Naltraxone and Oxycodone

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Kathleen55
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Someone mentioned that in the near future the oxycodone immediate release medication will have naltraxone added to the mix.  If this is true, what effect would that have on the patient?  I guess what I'm asking is - what is the deterent property of naltraxone?  I am prescribed a very high dosage of immediate release oxycodone (600 mg.per day).  Would the naltraxone make that dosage a thing of the past?  Thanks for any information you can provide.

kygiacomo
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no kathleen55 the naltraxone

no kathleen55 the naltraxone is ate up by the stomach acid..it deters ppl from injecting or [censored] the pill which alot of stats including mine KY has alot of abuser on this medication..so if ppl try to inject them wit this stuff in it they will go straight into witdrawel...but if u take the meds as u suppose to then it will be effective for pain..thats my understading of it..i was on subonxe years ago and it didnt affect me,but as u know ever paitent is differnt and we shall see how this turns out in the near future

allgood
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re: kygiacomo

"[T]he naltraxone is ate up by the stomach acid", said kygiacomo.

This is not true.

 

trivia:

Sometimes recovering alcoholics are prescribed Naltrexone to avoid relapsing.

celticgreenman
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Naltrexone

allgood is correct.  In this medicine, the addition of the Naltrexone, is not really for abuse prevention.  From PubMed:

"Oxytrex (Pain Therapeutics, Inc.) is an oral opioid that combines a therapeutic amount of oxycodone with an ultra-low dose of the antagonist naltrexone. Animal data indicate that this combination minimizes the development of physical dependence and analgesic tolerance while prolonging analgesia. Oxytrex is in late-stage clinical development by Pain Therapeutics for the treatment of moderate-to-severe chronic pain. To evaluate the safety and efficacy of the oxycodone/naltrexone combination, three clinical studies have been conducted, one in healthy volunteers and the other two in patients with chronic pain. The putative mechanism of ultra-low-dose naltrexone is to prevent an alteration in G-protein coupling by opioid receptors that is associated with opioid tolerance and dependence. Opioid agonists are initially inhibitory but become excitatory through constant opioid receptor activity. The agonist/antagonist combination of Oxytrex may reduce the conversion from an inhibitory to an excitatory receptor, thereby decreasing the development of tolerance and physical dependence."

 

People also often confuse Naltrexone and Naloxone.  They are not the same drug.

 

cgm

 

medic008
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cgm

I am at work for the next 12 hours, any chance you could link the article? Or anyone for that matter. That is something I have never heard of, but the research sound promising. Imagine not having tolerance issues on long term opiate therapy.
Thanks.

ackack
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Naloxone v Naltrexone

You are confusing Naloxone and Naltrexone.

Naloxone, a mu-opioid antagonist and K-opioid receptor agonist known as "Narcane," is used as an injection to reverse opiate overdose (from mu-opioid agonists like morphine and morphine derivatives as well as synthetics like darvocet, demerol, and fentanyl). Additionally, naloxone, considered to be clinically insignificant if used orally, because it is so poorly absorbed in digestion, decimated by "stomach acids" and other inhibitors of its bioavailability, can be paired with opioid analgesics (such as morphine, oxycodone, or the odd mixed agonist buprenorphine) but not alter the efficacy of the analgesic if used in its intended oral delivery system but serve to block all opiate effects if misused (ie insufflated or injected). Naltrexone, a similiar drug to Naloxone excepting that it is effective in oral form and used both for its dopaminergic effects as well as its antagonistic effects on mu-opioid receptors for recovering opiate addicts as a prophylactic measure and deterrent for other addicts since its block on the pleasure center renders drug and alcohol use and even behavioral issues completely anhedonic, thus supposedly reconditioning the recovering addict by negatively punishing addictive behavior (although it is in fact punishing the patient constantly by blocking the pleasure center, as the naltrexone is in no way selective).

ackack
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YET

If some moralist has prevailed in placing naltrexone in all formularies of oxycodone, and I had been taking high doses of oxycodone for some time, I would certainly switch over to another opiate.

Ivy
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ackack wrote:(although it is

ackack wrote:
(although it is in fact punishing the patient constantly by blocking the pleasure center, as the naltrexone is in no way selective).

Speaking of naltrexone,  don't you think the patient ought to be made aware of that little tidbit of information, and I would think it would be a good reason to keep it out of the medication for cryin out loud!

celticgreenman
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Oxytrex

medic008,

I got the abstract from PubMed.  This is the link:  http://www.ncbi.nlm.nih.gov/pubmed/17685875

Here are some similar articles (the first one is the paper noted above):

Oxytrex:  an oxycodone and ultra-low-dose naltrexone formulation.  Webster, LR.  Expert Opin Investig Drugs.  2007, Aug; 16(8): 1277-1283.

Oxycodone plus ultra-low-dose naltrexone attenuates neuropathic pain and associated mu-opioid receptor - Gs coupling.  Largent-Milnes, TM.  J Pain.  2008, Aug; (9(8): 700-713.

Oxytrex minimizes physical dependence while providing effective analgesia:  a randomized, controlled trial in low back pain.  Webster, LR.  J Pain.  2006, Dec; 7(12): 937-946.

Adding ultra-low-dose naltresxone to oxycodone enhances and prolongs analgesia:  a randomized, controlled trial of Oxytrex.  Chindalor, VL.  J Pain.  2005, June 6(6): 392-399.

 

This is the only formulation that I have found that is not using naltrexone as a deterrent to inappropriate use of the medicine.  For example, Embeda (morphine and naltrexone) specifically states that the naltrexone is there to help prevent abuse.  This other use is actually quite interesting.  If the problems of tolerance and hyperalgesia can be modulated, that would be a step in the right direction, and novel ideas concerning opioid medications have been fairly rare in recent years.

cgm

 

Kathleen55
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OK!

Thanks for the responses!  Now I'm REALLY confused!!  Let me ask this in simple terms because I'm not a science or biology student - Is the addition of this drug in the oxycodone formula designed to get rid of the "euphoria" that is sometimes experienced when taking this med?  Is that the "deterent" that folks are speaking of - I understand that it prevents using the oxycodone in ways other than orally, but for the patient taking it orally is this the reason that people would discontinue its use?  Thanks for your help! Kath

medic008
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Kath, The addition of

Kath,

The addition of naltrexone is being investigated to see if adding a very small dose to the oxycodone will help patients on chronic opiate therapy with tolerance issues. It would also help prevent hyperanelgisa, sometimes people become sensitive to even the smallest of pains and it feels like a broken femur, our the worst pain you should think of. This would not affect the pain control, but in a way help the way it works.

Cgm,
Thanks for the info, I can't believe it has been in studies for so long and I haven't heard about it. Then again, I only started my nursing career a year ago. I'm going to look at the other articles later this afternoon, right now, it's time for a class for CE credits :-(

Tyler