Didnt plan for surgery when I started this
Member
Join Date: Feb 2014
Location: Western NY
Posts: 1,209
Bartacomus - thanks for bringing up the topic of some of the science behind the suboxone. There were a couple points that you made that I wanted to follow-up on. None of these change your basic message, but I believe some of the nomenclature was off.
Heyzues - here I am hijacking another one of your threads with extensive science material. I hope you don't mind. In fact, I hope that you find it beneficial. Bupe has some rather unique features to it amongst the narcotic class. One thing that hasn't been mention yet is a short-term switch from suboxone to methadone. That would give you the pain relief from a full agonist, but it would be the closest match to your current suboxone program (i.e. dosing once or maybe twice per day). I think it is something to at least mulling over and discussing with your doctor if you like the idea. Also, I don't know about cross-tolerance between methadone and bupe, but methadone tends to have a low cross tolerance with a lot of other opis. That is why folks are able to go from mindboggling amounts of short-acting opis to doses of methadone in the tens of mg range.
Again, I have used short-acting opis after taking suboxone, but it was always to abort a switch from a short-acting opi to suboxone. I was able to feel the effects of the short-acting opi in those cases, but I also had only taken the subs for a brief period prior to that. From everything I have read on the subject it is dangerous to do so, because you typically have to take a substantially higher dose to be able to blow through the subs. For whatever reason though, in my case I didn't need to take that much more than normal. I doubt that would have been the case if I had taken the subs for a longer period of time.
Bupe actually works on the opiate receptors as a partial agonist, not an antagonist. However, it has an extremely strong binding affinity, and will essentially outcompete most other narcotic compounds for the receptor sites. Given the fact that the bupe only partially activates the receptors, it ends up generating less 'activity' than the full agonists (e.g. hydrocodone, oxycodone, morphine, etc.).
The bupe actually even outcompetes naloxone with it's extraordinary binding affinity, which is why folks are able to IV it despite the fact that the naloxone is supposed to prevent that. Even though the naloxone gets in the system via IV it has a lower binding affinity to the opiate receptors and the bupe binds instead of the naloxone. So it is binding affinity rather than bioavailability that is causing the naloxone to fail to stop the bupe. You are right though, naloxone has an insignificant oral bioavailability. Sublingually though, I was surprised to see that it has some bioavailability when the strips are used. In a recent thread on here I posted the report where I saw that. I don't remember the numbers off the top of my head, but I do know that it was enough for the naloxone to be pharmacologically active. The issue is that 2mg of naloxone is a LOT of it. Even 10% of that getting in your system would be a problem unless the bupe was able to outcompete it.
I have read a few reports on this topic, but it has been a while. Do any of the reports you read stick out in your memory as good ones to read? If so, I would be interested in checking them out. If you can send the title I can look them up. A link and/or pdf would be even better.
As far as the low dose naloxone goes, I believe the theory is that your body will naturally try to reach homeostasis via changes to the opiate receptors. While we get tolerance from repeated use of full agonists in the form of down regulated opiate receptors (e.g. changes in the actual number of receptors, changes to how sensitive the receptors are, etc.), in theory you could get the opposite if you were constantly exposed to something that will block the opiate receptors (i.e. naloxone). That is how the theory behind low-dose naloxone goes I believe.
Someone may be able to regain sensitivity to natural endorphins that way. I have to wonder if the complete blockage of opiate receptors would interfere with day-to-day life. Would you still get the feel-good effects of positive life experiences? Would exercise, chocolate or sex be as rewarding or would it be a dull shell of its normal self? It would be interesting to hear from anyone that has been on naloxone as to its impact on day-to-day enjoyment of life.
Personal Aside on Suboxone IV Myth:
By the way, I have found it to be mindboggling that suboxone does not work as it was supposed to, the medical community appears to be willfully ignorant of this. The drug manufacturers were only able to get the CIII status in the US because they pitched it as non-IVable. I have to admit that I have never personally IVd suboxone though. There are dozens and dozens of anecdotal reports from addicts saying that they did it though, and I have witnessed someone do it personally. The person that did IV the suboxone got lit up though. I am not sure if that was the naloxone working as marketed or if it was just precipitated withdrawal from taking the bupe too soon. In any event, a simple search on the web shows that there are a ton of folks out there that are IVing the subs. Surely there in an addict somewhere that told their sub doctor that the marketed effects of naloxone on someone IVing subs is a myth. I can see the sub doctor now rolling their eyes and saying to themselves "...great another know-it-all addict...don't they realize that I read the report issued by the manufacturer and it says that the naloxone will stop any high if it is taken IV...these addicts always come in here with the biggest ******** stories..."
Heyzues - here I am hijacking another one of your threads with extensive science material. I hope you don't mind. In fact, I hope that you find it beneficial. Bupe has some rather unique features to it amongst the narcotic class. One thing that hasn't been mention yet is a short-term switch from suboxone to methadone. That would give you the pain relief from a full agonist, but it would be the closest match to your current suboxone program (i.e. dosing once or maybe twice per day). I think it is something to at least mulling over and discussing with your doctor if you like the idea. Also, I don't know about cross-tolerance between methadone and bupe, but methadone tends to have a low cross tolerance with a lot of other opis. That is why folks are able to go from mindboggling amounts of short-acting opis to doses of methadone in the tens of mg range.
Again, I have used short-acting opis after taking suboxone, but it was always to abort a switch from a short-acting opi to suboxone. I was able to feel the effects of the short-acting opi in those cases, but I also had only taken the subs for a brief period prior to that. From everything I have read on the subject it is dangerous to do so, because you typically have to take a substantially higher dose to be able to blow through the subs. For whatever reason though, in my case I didn't need to take that much more than normal. I doubt that would have been the case if I had taken the subs for a longer period of time.
Originally Posted by Bartacomus 
Buprenorphine is also an antagonist even without naloxone in the treatment.
Originally Posted by Bartacomus
suboxone is the only buprenorphine compound I know of contains naloxone, which is to discourage abuse. The narcan/naloxone WILL rob receptor sites of opiates, but has no effect on Buprenorphine with a tiny oral bioavailability.
Originally Posted by Bartacomus
There are some reports now, that minute doses of narcan might actually promote analgesia.
As far as the low dose naloxone goes, I believe the theory is that your body will naturally try to reach homeostasis via changes to the opiate receptors. While we get tolerance from repeated use of full agonists in the form of down regulated opiate receptors (e.g. changes in the actual number of receptors, changes to how sensitive the receptors are, etc.), in theory you could get the opposite if you were constantly exposed to something that will block the opiate receptors (i.e. naloxone). That is how the theory behind low-dose naloxone goes I believe.
Someone may be able to regain sensitivity to natural endorphins that way. I have to wonder if the complete blockage of opiate receptors would interfere with day-to-day life. Would you still get the feel-good effects of positive life experiences? Would exercise, chocolate or sex be as rewarding or would it be a dull shell of its normal self? It would be interesting to hear from anyone that has been on naloxone as to its impact on day-to-day enjoyment of life.
Personal Aside on Suboxone IV Myth:
By the way, I have found it to be mindboggling that suboxone does not work as it was supposed to, the medical community appears to be willfully ignorant of this. The drug manufacturers were only able to get the CIII status in the US because they pitched it as non-IVable. I have to admit that I have never personally IVd suboxone though. There are dozens and dozens of anecdotal reports from addicts saying that they did it though, and I have witnessed someone do it personally. The person that did IV the suboxone got lit up though. I am not sure if that was the naloxone working as marketed or if it was just precipitated withdrawal from taking the bupe too soon. In any event, a simple search on the web shows that there are a ton of folks out there that are IVing the subs. Surely there in an addict somewhere that told their sub doctor that the marketed effects of naloxone on someone IVing subs is a myth. I can see the sub doctor now rolling their eyes and saying to themselves "...great another know-it-all addict...don't they realize that I read the report issued by the manufacturer and it says that the naloxone will stop any high if it is taken IV...these addicts always come in here with the biggest ******** stories..."
Member
Thread Starter
Join Date: Feb 2014
Location: not where you are
Posts: 70
as for methadone: way ahead of ya. I have been thinking that all along. Right along with what I am doing, but with some pain relieving effects. plus a very long half-life so in theory a very easy switch.
i doubt i will ever find a doc to agree though.
and, i live at least 3 hours away from the nearest city that would have a methadone clinic.
but yeah, i brought it up to my current doc who said 'methadone is evil'.
i doubt i will ever find a doc to agree though.
and, i live at least 3 hours away from the nearest city that would have a methadone clinic.
but yeah, i brought it up to my current doc who said 'methadone is evil'.
Member
Join Date: Feb 2014
Location: Western NY
Posts: 1,209
Heyzeus - that is a typical response from one of those dimwits. "Oh, your suggestion is 'evil', but I don't have a ******* clue what to do. It is too complicated, and I am too lazy to read research reports on it or to call a colleague."
It has been a while since I have graduated now, but I remember seeing the kids heading off to medical school. It is no longer the 'A' students. They are lucky to get the 'B' students these days. Going forward they are going to get paid less and less, which is just going to compound the problem. Helping people is great, but that isn't going to pay for their massive loans taken out to pay for medical school. It is a slow motion train wreck at this point.
It has been a while since I have graduated now, but I remember seeing the kids heading off to medical school. It is no longer the 'A' students. They are lucky to get the 'B' students these days. Going forward they are going to get paid less and less, which is just going to compound the problem. Helping people is great, but that isn't going to pay for their massive loans taken out to pay for medical school. It is a slow motion train wreck at this point.
Member
Join Date: Mar 2015
Location: Houston Texas
Posts: 45
I wanted to make a comment on that Suboxone Myth beforehand so bad, but held my tongue. However since you mentioned it Id like to bolster what you mentioned, so that people know these things have happened to more than just one person.
Suboxone is indeed abused by IV, and about the only good the naloxone provides is if someone already on a full agonist opioid attempts to inject Suboxone. If someone has regulated themselves on Suboxone, and then injects some, it has no effect. I am embarrassed to admit it, but I have tried this.. and didn't become sick. They highly advertise this stuff, and I cant believe it.. It is text book misinformation by these companies and docs.
as for nomenclature, I always know what I want to say, but sometimes get the wrong words. i.e. I should have said straight buprenorphine is an agonist-antagonist, instead of just saying it had antagonist effects.
I never put 2 and 2 together about even though oral bioavailability is tiny with narcan, but even though IV bioavailability is factors more available, that the end result is nil due to the Opiates relative affinity... and how someone regulated on Sub, can abuse and inject it, and not suffer the advertised reaction.
I wasn't as surprised about there being some b/a orally, but i also read later on, (ill try to find you the paper) that the method used to calculate buccal/sublingual bioavailability actually had a flaw in it, and is possibly misreported..
also, you wondered about naloxone and life interference, and i do know that Naloxone not only affects exorphines, but prevents the action of endogenous chemicals as well.
i will look for that paper you asked about, and the ones i mentioned.. i like the NIH website, they start with good abstracts and then summaries, and then sometimes youre allowed to read the entire report.
im sure i missed a hundred things i needed to reply to.. sorry if so.
oh, ill also testify being at a doctors who sent me home without my money or a proper treatment due to his/her lack of desire to investigate the claim.
Suboxone is indeed abused by IV, and about the only good the naloxone provides is if someone already on a full agonist opioid attempts to inject Suboxone. If someone has regulated themselves on Suboxone, and then injects some, it has no effect. I am embarrassed to admit it, but I have tried this.. and didn't become sick. They highly advertise this stuff, and I cant believe it.. It is text book misinformation by these companies and docs.
as for nomenclature, I always know what I want to say, but sometimes get the wrong words. i.e. I should have said straight buprenorphine is an agonist-antagonist, instead of just saying it had antagonist effects.
I never put 2 and 2 together about even though oral bioavailability is tiny with narcan, but even though IV bioavailability is factors more available, that the end result is nil due to the Opiates relative affinity... and how someone regulated on Sub, can abuse and inject it, and not suffer the advertised reaction.
I wasn't as surprised about there being some b/a orally, but i also read later on, (ill try to find you the paper) that the method used to calculate buccal/sublingual bioavailability actually had a flaw in it, and is possibly misreported..
also, you wondered about naloxone and life interference, and i do know that Naloxone not only affects exorphines, but prevents the action of endogenous chemicals as well.
i will look for that paper you asked about, and the ones i mentioned.. i like the NIH website, they start with good abstracts and then summaries, and then sometimes youre allowed to read the entire report.
im sure i missed a hundred things i needed to reply to.. sorry if so.
oh, ill also testify being at a doctors who sent me home without my money or a proper treatment due to his/her lack of desire to investigate the claim.
Currently Active Users Viewing this Thread: 1 (0 members and 1 guests)
