Opioids always wondered what determines what maintenance you receive ( methadone vs bup )

[Quere]

Would that change increasing the IV dose, ie 2 pills instead of one, or 2 instead of 4?
Is there a point at which the Naloxone overpowers the Buprenorphine?

No it doesn't, at least as I understand it. Binding affinities are static and don't change with dosage. Actually scratch that, there probably is a point where it would, in the same way that the blocking effect of buprenorphine can be (in some people at least) overwhelmed by increasing dosage of heroin (or other opioid) in order to get high.

But I imagine it would take a shitload of naloxone. I believe buprenorphine overdose is tricky for this reason, as it outcompetes naloxone in binding affinity and stops it from reversing overdose.

 

[Nicomorphinist]

There is a big part of the narcotic euphoria which is the result of the body feeling better than it did a moment ago in pain and/or withdrawal, and the bang which comes with injecting is a manifestation of this and is the direct physiological result of the opioid receptors being turned on . . . with methadone, or something else in the system already, the original state is not all the way down at feeling shitty, so the bang is what is missing. For example, one time when I got back from the chemists' with bottles of Dilaudid HP and equipment and potentiators &c, I still was high and pain free from very potent poppy pod tea, piritramide I shot into my leg several hours earlier, and extended release codeine HCl (Perduretas) so I realised that I would be even higher if I banged some D at this point, but it would be wasteful and there would be neither the bang nor the rush, as the rush in such a case is a parallel physiololgical experience caused by the release of histamine and vasodilation. So I waited several hours and was glad I did . . .

 

[Quere]

It certainly isn't an issue with the ratio present in suboxone tablets, I've injected at least 16mgs sub (maybe 32mg, was a long time back) before which comes to a total of 4 mgs naloxone (I think it's a 4:1 ratio of bupe/nal) and never experienced any WDs

 

[Quere]

There is a big part of the narcotic euphoria which is the result of the body feeling better than it did a moment ago in pain and/or withdrawal, and the bang which comes with injecting is a manifestation of this and is the direct physiological result of the opioid receptors being turned on . . . with methadone, or something else in the system already, the original state is not all the way down at feeling shitty, so the bang is what is missing. For example, one time when I got back from the chemists' with bottles of Dilaudid HP and equipment and potentiators &c, I still was high and pain free from very potent poppy pod tea, piritramide I shot into my leg several hours earlier, and extended release codeine HCl (Perduretas) so I realised that I would be even higher if I banged some D at this point, but it would be wasteful and there would be neither the bang nor the rush, as the rush in such a case is a parallel physiololgical experience caused by the release of histamine and vasodilation. So I waited several hours and was glad I did . . .

I totally agree. The contrast between withdrawal/high or sober/high is a big part of the rush. It never feels as good shooting mdone in the evening when I've still got decent blood levels from an oral dose that morning. But If I inject in the morning when I'm in withdrawal it's much more pleasurable.

 

[Nicomorphinist]

No it doesn't, at least as I understand it. Binding affinities are static and don't change with dosage. Actually scratch that, there probably is a point where it would, in the same way that the blocking effect of buprenorphine can be (in some people at least) overwhelmed by increasing dosage of heroin (or other opioid) in order to get high.

But I imagine it would take a shitload of naloxone. I believe buprenorphine overdose is tricky for this reason, as it outcompetes naloxone in binding affinity and stops it from reversing overdose.

When buprenorphine and other bridged oripavine derivatives like etorphine and dihydroetorphine were developed, they also developed a structurally related antagonist for them, diprenorphine, Merck 5050, which is the antidote/reversing agent which comes with the Immobilon large animal tranquilliser dart kit -- since they know that buprenorphine has such strong binding and have had difficult-to-treat overdoses because of this, does anyone know if there is an actual reason why diprenorphine is not available alongside naloxone?

In fact, diprenorphine is buprenorphine with a cyclopropylmethyl group added at the 17 position on the morphine carbon skeleton, where the N-allyl to make nalorphine, naloxone and so forth also goes, to make the antagonist, just as they have developed N-allyl and cyclopropylmethyl antagonists for practically all of the semi-synthetics and opiates (N-allyl-codeine aka nalodeine was the first antagonist discovered, in 1915) as well as levorphanol, pethidine, phenoperidine, and a number of others . . . in the case of naloxone, the N-allyl oxymorphone derivative, the corresponding cyclopropylmethyl antagonist is naltrexone . . .

 

[VanOccupanther]

I don't know about you guys but I rather liked methadone...once you go over 300mg it gets pretty nice.

Once, someone called the paramedics on me when I was nodded on phenobarbital and they thought I had OD'd on opioids. I wake up, and am plenty alert, and after pleading for them to not do it the paramedics inject me with an antagonist (mind you, i was on 380mg of methadone at the time). You can imagine the pure horror of that precipitated withdrawal (spontaneously and uncontrollably shitting myself).

I was there for a few hours, in sheer horror, and was released. Of course, i go back home and consume 890mg of methadone, which I believe was the largest dose I've ever consumed, and eventually fall asleep peacefully in a bowl of cereal. Fuck those paramedics.

That sounds horrible!!

At my clinic (in the uk) they gave me the choice of either meth or bupe (I had/have a fairly general opiate addiction, mostly oxy/dhc) I chose bupe as I’d heard from enough people that methadone is as bad if not worse than what I was doing. Bupe (subutex specifically) is no picnic either. I’ve been on it for nearly three years now, very sticky. And if you come off it after being on it for a while it really sticks to your receptors for a while and your old drugs of choice do little to nothing (for me this was about a fortnight).

 

[Nicomorphinist]

I have sometimes wondered about the wisdom of agents which actually do literally blockade the opioid receptors such as buprenorphine and giving people naltrexone after a certain point since morphine and oxymorphone are used In emergency medicine when people are having heart attacks not to kill the pain but because the drugs work on the heart to get it back in normal operation, and then of course, what happens to someone in an automobile accident or who got pushed out of a window? I hear discussions again amongst some pinhead Bolshevik dog-fucking drugs "experts" in the US about coming up with a "vaccine" for narcotic addiction -- sort of de Sade meets A Clockwork Melonhead . . . Jesus Christ, just leave these poor people alone . . . the cost of manufacturing open chain and morphinan synthetic opioids and farming and extracting morphine and the family are basically de minimis -- just make tonnes of it all day in and day out, and after shipping enough to the developing world, make it all available in vending machines like Sprite . . . of course, above a certain dose, narcotics make people love everybody and very patient, so the rehab billionaires are going to be begging for change on the street rolling around on a cart like Eddie Murphy in Trading Places, and in general, misanthropes who want to make things so hard for people and blame everyone for their problems will be even more marginalised and they won't be able to euchre people into listening to their sob stories and self-serving made up bullshit stories about drugs anymore . . . maybe if there is a riot somewhere they can put a little hydrocodone in the water tower and things will calm down . . .

 

[Quere]

I have sometimes wondered about the wisdom of agents which actually do literally blockade the opioid receptors such as buprenorphine and giving people naltrexone after a certain point since morphine and oxymorphone are used In emergency medicine when people are having heart attacks not to kill the pain but because the drugs work on the heart to get it back in normal operation, and then of course, what happens to someone in an automobile accident or who got pushed out of a window? I hear discussions again amongst some pinhead Bolshevik dog-fucking drugs "experts" in the US about coming up with a "vaccine" for narcotic addiction -- sort of de Sade meets A Clockwork Melonhead . . . Jesus Christ, just leave these poor people alone . . . the cost of manufacturing open chain and morphinan synthetic opioids and farming and extracting morphine and the family are basically de minimis -- just make tonnes of it all day in and day out, and after shipping enough to the developing world, make it all available in vending machines like Sprite . . . of course, above a certain dose, narcotics make people love everybody and very patient, so the rehab billionaires are going to be begging for change on the street rolling around on a cart like Eddie Murphy in Trading Places, and in general, misanthropes who want to make things so hard for people and blame everyone for their problems will be even more marginalised and they won't be able to euchre people into listening to their sob stories and self-serving made up bullshit stories about drugs anymore . . . maybe if there is a riot somewhere they can put a little hydrocodone in the water tower and things will calm down . . .

Yeah I feel sick when I here about those naltrexone depot injections they give these days. People use junk for a reason (s) and if you take away the ability to use junk to cope with their problems and don't provide any other treatment for those problems, what are they left with? A lot of pain/interpersonal problems/trauma etc and no way to feel better. I wouldn't be surprised if people killed themselves when they realise the problems causing the junk habit are still there but now they can't feel their drugs/get relief

 

[Nicomorphinist]

Yeah I feel sick when I here about those naltrexone depot injections they give these days. People use junk for a reason (s) and if you take away the ability to use junk to cope with their problems and don't provide any other treatment for those problems, what are they left with? A lot of pain/interpersonal problems/trauma etc and no way to feel better. I wouldn't be surprised if people killed themselves when they realise the problems causing the junk habit are still there but now they can't feel their drugs/get relief

It would be helpful if there were a complete physiological and pharmacological workaround to that kind of blockade, like causing similar effects by using completely different systems in the body and/or agents and techniques -- the fact that folks in prison discovered that they can use clonidine by itself to cause a seviceable functional equivalent of narcotic body load and anxiolysis is very interesting though I am not sure to what extent that can be extended and have things added to it. Loperamide won't work -- it is a full opioid agonist and is even sufficiently cross-tolerant with morphine that people taking it for diarrhoea need to index the dose, eventually go to diphenoxylate, then difenoxin, then something based on opium, codeine, morphine, or dihydrocodeine -- foiled again . . . The theory about the uncanny morphine-, piritramide-, and levorphanol-like feeling of ketamine at high doses is apparently zeroing in on some kind of agonism of the µ opioid receptor and side actions at NMDA and σ receptors and the same anti-nociceptive actions as levorphanol, piritramide, ketobemidone, methadone, dextromoramide, and other pure agonist opioids which hit all sorts of other things too. . . there is also the possibility I suppose of ketamine doing its work at one or more of the opioid receptors which are thought to exist but have not been definitively found and described yet -- ahh, 0 for 3

 

[HoldBack]

if dawn ever sets on me and forces me to go for maintenance at some point in life, what determines what they give you? ive never taken bup but methadone didn't really feel as great as morphine or oxy but it did the trick to keep wd at bay to say the least

It’s somewhat arbitrary.

I’ve been on both sub maintenance and mmt. Sub did not work for me. Methadone is extremely helpful but I haven’t been clean for a day in the 2 years I’ve been on it.

Sub has such a pronounced dose-response curve and ceiling effect (ie 8 mg and 24 mg will feel largely the same to most people. So the doctor tends to give you the dose they have seen the most success with. Of course they will factor in the severity of your addiction.

In terms of achieving abstinence, the only metric a doctor really looks at, The higher the dose a patient will tolerate, the better. Therefore, as long as diversion is not likely, most doctors will give you as much as you ask for (up to the 32 mg ceiling).

Methadone, on the other hand, is more complex as it’s a full agonist with accumulating respiratory depression.

At my clinic they ask if the dose is “holding you.” If yes, no dose increase will be considered. If no, a dose increase can be requested for the doctor to approve. Whether the doctor approves it is based on your ua results and attendance.

I could move freely up to 120. at that point they wouldn’t increase dose until my UAs were free of benzos (switched to kpin, tests came back negative).

I stopped requesting increases at 140 as I believe I’ve reached the peak of positive effects.

 

[Quere]

It would be helpful if there were a complete physiological and pharmacological workaround to that kind of blockade, like causing similar effects by using completely different systems in the body and/or agents and techniques -- the fact that folks in prison discovered that they can use clonidine by itself to cause a seviceable functional equivalent of narcotic body load and anxiolysis is very interesting though I am not sure to what extent that can be extended and have things added to it. Loperamide won't work -- it is a full opioid agonist and is even sufficiently cross-tolerant with morphine that people taking it for diarrhoea need to index the dose, eventually go to diphenoxylate, then difenoxin, then something based on opium, codeine, morphine, or dihydrocodeine -- foiled again . . . The theory about the uncanny morphine-, piritramide-, and levorphanol-like feeling of ketamine at high doses is apparently zeroing in on some kind of agonism of the µ opioid receptor and side actions at NMDA and σ receptors and the same anti-nociceptive actions as levorphanol, piritramide, ketobemidone, methadone, dextromoramide, and other pure agonist opioids which hit all sorts of other things too. . . there is also the possibility I suppose of ketamine doing its work at one or more of the opioid receptors which are thought to exist but have not been definitively found and described yet -- ahh, 0 for 3

Yeah what you mentioned about naltrexone and emergency pain relief for accidents and the like is also very concerning. That would be awful if someone with a naltrexone depot got severely injured and was unresponsive to opioid pain relief due to the antagonist.

Of course the abstinence-only-clean-freaks love naltrexone for opioid addiction despite having nowhere near the evidence base of conventional opioid agonist treatments.

I think these treatments should have had far more long term testing/research done on them before being allowed on the commercial market. I see that in the US judges are court ordering people into treatment with long term depot injections of these drugs instead of opioid agonist treatment (which has far, far more proof of effectiveness) just because of this dangerous misconception that methadone/buprenorphine and other opioid agonist treatments aren't "Real" recovery.

IMO one of the biggest problems with addiction treatment is that the people designing and administering these treatments have no interest in listening to what we want and what we think would help us become functional members of society because they believe they know what is best for us. They believe we should all strive to be "clean" and that this is inherently superior.

I couldn't give two shits about being "clean", what I want is to be able to be functional and relatively happy (of course noone is happy all the time) and if taking large amounts of opioids (and/or other drugs) everyday is what is required to achieve this then so be it.

 

[Nicomorphinist]

Yeah what you mentioned about naltrexone and emergency pain relief for accidents and the like is also very concerning. That would be awful if someone with a naltrexone depot got severely injured and was unresponsive to opioid pain relief due to the antagonist.

Of course the abstinence-only-clean-freaks love naltrexone for opioid addiction despite having nowhere near the evidence base of conventional opioid agonist treatments.

I think these treatments should have had far more long term testing/research done on them before being allowed on the commercial market. I see that in the US judges are court ordering people into treatment with long term depot injections of these drugs instead of opioid agonist treatment (which has far, far more proof of effectiveness) just because of this dangerous misconception that methadone/buprenorphine and other opioid agonist treatments aren't "Real" recovery.

IMO one of the biggest problems with addiction treatment is that the people designing and administering these treatments have no interest in listening to what we want and what we think would help us become functional members of society because they believe they know what is best for us. They believe we should all strive to be "clean" and that this is inherently superior.

I couldn't give two shits about being "clean", what I want is to be able to be functional and relatively happy (of course noone is happy all the time) and if taking large amounts of opioids (and/or other drugs) everyday is what is required to achieve this then so be it.

They have discovered that the human body makes its own morphine, codeine, hydromorphone, 6-monoacetylmorphine at a bare minimum and probably smack, a number of 1,4 and 1,5-benzodiazepines, DMT, 5-MeO-DMT, mescaline, oodles of ethanol, all manner of Tihkal and PhiKal entries and I believe psilocybin, psilocin, esters thereof, bufotenine, Angel Dust and/or Special K, dihydromorphine, probably all sorts of other morphine esters, and I think even nicotine, atropine, hyoscine, and all this certainly plus all the endorphins, naturally-occurring aphrodisiacs probably 800 000 times more potent than green M&Ms, and the fact that all of the above, and a number of other substances, have ready-made receptors made by the body and the probably arose in the first frogs, coelacanths, trilobites, or whatever . . .

Abstinence-only drugs and sex policy is the worst science fiction ever written, and everyone pushing it has some corrupt and sadistic and evil angle they are working, plus salving their egos because they see that people know they are idiots who do nothing but make themselves and everyone else miserable. Some of them have managed to find a way to make loads of dough from the whole thing, of course.

Even though the people prattling and crying crocodile tears about the fake opioid cri$i$ make a lot of us just sag and moan with tiredness and resignation when they get going, it is obvious that, amongst others:

• Chronic pain people,
• Folks who are at sixes and sevens with at least one other person or process or organisation because of taking drugs into their body,
• People who are exploring ways to live with drugs in a more workable way than they have been, like habituated people who see the metabolic hourglass over their heads and know it can cause them and others trouble,
• Everyone who cares about people in the above
• People who do not like government-assisted racketeering by people who own chains of rehab clinics and purvey junk science and hate philosophies about drugs and the people who use them
• People who are recovering who are being told by people like the miscreants above that what they are doing is not real recovery, such as Opioid Substitution Therapy, getting narcotics for diagnosed painful conditions, even if their addiction was not to narcotics to begin with
• People and organisations whose resources are being pilfered and misdirected to help these gangsters work on their fake cri$i$
• It seems like these gangsters and terrorists victimise more people all the time
• Doctors who are being terrorised by bureaucrats and politicians for helping people in pain

all of us and those who care about folks like that have to make sure they do not get away with spreading their lies and shoring up their protection rackets . . . there is research to do in a lot of cases, but the truth is all where it is easy to get to it, relatively speaking. It is also worth while to question their motives right to their faces too, because that is the worst part of it . . .

.. . and don't let these arseholes misdirect by blaming "Big Pharma" for whatever it is they object to -- big pharma and little pharma and some academics and non-profits make the medicines to help people in pain -- unless one owns an opium farm and a sophisticated organic synthesis lab at their house or wherever, someone needs to make the stuff, and at root the narcotic section of pharmaceutical companies, considering they have been terrorised by these people since before 1906 in the US and in some other locales since around then, what they are able to do is at least somewhat altruistic and especially these days is certainly courageous . . .

 

[Hezman94]

the uk will onlyy give it u taking heroin.
i told them i was taking morphine oxy off street and they jus said cut down
im on morphine script and they use slow release morphine in some countries for mainteance.

 

[Anthonysymington1967]

the uk will onlyy give it u taking heroin.
i told them i was taking morphine oxy off street and they jus said cut down
im on morphine script and they use slow release morphine in some countries for mainteance.

The uk will only give methadone for a heroin habit? Is that what you were meaning? Sorry that’s wrong mate. I’m on a small dose methadone maintenance of 30 ml for a Dihydrocodeine habit.

 

[DeathIndustrial88]

With the USA, I always figured the choice came down to whether you wanna give up your entire life or not, as in, being on methadone requires pretty much living next door to a clinic and having to go everyday, for an extended time until trust is achieved or whatever time limit they set. Where as with bupe, you can be given a take home script on the first day. Hell I got my first 30 day 12mg strip script that very first day. Bupe was nice in the beginning and much easier to get. I liked the up-and-go naturally stimulated feeling of bupe, probably because I was also a tramadol addict alongside a heroin addiction. But after 4 years of being on bupe, it has lost it's magic and cravings for heroin or a full agonist have returned. I would prefer to at least try methadone because I feel a full agonist will kill the psychological cravings better, but I don't have the time to give up my life to such a rigid program.

 

[negrogesic]

^^^Thank you for reviving this thread because it led to read nicomorphinists sentence:

"naturally-occurring aphrodisiacs probably 800 000 times more potent than green M&Ms"

 

[DeathIndustrial88]

^^^Thank you for reviving this thread because it led to read nicomorphinists sentence:

"naturally-occurring aphrodisiacs probably 800 000 times more potent than green M&Ms"

I've been compulsively reading all of nicomorphinists's posts. Very smart guy.

I was also shocked at the lack of people who didn't mention the ridiculous hoops some have to go through to be on methadone, making buprenorphine the only choice you can take. In my area, the clinics either offer one or the other (as in, none of the clinics offer an option). And the methadone clinics have outrageous obstacles. Although I wonder if it's changed much since the pandemic.

 

[negrogesic]

Methadone is good stuff.

It worked for me. As I've said I was on 380mg a day and eventually got sick of it. Been off it for a long time and while I'll always fuck with opioids to some degree I'm not burdened by physical opioid addiction, and when it does happen on occasion it is self limited.

It's weird too because methadone is now my favorite opioid. If someone offered me 40mg of methadone right now I'd take it in a heart beat. If someone gave me 1000 10mg pills I'd probably be able to contain myself to some degree. But I'd rather not be in that particular situation.

 

[DeathIndustrial88]

Methadone is good stuff.

It worked for me. As I've said I was on 380mg a day and eventually got sick of it. Been off it for a long time and while I'll always fuck with opioids to some degree I'm not burdened by physical opioid addiction, and when it does happen on occasion it is self limited.

It's weird too because methadone is now my favorite opioid. If someone offered me 40mg of methadone right now I'd take it in a heart beat. If someone gave me 1000 10mg pills I'd probably be able to contain myself to some degree. But I'd rather not be in that particular situation.

Did it stop producing any euphoria for your after being on it that long?

I've only ever had a few off chances to try methadone recreationally & I thought it was nice. I've been on bupe daily for 4 years now and even bupe gave me a nice feeling in the beginning. But now it's become so boring and I'm actually getting sick of it too. Always feeling so drowsy and my emotions are blunted (except for my pissed off ones lol). But I have no shame admitting i'm an addict and if I don't take something daily, I'm right back to drinking alcohol and DXM (if I can't find opioids). But since bupe is so boring now, i'm worried about picking up 'other' problems.

 

[negrogesic]

I think it did eventually stop having the same level of euphoria but it still feels like strong stuff.

My theory is that people should be allowed large doses of methadone so they are fully satisfied. Hopefully, like me, they just eventually get bored.

I never got full tolerance to the sedating effects of high dose methadone. I'd take my first dose in the morning (200mg) and two hours later id take a wonderful nap (when i wasnt working). In the afternoon id take another 180mg.

I was covered 24/7 and pretty toasty all the time. Eventually i just got bored and tapered off.

Problem was i never told them i was tapering off. I recieved all my methadone in 10mg pills (38 pills a day) and went only once every 3 months. I tapered down but saved the extras. It amounted to thousands of pills by the time i was off. I didnt touch them for years but eventually i did slowly use them all and did catch a very low level habit (like 20mg a day). The withdrawal was surprisingly bad from even that dose.

Those extra thousands of pills got me high as fuck. I would love a 40mg dose right now, bet I'd get high for 18 hours, with all that lovely methadone itching.

One of the best opioids imo, and ive tried a massive variety.