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Narcan: The Next Big Thing In Pain Management

Tchort

Bluelight Crew
Joined
Mar 25, 2008
Messages
2,392
They're going too far.

All for naught, as well. All for fucking naught.

It all started with Talwin; a few low-level healthcare workers came up with the T's & Blues combination, and shooting Pentazocine (which was unscheduled at the time) and Pyribenzamine (a.k.a. Tripellenamine, a common Rx cold/flu anti-Histamine of the day) spread across the country.

Then it started: Talwin NX. Pentazocine and Naloxone, combined in one pill. To stop intravenous abuse, they said. And it did: only, abuse never stopped, it just switched to oral and insufflation. A new combination was then discovered to be adequately euphoric to abuse: Talwin NX and Ritalin.

All was quiet for a couple decades, then Reckitt-Benckiser hit the lottery with their orphan drug Buprenorphine, owning the patents and branding rights for all of the Bupe products. The magic bullet that made this fortune and fame possible? Narcan. Add some, make money.

Suboxone; how a Big Pharma company reversed 80 years of American narcotics policy, the first bargaining chip at the peace table of the War On Doctors started in the '20s after the Supreme Court ruled on how to enforce the Harrison Act (by locking up doctors who prescribe narcotics addicts narcotics).

And how did they manage to take that giant step against the American Opiophobia? Put some Narcan in it.

Seriously. It worked for T's & Blues, remember? See, Pentazocine, Buprenorphine, both partial agonists, both have a long history of IV abuse and addiction, Naloxone cured the IV Talwin problem, we will prevent IV abuse of our Buprenorphine product from ever starting by putting the Narcan in first.

Sealed the deal; the FDA bought it. Only, no one ever thought to do bioassay tests on actual addicts, or run a trial on the drug use and abuse habits of sublingual Buprenorphine/Naloxone maintained patients (Come on, honestly, I know I'm not the only Suboxone patient who shot up his pills when everyone said the Naloxone would definitly cause precipitated withdrawals).

Doesn't matter though, Buprenorphine/Naloxone, the holy grail the drug warriors and drug czars of old were searching for, Suboxone, isn't half the myth they make it out to be.

But we forget the most important thing: it made Reckitt-Benckiser a mint. Europe had already accepted Buprenex, Subutex was just as readily jumped on without a hitch. Huge junk addict market in Europe to pry on, they didn't need the US and the rest of the world to make all that cash. But they did it anyway, Suboxone opened that door, and following suit parts of Asia followed us into Suboxone prescription maintenance (ask India and Bangladesh how well thats going now).

Anyway, thats the lead-up. Heres the point of the story:

Now that two working examples of narcotic/Narcan combination products are slick deal-makers in the American Big Pharma, Federal agency shakedown game, every other mom & pop pharmaceutical company is jumping on board with a Dope/Narcan product:

And they are getting approved! And funding! With excellent sales and profits projections!

The proof:

OXYTREK

While not Naloxone, it's still an antagonist, Naltrexone. Brought to us soon by Pain Therapeutics.

Oxycodone + Naltrexone in a pain relief pill.

Pain Therapeutics' oxycodone/naltrexone combination, OxyTrek. Factors driving the market rebound will include the premium pricing of these new therapies compared with current options, most of which will be available generically by the time the new drugs are launched.

"Improving on the significant side effects of analgesics is the near-term opportunity for drug developers, as it has been for many years, and a few companies will succeed in providing incremental improvements in safety or tolerability, despite the recent dramatic changes in the regulatory landscape," said Michelle Grady, therapeutic area director, Pain Management, at Decision Resources, Inc.

Meaning: "We're gonna make a ton of fucking money duping the government, the patients and the addicts"

The bells tolls already for OxyTrek:

Outcome Measures for this Clinical Trial

Primary Measures

The primary objective of this study is to evaluate the subjective effects of PTI-801 formulated with either 0.001 mg naltrexone or 0.0001 mg naltrexone compared to oxycodone alone in individuals with a history of opioid abuse.
Time Frame: At 30, 60, 90, 120, 150, 180 and 210 minutes post-dose

Secondary Measures

Secondary objectives include determining the safety and physiological effects of single doses of PTI-801 compared to oxycodone following oral administration in individuals with a history of opioid abuse.

Straight from the studies mouth, my moneys on results from this abuse liability tests putting OxyTrek well below likability for plain Oxycodone, in those w/o a history of opioid abuse and those with a history of opioid abuse.

Less abusable, less desirable, cause they put the antagonist in it. See? Easy. $$$

http://clinicaltrialsfeeds.org/clinical-trials/show/NCT00734461

Number 2:

EMBEDA

Morphine + an antagonist (which one is not known yet)

This is a juicy story.

Alpharma has asked the Food and Drug Administration to approve Embeda as a tamperproof medication for patients with moderate to severe chronic pain. The pills are formulated so that the euphoric effects of morphine are blocked when a patient crushes, dissolves or chews them. Patients often abuse pain pills by grinding them up to snort or inject.

Same old story, add antagonist, dope not so good to dope fiends, no addiction, better pain management results in old people, etc etc etc

BUT- in the same breathe that they ask for funding:

If Embeda is approved it would help offset lost sales of Alpharma's morphine drug Kadian, which is expected to lose patent protection in 2010. The drug was Alpharma's best-selling product last year with sales of $167.7 million.

Rival drugmaker King Pharmaceuticals Inc. (nyse: KG - news - people ) is trying to buy Alpharma for $37 per share, or about $1.6 billion. Sanderson said that if Friday's panel meeting goes poorly, King could drop that offer, which would sink shares of Alpharma. However, he said that outcome is unlikely unless the FDA panel "absolutely rejects" Alpharma's application, which is not expected.

Shares of Alpharma rose $1.81, or 6.3 percent, Wednesday to close at $30.66.

I don't think I need to add the Pharmaceutical/Industrial Complex commentary on that one. Same story as Suboxone, Talwin NX and soon OxyTrek: Make a mint with a new medication to brand and have exclusive patent rights to, get great publicity and approval from the gov't / medical authorities for making a less addictive, less abusable, abuse-resistant, etc product. Stock manipulation by slightly altering the best selling product, create a competitor for your own product, make more money on your products by making more money on your products- a brilliant plan.

So, thats it people. First a trickle, here comes the flood.

Combination Agonist + Antagonist opioid medications are the future, thanks to Big Pharma and the crooked insider-trading-esque laws we have regarding pharmaceutical branding, patents and distribution rights.

Don't worry though, as with every other "less addictive", "tamper-proof" pill they make, we will all still be able to abuse, shoot, snort, parachute, plug, smoke, and combine these new and yet to be developed pills and formulations.

After all, they're counting on it, all the way to the fucking bank.
 
There is a positive side: eventhough shooting opiate+naloxone/naltrexone pills precipitates withdrawal for addicts, it doesn't for people who aren't addicted to Opiates.
And since the amount of Naloxone in these pills is very low, it actually helps preventing tolerance and addiction (eventhough it reduces euphoria a little bit). Actually people have been using ultr alow doses (ULD) of Naloxone or Naltrexone with their Opiates to prevent tolerance.
 
Since I use my meds. for chronic pain and do not IV pills, this only matters to me because it will increase the cost of pain treatment. If something happens to my medical insurance (a real risk for most of us), I hope to convince my doctors to let me use the cheapest forms of Generic Oxy and/or Morphine available.

I do not think most legitimate pain patients will be bothered by this, except as it raises the cost of medical treatment.

Unlike many chronic pain patients who get very angry at people who abuse pain meds (and make them more difficult for legit patients to get treatment), I do NOT expect that anyone will adjust their behavior and drug abuse because their behavior causes problems for me. The other side of that coin is I don't care how hard the government makes it to inject pills (except for monetary concerns).

That was an informative post.

Merry Christmas everyone!

Will
 
I remember first hearing about that new oxycodone drug combination pill coming out and it scared the fuck out of me. I was thinking that I would have to end up driving hours to score some dope instead of getting some OC. But I'm on bupe now after two overdoses. In the future, opiates may be a real treat. This may just cause a bunch of OC junkies to turn to heroin a lot quicker than now. I know I'd be on heroin if it was around me.

On the other hand, addicts are always going to find a way to abuse narcotics. There may be less doctor shopping and abusing pain management meds and more use of street drugs. Who knows...
 
Since I use my meds. for chronic pain and do not IV pills, this only matters to me because it will increase the cost of pain treatment. If something happens to my medical insurance (a real risk for most of us), I hope to convince my doctors to let me use the cheapest forms of Generic Oxy and/or Morphine available.

I do not think most legitimate pain patients will be bothered by this, except as it raises the cost of medical treatment.

Unlike many chronic pain patients who get very angry at people who abuse pain meds (and make them more difficult for legit patients to get treatment), I do NOT expect that anyone will adjust their behavior and drug abuse because their behavior causes problems for me. The other side of that coin is I don't care how hard the government makes it to inject pills (except for monetary concerns).

I'm in the same boat as you and I think this just speaks to Tchort's point... in these situations the government is duped, the patients are screwed and basically everyone all round is fucked over somehow except big pharma who is making record profits.

Big Pharma needs to be reigned in quite a bit but I don't see the Obama admin doing much. They are the single most profitable industry in this country (in terms of their return per dollar spent) and they will only get bigger... we need to start doing something about this.
 
Tchort- I just want to say I find your posts very informative and I appreciate reading them. Of course it helps that our perspectives on such matters are so closely aligned =D
 
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You made me think cane, the U.S. should ban advertisements on T.V. for new medications that will cure anything and everything. They did this with cigarettes, why can't they do it with drugs?
 
Well atleast they play into our wants by making shit so easy to abuse and thus sell so well.
 
wiggi said:
You made me think cane, the U.S. should ban advertisements on T.V. for new medications that will cure anything and everything. They did this with cigarettes, why can't they do it with drugs?

I definitely feel that way. There is no reason for direct-to-consumer advertising... to all non-US BLers, are there TV ads for drugs in your country? From what I have read, few places in the world allow this.

A great documentary on the subject is Big Bucks, Big Pharma.

If you are sick, go to a doctor and tell them what ails you and then they will treat you. There is no legitimate medical reason for us to see ads and those ads are just ephemeral bullshit. Pharma companies claim they use ads to educate the public... like lyrica commercials are educating us about conditions like fibromyalgia, but they are just telling unhappy people that this pill will turn their life around. DTC Advertising boosts costs and profits, not our health.
 
My favorite ads are the ones about RLS. Thousands of people went to the doctor because they thought they had that condition solely because they shake their legs a lot.

Another classic,"I have herpes and my partner doesn't."
 
i was just prescribed Pentazocine and Naloxone, and i dont know what to do with it. im afraid of it making me sick. whats this about ritalin? im prescribed that too.
 
tchort, Don't forget where Obama got all his campaign money,Big Pharma. |Nothing is gonna change in thisnew administration. The FDA is a joke or should I say thefraud and deceit association. With this recession on , how many empty offices can you count inWashington. You can manipulate study numbers all day long, it won't matter, nothing is going to change. I have a couisin that works at the fda,he was told don't make waves and you keep your job. He graduated at the top of his class at a leading medical school. What a joke? Big Pharma wins again. Wonder how long before the american people start calling Obama... Ohbummer. Tchort asyou probably know thepatent is up on suboxone next year and it will become a generic drug. Watch out their at the gate and leading by 4 lengths is bigpharma, trailing behind by more then 5 lengths is this races favorite folks, the american people Merry Xmas Everybody Detoxguy
 
In short, these are the likely changes due to this new trend if it continues (which it will):

-Chronic pain patients will continue to be exploited financially. Notice how the most popular chronic pain medications change when a new brand patent expires, then how a new one just magically appears on the market to fill the void before the new generic form is on the market for long. OxyContin has had a generic for less than a couple years, Kadian is about to lose its brand-only status, here comes OxyTrek and Embeda- both made by smaller mom&pop pharma companies, but which are in the process of being bought by the big boys.

-The correlation between low dose / ultra-low dose antagonists + / - partial or full agonists has not been adequately established, for abuse, as an adjuvant for analgesia, or for slowing tolerance. There is only a very short history of this being studied; the cart is coming before the horse. Long term ramifications of these combo's are not understood.

-As others have stated, if there is a major shift in potent opioid formulations that actually does make it impossible to become addicted via IV (which I highly doubt), those addicts who are addicted to high dose IV Oxycodone, Hydromorphone, Morphine, etc will have no choice but to switch to street Heroin. But, these drugs will remain as recreational drugs for non-addicts ("joy bangers"), which are a larger consumer of prescription opioids than IV addicts.

-There is some evidence that injecting ultra low doses of antagonists with a partial or full agonist increases the pleasurability/intensity of the rush; which, depending on the pills formulation, may make it more desirable to abuse than a regular opioid-only pill (ex. Diconal. Addict lore has Diconal as a holy grail among IV rushes; but only because of the Cyclizine. Dipapanone by itself is basically identical to Methadone in its effects- the addition of a second non-opioid active ingredient made it more desirable to abuse).

-The evidence with Suboxone and Vivitrol is that regular, daily use of opioid antagonists can bring about nasty side effects, from headaches to severe nausea. The seriousness of these side effects was all but left out of the Suboxone prescribing guide, aside from the note that if the patient doesn't tolerate Suboxone to switch them to Subutex. I bet the already vulnerable chronic pain population will really appreciate these added health problems.


I do look to the Obama administration to make drastic steps forward in terms of progressive policies at home and abroad for the US. Completely overhauling the drug regulatory aspect of the Federal government (FDA, DEA, SAHMSA, DHHS, etc) is not going to be one of them; but that's ok with me. We shouldn't expect overnight shifts in how our country works, but he will definitly do a lot of good things, just not every good thing that we need (which may never be possible).

Purdue Pharmaceuticals is the best example of how crooked the industry is. They promised a less addictive, less abusable, superior pain killer in OxyContin. They said it was formulated against abuse/addiction. They said they were going to fix the OC diversion epidemic by actually making it tamper-proof, then didn't. Then, when the patent expired and generics started to be manufactured, generics were being manufactured by a company owned by Purdue itself- then, Purdue sued the company it itself owns to stop it from making generics of OxyContin; then came out with a new range of doses for OxyContin that were only available in the brand form. Gravy train never slows down for big pharma.

Anyway, if anyone finds news of more announcements/trials involving this new shylock business of slightly tweaking a patented brand opioid by adding minuite doses of an antagonist and re-branding, re-patenting it, please update everyone. I bet when these start hitting the shelves theres a new wave of fear and myth mongering (similar to the myths still being spread about Suboxone), followed by an explosion of abuse and Federal inquiries on why the unabusable medications are being abused.
 
Exactly.

If you take away people's OC's they'll turn to heroin.

The trend looks like replacing all of the strong narcotic patent medications with new brands of agonist or partial agonist + antagonist. Right now there is Pentazocine + Naloxone, Buprenorphine + Naloxone (which will most likely be approved for moderate to severe pain at some point), on the way is Oxycodone + Naltrexone, Morphine + an antagonist. Talwin, Buprenex, OxyContin and Kadian already have been replaced or are in the process of being replaced.

Next would be Hydromorphone, Oxymorphone, Fentanyl, Methadone + Naloxone or Naltrexone or another antagonist; Dilaudid, Opana, Fentora, Methadose; replaced by narcotic + antagonist brands.

That would mean a huge shift in drug using habits of the IV pill addicts. While OC is a major component, if you include the rest of the strong opioids that people are addicted to via IV, it would be a big change.
 
i was just prescribed Pentazocine and Naloxone, and i dont know what to do with it. im afraid of it making me sick.

It's gonna make you sick from precipitated withdrawal if you're addicted to full agonist Opiates, such as Oxycodone, Hydrocodone, Heroin, Morphine, Methadone, etc...
If you're not, then you should be worried about the side effects of Pentazocine: hallucinations, dysphoria...


As others have stated, if there is a major shift in potent opioid formulations that actually does make it impossible to become addicted via IV (which I highly doubt), those addicts who are addicted to high dose IV Oxycodone, Hydromorphone, Morphine, etc will have no choice but to switch to street Heroin.

We are lucky for now, it seems that laboratories still think that adding Antagonists such as Naloxone to Opiate pills prevents IV abuse... Of course, it doesn't.
Things will really get shitty when they will come with formulations that REALLY cannot be abused intravenously (making huge pills with binders that turn into gel into all solvents and burn the veins when injected? hopefully we'll be dead before they come with sadistic ideas like that...)

I think that for people addicted to IV Oxycodone, Hydromorphone and other full agonists, once they'll be prescribed these new pills, it's gonna be worth for them to wait ~24 hours until they're in full withdrawal then start shooting their new Oxy+Naloxone or whatever Opiate+Naloxone pills....

I think that's the choice most people will make rather than switching to Heroin...

___

Really I don't see these new formulations with an antagonist added as being a threat for Opiate lovers.
People will still get amazing highs from injection of these pills and get addicted to them.
It's just a change we're gonna have to get used to.

But once people will get used to them, they will be just as widely abused as Suboxone or Subutex, which are both getting more and more commonly abused intravenously and more and more people get addicted to them....
 
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A different perspective

Thank you for the information. I have a totally different take on things, though-- I happen to like capitalism; I think that the drive to make money is behind most of the things that have advanced science and technology. Had Microsoft not been able to make money (without getting into the past ten years of the monopolization debate), we wouldn't have the PC-- at least not with the advances we have now. Maybe we would have them eventually-- say in 2020 we would finally get a message board like this one... but believe it or not, the internet was NOT invented by Al Gore, and 'nonprofits' alone would never have come this far!

Anyway... as a recovering addict who got clean 'the old fashioned way' but who now treats addicts with either Suboxone or residential rehab (not both-- they don't mix), I know without a doubt that Suboxone has saved lives in my own practice alone-- and I know that there are tens of thousands of people alive right now who would be dead had Suboxone not been available to them. No doubt.

Yes, people abuse it-- as you know, people abuse everything. But that doesn't make a med 'evil'-- it makes the person 'stupid'. In the prison where I used to work as a psychiatrist the inmates abused clonidine, wellbutrin, benadryl-- the meds aren't the problem.

I just posted on my blog, Suboxone Talk Zone, how excited I am to see the profit motive finally apply for the treatment of addiction. We (addicts) have sat by as pharma comes up with new treatments for so many diseases... but addiction has been viewed as not worthy of investment. When Suboxone came on the scene, my hope was that it would get the attention of other pharma companies here in the US, where the big bucks are spent on product development. and I see that as a good thing!!!

As far as 'big bucks' for R-B, they messed up ROYALLY-- they had the opportunity to make profits at least ten-fold higher. Suboxone has been around for 7 or 8 years now, and people still don't know what it is!!

You probably know this, but bupe has been around for 30 years-- and the addiction of naloxone does nothing to the formulation except satisfy the politicians who approved the change in drug law that allowed it.

Tchort, I would like to discuss this further with you-- I tend to drop in this site and maybe more people here are up on this stuff, but most people don't know the history of opiate law in the US. I am trying to figure out your exact objection and perspective on opiates, addiction, pain treatment, pharma-- what is it that you see to be a problem? The fact that someone is making money? Or do you have the impression that these new meds are somehow harmful? I am not trying to be confrontational-- I really want to know.

I was an anesthesiologist for years until my opiate addiction (IV fentanyl is quite seductive), and now I am a psychiatrist, and I treat chronic pain and addiction along with other psych conditions. I also have a PhD in Neurochemistry-- yes, drugs have sort of been my whole life! When I give a pain patient narcotics for a long time, I know for certain what will happen-- they will change the patient's personality and make the person 'one dimensional', with the narcotic at the center of life. If I use a partial agonist like bupe, that DOES NOT HAPPEN. That is a fact-- anyone who doesn't believe it is simply wrong. I have seen it over and over, literally hundreds of times-- and I have started many, many people on bupe who would testify to the difference in how they feel. I watch my patients closely; a few have played with the Suboxone, but the people who are a bit older and truly sick of being addicts are so grateful for buprenorphine, as it has given them their lives back. So there is no doubt in my mind that at least with Suboxone, the drug can be a tremendous discovery for some.

As for the others you mention, I don't know if they will be anything positive or not; I wonder about the value of an orally-active antagonist given with an agonist. I do note, though, that people who take Suboxone and then return to pain pills (for pain that is too severe for buprenorphine to handle) tell me that the oxycodone never quite feels the same as it used to. I wonder if that is a result of the temporary use of a med with antagonist properties.

Anyway, Tchort, would you have any interest in writing something for my blog about this topic? I would have the post as a 'guest post' about your take on new developments in opiate medications, as a counterpoint to my post. Please consider it-- you are welcome to identify yourself as you wish, including linking to wherever you want. I get 200 hits per day-- nothing major, but many of the hits are from regular readers who are fairly sophisticated in their knowledge about addiction. If you are willing, e-mail me at [email protected] . The blog, if you are interested, is called Suboxone Talk Zone, and I am 'SuboxDoc'.

Jeffrey T Junig MD PhD AKA SuboxDoc
Suboxone Talk Zone
 
In Canada eh, your talwin comes without naloxone, your hycodan without atropine/APAP, and its mostly IR tablets.

feels good man, almost as good as bagged milk. Funny thing tho, its the same produts made by the same company for a different market..its just our goverment (and by extension people, as govt repersents the people) are not all "ZOMG drugs are bad mmmm'k"
 
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