Tamper-proof prescription drugs may halt abuse

[nabraxas]

29 June 2008

NewScientist.com news service

Jim Giles

IT'S a class of drug abused by 1.5 million Americans. To quit, addicts have to go cold turkey: vomiting, diarrhoea, insomnia. Thousands die every year from overdoses. Add up the days lost from work and the money spent caring for addicts, and the toll reaches $10 billion annually.

You'd be forgiven for thinking that the drugs in question are crack cocaine or heroin. Instead, the culprits are prescription painkillers such as oxycodone and hydrocodone. By binding to and disrupting the activity of brain cells that control the experience of pain, they ease the suffering caused by a range of conditions from back problems to terminal cancer. When milder painkillers fail, opioids bring vital relief.

Around a decade ago, when medical organisations began encouraging doctors to do more to help patients in pain, opioids, which can be formulated to offer long-lasting relief, seemed to be the answer. But although pain management has improved, the huge rise in prescriptions is fuelling an epidemic of opioid abuse (see Graph), which is costing lives. In 2005, prescription opioids played a role in 8500 fatal overdoses, more than the figures for cocaine and heroin combined.

"Judged by any measure - person years of life lost, healthcare costs, self reports of drug abuse - the prescription drug problem is a crisis that is steadily worsening," said Leonard Paulozzi, an epidemiologist at the Centers for Disease Control and Prevention in Atlanta, Georgia, at a recent Senate hearing on unintentional drug overdoses. Studies have also shown that people are turning to the internet in droves to find ways to tamper with prescription drugs (New Scientist, 3 June 2006, p 6).

Now drug companies are fighting back with a solution of their own - tamper-resistant opioids. Even if some people find ways around these new pills, experts say that anything that makes abuse harder will help cut the numbers of addicts.

None of the new pills has yet been approved for sale. But earlier this month, Pain Therapeutics of San Mateo, California, and King Pharmaceuticals of Bristol, Tennessee, asked the US Food and Drug Administration (FDA) to approve Remoxy, a new form of OxyContin, one of the most widely prescribed opioid-based painkillers.

A bitter pill to swallow

Part of OxyContin's value as a painkiller is its ability to release the opioid oxycodone over a 12-hour period. But if someone crushes the pill and then snorts or injects the powder they can get the entire dose at once - along with an intense high.

To remove this possibility Remoxy's makers mixed oxycodone with gelatin to form a rubbery pill that simply bends when hit with a hammer.

“They mixed the opioid oxycodone with gelatin to form a rubbery pill that simply bends when hit with a hammer”

In some cases, instead of crushing pills, addicts may try to dissolve them and drink or inject the solution. But James Green of King Pharmaceuticals says the company's tests show that if people put the pill in water and then drink it, they don't get all the oxycodone at once. He declined to explain why, saying the results were commercial secrets.

Meanwhile, Grünenthal of Aachen, Germany, is taking a similar approach by developing opioid pills that are super-tough. In tests at the New York State Psychiatric Institute, 40 OxyContin addicts were given a placebo version of Grünenthal's pill and asked what they would like to use to crush it. "They asked for razors, knives, hammers, paperweights, pliers," says Sandra Comer, who helped run the tests. Each received their instrument of choice. Some were able to break the pill into a few smaller pieces, but none could crush it. "Someone asked for a blender," adds Comer. "The pill just spun around."

Those safeguards should deter at least some abusers - one of the tragedies of the current problem is the number of young people abusing opioids. Arthur Lipman, a pain expert at the University of Utah in Salt Lake City, says that teenagers often steal opioids from their parents for use at parties. Surveys of American teens show that around 10 per cent have abused an opioid in the past year. But if teenagers cannot easily get a high, they are likely to find the drugs less attractive. "That could be life-saving," says Lipman.

More-experienced addicts pose a greater challenge. Comer's work suggests that a hard pill prevents casual abuse, but it won't be so easy to defeat determined addicts. They may find a way of dissolving Grünenthal's pill, while methods for tampering with the rubbery Remoxy pills are already being discussed on internet chatrooms devoted to opioid abuse.

So Alpharma of Bridgewater, New Jersey, has created Embeda, a morphine pill that might prove harder to abuse. Like OxyContin, its active ingredient morphine tends to come as a slow-release pill that is commonly crushed by addicts. But Embeda has a core made of a substance called naltrexone, which binds to opioid receptors in the brain, preventing the morphine from reaching the same receptors. The core is coated to prevent the naltrexone from being absorbed into the body if the pill is simply swallowed. If crushed, the naltrexone is released and mixes with the morphine, so if the powder is then snorted, the morphine won't have any effect. Alpharma plans to apply for FDA approval next month.

No one is under any illusion that the tamper-resistant pills will deter everyone. "I don't know if addicts have better imagination than our people," says Jack Howard of Alpharma. "But they are pretty smart."

Some even think the drugs could make things worse. Labelling them as abuse-resistant could make doctors less likely to monitor patients for signs of abuse or even make patients think the drugs are safer. Partly because of these fears, members of an FDA advisory panel in May voted against approving another tamper-resistant opioid developed by Purdue Pharma of Stamford, Connecticut, which makes OxyContin. "You want to ensure that the problem you're trying to solve doesn't become worse," says Frank Vocci of the National Institute on Drug Abuse in Bethesda, Maryland, who voted against approval.

However, Purdue could gain approval if the labelling on the new opioid was cautious enough to prevent doctors assuming the product was safe, he says. Experts say the other tamper-resistant opioids have a good chance of getting approval if they are labelled appropriately.

[Legba]

Opioids are physically addictive. If it is known that a large number of people are abusing these pills and steps are taken to prevent it, the addicts are likely to source their fix from the streets where the taliban sell their version of this drug.

Isnt it illegal to assist the terrorists?

Are the people who have been prescribed these drugs and are now hooked not worthy of any consideration if they resort to criminal means in order to feed their addiction?

[t st tantra]

a report on the radio claimed prescription opiates were the most common injected drug.

more used than meth or heroin.

buyers knew what they were buying!

t s t .

[Auxin]

Its a sick joke of course. These companies support the addictions of millions of people, the majority of which take the pills as directed every day, every week, every month, for years on end. The companies are only willing to 'fight' 'abuse' of the drugs if the consumers in question are unwashed and on the street and thus giving the drug industries a bad image. Its offensive that some of the biggest addictive drug pushers in human history try to stop the dirty and poor from using their product cause its bad for marketing.

[2b]

I imagine that this challenge will be over come, the same efforts are in place for cold pills but there seems to be an army of amateurs finding ways around it.

[Smiling Cloud]

Doesn't vinegar break down gelatin? I remember someone telling me that, not in this context at all, but i'm pretty sure it does. I really don't think people should be banging up pills, it is SO bad for your veins. And if you are going to have a habit, you going to want those veins for as long as possible. I still don't understand why they don't just give people what they want. A few weeks after they release these pills peole will have worked out what to do with them so why don't they stop playing games and hand out vials of whatever. I spose they make medicines for fucked veins as well though, so maybe thats it.

[mu!]

I really don't think people should be banging up pills, it is SO bad for your veins.

I'm a little fuzzy on this one.. can you explain how bad it is for your veins? references would be dandy too

[Conan Troutman]

DONT SHOOT PILLS PLEASE

shooting pills is wrong and dangerous, even with a 'wheel filter' chances are you are injecting things from the pill that are not supposed to be directly in your blood stream...there is a reason we have a GI tract ;)