[en bloc]

There have been lots of comments about pain meds in recent threads. I didn't want to hijack a thread, so figured it be best to start a new one.

My question is in regards to the new FDA guidelines about limiting Acetaminophen. They specifically mention it in pain meds like Percocet....which as most here know, I take to manage my pain.

They are saying even the 325 mg in each Percocet is bad for the liver if taken regularly. It has taken me 17 years of pain and trying every medication out there and now having significant damage from steroids to finally have good results with Percocet, only to learn that I may need to change due to the Tylenol, not the narcotic. So I must ask...is Oxycontin/oxycodone by itself as effective? I see many here take Oxycontin...and then take Percocet for breakthrough. That sort of tells me that it is either not the same or not as effective for some reason.

Any and all input would be greatly appreciate.

[Susanne C.]

Mrs. D. Would know far more about this but my understanding is that acetaminophen like caffeine is a potentiator- it makes the main medication more effective. I am trying to drink a cup of coffee each afternoon as well to try and maximize my medications, and minimize the fatigue they all induce. I have always been a tea drinker, but coffee has more than twice the caffeine.

It seems to me that the 325mg is a small dose compared with the 1000mg of a regular dose of extra strength Tylenol.

The warnings I have seen, and been given by my own doctor, center around combining Percocet thoughtlessly with NyQuil or alkaselter cold medicine, both of which contain large amounts of acetaminophen. I am not sure that if one does not take any additional acetaminophen that the amount in Percocet alone is a problem.

The reason for taking OxyContin or in my case MS Contin, is to keep a steady amount of medication in the bloodstream, reducing the need for as needed medication. They are time release, and doctors are advised to use them rather than shorter acting meds which can result in pain getting out of control.

[en bloc]

Thanks for the reply. I will look forward to see if MrsD has anything to add, but your thoughts sound both knowledgeable and logical. I know that steroids are potentiators for antibiotic, but never thought of the acetaminophen in this way.

They (CNN running this story on new FDA guidelines) did mention people not realizing they were getting much more when combining cold meds, etc. But they specifically used Percocet in the same context as the cold meds (hidden moderate doses). And that 325mg used regularly is actually more damaging to the liver then periodic doses of 1000 mg.

Quick follow up question(s): Does Oxycontin or MS Contin contain acetaminophen? If not, does the caffeine actually (noticeably) help for effectiveness, or more just to reduce the fatigue?

I cannot consume caffeine due to diabetes insipidus (which has nothing to do with sugar diabetes) and profound autonomic neuropathy affecting my BP. Do you know of other potentiators for pain meds (other then caffeine)?

[Dr. Smith]

Originally Posted by en bloc

Quick follow up question(s): Does Oxycontin or MS Contin contain acetaminophen?

No. There is no acetaminophen in Oxycontin or MS Contin.

If not, does the caffeine actually (noticeably) help for effectiveness, or more just to reduce the fatigue?

Caffeine is a potentiator, but effectiveness depends on the individual and generally their sensitivity to caffeine.

There are many potentiators; aspirin, acetaminophen, ibuprofen, and caffeine are the common ones combined with pain medications. Other medications can act as potentiators as well, but that's best left between patient and doctor, as potentiators are basically medication interactions.

The deleterious effects of acetaminophen on the liver can be attenuated by taking N-Acetyl Cysteine (NAC) along with the acetaminophen.

Oxycodone, the active ingredient in Percocet and Oxycontin, is very effective on its own; it is ostensibly 1-1/2 times as potent as morphine taken orally, but that will depend on the individual.

Doc

[mrsD]

There are other reasons that other ingredients are added in RX pain medications.

1) as a potential discouragement to abuse. However, most determined people ignore this.
Also to extend patent coverage by the manufacturer. The addition of acetaminophen to Tramadol is an example of this. This gives the manufacturer a longer time interval to make money because the mixture is patented...so that patent has to expire before generics can come out.

2) Acetaminophen does not act on mu receptors like the opiates do. This drug has a long history:
http://en.wikipedia.org/wiki/Paracetamol
not mentioned in this article is acetanilide:
http://en.wikipedia.org/wiki/Acetanilide
This was called Dr. Miles' pain pills in the past. Miles labs grew from that, and was bought by Bayer ultimately. Acetanilide was found to be toxic, but acetaminophen was derived from it. The risk of toxicity remains, but is less ...unless you overconsume it.

We know today that acetaminophen does have some anti-inflammatory actions, so that is useful, even though it is a mild effect. Also it has been added to the drug list for patients to avoid who use coumadin. Considering it has been around for so long, it sure took decades to learn more about it. I still cannot find an explanation of "how it works" on pain though!
This link from the official website is still vague on mechanism of action:
http://www.tylenolprofessional.com/pharmacology.html

Analgesia

Although the exact site and mechanism of analgesic action is not clearly defined, acetaminophen appears to produce analgesia by elevation of the pain threshold. The potential mechanism may involve inhibition of the nitric oxide pathway mediated by a variety of neurotransmitter receptors including N-methyl-D-aspartate and substance P.

If a person has liver damage from hepatitis, or cancer, or other reasons, then the 4000mg ceiling for acetaminophen becomes much lower. 2000-2500mg is often mentioned, and often suggested as a daily ceiling for most people today, but it is not widely accepted.

The big problem with it is that there are so many mixtures on the
market with it in it. Tylenol PM, Excedrin migraine and most of the cold/cough mixtures. One has to be very careful with OTC products today in general, as they can have confusing ingredients.

Acetaminophen has been around for a long time...its parents were very toxic. Phenacetin was just taken off the market in other countries around late 70's early 1980's or so. The old APC's sold around the world were aspirin, phenacetin, caffeine. They were more common in Australia and Europe, and the phenacetin caused kidney cancer. Acetanilide was replaced by phenacetin, which was replaced by acetaminophen...but the whole family is one with potential toxicity.

The Percocet content of 325mg acetaminophen is quite negligible as a pain reliever. It is in there mostly for historical reasons, as the patent is quite old. The other strengths were added much more recently. Percocet comes in many combinations:

Oxycodone Hydrochloride, USP 2.5 mg*
Acetaminophen, USP 325mg
*2.5 mg oxycodone HCl is equivalent to 2.2409 mg of oxycodone.

Oxycodone Hydrochloride, USP 5mg*
Acetaminophen, USP 325 mg
*5 mg oxycodone HCl is equivalent to 4.4815 mg of oxycodone.

Oxycodone Hydrochloride, USP 7.5 mg*
Acetaminophen, USP 325 mg
*7.5 mg oxycodone HCl is equivalent to 6.7228 mg of oxycodone.

Oxycodone Hydrochloride, USP 7.5 mg*
Acetaminophen, USP 500 mg
*7.5 mg oxycodone HCl is equivalent to 6.7228 mg of oxycodone.

Oxycodone Hydrochloride, USP 10 mg*
Acetaminophen, USP 325 mg
*10 mg oxycodone HCl is equivalent to 8.9637 mg of oxycodone.

Oxycodone Hydrochloride, USP 10 mg*
Acetaminophen, USP 650 mg
*10 mg oxycodone HCl is equivalent to 8.9637 mg of oxycodone.

from http://www.rxlist.com/percocet-drug.htm

For a long time the oxycodone plain immediate release tablets were being sold without FDA clearance...and there was a shortage of those a few years back when the FDA demanded new drug applications for them. (the same thing happened with some morphine formulations) Percocet is an old drug...in fact it was the second oxycodone containing drug FDA approved and for many years was the only form. It went thru the channels for FDA approval properly. The first was from the same company and was called Percodan...and had aspirin instead of acetaminophen.
But in the late 70's acetaminophen started being mixed with codeine, and Percocet closely followed. Previously codeine was mixed with apc's...and was called Empirin #2,3,4.
There was also Phenaphen 2, 3, 4... that had phenacetin in it as well and it was the competition for Empirin's. Those had to be reformulated and Empirin /codeine, today has no caffeine or phenacetin.

There are still dentists today prescribing Percodan and Empirin with codeine. They prefer the aspirin for the anti-swelling effects.

[Wide-O]

Originally Posted by mrsD

1) as a potential discouragement to abuse. However, most determined people ignore this.
Also to extend patent coverage by the manufacturer. The addition of acetaminophen to Tramadol is an example of this.

Interesting. I had a talk with my GP about this very subject; I wondered why she didn't just rx me tramadol instead of Zaldiar (which is 37,5mg of tramadol with the 325mg of paracetamol).

She is convinced that for some reason - in her experience - the combination does work better than if you would take them separately. The neurologist - I asked him the same question - agreed.

Now, I'm not saying that they are right. But she does not think I would abuse tramadol, and would be happy to give me the "pure" version instead.

BTW, the max dosage of Zaldiar is 8 per day (I do 4 to 6, and less lately). That's a potential maximum of 2600mg of paracetamol/day - I'm guessing there is a reason for it to be 325mg in the different combinations?

[mrsD]

I am thinking that in the case of tramadol it was purely a patent trick. In the US we see all sorts of patent tricks to extend exclusivity to the manufacturer. The most famous was
Furadantin----->Macrodantin----> to Macrobid
This gave the company about 30 yrs of exclusivity and major bucks. Tramadol with acetaminophen also has LESS Tramadol per tablet, necessitating people taking MORE tablets for the desired effect and hence selling more making more $$ for the company. They lowered the Tramadol to 37.5mg from 50mg per.
So of course two of these would work better than one 50mg tablet. I always laugh at the .5mg on some of these creative dosage forms. Now really would 37.5 be better than 37? This is to make generics more difficult to make, IMO.

Another:
Darvon ----> Darvon compound-65----> Darvon N---- 100mg----->Darvocet N (now all removed from sale by FDA as "toxic"....that was 50+ yrs on the market!

The most common patent extender is to make a drug long acting...delayed release: (in the MacroBid example above, MacroBid is extended release meant to be taken twice a day instead of 3 or 4 times a day.

Paxil----->Paxil CR which is funny because the action of Paxil is slow in the body anyway, and has a long half life! Paxil CR had another moment of embarrassment as it was closed down by the FDA as not working...it was unavailable for quite a while as it was "fixed".

Another trick is to have the manufacturer hold onto information about "active metabolites"....and then release the new active metabolite after patent expires on the parent drug.

Seldane----> Allegra
Claritin ----> Clarinex

[Dr. Smith]

Originally Posted by Wide-O

I'm guessing there is a reason for it to be 325mg in the different combinations?

325 x 8 (max per day) = 2600 (max chronic/long-term dose/day of acetaminophen).

Other combinations are/have been available, e.g. 500, 650 http://en.wikipedia.org/wiki/Oxycodo...ol#Formulation

Doc

[Susanne C.]

I do have a bottle of aspirin with caffeine, I take one occasionally if I feel like I need all the help I can get. Since the severity of my symptoms vary from day to day I can't really tell if anything makes a difference in the pain levels. The coffee is keeping me from falling asleep in the afternoon. I know the weather and my hormone cycle are more than a match for any tricks I try. Hoping menopause will help!

[ger715]

Originally Posted by en bloc

There have been lots of comments about pain meds in recent threads. I didn't want to hijack a thread, so figured it be best to start a new one.

My question is in regards to the new FDA guidelines about limiting Acetaminophen. They specifically mention it in pain meds like Percocet....which as most here know, I take to manage my pain.

They are saying even the 325 mg in each Percocet is bad for the liver if taken regularly. It has taken me 17 years of pain and trying every medication out there and now having significant damage from steroids to finally have good results with Percocet, only to learn that I may need to change due to the Tylenol, not the narcotic. So I must ask...is Oxycontin/oxycodone by itself as effective? I see many here take Oxycontin...and then take Percocet for breakthrough. That sort of tells me that it is either not the same or not as effective for some reason.

Any and all input would be greatly appreciate.

Some years ago,For the same reason as you mention, the tylenol, I had the doctor give me a script without the tylenol. Not the same. The Tylenol really makes a big difference. I have been using Percocet 7.5/325 for the past few years. I take it 3 to 4 times a day. I had asked for the lowest dose of Tylenol. From what I have read; the problem is with a much much higher dose than taking this amount daily. For the relief I get, along with taking Oxycontin daily, it's worth it. It has enabled me to at least make it thru each day with the 24/7 pain more tolerable.



Gerry