Silk Road forums
Discussion => Off topic => Topic started by: OperationPsyops on October 21, 2012, 01:28 pm
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2721267/
Suboxone is proven a crap pile - and I take that crap daily! No wonder we can't trust "certain government branches." This is c-r-a-z-y :o it should be illegal, and dammit, someone from the FDA should be doling out some answers >:( >:( >:(
We've known the drug manufacturer, who shall remain unnamed to prevent trouble, was doing away with the pill version, after convincing individual states and the FDA that the pill version was suddenly not safe to use - and why it was replaced with film. By doing away with the pill form, the drug manufacturer extended the patent for the Naloxone and buprenorphine combo, better known as Suboxone, until 2025! The manufacturer actually convinced the powers that be that the Sub pill we've been taking for years is suddenly unsafe to take and no longer available as of 9/25/12. Dirty, dirty, dirty. But...
The Naloxone is only used in combo with buprenorphine (those 2 drugs mixed = Suboxone) as a drug used to counter the effects of opiate overdose but studies have already shown that Naloxone is ineffective at preventing Suboxone abuse & Naloxone isn't even strong enough to reverse any effects of a buprenorphine overdose - but that's the whole reason Naloxone is an ingredient in Suboxone but according to the study, the buprenorphine is essentially the only drug working in the Suboxone (unless addict is only a very mild opiate user but not a "serious real-world addict"). So, even though studies have proven this to be true, why is the Naxalone still being used in Suboxone? Oh, I know why! Maybe because without Naloxone, the remaining ingredient would only be some cheap, readily available buprenorphine!
ASSholes >:(
I'm mad now so best quit while I'm ahead...
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first, i agree its fucked they could take the pill version off the market, but its completely due to profits from the patent and not because the naloxone doesnt work
you must have either misread or incorrectly interpreted the article you refer to because i interpreted it differently. your claim that it proves the only working ingredient in suboxone is the buprenorphine is wrong unless i really missed something. actually to me, it provides evidence for the exact opposite.
first you must understand a few things about the article - one is that this has no real meaning towards addiction because the entire article focuses on anti-nociception which is essentially pain relief. second, the supraspinal and spinal adminstration is not representative of actual ROAs, because no one administers the drug directly to their CNS or spine alone...
what the paper does say is that for pain relief there is an another mechanism at the level of the peripheral nervous system besides just the mu opioid receptor, which they provide evidence to suggest is the NOP receptor. however they even claim "this additional supraspinal component of buprenorphine does not negate the coexistence of an opioid component."
they also say that when naloxone is administered to the CNS it causes antagonism of bups effect on the mu receptor, which is, most simply put, the receptor responsible for the majority of the addiction. you can see this because the other inhibitor, PTX, of the G protein category, which includes mu, administered intra-cerebroventricularly (into the brain) also decreased anti-nociception.
therefore naloxone definitely could still have the intended effect of preventing people from shooting the bup, though some may claim it dosent work - there are definitely others that will confirm it keeps them from shooting it, unlike subutex. therefore i believe what you say about only the bup working and the naloxone having no effect is not accurate
not only that but ultra low dose antagonists have actually been shown to potentiate the effects of mu agonists - and therefore may be increasing the beneficial effects of bup, but thats a completely different paper and thread
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In the UK the addiction treatment agencies have completely backtracked over the years on their belief that buprenorphine is a cure-all wonder drug. The main method of treatment has now reverted back to methadone, or rather physeptone. One reason given for this is the treatment with bupe was not delivering the results that were expected, although the comparatively inexpensive physeptone might be the more accurate reason. Bupe is usually given as Subutex in the UK, which I believe only has bupe as the active ingredient.
MicroRNA, do you know anything about the longterm side effects of taking buprenorphine? In particular with respect to the receptors (mu, NOP, etc.) or other brain functions. Although, I only have a small case study that is nowhere near large enough to give statical predictions for the wider population, I truly believe we will begin to hear about unexpected long term side effects from bupe. A drug that was only ever meant for short term use originally.
Personally, I can't stand the stuff, for reasons I have gone into in length before, and I'm much happier taking my street bought methadone and not having to deal with the BS from the addiction agencies.
But everyone is different, especially when it comes to methadone vs. buprenorphine, the effects these drugs have seem to vary wildly from one patient to the next.
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i am definitely not advocating long term use of bup - my main point was just that the article provides evidence to back the claim naloxone is not "working" is not accurate imo
i think it is a horrible idea for people to maintain long term on bup especially on the doses that are common these days - we really dont understand its effects long term certainly, but i do know the potency and impact on the opioid system, specifically the mu receptor and its down-regulation, are probably greatly under-estimated. i mean its fucking ridiculous docs will try to maintain people at dosages like 16 or even 24 mg... no wonder people are having issues getting off it... i think if one was going to use it long term the dose should be no greater than 1 mg and even then should be warned about the very likely at least prolonged even if mild acute withdrawal and a greatly extended duration of PAWS - i think the thing is no one really makes clear just how potent bup is actually
i do think however that it is truly a "miracle drug" for certain individuals who use it in the proper manner- but not everyone reacts the same way obviously. imo the most effective manner to use bup is for a short duration detox (or who just need to put off withdrawals for a couple days till their order arrives lol) - where bup allows an individual who truly wants to stop using but is unable to quit to benefit from reduced withdrawal and cravings if they are one of the lucky ones
rather than maintaining on these crazy doses though, an initial moderate dose should be used to stabilize, like 8 mg depending on the addiction severity, and then very quickly tapered to 2 mg in the first few days. then the last days of the first week get doses down around 1 mg, followed by the second week of around .5 mg, then quickly progressing to every other day 0.25 - 0.5 mg by the beginning of the third week. after three weeks it would be best to jump off or do one more week of the smallest amount possible every few days and then just handle the much more bearable withdrawal from there. no more than a few weeks, to a month absolutely, if they want to avoid the negative effects of bup w/d for the most part
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MicroRNA I completely agree with you that these high dosage, long term courses of bupe are a 'horrible idea'.
I didn't mean my for previous post to sound confrontational in any way. You've come across as someone who has a lot of knowledge on this subject, and I was just trying to tap into your knowledge.
I'm a strong believer that knowledge is key when it comes to harm reduction. :)
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Naloxone is not active unless injected. It is poorly absorbed because of it's size and ability to dissolve in fatty substances is exceptionally weak. Instead, when taking Suboxone as prescribed, naloxone is swallowed and absorbed in the small intestine. Naloxone is completely destroyed at the liver before it ever even reaches the systemic circulation (first pass metabolism).
All of the benefits of Suboxone come from the partial agonist buprenorphine. The ceiling effect of buprenorphine (the point at which taking more Suboxone does no good) causes a reduction in cravings. Naloxone does absolutely nothing to those reduce cravings or reduce euphoria, IF it is not injected.
Saying addicts shouldn’t use buprenorphine because it doesn’t have the opioid blocker and as a result, is addictive, unsafe or causes one to get a "high" is only partially correct; It is true that buprenorphine does not have the opioid blocker naloxone. but, naloxone has nothing to do with how Suboxone works - the ‘opioid blocker’ in buprenorphine IS buprenorphine and being a partial agonist has the same antagonist properties as Suboxone. (Info can be found here: http://www.ncbi.nlm.nih.gov/books/NBK64245/)
It is rare to find an addict with buprenorphine as their preferred drug and as long as its not being shot up and is taken by those wanting to end their opiate addiction, both buprenorphine and Suboxone are equally effective . If an addict wanted to shoot up, heroin would be cheaper vs buprenorphine, so it would be unlikely an addict would choose to shoot up the more expensive buprenorphine. Numerous studies over this last year highly suggest that those who have injected Suboxone in the past did not experience the withdrawals that would be expected from combining a low-affinity antagonist with a high-affinity partial agonist.
Naloxone was only added to Suboxone in an effort to dissuade patients from injecting the tablets. Naloxone is supposed to induce precipated withdrawals and prevent any euphoria, etc., but because buperenorphine is more attracted to opioid receptors vs. naloxone, it does not induce precipated withdrawals or prevent getting high.
Imo, the difference is buprenorphine is only about 3 bucks and I believe misinformation, all around, is what allows the makers of Suboxone to continue to roll us over and have their way.
http://www.ncbi.nlm.nih.gov/pubmed/11862344
http://www.ncbi.nlm.nih.gov/pubmed/11064186
http://www.ncbi.nlm.nih.gov/pubmed/8689806
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I was told that even if the naloxone is present in Subs, the binding affinity of Bupe is so strong it beats out any other substance to the receptor.
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I was told that even if the naloxone is present in Subs, the binding affinity of Bupe is so strong it beats out any other substance to the receptor.
That's true and can be found in this study on page 5:
http://www.naabt.org/documents/Practical_Conciderations%20.pdf
As for the patent, many people have been told many things, including one drug rep who gave the following as a reason to Dr. Burson (addiction doc):
“And don’t you think the tablets are a relapse trigger? Nearly all patients had been addicted to opioid tablets, and using them to get high. Now if you prescribe a tablet to treat the addiction…the sound of pills rattling in a bottle is a trigger for many addicts. If the patient has snorted pills, they may misuse the tablets and crush them into a powder to snort.” ::)
That can be found here: http://janaburson.wordpress.com/2012/05/12/pharmaceutical-companies-behaving-badly/
But omg, Dr. Junig, a psychiatrist in WI treating addicts, has the best letter ever written to a CEO. He addresses the issue of naloxone being worthless in Suboxone.
http://www.suboxonetalkzone.com/dear-ceo/
There's tons of research, using the scientific method, found on many legit sites online. Obviously, the sites I list in this reply are doctor's opinions but I did post numerous links yesterday with research. Also, I need to correct a comment I made yesterday...bupe is only about $3 per pill, not just a $3 price difference compared to Sub, which is triple 3 bucks per film!
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WOW! That letter is awesome.
I'm curious to know how many patients taking Suboxone go through insurance. Those $50 coupons seem like they were made to motivate the doctor/patient to switch to the film. It has been nice to get my subs w/o a copay but I worry if and when they discontinue the promotion. That being said, I feel for the people w/o insurance. The prices for office visits and medicine is ridiculous.