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Drug Maker Develops "Abuse-Resistant" Oxycontin

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In response to the epidemic of opiate addiction, Purdue Phrama LP the maker of Oxycontin, has developed a new version of the powerful painkiller that's "harder to abuse." According to an AP article, the government will soon be examining this new incarnation of the drug and evaluating the manufacturer's lofty claims. How could this drug be made "abuse-resistant?" Details, inside...

Oxycontin, essentially a synthetic opiate, was developed in 1996 and hailed as a breakthrough in painkillers. It was designed to be swallowed and digested over a period of 12 hours in order to keep a steady flow of medication available to pain sufferers. It wasn't long before abusers discovered they could achieve a heroin-like high if the pills were crushed and snorted or prepared into an injectable solution.

The DEA found that the deaths from this class of drugs quintupled by 2001. Amidst the growing number of lawsuits and pressure by the FDA, Purdue Pharma developed an abuse-resistant version of the drug. The company has developed a plastic-like coating that is fused to the tablet making it difficult to crush. The coating is also designed to transform the pill into a "gelatinous mess" if the user tries to prepare it for injection. Purdue Pharma says the new pill dissolves just as effectively as the current pill when used properly.

From what we know about drug addicts, they are very resourceful when it comes to getting their drug. Dr. Bob Rappaport of the FDA wrote, "There is no perfect formulation that can resist all forms of tampering." We are inclined to agree, Dr. Bob. While this new version may be a step in the right direction, we remain doubtful of its actual efficacy. However, there may be some very neat, white-linen wearing drug addicts who will be put off by a "gelatinous mess." Who knows?

Oxycontin that's harder to abuse? Fda debates new version [AP]
(Photo: freerangestock)

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It's a good idea in theory, but I'm reminded of the old saying "when you build a better mousetrap, someone else builds a better mouse."

Drug addicts are surprisingly crafty when it comes to getting their fix.

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"We get vests."


"They get armor-piercing rounds."

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There are ways of making drugs abuse resistant. One example is the opioid Diphenoxylate, which is used for diarrhea. To keep people from taking 30 pills, they added a small amount of atropine to each pill. If anyone were to attempt to get high off it they would be in for an experience they wouldn't soon forget.

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I have chronic back pain. I take this medicine to live. If this will deter fools from abusing this highly potent and addictive drug, I'm all for it.

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Instead of going to the expense of having to develop a "abuse resistant" drug, the medical boards need to go after these doctors that prescribe outrageous amounts of these powerful painkillers (everything from methadone to oxycontin)to everyone with a "backache" that comes to see them. Even in the small town I live in we have had 2 kids I know of die from OD'ing on these drugs and literally almost everyone I have come across seems to be addicted to pain pills to some extent. It is so sad.

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Purdue executives are on record about 7 or 8 years ago- I believe testifying in front of congress- about how Oxycontin could not be abused due to it's time release mechanism. This is just another way to show plausible deniability so they can keep producing their cash cow.

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@SkyeBlue - you know all about the system. You MUST be a dr. RIGHT?

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Oy, didn't science try to do this with Heroin and screwed up royally? It was supposed to be a less addictive form of Morphine....


"From 1898 through to 1910 heroin was marketed as a non-addictive morphine substitute and cough medicine for children."
[en.wikipedia.org]

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@SkyeBlue: Keep in mind that it's not uncommon for drug addicts (especially those who abuse prescription drugs) to shop around for multiple doctors in order to have a steady stream of their drug of choice. Sometimes they'll even fixate on the fact that it was prescribed by a doctor as justification that it's ok to take what they do (conveniently forgetting that they lied to the doctor to get the drugs in the first place).

Addicts can be an amazingly, and, at times, frighteningly resourceful bunch when it comes to getting their fix.

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Scrape off the coating, or cut it in half and dig out the inside. Partially dissolve the coating with whatever liquid can do the job quickly, dry it off, then have at it. Harder to crush? I have a hammer that loves to be challenged.

I wouldn't know if any of that works, but I'm guessing the addicts are willing to make an effort.

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@SkyeBlue:


It's ALWAYS the doctors fault right? It's not the guy who shows up at the ER at 2am complaining of debilitating back pain? It's not the woman who goes to 4 different doctors to get scripts for benzos. It's not the person who has a legitimate rx for these drugs but sells them to make a little money, nor is it the fault of the kids who steal them from their parents and grandparents. NO, it's the doctors fault!
In fact, there isn't much that isn't our fault. A morbidly obese, smoker, whose baby is born with severe mental retardation? DOCTORS FAULT!!!!!
Man who fails to take his cholesterol meds, eats like Sally Struthers at a buffet, smokes and drinks has an MI? DOCTORS FAULT.


I honestly don't know why I decided to practice medicine in a country where people blame you for everything and won't take a damn bit of responsibility for anything that happens to them.

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Rush Limbaugh is going to be pissed.

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@Cerb: Aww... chin up, l'il camper... I don't blame Docs.

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And I'm betting that "gelatinous mess" gets ya' high as hell.

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@SkyeBlue:

That just makes it difficult for people with chronic pain to get the actual drug because doctors are afraid that someone's going to come after them for prescribing too much pain pills. Just ask my friend who does have chronic back pain! She's always getting the run around from doctors who have to cover their butts so they don't have the Feds busting down their door in a drug raid. :/

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I hate it when my comments get eaten! This will probably double post...

The doctors have to cover their butts from the feds because they have to be careful they'll be accused of over prescribing.

I have a friend who is actually has chronic pain, but she's always getting the run around from her doctors over her pain pills (30 a month does NOT an addiction make).

The doctors lose, the patients lose. If they make it harder for the addicts, even better. Why the flack?

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@savvy9999: He'd be pissed if he could hear what we were saying.

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@chrisjames: The story says that the plastic coating makes it more prone to break into large fragments than into a powder. Good thing there's not a simple device that can crush things into powder. Oh wait.

If the coating is embedded throughout the tablet, then the gelatinous mass might keep people from injecting it, but most addicts probably wouldn't care about the possible embolism it could induce. Not sure what the effect would be if it was snorted.

On the whole, it's probably a good thing though.

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@alice_bunnie:

Exactly. I personally think the government is already harassing doctors, especially pain management specialists, too much re: these pain meds. The DEA can and does investigate any doctor that prescribes too much of this stuff, even though it may just be a coincidence. As a result, many doctors are now reluctant to write a prescription for effective pain relief to patients who actually need it. This problem is not the doctors' fault; it's the fault of addicts and the DEA (and the larger failure of the War on Drugs).

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You will never stop the abuse, coming from someone in recovery of opiates.

They made generic OC that was 'tamper resistant' and it didn't stop anyone.

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And the new deliver method allows them to extend their patent protection! Awesome its a win win, harder for addicts and their profits are bound to increase!

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@Pro-Pain: Me too, brother. I take the stuff as prescribed: it changes the pain from my three torn disks from "horrific" to "barely tolerable."
Meanwhile, the clerks at the pharmacy look at me like an amateur abortionist every month when I fill the prescription... and I have to worry about getting jacked on the way to the car.

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Ok, so maybe it won't work. Who's got a better solution? Should doctors and pharmaceutical companies just stop trying to fight abuse?
I haven't seen anyone here demand that oxycontin be taken off the market. There is a legitimate use for it. Wouldn't a technological solution to drug abuse be preferable to raids and shootouts?

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Good news! It's a suppository!

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@Kajj: Yes, it would certainly be preferable if it could be done. I just don't believe in any "solution" to an illegal drug problem that involves reducing access to the drug for non-abusers. Same goes for the pseudoephedrine being put behind the counter. I oppose that because I shouldn't have to suffer and have my privacy invaded just because some people make meth. It's not my problem that they are idiots.

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Its not like most of these methods are a breakthrough, methods for making pain killers abuse resistant in this manner have been around for decades. A quiet troll through some of the boards about injectible drugs suggest that people watch for 'certain' pills because some of them are imbued with wax and other wonderful deliberate impurities, to make using heat to dissolve them a dangerous prospect. They 'harden' again when they cool, making injecting them difficult and dangerous.


Trying to stop insulfation (snorting) is a little harder without impairing or alterring the drug's active properties, but I'm not sure an 'anti-crush' coating will stand up to someone trying really hard to powderize it. A better bet would be something like the addition of silicates, something that disolves easily inside the stomach where there's ample moisture and acid, but that would be next to impossible to get up your nose in any quantity.


Addicts are always going to find a way around things though, the level of desperation is certainly there, and the level of information is higher than ever. Chances are the really interested parties are already thinking up ways around these protections.

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@Cerb: yes atropine was added to keep people from abusing lomotil, however, one can still take it with a p-glyocoprotein inhibitor such as quinidine to still get the high. However, most drug addicts don't know this because it requires another prescription to get but it can be done.

...point being - you can find ways around it.

From what I have seen, it is no one specific person's fault. There are a handful of MDs who will give a patient about anything they want. However, there are also people who really do need their pain relievers but get their prescriptions stolen from other people. Usually from a kid or from the person picking up their prescriptions for them.

@alphafemale: Yes heroin originally was meant to help overcome morphine addiction. But it also turned out bad. BTW it is still used in England medicinally but not in the US.

As far as I am concerned, this is another method for the drug company to get another patent to make money off of a pain medicine. The trend now is to try and make medicine that is difficult to tamper with.

Let's take a look at Vyvanse from Shire pharmaceuticals. It is amphetamine connected to L-lysine which is an amino acid. It is marketed as being safer and more difficult to abuse. Shire tried to get it approved by the FDA is an UNCONTROLLED SUBSTANCE! AMPHETAMINES AS AN UNCONTROLLED SUBSTANCE!! However, anyone with basic organic chemistry knowledge can see very quickly that it takes just a strong acid or base to separate the lysine from the lisdexamfetamine and thus yield a potent narcotic.

Therefore, I honestly believe these drugs are made just to make money. You know the drug Ambien CR or Coreg CR? Want to know what the CR stands for? CONTINUED REVENUE!

All in all, drug seekers will ALWAYS find a way to extract the drug from its dosage form. Count on it. Designing drugs to combat it may sound good, but it is futile. (Think of piracy protection on DVDs, within first week it is always hacked but companies like blu-ray still use it as a selling point to beat out the other competition; in this case HD.)

-Phex
-3rd Year PharmD/MBA Candidate

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I'm with cerb, just put something in there that, in high enough doses, will make them think twice about abusing it again. That's what they do with Vicodin. It has tylenol in it which, supposedly, in a high enough dose, would make you pretty sick.

And don't blame the doctors for the addicts, there's plenty of more legitimate stuff to blame them for. My uncle went in for a routine endoscopy, only his doctor did some other procedure he hadn't agreed to. They perfed his bowels and he died from sepsis a month later. All the while they were treating him for pancreatitis, which means they just didn't feed him.

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this reminds me of the same thing they did for Ritalin back when I was in high school. Some kid I knew had a special pill that if you tried to crush it, it would turn to water. Big whoop.

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@kallawm: The tylenol in Vicodin doesn't make the person feel bad. It is there to help add to the pain relieving effect, but if a person takes over 4 grams (4000 milligrams) of tylenol via Vicodin a day, that can lead to liver failure.

-Phex
-3rd Year PharmD/MBA Candidate

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@kallawm: They already did that - it's called Percocet. Percocet is just oxycodone (same thing that is in Oxycontin) with "Tylenol" in it. I still don't think that's a very good solution, because I shouldn't have to take another (potentially toxic) drug just because of addicts. Not everyone can take acetaminophen safely. Also, my understanding is that addicts can separate out most of the acetaminophen relatively easily anyway, getting it down to a level where it's not too dangerous.

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@Phexerian: When I broke my arm last year, they prescribed me Vicodin (the break was in a place where they couldn't fully immobilize it, so it was pretty painful for a couple of weeks). I could barely even tell I had taken it as far as either side effects or pain relief. Since that didn't work, they upgraded me the next day to Percocet. That worked a little better for the pain, but still not that well, and certainly didn't produce any kind of "high". I didn't want to ask for a higher dose, since they had already questioned me suspiciously when I said the Vicodin didn't work at all and wanted something stronger.

This got me to thinking: are some people just naturally way less sensitive to opioid drugs? If so, how are doctors supposed to tell that apart from so-called "drug seeking behavior"?

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Sadly, I believe that people who want to get high will find a way to do so-- by whatever means necessary. You've heard about that thing where teenagers choke themselves to get a head rush, perhaps? Yeah. There will always be people out there who will do anything for a fix, and you just have to try and minimize it as best you can. And I truly believe most doctors try and do that.

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Legalization.

Want to get addicted? Then become a registered addict, drop your rights down to felon status voluntarily, and go get your heroin at the drug store for $0.50 a dose.

Commit ANY crime, you lose the privilege of buying your drugs legally for a year.

Add the death penalty for selling the stuff to children, stick a fork in it, and call it done.

If some adult moron wants to commit slow suicide, let him. My rights are more important to me than some idiot addict's life.

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For those who don't know what Atropine does: a nasty suprise indeed.

A common mnemonic used to describe the physiologic manifestations of atropine overdose is: "hot as a hare, blind as a bat, dry as a bone, red as a beet, and mad as a hatter".

Adverse reactions to atropine include ventricular fibrillation, supraventricular or ventricular tachycardia, dizziness, nausea, blurred vision, loss of balance, dilated pupils, photophobia, and possibly, notably in the elderly, extreme confusion, extreme dissociative hallucinations, and excitation. These latter effects are due to the fact that atropine is able to cross the blood-brain barrier. Because of the hallucinogenic properties, some have used the drug recreationally, though this is very dangerous and often unpleasant.

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@oldgraygeek: My fiance has (had) 3 torn discs and was on Oxycontin for a long time. She had a procedure that closed her discs a few years ago and had been relatively pain free until she fell last summer and re-tore one of them. She just had back surgery where they fused her at L5-S1 and she is getting back to her nearly pain free state. You should look into what kind of procedures they can do now days. Btw she is 28 so getting fused is huge, but she hasn't lost any mobility.

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@Phexerian:


Wouldn't adding Quinidine (a p450 inducer) just mean the opioid would be cleared faster? Pharm is not my strongsuit but I was under the impression that opioids were cleared via P450.


Cerb
M3

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Can you imagine what a world of good it would do if addicts used their skills and determination to get a fix to, I don't know, invent or explore or attempt to positively contribute to society?

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@johnva: I don't buy that stuff anymore because I have issues with being treated like a criminal just for being sick. I don't care what that does to their profits. They obviously don't want to make it easy to get their product when you have a legitimate need for it. Fine; their competition does, so they get my purchase.

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...Somewhere in NYC, a fat man cowering behind a radio microphone sobs bitter tears. While his maid staff sighs, puts their shoes on and anticipates a very long night of pill-fetching.

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@alice_bunnie:
That just makes it difficult for people with chronic pain to get the actual drug because doctors are afraid that someone's going to come after them for prescribing too much pain pills. Just ask my friend who does have chronic back pain! She's always getting the run around from doctors who have to cover their butts so they don't have the Feds busting down their door in a drug raid. :/


Not an hour ago a friend of mine just told me that her husband, who she has admitted to me is faking his back problem, just went in and had his meds "Upped" from just methadone to methadone and oxycontin. The doctor continues to give this man pain medicine even though he refuses ANY surgery or treatment to fix his "problem". This has been going on for 4 years. Their 16 year old son just died back in January from an overdose of Methadone and Xanax! He was regularly stealing pills from his parents before he died. It is very prevalent, especailly in the area where I live for people to "doctor shop", since we live not far from the AR/OK state line and no is the wiser. If so many people were not getting prescriptions for this pain medicine that they obviously don't need then the streets wouln't be saturated with it.


We DEFINITELY need a nationwide, computerized system available to track who is getting what and where. It is the bad people that DO make it hard on the people who legitimately need pain medicine.

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@johnva:


Neither Vicodin or Percocet worked for me either. I was in a motorcycle accident and got no relief from either of them (even at a slightly higher does then reccomended). I am no doctor but it wouldnt surprise me if some types of painkillers just dont work for some people.

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I remember some guys were developing a version of Oxycontin that included a pepper-additive, so that when you tried to crush and inhale the pill, you'd get a nose full of hot pepper.

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Whats to stop someone from taking a razor blade and just cutting or scrapping this cover off?

If people want to get high let them. Who really cares? If they want to hurt their own bodies who am I or you to tell them to stop?

Hell oxy abuse has less issues (aside from legal) then alcohol or smoking but those are both legal.

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So then they'll just move on to heroin, which is what most Oxy abusers eventually do anyway, because it's cheaper and, many times, easier to obtain.

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Someone should ask Rush Limpballs how he feels about it.

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@parad0x360:


Um, actually Oxy abusers exhibit similar addictive symptoms as heroin users (since Oxy is an opiate). I hardly think you can say Oxy abuse has less issues then alcohol or cigarette addiction. When was the last time your uncle robbed someone or stole and sold your playstation to buy a pack of Pall Malls?

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@Cerb:


yeah they are cleared via p450 usually 2d6 or 3a4. taking an inducer would speed up the clearance. to be honest i am not sure of his idea of a p-glycoprotein inhib to block the effects of atropine...though i got my pharm.d. a few years ago so i would have to research it.

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@ johnva
Correct me if I am wrong, I thought oxycodone was just the generic for Vicodin.


And for those that want Percocet but can't have Tylenol just ask for Percodan which is the same base mixed with Motrin instead.

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@chemicalx9


Is this atropine the same stuff the give soldiers to inject themselves with in case of NCB attack?