any sort of naloxone therapy. That shit is reserved for the worst of the worst, people who just cannot stop using, and they get an implant that basically prevents them from getting high (kind of like suboxone, except via different chemical methods and ROAS). It has also been used novelly in combination with opiates to prevent some stomach effects of opiates, as well as supposed use to prevent abuse of opiates (aka suboxone, although I disagree that it even has an effect with suboxone). It definitely has its place in reversing overdoses as well, and yes even helping with tolerance in lab mice and clinically controlled settings.

You just need to take a break, using naloxone is going to provide you with no benefit.
 
If you only need to use more "more than one 30" to get you where you want, you in no way shape or form need to be undertaking any sort of naloxone therapy. That shit is reserved for the worst of the worst, people who just cannot stop using, and they get an implant that basically prevents them from getting high (kind of like suboxone, except via different chemical methods and ROAS). It has also been used novelly in combination with opiates to prevent some stomach effects of opiates, as well as supposed use to prevent abuse of opiates (aka suboxone, although I disagree that it even has an effect with suboxone). It definitely has its place in reversing overdoses as well, and yes even helping with tolerance in lab mice and clinically controlled settings.

You just need to take a break, using naloxone is going to provide you with no benefit.

I was under the impression that opiate tolerance could not be reversed with time like other drugs. At least this is what many of my friends have told me, but I'm going to assume you are correct because chances are, you have much more knowledge and experience with this subject.

But on the topic of naloxone being reserved for the worst of the worst, correct me if I misunderstood the context of your post, but these naloxone ampules I have are never going to be touched anyways simply because no one in my household has any clue what it is, and they wouldn't have a need for it anyway (unless someone OD'd in my house). They have just been sitting in this box for years. My point is I'm not really taking it from anyone who needs it. Also, if you didn't already know this, I wasn't intending use the naloxone to prevent me from using, I was planning on using miniscule amounts to re-sensitize my opiate receptors.

How long of a break do you suggest I take? I'm sure there are multiple factors which should determine this because everyone's body is different, but if there was an average, what would that be?
 
I was under the impression that opiate tolerance could not be reversed with time like other drugs.

People may disagree with me, but I think it really depends on your ROA. Oxycodone for me was just never enough in general. I know people who only use one 30mg IR a day, and they are generally pretty content. I think maybe your expecting to go back to how it was when you first started using? The nods/euphoria/talkativeness/chain-smoking. Maybe try potentiating it with an anti-histamine? Hydroxyzine is a popular one~ Really tho', If I were you... I would just do without the 30's my friend. Oxycodone is a really expensive painkiller... that is just my .02. Anyway lay off for a month or so, maybe try plugging, or insufflating? I don't really know, a tolerance to opiates really isn't a good thing anyway you look at it. I would suggest maybe trying a different opiate also, like hydromorphone, you might be one of the lucky few who really gets something off of it orally :D
 
It's one thing to use heroin then expect to be able to enjoy low dose codeine again, it's another to say time doesn't reduce opiate tolerance - it does.

It may take a generous amount of time, but it will happen.
 
Right now they are running clinical trials with an oxycodone/naloxone mix for chronic pain.
http://clinicaltrials.gov/ct2/show/NCT00513656
It seems as though they are trying this mixture in order to prevent/lessen tolerance. If they are running clinical trials then it is most likely geared towards the general public and not just the worst of the worst.

Dosage probably has everything to do with it though so without extensive trials your most likely not going to get the right combo. IMO it probably wouldn't hurt to try titration. If you only partially block tolerance at first it is still better than full tolerance.

I don't have a link but I seem to remember reading Jonathan Ott did some self experiments with codeine/naloxone mixtures and had some success.
 
Well, I can rail 5mg of Opana ER (oxymorphone), and get more fucked up thenf if I was to rail a whole 30.

Unfortunately Opana ER has been reformulated, and I have never touched a IR Opana in my life.

Heroin sucks, its too inconsistent (I've only been high on tar twice and since then I have never found anything that would get me high, plus its gross as hell). I actually got ripped off spending a ridiculous amount on .2 of "the best tar hes ever seen" from a guy who knows I'm going to see again, and tar from the tenderloin got me slightly higher then the one from the guy I actually know.
 
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By "naloxone is usually reserved for the worst of the worst" DooMMood didn't mean that you will be taking it away from people who need it more, just that you don't really need it and it's probably not worth the risks and not generally used for your purposes . By "worst of the worst" he/she just meant people who are severely addicted to opioids. Your tolerance issue is minor in comparison. If you normally use oxys about once a wk, then you should only have to take a few wks off to bring your tolerance down. You are not in a situation like some people where you can't even take 12 hours off without going into serious withdrawals and would never be able to take enough time off to decrease your tolerance.

However, it sounds like DooMMood was - in part of his/her post - confusing naloxone with naltrexone, which is a different drug, used in implants etc to block addicts from getting high from opiates and therefore discourage them from using.

Naloxone is primarily used to to counter opioid overdoses, and as an ingredient in Suboxone (which also contains buprenorphine) to prevent people from injecting their medication (although some people do debate that when included with buprenorphine in Suboxone whether it really has much of an opioid blocking effect, or at least doesn't completely block opioids from working in users taking high doses of Suboxone, but that's another issue). Small amounts of naloxone has also recently started to be included with some other oral opioid medications, supposedly to decrease side effects like constipation, and to make the medications harder to "abuse" (it is supposed to have much stronger opioid-blocking effects when injected or taken in large quantities). Naloxone isn't very long-lasting, so, while taking it soon after using opioids will put you into precipitated withdrawals, one shouldn't have to wait as long after taking it before resuming opiate use. So, it could potentially help to lower your tolerance I suppose. Personally I wouldn't bother. And I have no idea what the "right" quantity would be. Also, if you can wait until all the drug is completely out of your system before taking the naloxone, (in order to avoid any possibility of precip. WDs) then I don't know what difference it's going to make as opposed to just waiting without taking anything.

Opioid tolerance is not something that never goes away. But you'll likely never be able to experience the high quite like it was your first several times, even if your tolerance has gone back down. I was treated with naloxone for heroin overdose once and the next day when I used heroin again it still wasn't like going back to the first time I tried heroin.

If you are insistent about undertaking this experiment, then there are several ways naloxone can be administered. The first is injection into a vein - normally done for speediest effect in an emergency for opioid overdose. The second is injection into muscle. The third is nasally. And the last is orally, although I don't know whether this would suit your purpose. When administered orally in small quantities, it usually only really affects the digestive system because it has low systemic bioavailability due to first pass metabolism by the gut and liver.
 
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By "naloxone is usually reserved for the worst of the worst" DooMMood didn't mean that you will be taking it away from people who need it more, just that you don't really need it and it's probably not worth the risks and not generally used for your purposes . By "worst of the worst" he/she just meant people who are severely addicted to opioids. Your tolerance issue is minor in comparison. If you normally use oxys about once a wk, then you should only have to take a few wks off to bring your tolerance down. You are not in a situation like some people where you can't even take 12 hours off without going into serious withdrawals and would never be able to take enough time off to decrease your tolerance.

However, it sounds like DooMMood was - in part of his/her post - confusing naloxone with naltrexone, which is a different drug, used in implants etc to block addicts from getting high from opiates and therefore discourage them from using. (Naltrexone lasts a lot longer and is not generally used to reverse opioid overdoses).

Naloxone is primarily used to to counter opioid overdoses, and as an ingredient in Suboxone (which also contains buprenorphine) to prevent people from injecting their medication (although some people do debate that when included with buprenorphine in Suboxone whether it really has much of an opioid blocking effect, or at least doesn't completely block opioids from working in users taking high doses of Suboxone, but that's another issue). Small amounts of naloxone has also recently started to be included with some other oral opioid medications, supposedly to decrease side effects like constipation, and to make the medications harder to "abuse" (it is supposed to have much stronger opioid-blocking effects when injected or taken in large quantities). Naloxone isn't very long-lasting, so, while taking it soon after using opioids will put you into precipitated withdrawals, one shouldn't have to wait as long after taking it before resuming opiate use. So, it could potentially help to lower your tolerance I suppose. Personally I wouldn't bother. And I have no idea what the "right" quantity would be. Also, if you can wait until all the drug is completely out of your system before taking the naloxone, (in order to avoid any possibility of precip. WDs) then I don't know what difference it's going to make as opposed to just waiting without taking anything.

Opioid tolerance is not something that never goes away. But you'll likely never be able to experience the high quite like it was your first several times, even if your tolerance has gone back down. I was treated with naloxone for heroin overdose once and the next day when I used heroin again it still wasn't like going back to the first time I tried heroin.

If you are insistent about undertaking this experiment, then there are several ways naloxone can be administered. The first is injection into a vein - normally done for speediest effect in an emergency for opioid overdose. The second is injection into muscle. The third is nasally. And the last is orally, although I don't know whether this would suit your purpose. When administered orally in small quantities, it usually only really affects the digestive system because it has low systemic bioavailability due to first pass metabolism by the gut and liver.

Thank you for the clarification.

I understand the basic pharmacokinetic properties of naloxone and naltrexone on the brain and the primary use to knock off opiates off of your receptors due to the high binding affinity of both of them, and to be honest I pretty much figured that this idea was pretty ridiculous from the start. My main motivation for attempting this kind of experiment was due to reading prior threads on bluelight explaining how naloxone was used in rats to reverse tolerance by basically "re-sensitizing" the receptors by using tiny miniscule amounts every day. Now this has never been tested on a human as far as I know, and I dont feel like I have enough experience to administer such small doses for someone with such a tiny tolerance. There are just to many factors in the way for someone with such a basic understanding, like the terribly short half life for example. Besides the obvious motive of reversing my tolerance, I am of of those "what if" type of people; the whole idea of reversing a tolerance fascinates me.

But all in all, this whole idea seems too unrealistic to attempt. I'm going to take a break for a couple months. But of course I am still going to look into this for shits and gigs along the way.

Although.... Speaking of naltrexone, what if one was to start a regimen of oral naltrexone tablets while on an "opiate break" to speed up the "re-sensitization" of the receptors? My main logic behind this is that by blocking endorphins from certain receptors (naltrexone is a partial antagonist I believe), your endorphins will be running at their peak after stopping the regimen and therefore your tolerance will be reduced significantly.

But then again.... I could just be completely naive about this whole entire subject.
 
Hmm... do you have an illicit supply of naltrexone or would you be getting it by prescription? And if the latter, does your dr already know you are an opiate user? Because I wouldn't want to have that on my prescription record unless absolutely necessary.

ETA: Either way I think it would be the same situation as the naloxone and not worth it. Naltrexone might even be a worse idea than naloxone. You have to wait 10 days after taking an opioid before even starting naltrexone and by that time I don't see how much difference it would really make to your tolerance level compared to abstinence alone. It also has some unpleasant side effects. And using either of these drugs, especially naltrexone because it is longer-lasting, puts you in a situation where, were you to say be in an accident and seriously need pain relief you would find yourself in a very bad situation.
 
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Tolerance does go down after quitting but it doesn't take as long as your first time to get back to where you were at the 1st time you maxed out.. ......
 
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