could injecting Suboxone reverse opiate OD?

[chronicpain247]

OK, here is something Swim was thinking about after listening to NPR today when they were talking about giving out nalaxone nasal inhalers that come in opiate rescue kits, in major cities. Which Swim thought was really cool.

Anyway Swim was told by a doc once in a suboxone treatment program that the reason there is the small amount of nalaxone in Suboxone is to prevent the IV use of the medicine. Swim was told that naloxone is very poorly absorbed orally but very efficiently by IV and when shooting Subs the nalaxone would prevent any effects from the Bup.

So what Swim was wondering was if someone was ODing could someone give them an injection of Suboxone and have it act much like a narcan shot?

Swim have read on this and other forums people saying that the reason you will go into instant Withdraw if you take Suboxone before you are in WDs already, is because of the naloxone but according to the docs Swim have talked to that is not the case, but rather the reason for this is because Bupanorphine adheres much more strongly to the opiate receptors than other opiates and it actually rips the other opiates off the receptors and throws you into WD, and that the naloxone is not even absorbed orally at all. So if swims therory is right then you would have to inject the Subs to bring someone back from the brink.

Does anyone know if this would work? if so the maybe some IV users would consider keeping some Subs around for this purpose.

[samuraigecko]

Originally Posted by chronicpain247

. . . . but rather the reason for this is because Bupanorphine adheres much more strongly to the opiate receptors than other opiates and it actually rips the other opiates off the receptors and throws you into WD, . . .

This is not actually the case. The amount of opiate introduced into the body is far greater than the amount of endomorphin produced by the body (a type of endorphin which opiates mimic to produce the euphoric effects).

The introduced chemical, in this case the opiate, travels faster than the natural endorphin which it mimics and therefor adheres to the receptor surface quicker because it can get there quicker. As the introduced opiate is depleted and its metabolite released from the receptor and back into the system another takes its place. This all happens rather quickly (constantly, within seconds, for the duration of the acting period of the drug). Think of it as allowing someone into your house for 6 hours and letting them flick the light switch on and off.

The reason why Naloxone works is because it can get to the receptor before the other opiates can. I.E: it moves faster than either the natural endorphin or the introduced mimic, Therefor making a BLOCKADE against the receptors which lasts longer than the life of the introduced opiate itself. Think of this as being able to get to previously mentioned light switch BEFORE the other person and not allowing them to switch it on and off.

Since the actual opiates which are adhering to the receptor surface with the nitrogen bond are basically doing their job and then moving on rather quickly then this allows the Naloxone to reach and adhere to the receptor making the block before the next introduced OD opiate can reach it. Naloxone does not actually "kick another opiate off the receptor" but rather replaces it as the introduced opiate has to leave the receptor rather quickly. Naloxone, because of its structure, remains on the receptor for longer, altho this is still seconds, but there is more naloxone molecules waiting in line which have pushed all the other opiates out of the line.

Think of this as being in line for a heavy metal concert and then a heap of big ass furry bikers roll up and kick in front of everyone in the line. There is a bit of a fight for the positions but ultimately the bikers end up winning. Even though you would still be IN the line the bikers are always gonna get there first because there is a larger supply of them which have the muscle to move quicker and the boldness to do so. So by the time you reach the concert there is nothing to do except for watch the backs of the said bikers. LOL.

One has seen the injection of suboxone done when someone has wanted to "come down" off his hit (for a reason) and it did not work so the answer would be No, it doesn't work. At least not in that instance.

hope this has been of help.

[chronicpain247]

Originally Posted by samuraigecko

This is not actually the case. The amount of opiate introduced into the body is far greater than the amount of endomorphin produced by the body (a type of endorphin which opiates mimic to produce the euphoric effects).

Thank you for all the great info. I always like to learn more and understand better.

One thing though, I am sure your correct in saying that the idea would not work, but what swim had said about the other opiates being ripped off the receptors, was actually in reference to what the Buprenorphine does, not the naloxone. At least this is what swim was told by his addiction specialist: when a person takes Bup and they are not in complete withdraw yet, meaning that the other opiates are still present in the system, that the bup, not the naloxone, is strong enough to attach itself to the receptor and therefore send said person into immediate withdraw. Swim was told that when taken orally the small amount of naloxone in Suboxone does not even have any effect do to its poor ability to be absorbed orally. Is this correct?

the process you mentioned may be the same, regardless of the drug doing it, but in the sentence you quoted I was actually talking about the effects of the Bup and not naloxone. Do you know why this happens and is it the same process as the one you mentioned, only performed by the Bup and not the naloxone?

This is kind of off the topic since we already established that an injection of suboxone will not bring you out of an OD, I just wanted to clarify what I was talking about.

thanks for being cool about the misinformation and not jumping down my throat like some people.

[samuraigecko]

Originally Posted by chronicpain247

... what the Buprenorphine does, not the naloxone. At least this is what swim was told by his addiction specialist: when a person takes Bup and they are not in complete withdraw yet, meaning that the other opiates are still present in the system, that the bup, not the naloxone, is strong enough to attach itself to the receptor and therefore send said person into immediate withdraw....


...thanks for being cool about the misinformation and not jumping down my throat like some people....

The specialist only said it in terms like that because he is probably used to talking to more uneducated people and tried to put it in a way that a layman could understand better. Bupe does not actually kick opiates off the receptor but rather has a higher affinity for binding TO the receptor and once there it sits on the receptor for longer. (remember that this all happens in seconds but continually over the duration).

So if a person was on bupe and tried to shoot some Heroin of Morphine then because the bupe sits on the receptors for longer it acts like a guard against that receptor and the introduced opiate just moves along doing nothing. Think of this as an underage geek (the Morphine) walking past a nightclub he wishes to get into but the bouncer (the bupe) already knows the deal and will not let him in anyway.

One can also think of it like magnets (since it attaches by electromagnetics to the receptor in the first place)

... does not actually kick opiates off the receptor but rather has a higher affinity for binding TO the receptor ...

So one can see that naloxone and buprenorphine both have a higher affinity for bonding to the receptors than other opiates. Think of this as magnets of different strengths. The stronger magnets are going to attach themselves before the weaker magnets can. Once the site is filled the magnets can no longer attach because there is nothing for them to attach to. As the OD opiate (lets say Heroin) gets used up by the receptor and moves away (this happens within seconds) the Naloxone muscles past the other opiates and attaches itself producing an almost instant withdrawal because of its "magnetic attraction" or higher affinity for binding to the receptors. (This only applies to naloxone and not buprenorphine. Naloxone can "muscle past" but buprenorphine can only guard.)

One never jumps down another's throat, there is no such thing as a stupid question or even stupid people. Some people are actually SMART enough to ask questions which they are curious about, but some people view that as a weakness or stupidity for some reason which is why SWIY may have encountered resistance at some questions. There are other people out there whom think a certain way and cannot be swayed from their line of thought because they will always think they are right, thats just human nature for a % of people to do that. One will find that SamuraiGecko will ALWAYS answer a question with integrity and politeness and will try to answer the question as accurately as possible. Most of the time SamuraiGecko will also post links (as one may have seen in other posts by him) which will show that SamuraiGecko is infact telling a scientifically substantiated truth.

His advice would be to ask the questions SWIyou want to ask, who cares about the others. There are people here just like SamG who are willing and able to answer ANY question informatively and well with both integrity and politeness. One will begin to notice whom these people are just by the "tone of voice" in their posts and their reputation feedback (but do not go by feedback alone, make sure one can "sense the tone").

Hope this has been of help peace.

[chronicpain247]

Swim could swear that he wrote and posted this reply last night but I guess he was too far out there after 120mg of oral MS and 60mg of oxy up the old wazoo! He probably wrote it then forgot to post it, or maybe the wife walked in and he had to hide it. anyway here goes..

Originally Posted by samuraigecko

Think of this as an underage geek (the Morphine) walking past a nightclub he wishes to get into but the bouncer (the bupe) already knows the deal and will not let him in anyway.

First off Samurai let me just say that I really get a kick out of you analogies, they are hilarious, but yet informative!

Originally Posted by samuraigecko

As the OD opiate (lets say Heroin) gets used up by the receptor and moves away (this happens within seconds) the Naloxone muscles past the other opiates and attaches itself producing an almost instant withdrawal because of its "magnetic attraction" or higher affinity for binding to the receptors. (This only applies to naloxone and not buprenorphine. Naloxone can "muscle past" but buprenorphine can only guard.)

One question...If SWI-anyone was ODing and was giving narcan would that someone go into immediate full blow withdraw? I'm not saying that one would rather OD and possibly perish that WD, just curious. If so that has got to suck though, one minute your high as hell, the next you wake in a hospital and are in full blown WD. Ughh!! What a nightmare! If that is the case, how long does the naloxone hang onto the receptor before you could get another opiate onto there in order to get well again?

Thanks for all the good info. Swim does not IV but he just thought that this may be helpful if someone was in trouble and it actually works, plus his brain just never stops going and these are the kind of things he thinks about. Although he does think about other things besides drugs, just not that often!

Swim has only been on this forum for a short time but he has definitely noticed the tone swiy speaks of. Some of us are just so full of or selves that we think that we know it all and could never be wrong.

"No one is always never wrong."
(is that one of those double negative things that actually means that they ARE never wrong? I never did do that well in English class.) anyway...

on the other hand swim has also seen that this site and the majority of the people on here are just a wealth of information, and he is very appreciative to have a resource like this out there. so thank you all for you kindness and generosity!
Without all of you Swim would never have learned about sticking opiates in his butt! Where would Swim be with out you all? Probably right where swim is now, just with a drug free rectum...

One more thing how does one get these reputation points that you speak of? How do I know if I have any? What happens when you get some?


Thanks. Swim's colon and he thank you!

[samuraigecko]

Originally Posted by chronicpain247

Swim could swear that he wrote and posted this reply last night but I guess he was too far out there after 120mg of oral MS and 60mg of oxy up the old wazoo! He probably wrote it then forgot to post it, or maybe the wife walked in and he had to hide it. anyway here goes..

First off Samurai let me just say that I really get a kick out of you analogies, they are hilarious, but yet informative!

One question...If SWI-anyone was ODing and was giving narcan would that someone go into immediate full blow withdraw? I'm not saying that one would rather OD and possibly perish that WD, just curious. If so that has got to suck though, one minute your high as hell, the next you wake in a hospital and are in full blown WD. Ughh!! What a nightmare! If that is the case, how long does the naloxone hang onto the receptor before you could get another opiate onto there in order to get well again?

Thanks for all the good info. Swim does not IV but he just thought that this may be helpful if someone was in trouble and it actually works, plus his brain just never stops going and these are the kind of things he thinks about. Although he does think about other things besides drugs, just not that often!

Swim has only been on this forum for a short time but he has definitely noticed the tone swiy speaks of. Some of us are just so full of or selves that we think that we know it all and could never be wrong.

"No one is always never wrong."
(is that one of those double negative things that actually means that they ARE never wrong? I never did do that well in English class.) anyway...

on the other hand swim has also seen that this site and the majority of the people on here are just a wealth of information, and he is very appreciative to have a resource like this out there. so thank you all for you kindness and generosity!
Without all of you Swim would never have learned about sticking opiates in his butt! Where would Swim be with out you all? Probably right where swim is now, just with a drug free rectum...

One more thing how does one get these reputation points that you speak of? How do I know if I have any? What happens when you get some?


Thanks. Swim's colon and he thank you!

On each post there is a little red heart, you can click on this to add to the persons reputation.

Think of this as clicking on the heart on the top right of someones post and either approving or disapproving of their information or advice! LOL (had to do it)

SWIyou can either give good reputation points or bad reputation points. They create "reputation points" which shows the majority of the time weather or not a person knows what they are talking about.

Naloxone only stays on the receptor for a little longer than any other normal opiate. However, because of the saturation of the dosage given there will always be those naloxone molecules there to muscle in on spots which could normally be taken up by the OD opiate. Therefor the OD opiate never gets the chance to keep going on its little mission because it gets metabolized by that time.

One and SWIM have never had naloxone and one has no idea how long it takes for it to wear off and another dosage of good opiates to be effective. One is sure that WIKI would probably have the data for this though.

"Did they get high?"
"Hell yea, it Rectum"
LOL

Peace and have fun, hope it was informative

[psyche]

I think there's no naloxone in buprenorphine. Buprenorphine is only a partial agonist on the opioid receptors, and that's why it isn't as good as heroin or other full agonists. But it has a strong affinity for the receptors, so there's no point using other illegal opioids when being in rehab and treated with it. I've read that it has stronger affinity for these receptors than naloxone, and that's why they use respiratory stimulants instead of naloxone in case of buprenorphine OD.

[chronicpain247]

Originally Posted by psyche

I think there's no naloxone in buprenorphine.

No buprenorphine has no Naloxone in it but Suboxone does. It comes in two dosages, Im not sure off the lower one but I know that there is a 8mg one. I think it is 8mg of buprenorphine and 2mg of naloxone.

[psyche]

Oh yeah... suboxone. That comes as a surprise as I remember someone refuting this claim. So, if all these facts were true, then the only way it would make sense would be that naloxone would have weak bioavailability when taken orally, it would have more binding affinity on kappa-receptor to induce dysphoria if taken intravenously, and buprenorphine would be dominant at the mu-receptor as I read, but not a full agonist to prevent other opiates being used with it. That's how my sleep-deprived brains would make out the whole story, any corrections/comments?

[Laudaphun]

SWIM posted this story awhile ago somewhere else...

SWIM always told his friends that in his theory, that a suboxone should be able to be injected in the event of an overdose as a last resort. This is a true story. Ironically, SWIM went down for the count one time... his friends tried everything he'd trained them to do in the event of an OD. While they were not able to bring SWIM back to consciousness they grew more and more concerned. *The events in this story are mostly second hand account, as SWIM himself was unconscious and unaware of what was going on...

The tale goes like this. SWIM had not been using opiate for several months due to circumstances brought about by the legal system. Now, during this time, SWIM's friend had aquired quite a tolerance. Up until that point in time, it had always been SWIM with the highest tolerance. SWIM I.V. one stamp bag. While his friend I.V.ed a bag as well. SWIM's friend then did two more. SWIM was still pretty blasted from the first one and nauseous he might add, however SWIM's friend gave him another free bag to shoot. Well, SWIM was a little hesitant as he was a little nauseous from the first still(which had been several hours earlier), however proceeded to throw caution to the wind. Upon injection, SWIM felt an immense rush and knew he was gonna be nodding very soon, so SWIM thought to himself, "man, i gotta hurry and clean this rig before I nod out." It was an especially powerful rush. That was the last thing SWIM remembers. Everything after this is what SWIM's friend told him happened, so take it as you will.

SWIM's friend said after fixxing up, pulling the needle out, and then drawing water up into the syringe to rinse it out, he just dropped... hit the floor like a sack of potatoes. SWIM's friend who will be referred to as SWIF from now on became very concerned immediately. He tried to wake up SWIM but with no avail. He threw cold water all over SWIM to try to wake him up LOL. SWIF said that he began to lose SWIM's vitals. SWIF didn't think SWIM was breathing, and pulse kept getting weaker. Eventually, SWIM began turning blue and SWIF could detect no pulse or breathing... could not wake SWIM up. It should also be noted that SWIF and SWIM were WAY out in the country... it would have taken an ambulence 30 minutes to get there minimum. So out of desperation, SWIF attempted to dissolve a suboxone and shoot up SWIM with it... This is where SWIM actually began to come to. SWIM remembers his friend slapping him with both hands, crying and telling him to wake up. SWIM didn't understand, SWIM was actually kind of pissed (upon first regaining consciousness) cause he was in one of the most intense nod/high he'd ever had. SWIM remembers telling SWIF that he was awake, but it was like SWIF couldn't hear him... SWIM kept telling SWIM that he was awake, and finally it was like SWIM came out of a daze all of a sudden and that amazingly intense euphoria turned to nauseau, dizziness, and dysphoria. At this point SWIM attempted to sit up but he couldn't. SWIF, in tears picked up SWIM and carried him to the chair as SWIM was not able to sit up under his own strength. SWIF held SWIM for some amount of time, sobbing and telling SWIM that he almost died and recounted the details of this story that SWIM could not remember. It was sort of a weird thing I guess, 1 grown man holding another crying for the longest time. Occasionally SWIF had to carry SWIM to the bathroom so he could vomit. SWIM remembers his chest hurting so bad from the dry heaves... there was just nothing to come up but he heaved and heaved. Please note that SWIM and SWIF were and are still best friends, not gay or anything... however at the same time it was a very intimate moment when a best friend thought he just watched his best friend die from a bag he'd just given him. It should also be noted that SWIF got on went to a Dr. and got on suboxone legally after this incident and has been on it and clean from Heroin for 3 years.

Back then, SWIM always figured that the naloxone in a suboxone pill could be used in an I.V. preparation to reverse an OD with a full agonist... but now SWIM thinks maybe the actual Bupe would bring someone out of an OD.

SWIM does not know if this is what saved him. Perhaps he just got lucky and came out of it from his friends constant slapping and prodding. SWIF did say that it was very difficult to create and I.V. solution so SWIM wonders how much actually got into him. Did the suboxone save him or was it just luck? SWIM doesn't know. But if Bupe will push someone into percipiated withdrawl by knocking off heroin from the opiate receptors in the brain, why not reverse an overdose? Despite the supposed difficulty in converting a suboxone pill into an injectable solution, buprenorphine would require only a tiny dose via I.V. to have an effect as comared to sublingually. SWIF did say that it was shortly after the suboxone injection that SWIM woke up. SWIM always had to hit SWIF as he had a hard time hitting his own vein, so it is very likely that the injection probably missed SWIM's vein and ended up being an IM or subcutaneous. I make no claims, I merely am relating a story, and a theory.

[Nin207]

I work for a program called the Overdose Prevention Project where I facilitate educational/support group at the county jail. This week in group I was asked if you could use Suboxone to reverse an overdose. I was not sure how to handle the question. I ended up telling him that I would not recommend it and decided that I would do a little research on this subject so that when it comes up again I am better equipped to answer it.

AFOF told me this story once where a girl is with a few friends and they all shoot up a bag of heroin and she ends up overdosing. After scrambling around to try to revive her one of the guys in the room pulls out his script for Suboxone and dissolves it into water to put it in a syringe. He ends up injecting her with it and shortly after she comes to. And, just like in this story she becomes very ill after for about 24 hours of vomitting. Now again no one can be sure if it was the suboxone that brought her back and I know that there are many myths regarding bringing someone back from an overdose that just happens to work in some situations but in the end is just a myth and does not have any reason for actually working. But this does have me wondering.