Posts Tagged ‘oxycontin’

Targin

By Trevor Shewfelt, Pharmacist at the Dauphin Clinic Pharmacy

 

We now have this and most other articles published in the Parkland Shopper on our Website.  Please visit us at www.dcp.ca

The information in this article is intended as a helpful guide only.  It is not intended to be used as a substitute for professional advice.  If you have any questions about your medications and what is right for you see your doctor, pharmacist or other health care professional.

Ever heard the expression driving with the brakes on?  That’s what I thought of when I first read about a new pain killer called targin.  It is made by Purdue, the same company that makes oxycontin.  Just like oxycontin, targin has the pain killer oxycodone in it.  And like oxycontin, targin is a slow release product so a patient only needs to take the medication every twelve hours.  The unusual thing about targin is it has a second ingredient in it.  That ingredient is naloxone.  Naloxone is an opioid blocker and is usually used as an antidote to stop an opioid like oxycodone from working.  I thought adding naloxone to targin was like hitting the brakes on your car when you wanted to accelerate.

How do opioids like oxycodone work?  Well, all opioids were originally derived from the opium poppy.  People have been using opium as a pain killer and for other medicinal and recreational purposes for 1000’s of years.  Morphine was the first commercially available opioid pain killer.  It was derived from the opium poppy about 200 years ago.  It is still a very good pain killer, but over the years chemists have tinkered with it.  Within the last century, chemists have come up with several semi-synthetic opioids.  One of them was oxycodone.  Oxycodone is 2-4 times stronger than morphine so it is a better pain killer.  Like all opioids, oxycodone works by attaching to opioid receptors.  When it attaches to these receptors it kills the pain and also causes its side effects.  Side effects from oxycodone can include: constipation, drowsiness, respiratory depression, nausea and vomiting.

Naloxone is kind of the opposite of oxycodone.  Naloxone also attaches to the opioid receptors in the body.  But it doesn’t cause any pain killing.  In fact, we don’t think it does much of anything.  But it does do a good job of keeping other opioids like oxycodone off of the receptors.  That is why naloxone is one of the medications we can use as an antidote for an opioid overdose.  If someone shows up at the emergency room with the symptoms of an opioid overdose, one of the medications the doctor may inject into them is naloxone.  That can quickly reverse the effects of the opioid and get them conscious and breathing again.  So if naloxone is an antidote to an oxycodone overdose, why would you put it in the same pill as oxycodone?

Naloxone works differently if it is taken orally than if it is injected.  Naloxone goes into intestine, gets absorbed and goes to the liver.  The liver breaks down 97% of the naloxone before it gets to the rest of the body.  We call this first pass metabolism.  This means that the naloxone never leaves the gut.  So, the naloxone blocks the effects of the oxycodone only in the gut but not in the rest of the body.  This is actually a very useful effect.

Constipation is a problem whenever we put a patient on an opioid pain killer like oxycodone.  Other opioid side effects like being drowsy or being nauseous will get better after a person is on the opioid for a few days.  But the problem with constipation never goes away.   In fact we often start people on long term opioids on laxatives for the entire length of time they are on the opioid pain killer.  So the theory is that if we give the oxycodone and the naloxone together we could get the pain killing of the oxycodone but have the naloxone only block the constipation.

There have been a couple of small studies looking at this.  A small study with 265 patients in it by Lowenstein et al in Expert Opinion in Pharmacotherapy in 2009 looked at patients with moderate to severe chronic non-cancer pain for 12 weeks.  One half the group had long acting oxycodone (like oxycontin).  The other half had long acting oxycodone and long acting naloxone together (like targin).  The pain control was similar in both groups, but the group that had the oxycodone and naloxone together had less constipation.  Although the trial was small, this is a promising outcome.

Another interesting effect of putting the oxycodone and naloxone together is that makes the drug harder to abuse.  Oxycontin has a reputation as a medication that is often abused.  Abusers take the medication in ways that were never intended.  Targin is intended to be swallowed whole, and not crushed.  If targin is taken in ways it was not intended, the naloxone won’t just stay in the intestine.  The naloxone will go into the rest of the body and the abuser has a good chance of experiencing violent and unpleasant withdrawal symptoms.  So targin may be harder to abuse than oxycontin.

The mixture of oxycodone and naloxone in targin is a interesting idea.  Although the studies are small, targin may be a decent opioid pain killer that causes less constipation than others in its class.  Targin may be harder to abuse than other opioid pain killers.  And my initial skepticism about combining an opioid pain killer and an opioid blocker in the same pill seems to be misplaced.  Driving with the brakes on may not be such a bad idea after all. 

As always if you have any questions or concerns about these or other products, ask your pharmacist.

Oxycontin EDS

By Trevor Shewfelt, Pharmacist at the Dauphin Clinic Pharmacy

Have you heard Trevor on the radio?  Listen to 730 CKDM Tuesday Mornings at 8:35 am!  We now have most of the articles published in the Parkland Shopper on our Website www.dcp.ca

 The information in this article is intended as a helpful guide only.  It is not intended to be used as a substitute for professional advice.  If you have any questions about your medications and what is right for you see your doctor, pharmacist or other health care professional.

 Oxycontin is a long acting, powerful narcotic pain killer.  It is often used to treat severe pain like that experienced by cancer patients or severe arthritis where other pain medications won’t work.  Unfortunately, oxycontin has a bad reputation.  It has been called “Hillbilly Heroin” as it has become a popular drug of abuse.  Because it has been abused, the Manitoba government is in the process of making it more difficult for patients to get oxycontin paid for by the Pharmacare program. 

 Why does oxycontin work so well as a pain killer and why has it become popular for abuse?  Well it starts with opium and the opium poppy.  There is evidence that people were growing opium poppies in Mesopotamis at least 5000 years ago.  Opium poppies were traded into Egypt, Greece and Europe.  Hippocrates, the father of medicine, would have been aware of opium in ancient Greece.  Alexander the Great is credited with bringing opium to the far east.  From the 1600’s on opium became the main commodity the British traded with China.  They even fight a few wars over it.  In the early 1800’s, Friedrich Serturner in Germany discovered how to extract morphine from opium. 

 Opium seems to have always had its problems with addiction.  The extraction of morphine was thought to be a great break-thru as it made the opium like pain killing effects more reliable, longer lasting and safer.  Morphine was even called “God’s own medicine”.  Morphine is usually referred to as the original narcotic.  All the modern narcotic pain killers, including the oxycodone in oxycontin, are derived from morphine.  As good as morphine was and a safe as it was compared to opium, problems with addiction seem to have started early as well.  Morphine was used during the American Civil War.  In that war, there were reports of hundreds of thousands of cases of “soldier’s disease”.  Soldier’s disease of the American Civil War is now interpreted as symptoms of morphine addiction.

 All the modern derivative of morphine tried to create a safer, more effective pain killer.  One of the most unfortunate examples was heroin.  It was developed in the late 1800’s and early 1900’s by Heinrich Dreser in Germany for the Bayer company.  Apparently heroin was originally marketed as a safe pain killer for children.  Then it was marketed as a way to step down off of morphine in adult patients.  Unfortunately, although heroin is a stronger pain killer than morphine, it is also much more addictive.

 Oxycodone, the active ingredient in oxycontin, was also developed in Germany in the early 1900’s.  It is a stronger pain killer than morphine and has the potential to cause slightly fewer side effects.  It has been in different pain killers over the years, including in Percocet.  Oxycontin was marketed by Purdue in the 1990’s.  Its advantage is that is it very long acting.  Most people can use just 2 pills a day 12 hours apart.  Unfortunately, like other narcotics going back to opium, there have also been problems with addiction and abuse.  Rightly or wrongly, oxycontin abuse seems to have received a large amount of media attention in the last few years.  So the Manitoba government has decided to act.  Although I understand the government’s desire to reduce prescription medication abuse, I worry about patients who need the pain relief.  Some of them may get caught in the new paperwork and not be able to afford their medication.

 The new rules work through the Part 3 EDS system.  EDS stands for Exceptional Drug Status and is an appeal process your doctor can do on your behalf.  If you have never been on oxycontin before, and your doctor decides you need it, he or she can fill out forms to say why your pain is very severe, and why other drugs won’t work for you.  If Manitoba Health doesn’t like the paperwork, they won’t pay for it, even if you go over your pharmacare deductible. 

 If you are on oxycontin right now, you have a little time.  The government has put in a grandfather clause until May 26, 2010.  That means you have between now and May 26 to contact your doctor and ask them to fill in the Part 3 EDS paperwork.  After May 26, all patients on oxycontin, new and existing, will require a Part 3 EDS to get coverage from Manitoba Health.  If you get the letter from Manitoba Health saying you have a Part 3 EDS, remember your medication is still not necessarily free.  You still have to spend your pharmacare deductible before Manitoba Health will pay.

 Do I think these new oxycontin rules will fix the problems with abuse and addiction?  Not to be a pessimist, but probably not.  There are other medications to abuse if you have an addiction.  And although Manitoba Health is well intentioned, we have been dancing with the fantastic benefits and dangerous pitfalls of the opium like drugs for over 5000 years and I don’t think this will be the last song.

 As always if you have any questions or concerns about these products, ask your pharmacist.

Oxycontin – Audio

 By Trevor Shewfelt.  Recorded by the nice people at 730 CKDM, The Parkland’s Best Music

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