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Thread: *Safely* Easily Remove Naloxone From Suboxone

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    #26
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    Before subutex, there were other, lower dose buprenorphin pills (Temgesic to name one) so it's reasonable to assume the patent for buprenorphine-only medication was approved before subutex came out.

    Also I'm pretty sure there was actually more than 2 years between tex & xone, but I'd have to check on this.

    Also FDA is an american institute, is it not? And subutex, suboxone & others are marketed worldwide? There's a huge market for buprenorphine in europe. And the company that held the patent for subutex is european. So I don't see why they'd specifically want to "trick the FDA"... or maybe they would, but that definitely is not the reason Suboxone was made, else they'd have marketed it in the US only...

    From wiki

    Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, available generally as Temgesic 0.2 mg sublingual tablets
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    started suboxone this past sunday 
    #27
    Talking
    I have been user of ppt for almost 3 yrs. I recently used heavily ppt for 4 days before starting on suboxone. I started suboxone 12 hours later. I did not experience any WD and feel it is helping me tremendously. I have 2nd doc appt tomorrow plus drug test. 1st drug test last week i could not pee because I was in Wd and could not eat or drink anything. I guess they thought I was trying to get out of it lol. I tried like 5 times and drank 15 small cups of tap water and still couldnt pee. That was how dehydrated I was. I was so happy when I finally peed. Anyway my opiate level was 1700. It might be higher tomorrow i dont know. But it is my third day today on bups and I can say I feel in control now whereas before I felt helplessly no control and bound to this aweful tea. I loved the tea. I loved that relaxing feeling when you lay down and your in that twilight state forever. But I hated sleeping too much. I want my life back and I want to feel normal again. So pray for me. I dont have any money because I lost my job and my mom is helping me through this. Thank god my hubby got good job now. I was a nurse so you see where I am coming from. I will be so proud of myself to get through this. I finally have some hope now. Sent last box of poppys unopened back-return to sender on it!!!
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    #28
    Listen, people I know this post is a little old but I can settle this feud. The reason the naloxone is in suboxone is only to keep people from injecting it... this is feasable because of something called bioavailability. When taken sublingually naloxone isn't absorbed well at all and bupe is. When injected the opposite is true. So the naloxone is the active chemical reaking havoc on your receptors when you inject a suboxone. This is the true reason why there is 2 different drugs... no big conspiracy, only pharmacology and different circumstances and uses for the drugs.
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    #29
    I'm sure you're not telling anything new to anybody here. That is common knowledge amongst opioid-users. It's the same story with the famous tilidine/naloxone-combo ("Valoron N").

    But I see that this was your first post at Bluelight. A warm WELCOME then!


    Peace! - Murphy
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    #30
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    Quote Originally Posted by ganzy1003 View Post
    Listen, people I know this post is a little old but I can settle this feud. The reason the naloxone is in suboxone is only to keep people from injecting it... this is feasable because of something called bioavailability.
    It's not at all feasible. Buprenorphine having way higher receptor affinity than naloxone effectively renders the naloxone to an expensive filler.

    When taken sublingually naloxone isn't absorbed well at all and bupe is. When injected the opposite is true. So the naloxone is the active chemical reaking havoc on your receptors when you inject a suboxone.
    No it doesn't, when injected the naloxone doesn't even reach your receptors if they are already saturated with buprenorphine (ie. when you use regularly). Even for someone who only uses occasionally, the naloxone will at most slow the come-up of the buprenorphine.

    This is the true reason why there is 2 different drugs... no big conspiracy, only pharmacology and different circumstances and uses for the drugs.
    This is what the pharmaceutical companies want you to believe. But ask yourself this: do they really have your best interest in mind? If adding naloxone to their pills gives them the opportunity to make a lot more money, don't you think they can come up with whatever justifications for it - like "deterring abuse", for which the naloxone is completely useless?
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    #31
    You may be correct when you say that there would be a minimal effect once the user had been taking subs and the bupe was already on the receptors, however, the people "they" want to deter from abusing aren't the people already using as prescribed. They are deterring opiate addicts from using this as just another drug because after all the only people getting bupe for the most part is opiate addicts, and who are they most likely to give these pills to if they were abusable? Other addicts. As to your first comment, bioavailability when injected for bupe is slim to none meaning barely any bupe gets through to your brain while at the same time the narcans BA is high thorugh iv so a shitload goes right on through to ones brain making this the perfect combo for deterring abuse. You don't think the fda knows about the games big pharma plays? People on a blog can unravel the conspiracy but all the scientists and experts at the fda can't? No there was no trickery, this was a valid new formulation to the drug with a purpose.
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    #32
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    You may be correct when you say that there would be a minimal effect once the user had been taking subs and the bupe was already on the receptors, however, the people "they" want to deter from abusing aren't the people already using as prescribed. They are deterring opiate addicts from using this as just another drug because after all the only people getting bupe for the most part is opiate addicts, and who are they most likely to give these pills to if they were abusable?
    I'm sorry but you don't know what you are talking about. Buprenorphine alone will precipitate withdrawal symptoms if given to a person who is addicted to full mu agonists. The naloxone is totally unnecessary for this purpose. Yet, people still manage to abuse buprenorphine (subutex and suboxone) and IV them, they just need to take a break from the full agonists for a few days when switching to buprenorphine.

    As to your first comment, bioavailability when injected for bupe is slim to none
    Where do you get this idea? That's pure bullshit.

    while at the same time the narcans BA is high thorugh iv so a shitload goes right on through to ones brain making this the perfect combo for deterring abuse.
    No. Just, no. They both go to the brain, bupre hits the receptors, naloxone doesn't since the bupre is already blocking the receptors. Naloxone then finds it's way to whatever other receptors it has affinity for or gets metabolized, but it does nothing to prevent the effects of buprenorphine.

    You don't think the fda knows about the games big pharma plays? People on a blog can unravel the conspiracy but all the scientists and experts at the fda can't? No there was no trickery, this was a valid new formulation to the drug with a purpose.
    Yeah, keep telling yourself that. Why are you so keen to stick up for pharma companies anyway? You work for Reckitt Benckiser or something?
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    #33
    "Because of its opioid agonist effects, buprenorphine is abusable, particularly by individuals who are not physically addicted to opioids. Naloxone is added to buprenorphine to decrease the likelihood of diversion and abuse of the combination product. Sublingual buprenorphine has moderate bioavailability, while sublingual naloxone has poor bioavailability. Thus, when the buprenorphine/naloxone tablet is taken in sublingual form, the buprenorphine opioid agonist effect predominates, and the naloxone does not precipitate opioid withdrawal in the opioid-addicted user."

    Straight from the experts....

    You know, you shouldn't be so quick to blow off people, even if you think you are probably right. Keep an open mind. I know there are hordes of idiots spewing bullshit on this site 24/7, and I can understand your reluctance. Yes, the companies want to make money.... And their practices as a whole aren't perfect. However, they supply the public with medications that benefit us, and in turn they get what they want as well. Money. Suboxone's formulation was created to stop abuse, the company created it because there was a market for it. Period. I'd rather have the companies around than not have medicine at all.

    Naloxone via the parenteral route, however, has good bioavailability. If the sublingual buprenorphine/naloxone tablets are crushed and injected by an opioid-addicted individual, the naloxone effect predominates and can precipitate the opioid withdrawal syndrome.
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    #34
    ^ Sorry fucked up the quote when pasting it.


    "Because of its opioid agonist effects, buprenorphine is abusable, particularly by individuals who are not physically addicted to opioids. Naloxone is added to buprenorphine to decrease the likelihood of diversion and abuse of the combination product. Sublingual buprenorphine has moderate bioavailability, while sublingual naloxone has poor bioavailability. Thus, when the buprenorphine/naloxone tablet is taken in sublingual form, the buprenorphine opioid agonist effect predominates, and the naloxone does not precipitate opioid withdrawal in the opioid-addicted user.

    Naloxone via the parenteral route, however, has good bioavailability. If the sublingual buprenorphine/naloxone tablets are crushed and injected by an opioid-addicted individual, the naloxone effect predominates and can precipitate the opioid withdrawal syndrome.

    Under certain circumstances buprenorphine by itself can also precipitate withdrawal in opioid-addicted individuals. This is more likely to occur with higher levels of physical addiction, with short time intervals (e.g., less than 2 hours) between a dose of opioid agonist (e.g., methadone) and a dose of buprenorphine, and with higher doses of buprenorphine."
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    #35
    Dude you people are (some of you) idiots.


    Dread is 100% CORRECT

    Naloxone really doesn't do anything. The only thing it really does is decrease the "rush" when injected.

    PERIOD.
    ITS (naloxone combo) NOT A BLOCKER. ITS NOT THE CAUSE OF PREc-WD!
    BUP DOES THE BLOCKING!!!

    As oxymorphone said, THIS HAS BEEN COVERED!

    Sorry for yelling. I just cant stand too see this shit all the fucking time. People do some fucking research.
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    #36
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    Naloxone via the parenteral route, however, has good bioavailability. If the sublingual buprenorphine/naloxone tablets are crushed and injected by an opioid-addicted individual, the naloxone effect predominates and can precipitate the opioid withdrawal syndrome.
    Ok, I'm so tired of explaining the same thing over and over, so this will be the last time. Seriously.

    Naloxone doesn't precipitate the withdrawals. The buprenorphine does. All the naloxone does is give you the runs, when it binds to the mu-receptors in your gut. I noticed this effect very clearly when I started my suboxone meds - each time I took my dose I could accurately predict myself to be in the toilet 30 minutes later. Although when you get used to the dose this effect becomes less noticeable.

    Ok, one more time then. 8mg buprenorphine + 2mg naloxone are dissolved (and hopefully also filtered properly if you know what's good for you) and injected into bloodstream. The blood carries the active substances to the brain, where they pass the BBB (look it up) and finally, they find the mu-receptors. Buprenorphine, having a binding affinity (look it up) orders of magnitude higher than naloxone, binds to the receptors. Some naloxone may bind, but will be quickly replaced by buprenorphine (again, due to higher binding affinity) result: buprenorphine is bound to mu-receptors = mu-receptors are saturated = no mu-receptors remain available for naloxone to bind.

    Now what happens in opioid-addicted individuals is, that their body is used to full mu-agonism (ie. the receptor being activated 100% ). Buprenorphine is not a full agonist at the mu-receptor, it is partial, ie. it only activates it less-than-100% so effectively the opioid-addicted-individuals brain is getting less mu-agonism and therefore goes to withdrawal. Nothing in this is caused by naloxone.

    The addition of naloxone to the formulation was simply a shady trick to extend the patent and make more money out of a drug (buprenorphine) when it's patent was expiring. It doesn't take a supr genius to figure this out.
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    #37
    youre right about everything you said except the thing is that the bupe doesnt even make it to the brain... thats what bio-availability is, it is measured in percents. so thats to say there is a 30% BA orally and 60% rectally for example. So you get 30 percent of the drug one route and 60 the other. So, when injected the BA of Bupe is almost zero, meaning no noticeable amount of it got through. On the other hand when ived naloxones BA is VERY high meaning a shitload got through. So bupe plays NO ROLE WHEN INJECTED. Thats what i have been saying. I know all about the affinity levels and youre right when the two fight it out Bupe wins. But they arent fighting when you inject, its the narcan all alone. By the way this has nothing to do with molecule size and the Blood brain barrier, both of these are small in molecular size, i know you wanted to bring it up to sound smart... you dont have to prove anything to me you seem very knowledgeable, but in this case you misunderstood what i was saying and was also unaware of what i was talking about. A deadly combo when trying to debate. Look up the numbers and also look up what bio-availability is so you can understand that it isnt a conspiracy. its big pharma charging too much for something there is a market for. I am not okay with the price, but the reason for the formula change is valid.
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    #38
    can anyone please back me up on this? I know I'm right and only one person has bothered to agree with fact. I dont want to be one of those people who starts throwing all kinds of quotes from journals. I know some one in this forum has heard of BIO-AVAILABILITY.
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    #39
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    Quote Originally Posted by ganzy1003 View Post
    youre right about everything you said except the thing is that the bupe doesnt even make it to the brain... thats what bio-availability is, it is measured in percents. so thats to say there is a 30% BA orally and 60% rectally for example. So you get 30 percent of the drug one route and 60 the other. So, when injected the BA of Bupe is almost zero, meaning no noticeable amount of it got through. On the other hand when ived naloxones BA is VERY high meaning a shitload got through. So bupe plays NO ROLE WHEN INJECTED. Thats what i have been saying. I know all about the affinity levels and youre right when the two fight it out Bupe wins. But they arent fighting when you inject, its the narcan all alone. By the way this has nothing to do with molecule size and the Blood brain barrier, both of these are small in molecular size, i know you wanted to bring it up to sound smart... you dont have to prove anything to me you seem very knowledgeable, but in this case you misunderstood what i was saying and was also unaware of what i was talking about. A deadly combo when trying to debate. Look up the numbers and also look up what bio-availability is so you can understand that it isnt a conspiracy. its big pharma charging too much for something there is a market for. I am not okay with the price, but the reason for the formula change is valid.
    This post is so full of shit I don't know whether to laugh or cry.
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    #40
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    Quote Originally Posted by ganzy1003 View Post
    can anyone please back me up on this? I know I'm right and only one person has bothered to agree with fact. I dont want to be one of those people who starts throwing all kinds of quotes from journals. I know some one in this forum has heard of BIO-AVAILABILITY.
    Where the fuck do you get the absurd notion that buprenorphine would have "low bioavailability when injected"?

    Do you even know what bioavailability MEANS?

    Bioavailability as a concept doesn't even apply to IV use. By definition, anything that is injected has 100% bioavailability (unless it gets metabolized by blood enzymes or something which buprenorphine doesn't.)

    See: http://en.wikipedia.org/wiki/Bioavailability

    In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation
    So when you inject, do you know where the stuff you inject ends up to? It ends up in your bloodstream, ie. systematic circulation. ONE HUNDRED PERCENT.


    Sheesh, I don't even know how to make this any more clear.
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    #41
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    Haha, I can't resist...

    Quote Originally Posted by ganzy1003 View Post
    BIO-AVAILABILITY.
    You keep saying that word. I don't think it means what you think it means.
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    #42
    You are right about the inject ba its always 100, I was high when I wrote the post and it made sense then but no longer. Maybe it is a big conspiracy to lengthen the patent and they took the opportunity cause law enforcement demanded it. But what I'm not getting is why I am hearing so many accounts of people getting pwd with suboxone and not subutex. Its not an isolated case, its very common to hear that. I mean when the injection takes place there is a much higher ratio of naloxone to bupe and that must have some effect? Like some of the receptors not being covered by the dose of bupe and the naloxone grips the remaining receptors so in turn its like taking a low dose of opiates which would send me into wd, like many other dependants.
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    Not worth the effort. 
    #43
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    The naloxone has been proven time and time again to not have an effect on the experience. It has been known to cause headaches and nausea in some people, but since the bupe has such a higher binding affinity at the mu-opiate receptor the naloxone has no chance of attaching.

    I think the reason the bupe seems stronger when you do this is because it has been said that the subllingual bioavailibility can be increased by as much as 20% by taking your subs in an oral solution by crushing your dose and dissolving in a solution of water and high proof grain alcohol.

    I am almost positive that the makers of suboxone knew the naloxone would be useless, the reason it was added was so they could market suboxone without infringing on the patent for subutex and also to compete with subutex. This shouldn't surprise anyone, drug companies have done much more heinous things to make money, like when Purdue said OxyContin was not addictive...
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    #44
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    Quote Originally Posted by dread View Post
    Before subutex, there were other, lower dose buprenorphin pills (Temgesic to name one) so it's reasonable to assume the patent for buprenorphine-only medication was approved before subutex came out.

    Also I'm pretty sure there was actually more than 2 years between tex & xone, but I'd have to check on this.

    Also FDA is an american institute, is it not? And subutex, suboxone & others are marketed worldwide? There's a huge market for buprenorphine in europe. And the company that held the patent for subutex is european. So I don't see why they'd specifically want to "trick the FDA"... or maybe they would, but that definitely is not the reason Suboxone was made, else they'd have marketed it in the US only...

    From wiki
    I think the reason had more to do with them getting their own patent for the medication and competing with subutex, they thought that most doctors would use Suboxone because its less abusable and just as effective and then they would have the patent for a few years so they could make a good amount of money before companies started making generics. Also, I'm not sure about this but I think a patent is valid on an international scale.

    I found the best way to understand drug companies is to think of them as having the sole goal of making money by whatever means necessary, think of Purdue marketing OxyContin as "non-addictive" they had to know this was false but they knew they would make so much money before the claim was challenged and they got sued that they could afford a lawsuit and still come out with more money than they would have if they told the truth about it being just as addictive as other pain pills. But im starting to rant sorry!
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    #45
    You know what I think the true answer is? I've been looking into it and it seems the naloxone competes and slows the onset of the bupe. This would cause unpleasant symptoms for an abuser of opioids trying to use this as another recreational drug, briefly I might add but long enough for the addict to avoid abusing if he can. I think its a longshot idea at deterring abuse but was good enough to convince a lot of people. No one said the drug companies are stupid. Its actually just great marketing I give them props they even had me fooled for awhile with the cross on the back of each tablet
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    #46
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    I've been looking into it and it seems the naloxone competes and slows the onset of the bupe.
    In my experience, this is only true with small dosages and occasional use.

    But what I'm not getting is why I am hearing so many accounts of people getting pwd with suboxone and not subutex.
    I can see several reasons:
    1. in many places suboxone has pretty much replaced subutex, or is much more common / easy to get. Therefore you would get more reports of possible ill effects of suboxone.
    2. Some people are allergic to naloxone.

    I think the reason had more to do with them getting their own patent for the medication and competing with subutex
    Subutex and suboxone are made by the same company.
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    #47
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    Here is a story I want you all to argue over. A little background, I was on heroin, went on suboxone, went off suboxone, then found a way cooler doctor. this doctor rxed me as much suboxone and alprazolam as I wanted (not to mention ambien and clonodine too all at once).

    Anyway I got to shooting my suboxone...no problems ever involving precip wd. One time 2 days after taking methadone I did one and got an idea of what precip wd's could be. Then the generics came out so I got switched to subutex a month before the realease to make a seemingless switch to generics. They worked well IV too. After discontinuing my sessions with that doc, the most logical thing to do to not be sick was to take tramadol every day.

    THis brings me to my point. Everyone says tramadol mixes with bupe and I tend to believe them HOWEVER if you are on tramadol and shoot suboxone it gives a very distinct feeling of partial precipitated withdrawl. I am guessing the naloxone is displacing SOMETHING since the feeling is too wierd to be anything else, however with just buprenorphine, you will not deal with this unpleaseness.

    I would really like a better explanation of what is happening. My friend overdosed on a few things tramadol was one of them (and the only opioiod in the cocktail). He went to the ER and got naloxone IV. He confused all the doctors cause the naloxone would cause him to wake up for 5 min before fallin back asleep. They repeated administration and watched this happen a few times. Any thorys welcome as long as they make sense.
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    #48
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    One time 2 days after taking methadone I did one and got an idea of what precip wd's could be.
    Methadone is notorious for not being compatible with buprenorphine. When they switch you from methadone -> bupre in a medical setting there's always a few days transition without either medication. There's a good reason for this, as I imagine you found out.

    Everyone says tramadol mixes with bupe and I tend to believe them HOWEVER if you are on tramadol and shoot suboxone it gives a very distinct feeling of partial precipitated withdrawl. I am guessing the naloxone is displacing SOMETHING since the feeling is too wierd to be anything else, however with just buprenorphine, you will not deal with this unpleaseness.
    Have you tried pure buprenorphine while on tramadol? People react differently to different substances.
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    #49
    i actually need some help here people, I tried quitting H today. I have a habit average of about 1.5 grams of pretty good BT a day. I do inject. I brought myself down to twice daily (or 1 gram) meaning i can shoot up every 10-12 hours without too much discomfort. I waited almost 15 hours today, and i was in a mild to almost moderate WD. I plugged about 6 MGs of suboxone in a solution. I was sent into PWD in about 20 mins. I quickly took a shit because it started giving me major diarrhea and i was nauseous. I then shot up about half of what i normally do recreationally, about .25 g. The PWDs went away for the most part, so my question is how do i proceed if i want to quit? I have the suboxone in me and i know its doing something because im not high really i just feel normal. Clear headed and all that. I feel almost like im just on subs. Now do i just take anohter sub when i start to feel a little crappy cause I already have the drugs in my system or what?
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    #50
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    Try to stay without as long as you can. Preferably something like 24-48 hours. Then start the suboxone.
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