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Opioids Buprenorphine - euphoria, analgesia, dependence & addiction.

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Bluelighter
Joined
Apr 12, 2013
Messages
1,483
http://michaellinnell.org.uk/michae...d_punishment/pdf/CP6_Tart mermaid subutex.pdf


I just wanted to make sure that everyone got the chance to see this great work by a hero of HR, Michael Linnell; a gentleman, a gentle man and a man with the patience to be my friend.


I am sorry if these questions have been asked before but for further research into treatment of opioid dependence, can I ask anyone with personal experience as a user or friend/relative of user. No names, no pack drill.

1)Is buprenorphine euphoric? I was prescribed Temgesic for pain and even 2mg sublingually only gave a light feeling of wellbeing on par with 60mg of DHC. It was quite effective as an analgesic.
2)How does buprenorphine abstinence syndrome compare to that of dihydrocodeine, methadone and morphine?
3)How well does buprenorphine blockade other opioids? I know Suboxone was introduced to prevent euphoria but since it's Ki is similar to that of naloxone and it's T1/2 much longer, I've come across IV usage.
4)Has it been a useful stepping stone to getting off full agonists and/or has it been a stepping stone to full agonists? I have tried many opioids and think it a better option than tramadol, for example.

I am asking these questions as part of research into a possible update on HR information concerning the use of buprenorphine. Since the original booklets, the formulations have changed and new opioids have reached the market. I cannot see a good reason for oxycodone to have been introduced. The BNF specifies it as a second-line drug only to be used after morphine 'or similar high potency opioid' has failed to provide sufficient relief. We also have hydromorphone which from the limited amount I know seems somewhat less abusable than many other potent opioids. I have read many US users saying that hydromorphone is 'all about the rush'. I know oxymorphone is highly prized but I think I have only ever read a single report on Levo Dromoran (levorphanol) and that was oral use. The description was of a classic dual μ/NMDA ligand (long rush & sustained euphoria). Is it so rare that it has never been taken parenterally. This last point is because the UK still has Diconal (dipipanone + cyclizine), Scandinavia still has Ketogan (ketobemidone) and much of Europe still has Dipidolor (piritimide) or Heptalgin (phenadoxone).

At the other end of the spectrum, China widely uses A-237 (1-butyryl-4-cinnamylpiperazine) which appears to be another partial agonist although derivatives listed on the Eunoia Disc show some quite potent derivatives. If they are still partial agonists, they may be of some utility.

I thank you all for your time and if the booklet does end up being printed, how shall I best credit people?
 
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1. no, except for the first couple times using it with no opiate tolerance
2. its just like being off any opiate, unless you mean acute wd from bupe, in which case its milder but wayyy more drawn out than say morphine
3. not enough to stop someone from getting high if they really want to. ive gotten high on dope literally hours after dosing bupe, it just takes much more of the opiate of choice to replace bupes binding to the receptors. fentanyl breaks through it easily
4. im sure its been helpful to some people depending on their situation and choices around it, for myself it was a stepping stone to being able to stay on dope for years, selling my script and also saving it so as to avoid ever really having to deal with acute opiate wd...made me more plugged into the scene since i found new people wanting to buy bupe, and in that found new hooks for dope. but everyones gotta story, there are cases where bupe has helped people get off dope and get their lives together, just in my case its not one of them
 
The short duration of action is what makes hydromorphone different from the dual mu-opioid/NMDA receptor related opioids but it has properties similar to morphine and hydrocodone and metopon in particular, being a 14-dihydromorphinone like the latter two and oxymorphone, oxycodone, acetylmorphone and so forth. In addition to the others listed in the fourth item, it is possible that dextromoramide and proheptazine also have NMDA action.
 
http://michaellinnell.org.uk/michael_linnell_archive/crime_and_punishment/pdf/CP6_Tart mermaid subutex.pdf


I just wanted to make sure that everyone got the chance to see this great work by a hero of HR, Michael Linnell; a gentleman, a gentle man and a man with the patience to be my friend.


I am sorry if these questions have been asked before but for further research into treatment of opioid dependence, can I ask anyone with personal experience as a user or friend/relative of user. No names, no pack drill.

1)Is buprenorphine euphoric? I was prescribed Temgesic for pain and even 2mg sublingually only gave a light feeling of wellbeing on par with 60mg of DHC. It was quite effective as an analgesic.
2)How does buprenorphine abstinence syndrome compare to that of dihydrocodeine, methadone and morphine?
3)How well does buprenorphine blockade other opioids? I know Suboxone was introduced to prevent euphoria but since it's Ki is similar to that of naloxone and it's T1/2 much longer, I've come across IV usage.
4)Has it been a useful stepping stone to getting off full agonists and/or has it been a stepping stone to full agonists? I have tried many opioids and think it a better option than tramadol, for example.

I am asking these questions as part of research into a possible update on HR information concerning the use of buprenorphine. Since the original booklets, the formulations have changed and new opioids have reached the market. I cannot see a good reason for oxycodone to have been introduced. The BNF specifies it as a second-line drug only to be used after morphine 'or similar high potency opioid' has failed to provide sufficient relief. We also have hydromorphone which from the limited amount I know seems somewhat less abusable than many other potent opioids. I have read many US users saying that hydromorphone is 'all about the rush'. I know oxymorphone is highly prized but I think I have only ever read a single report on Levo Dromoran (levorphanol) and that was oral use. The description was of a classic dual μ/NMDA ligand (long rush & sustained euphoria). Is it so rare that it has never been taken parenterally. This last point is because the UK still has Diconal (dipipanone + cyclizine), Scandinavia still has Ketogan (ketobemidone) and much of Europe still has Dipidolor (piritimide) or Heptalgin (phenadoxone).

At the other end of the spectrum, China widely uses A-237 (1-butyryl-4-cinnamylpiperazine) which appears to be another partial agonist although derivatives listed on the Eunoia Disc show some quite potent derivatives. If they are still partial agonists, they may be of some utility.

I thank you all for your time and if the booklet does end up being printed, how shall I best credit people?

The thing with levorphanol now is that it is something like $100 US a tablet because the price was jacked up by that Shkreli fellow who spent time in the cooler. It lasts a long time when injected and of oral levorphanol, IM levorphanol, IV levorphanol as part of an old-school general anaesthesia technique, and the racaemate, Dromoran by itself or with a tiny amount of levallorphan, which is the levorphanol analogue of naloxone, I liked Dromoran the best and when I did have a script for levorphanol years ago I would take DXM with it to make it work better, The closest drugs to morphine made by total synthesis, and the euphoria feels like it, though I prefer the big M, whole opium products, morphine esters like nicomorphine, 14-dihydromorphinones like hydromorphone, oxymorphone and hydromorphinol, and some of the synthetics like phenadoxone, dipipanone, dextromoramide, piritramide, and ketobemidone.

China also uses dihydroetorphine the same way buprenorphine is used elsewhere, and two things I have heard of being available in Taiwan for maintenance and detox are a concentrated dextropropoxyphene linctus and/or effervescent tablets, and some pretty high-dose extended-release tramadol tablets.

I was not impressed by the euphoria of buprenorphine and try to avoid the bridged oripavine derivatives and fentanils because for all we know, above a certain level of affinity, exogenous agents could very well burn out opioid receptors rather than merely sticking and becoming unstuck.

I think that extended-release dihydrocodeine with injectable dihydromorphine or dextromoramide for intense craving incidents would be an ideal maintenance and slow detoxification protocol for a lot of people. Austria started the ER DHC over a decade ago and the Netherlands tried the dextromoramide idea with good results. Then there is always injectable hydromorphone and oral ER morphine too. Heroin addicts would really like nicomorphine and I personally think that acetylmorphone could do a wonderful job on that kind of thing and chronic pain -- a Dilaudid with legs with a come-up like smack.

In fact, the discussion of using extended-release DHC (Codidol) and morphine (MST Continus) started the same week that the new Suchtmittelgesetz went into effect in 1998 and methadone laws had to be tightened up because of accession to the European Union. That really cooked my goose. Turned me into a hard case Eurosceptic overnight. The 1920 Constitution is a real beauty -- the Constitutional Court has apparently ruled at least twice that Austrians have a right to take narcotics, and there is, to the best of my knowledge and belief, nothing as clear cut about not helping addicts as the US Harrison Narcotic Act 1914. Most countries don't, actually.

If methadone works well for somebody, so with levomethadone, which is methadone with the cardiotoxic dextro isomer removed.

The optimum may be a box of dry ampoules of smack and a phial of naloxone with some darts and sterile water once a week, and maybe some Klonopin for bedtime, and a chat with a nutritionist a couple of times a year, to be perfectly candid. Primary narcotic addicts and habitués are sensible, drearily sane, and bedrock stable people with a hell of a metabolic hourglass over their heads in my experience, and that would be of more use than seeing a head shrinker..
 
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