The new non-abusable painkiller

[Lehendakari]

Drug designed to fail the test

Alpharma developing tamper-resistant pain pill to help deter abuse

Friday, November 09, 2007 BY JEFF MAY

Times Staff
The odds of developing innovative new medicines are getting higher for the pharmaceutical industry. So, it may come as a surprise Alpharma researchers are painstakingly designing a drug to fail -- at least in special circumstances.
The Bridgewater company sells a synthetic version of morphine, which -- like many painkillers in the opioid class -- is subject to abuse and addiction. But Alpharma has come up with technology to suppress the billowing high recreational drug users get when they crush painkiller capsules to thwart its time-release formulation.



In an abuse-resistant version of its Kadian morphine drug, now in late-stage trials, the company embeds a tiny naltrexone core in each of the 100 to 200 tiny pellets that make up the capsule. Naltrexone inhibits morphine-induced euphoria, so if the pellets are crushed or dissolved, it acts as the ultimate buzzkill. If the pill is taken normally, the naltrexonecore remains intact and inert.
"If you tamper with it, that's when it is released," said Joseph Stauffer, chief medical officer of the company. "People have tried to combine antagonists in the past, they just haven't got this far."
The scope of the problem is huge. Some 4.7 million people abuse prescription painkillers in the United States -- almost twice the rate of cocaine abuse, according to a 2005 federal study. Suggestions to curb addiction include tamper-proof prescription pads for doctors, drug screening for chronic pain patients on long-term prescriptions, and prescription monitoring by regulators, according to a Journal of the American Medical Association article earlier this year. But because drug abusers mostly filch prescription painkillers from friends and family members, one of the most effective means to cut improper use is to create a tamper-resistant capsule.
Drugs like morphine and Oxycontin -- a widely abused painkiller the radio host Rush Limbaugh was linked to when he confessed to a prescription drug addiction in 2003 -- are poorly absorbed by the body when taken in an oral form. Capsules tend to have relatively high doses because much of the active ingredients leave a patient's body without having an effect. But drug abusers who crush or dissolve painkillers and inject them -- a more efficient means of delivery -- can get an immediate, potent high.
To develop its abuse-resistant version of Kadian, also known as ALO-010, Alpharma enlisted some unlikely trial subjects: recreational drug users with finely tuned perceptions of morphine highs. The company needed to hire what are in effect connoisseurs of drug euphoria because some abuse trials have been skewed when subjects couldn't distinguish well between the effect of an opioid drug and that of a dummy pill, said Lynn Webster, who runs Lifetree Clinical Research in Salt Lake City and was one of the lead investigators for the tamper-resistant drug. "'We have to have subjects who can help us develop these products," Webster said.
He said none of the subjects were addicts. Most were experienced drug users who had agreed to participate after reading advertisements for the trials.
The company's latest Phase 2 trial of ALO-010 measured a different patient population: osteoarthritis patients who suffer chronic pain. The study found the naltroxene in the capsules did not interfere with pain relief when the drug was taken properly.
Phase 3 studies of the drug are now underway, and Alpharma wants to be in a position to market the drug by 2009, assuming regulatory approval. The company's research suggests half of the prescription pain market will be captured by abuse-resistant drugs by 2010. Some analysts have suggested the time is limited, because other companies are developing similar products.
"It's just the start," Stauffer said.
Alpharma has not said how much the abuse-resistant version of Kadian will cost, but Stauffer said production of the capsules is "extremely time-intensive" compared to ordinary morphine.

http://www.nj.com/business/times/ind...330.xml&coll=5

[whirlybird]

SWIM has come across either 10 or 20mg (cant remember) oxycontin. The person that had it said it could only be eaten, because if it was crushed it would be no good. SWIM thinks that the person claimed it would destroy the drug when exposed to the air. Whatever the case, abuse-proof drugs are not only being developed, they are already in use (at least in the USA). Oh yeah, btw they were generic oxys.

Reputation Comments on this post:

thank you for your comments

[juanathan]

always remember that the consumer can choose what and what not to ingest! pharmaceutical companies have ungodly amounts of power and sway and money invested in all sorts of things, but if consumers do their homework and know which companies/generics have the anti-tamper safeguards and which do not, it might be possible to subvert the whole system. i would imagine there would always be at least one alternative that someone can be prescribed WITHOUT the safeguards (i.e. allergic to naltrexone?), unless the FDA makes tamper-resistant opiates/amphetamines mandatory. that would be a bitch.

[Paracelsus]

unless the FDA makes tamper-resistant opiates/amphetamines mandatory. that would be a bitch.

That would never happen, because not all patients are ambulatory (many will still need IV opiates, etc). They may promote the use of tamper-resistant pharmaceuticals though.

Whatever the case, abuse-proof drugs are not only being developed, they are already in use (at least in the USA).

Do you have any sources for that besides dubious claims (many people actually snort crushed OxyContin)? Of course there are simple long-release formulas, but are you sure there are advanced techniques such as the naltrexone core? I have a hard time believing that, especially with generics.

if the pellets are crushed or dissolved, it acts as the ultimate buzzkill. If the pill is taken normally, the naltrexone core remains intact and inert.

That is interesting. I wonder if it will be listed as an inactive ingredient then.

Of course ways will be found to abuse these. If the naltrexone core truly stays perfectly intact while in the body, one could simply let the pills dissolve in water kept constantly somewhere close to body temperature until only the little core is left, along with insoluble inactives. Maybe an "EWWE" (extended warm water extraction) will one day become as popular as the CWE

Reputation Comments on this post:

aye

[whirlybird]

The oxys SWIM came across were not simple long-release formulas. The elephant that had them has scraped off the coating to long-release oxys and snorted them. The way SWIM understood it, these were not like that. Around here, oxys are more commonly snorted than eaten. The ones that like to eat them are few and far, which is why the oxys the elephant had were so cheap. SWIM is going to try to find the elephant and ask a few questions about those oxys. Will post again after more research. Besides the naltrexone core and time release pills with a coating, are there any other ways to time-release a pill? Paracelsus, when you say long-release formulas, are you speaking of the coating type long-release pills or do they actually modify the formula so the drug becomes active over whatever period of time? If so, then thats probably what the elephant had, but SWIM has never heard of anything like this. Then again, SWIM isn't too big on pharms.

[Zaprenz]

^One of the more elegant and simpler ways SWIM read of making an oral formulation unsuitable for injection is simply putting something like capsaicin (from chilli powder) in with the active drug. Digested via the oral route the amount of capsaicin has little effect, injected or snorted though and it is extremely painful.



The problem is the criminalisation of such drugs and the witch hunt of prescribers but SWIM at least sees the relative benefit (assuming they are successful - which is possibly a big assumption) of these tamper proof medicines - people in serious pain who have an urgent need for them might get hold of them easier (because prescribers may be more willing to prescribe them)