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Low Dose Opioid Blockers Naltrexone and Naloxone May Aid Problematic-Pain Relief, Research Review Finds

  [ 10 votes ]   [ 4 Comments ]
www.ProHealth.com • April 23, 2009


“Low doses of opioid antagonists have been postulated to “reset” the opioid-receptor system for a period of time, which seems analogous to how rebooting a malfunctioning computer clears memory, refreshes the software, and often restores normal function.”

According to an evidence review from Pain Treatment Topics (http://Pain-Topics.org), opioid antagonists like naloxone and naltrexone - which block opioid drugs from activating their receptors - may be surprisingly helpful for relieving difficult-to-treat pain conditions.

Achieving effective, durable, and safe pain relief, especially in patients with chronic and/or severe pain conditions, can be difficult. For many types of pain, prescription opioids are among the most effective analgesics. Yet, there is a growing body of evidence suggesting potential benefits of opioid antagonists, particularly naloxone and naltrexone.

This is somewhat unexpected because these drugs displace opioid molecules from their neuroreceptors, and block opioids from attaching to and activating those receptors. [Blocking the opioids’ normal effects in dependent or overdosed patients.]

In a peer-reviewed, evidence-based report for Pain Treatment Topics, editor Stewart B. Leavitt, MA, PhD, describes naloxone and naltrexone pharmacology, and the theoretical foundations of opioid antagonists for pain management.

Titled “Opioid Antagonists, Naloxone & Naltrexone - Aids for Pain Management,” the 16-page report includes summaries of 17 studies - case examples and clinical trials - investigating opioid-antagonist therapy in adult humans.

For free access to the complete report with references, click here.

Naloxone and naltrexone have been extensively studied in the past, and are FDA-approved for the treatment of alcoholism or opioid addiction (naltrexone) or opioid overdose (naloxone). A long-acting form of naltrexone for intramuscular injection also is approved for addiction therapy. These antagonists also are being used or tested as ingredients in specially formulated opioid analgesics to deter their misuse or abuse.

Leavitt notes, however, that “doses of naloxone or naltrexone used in pain management are generally much smaller than in other applications; either in the 1 to 5 mg range, referred to as ‘low dose,’ or less than 1 mg, in microgram amounts, designated as ‘ultralow dose.’

In animal studies and human trials, low- or ultralow-doses of antagonists appear to enhance the pain-relieving efficacy of opioid-agonist analgesics, such as morphine, oxycodone, and others. Along with this, tolerance to and physiologic dependency on opioid analgesics, as well as certain opioid side effects, may be diminished.

Furthermore, low-dose naltrexone has been successfully tested by itself as monotherapy for the management of several pain-related conditions, including Crohn’s disease, irritable bowel syndrome, and fibromyalgia. [See for example the recent report, “Inexpensive drug naltrexone appears to relieve fibromyalgia pain in Stanford pilot study.”]

Explanatory mechanisms of action behind the benefits of opioid antagonists in pain management are still under investigation.

• Essentially, appropriately low doses of opioid antagonists have been postulated to “reset” the opioid-receptor system for a period of time, which seems analogous to how rebooting a malfunctioning computer clears memory, refreshes the software, and often restores normal function.

• With opioid-agonist therapy, the body becomes better attuned to the beneficial effects of both external opioids, such as morphine, and naturally occurring internal opioids, such as endorphins.

Clinical research to date on low- or ultralow dose applications of opioid antagonists for pain management in humans has been limited. Still, the available evidence described in this report suggests a number of possibilities that may be of interest to healthcare providers and their patients with pain, including:

• Brief detoxification using naloxone for difficult cases of opioid-unresponsive intractable pain, opioid tolerance, or suspected opioid-induced hyperalgesia.

• Ultralow-dose naloxone combined with various opioid agonists for managing
postoperative pain.

• Ultralow-dose naltrexone (oral) or naloxone (intrathecal) as a component of intrathecal opioid analgesia for difficult cases of intractable pain.

• Ultralow-dose oral naltrexone combined with opioid agonists to provide an opioid-sparing effect, offering equivalent pain relief at lower opioid doses.

• Oral ultra-low dose naloxone or naltrexone combined with oral opioid analgesics to help prevent or reverse opioid-induced constipation and to potentially reduce other opioid side effects.

• Ultralow-dose naltrexone to help facilitate more comfortable opioid-agonist tapering.

• Low-dose naltrexone monotherapy for Crohn’s disease, and possibly for fibromyalgia and short-term treatment of irritable bowel syndrome.

“Although further investigations to assess the safety and efficacy of these applications would be appropriate,” Leavitt suggests, “both of these agents have passed animal and clinical toxicity studies, and have been used for years in applications other than those described in this research report.

“Therefore, it is not surprising that they have exhibited favorable safety profiles when applied at low- and ultralow-dose levels, with few notices of adverse events or side effects at these doses when used individually as monotherapy or in combination with opioid analgesics.”

“Naloxone and naltrexone are available today as generic, economically priced drugs, and it is important that practitioners become aware of the therapeutic options that these may provide for patient care,” Leavitt concludes.

“However, it must be understood that opioid antagonists are not yet FDA-approved for pain management purposes, so low- or ultralow-dose naloxone or naltrexone would need to be cautiously prescribed off-label for compounding at properly equipped pharmacies.”

* * * *

NOTE: The contents of this report are for educational purposes and are not intended to endorse or promote the off-label prescribing of any drugs. Practitioners are advised to study the available evidence and use professional discretion in their prescribing decisions.

Source: Pain Treatment Topics press release, Mar 2009




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Article Comments Post a Comment

Subutex OK, but I would not use Suboxone......
Posted by: shadowsmom42
Apr 29, 2009
My husband is on Subutex. Has done very well on it. Subutex does NOT have Naloxone or Naltrexone in it. However, the doctor all of a sudden is now trying to talk him into going on the Suboxone which DOES have Naltrexone in it. But I don't think that's a good idea. What happens when, in an emergency, the ER doctors have to give you IV pain meds?? If they were to do that, it would throw the person into a severe withdrawal effect if you have the Naltrexone or Naloxone in your system. And if you're on Suboxone, it will. Also, my husband is now on Subutex for pain relief to help prevent him from going back on stronger pain relievers. He was never an IV user. He does very well on it and I don't see any reason for the doctor to now put him on Suboxone after two years.....
Reply Reply

 
reply
Posted by: moineau
Jul 13, 2010
that's what doctor's do, one small complaint about a side effect or even their own whimsy, they change people's medications. it's really horrible, esp. when a drug has been working pretty well. my friends with depression or mental illness have it the worst. that's why i rarely even go to doctors anymore, even though i've been very ill with fibro and cfs for years. i just pick up medication and only go in when they absolutely demand it. they have nothing to offer me...

 

 
shadowsmom42 Is Not Correct. (It's an easy mistake!)
Posted by: pressingtheissue
Sep 12, 2011
shadowsmom42 was trying to explain a bit about Suboxone, Subutex, Naloxone, and Naltrexone. However she made a few important and very common mistakes. Let me try and help:

1. Suboxone is Buprenorphine and Naloxone.

Buprenorphine is a partial antagonist. In layperson's terms; It attaches to your Opiate receptors very aggressively and then does a great job of not letting any other opiates in.

Naloxone is a full opiate antagonist. It is used to reverse the effects of an emergency overdose. It works if injected or if snorted (preferably in a mist form).

You will not go into withdrawal when on Suboxone if you inject or take opiates. You just wont feel any of the desirable effects.(That is due to the Buprenorphine. The Naloxone has nothing to do with it!) In fact, the Naloxone does not even go into your system unless you snort or inject Suboxone. You will go into Immediate withdrawal if you try to snort or inject Suboxone!

So Basically Your husband would be taking the same drug only with an "anti abuse" protection added to it.

 

 
shadowsmom42 Is Not Correct. (It's an easy mistake!)
Posted by: pressingtheissue
Sep 12, 2011
shadowsmom42 was trying to explain a bit about Suboxone, Subutex, Naloxone, and Naltrexone. However she made a few important and very common mistakes. Let me try and help:

1. Suboxone is Buprenorphine and Naloxone.

Buprenorphine is a partial antagonist. In layperson's terms; It attaches to your Opiate receptors very aggressively and then does a great job of not letting any other opiates in.

Naloxone is a full opiate antagonist. It is used to reverse the effects of an emergency overdose. It works if injected or if snorted (preferably in a mist form).

You will not go into withdrawal when on Suboxone if you inject or take opiates. You just wont feel any of the desirable effects.(That is due to the Buprenorphine. The Naloxone has nothing to do with it!) In fact, the Naloxone does not even go into your system unless you snort or inject Suboxone. You will go into Immediate withdrawal if you try to snort or inject Suboxone!

So Basically Your husband would be taking the same drug only with an "anti abuse" protection added to it.

 

 
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