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Delayed release drugs

Over the last 10-15 years, there have been attempts to lengthen the effect of the short-acting opiates by incorporating these drugs into preparations that slowly release the medication.  This way, the drug is absorbed over a longer period, and the serum level of the medication remains on a more constant level.  This was felt to be especially useful for pain lasting all day long.  Both the highs and lows can be avoided and the patients would benefit from pain relief around the clock.

While many of these goals have been accomplished, there are still problems:  First, pain levels fluctuate throughout the day so there is still a need for a short acting agent for breakthrough pain.  Second, the medications do not seem to have the duration of clinical effect that has been advertised.  This results in the doctors increasing the frequency of administration of the medications.  However, the drugs were never studied at the more frequent administration schedules, so their effects are less predictable.  Thirdly, these medications are still metabolized quickly after absorption.  If you miss a dose of medication you will go into a quick, profound withdrawal syndrome.

Another problem is that the mechanisms that were responsible for the slow release of medication could be bypassed.  Pills can be chewed, snorted, injected and patches could be licked.  This caused an intense high similar to heroin and the drugs quickly became sought after by addicts.  The problem has become especially acute with Oxycontin, although it is a risk with every preparation.

Last, there is a lack of clear guidelines on how to use the medications; one doctor might develop an individual approach that another doctor might question.  This has resulted in some doctors being labeled as pill pushers and other doctors staying away from these drugs entirely.  

I personally believe that the use of poorly conceived schedules of medication administration have led to erratic drug levels in the patients.  This, in turn, has led to problems with tolerance, physical dependency and abuse. 

Slow Release morphine-
(MsContin, Kadian. Avinza) 

MsContin has been around the longest of any delayed release medications.  It gives great pain relief but some patients are susceptible to the side effects of sedation and nausea.  The pill can be abused by chewing.  It is supposed to be taken every 12 hours but most doctors will give it three to four times daily.

Kadian has a different mechanism of drug release and it is supposed to be given once daily (but some docs give it twice daily).  One advantage is that it is difficult to chew. It comes in a capsule like Contact Cold Medication, with mini beads containing the medication.  These beads are too small to be easily chewed.    I consider this to be the safest preparation in terms of safety from abuse.  Some patients have found it less effective than equvalent strengths of the other preparations.  I suspect that is because  they miss the more rapid increase in morphine drug levels seen with the other preparations.

Avinza is a different opioid medication that is advertised as being a true once daily pain medication.  There is an initial release of morphine  consistent with a rapid release preparation and than a  slow release throughout the day.  As an addiction specialist, the rapid release concerns me.

Slow release oxycodone- (Oxycontin)

This medication has been heavily marketed in a medical atmosphere more tolerant of pain medications.  Its’ use has skyrocketed, but it has also been widely abused.

Oxycontin is a better-tolerated medication than the morphine products.  There are fewer problems with nausea and fatigue.  Although it is supposed to last for 12 hours, the effect is actually only for 8-12 hours.  Many doctors prescribe it 3 and 4 times a day.  This concerns me.  A new pill is taken before the last one is fully absorbed.   My belief is that this results in unpredictable spikes in the serum drug level.  This causes euphoria and increased tolerance.  I had severely restricted my own use of this medication several years ago because I had found that I was forever increasing the dosages  

Unfortunately, another problem I encounter is that addicts know about Oxycontin.  Many less honest people come into the office making up stories in order to a get a prescription.  The recent stories about it have scared many doctors from prescribing pain medication.

For a time, I had used the drug with greater caution.  I did not use the drug more frequently than every 12 hours.  I knew that my patients experienced pain at the end of the dosing interval.  However, I believe this schedule minimized the development of tolerance.  When they took their next dose 12 hours later, they got prompt relief of the pain.  When I was doing this, my problems with the need for dose escalation almost vanished.  Many doctors disagree with me and continue to use this medication frequently.  This is why each patient has to decide what is the right approach for him or her. 

There are tremendous problems with abuse and diversion of Oxycontin.  It is abused more widely than the slow acting morphine drugs.  It is not clear why this is so.  Is it because the drug is more widely marketed and used?  Is it because its’ effects are widely known throughout the drug abusing population?  Or, is it because the drug is somehow more addictive?  After all, we have not seen as much of a problem with MsContin, which has been around longer.

Slow-release fentanyl patch- (Duragesic)

This is a well-tolerated and potent medication that is quite effective.  Sedation and nausea are minimal.  It is in a patch form and the medication is absorbed through the skin.  It is to be used every three days although I often used it every two days.  There is a clear-cut fall in the serum level on the third day.  I felt comfortable using this more often (as compared to Oxycontin) because you could remove the prior patch from the body when placing a new one. 

Problems include skin reactions and the patch coming off.  The first problem is solved by the use of Benadryl or other antihistamines.  Pre-treatment of the skin with a steroid spray may also help.  The second problem is helped by the use of Bio-occlusive dressings that can be obtained from the company (Janssen).

This drug is also subject to abuse but studies show that this is less of a problem.  I like this drug a lot.   

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