U.S. - It's Proven To Save Lives, So Why Is Maine Opposed To Narcan?

[pmoseman]

"When administered in usual doses and in the absence of opioids or agonistic effects of other opioid antagonists, it exhibits essentially no pharmacologic activity.
...
In the presence of physical dependence on opioids, Narcan will produce withdrawal symptoms."
FDA

THE FOLLOWING IS CURRENTLY UNDER DEBATE: "Narcotics and Narcan share the same receptor sites. So it is just a matter of the amount of each in any sequence. You can titrate downward to block narcotic effect or if you go too far that way add some more narcotic medication to go upward again."
Hospice Patients Alliance

I would not encourage people to administer more narcotic. The effect of the overdose may outlast the 90-120 minutes of Narcan working, prolonging the overdose event.

EDIT: "Because naloxone has a half-life of 1-1.5 hours, considerably less than heroin and morphine, taking more opiates can bring on a second overdose."
International Overdose Awareness Day

 

[neversickanymore]

Sorry Pmose i think you should go back and take a look at how the science works.. cant just reverse the nalaxon by adding more opiates.. cause the chemical with the greatest affiliation for the receptor still wins.

 

[pmoseman]

Sorry Pmose i think you should go back and take a look at how the science works.. cant just reverse the nalaxon by adding more opiates.. cause the chemical with the greatest affiliation for the receptor still wins.

Ya. I think I got science figured out. Hospice Patients Alliance said Chuck Phillips MD said that, and I disagree with what he said but I have never administered these drugs.

I assume with a set-up like they got at the hospital that this works. Why they would advise this if not true I do not know. That would be dangerous.

If you think of Narcan as having the higher probability than narcotics, instead of greatest affiliation wins 100% of the time, which is possibly not the right way of looking at it, then increasing narcotic will cancel out Narcan.

 

[ro4eva]

Republican Gov. Paul LePage opposes a bill that would put Narcan in the hands of more first responders as well as relatives of addicts. LePage vetoed a similar measure last spring, saying it would provide a false sense of security to drug abusers.

Naloxone (Narcan) is known to work by competing with potent opioids - such as heroin, fentanyl, oxymorphone, methadone, and so forth - for μ-opioid receptors throughout the CNS.

For fuck's sake, it's such an effective medication for treating opiate/opioid overdoses that it's on the WHO's List of Essential Medicines!

Mr. LePage: Should a heroin user in Maine end up IVing some "Bud Light" smack, which is reported to be a mixture of diacetylmorphine and fentanyl, and (s)he ends up fatally ODing because Narcan was not readily available to first responders, should you not be held at least partly responsible?

 

[ro4eva]

Ya. I think I got science figured out. Hospice Patients Alliance said Chuck Phillips MD said that, and I disagree with what he said but I have never administered these drugs.

I assume with a set-up like they got at the hospital that this works. Why they would advise this if not true I do not know. That would be dangerous.

If you think of Narcan as having the higher probability than narcotics, instead of greatest affiliation wins 100% of the time, which is possibly not the right way of looking at it, then increasing narcotic will cancel out Narcan.

I may have missed one or more of your earlier posts in this thread, therefore this reply may be pointless (in which case I apologize).

Naloxone (Narcan) has an extremely high binding affinity for the μ-opioid receptor.

Among commonly used μ-opioid agonists (both recreationally and therapeutically), injected (IV/IM/SC) naloxone will compete with and knock or kick off (remove) pretty much any opiate/opioid (the possible lone exception being the partial agonist buprenorphine IIRC).

It will then bind indiscriminately to μ-opioid receptors throughout the CNS/brain and antagonize (deactivate) them until the drug-antidote is broken down by the liver into inactive compounds and eliminated by the body (half-life is about 75 minutes).

As the drug is metabolized by the liver, the opiate/opioid which had previously occupied and agonized (activated) the μ-opioid receptors (before being kicked off by the naloxone) will begin to once again bind itself to any freed up μ-opioid receptor sites.

Multiple injections of naloxone are often required in order to fully saturate all μ-opioid receptors in the CNS/brain, and also due to the short half-life of the drug-antidote when compared to a potent opioid such as methadone, which has a an average half-life of about a day IIRC.

Therefore, properly dosed/spaced out naloxone injections effectively reverses a μ-opioid agonist's (e.g. heroin) effect on a user's breath rate (possibly fatal respiratory depression) by continuously occupying and antagonizing (deactivating) μ-opioid receptor sites until the body has had enough time to break down and eliminate the heroin or other μ-opioid agonist, after which, the naloxone injections are usually no longer required.

 

[pmoseman]

Even if you assume a lot of narcotic users will get a kick out of using Narcan by pushing themselves closer to the edge of a narcotic OD, even though that is not why most victims OD, but let's assume most will do that for a boost and feel safer with Narcan.

Those types of narcotic users are not going to be killing themselves any more than they already do; they will just be wasting their narcotics and going through the Hell of withdrawal whenever they are forced to use Narcan.

Addicts don't want to waste their narcotics.

People OD because they are trying to quit. I remember with cigarettes relapsing many times. If you do that with narcotics then your lower tolerance could kill you. Which is why Naloxene (Narcan) should be encouraged, because it helps people trying to quit.

 

[pmoseman]

... because Narcan was not readily available to first responders, should you not be held at least partly responsible?

If it was due to some legal activity. I am thinking you mean "culpability" when you say that. The governor is not alone on this, with medical workers supporting him.

The best choice is typically what causes the most people to share the burden.

I may...

Are you saying the MD is wrong? Believe me, I want nothing more than to edit my earlier statement and shoot an angry email off to that Hospice website. I just don't know enough about it.

 

[ro4eva]

Are you saying the MD is wrong? Believe me, I want nothing more than to edit my earlier statement and shoot an angry email off to that Hospice website. I just don't know enough about it.

Dr. Phillips answers:

"Narcotics and Narcan share the same receptor sites. So it is just a matter of the amount of each in any sequence. You can titrate downward to block narcotic effect or if you go too far that way add some more narcotic medication to go upward again."

It has always been my understanding that if a patient's μ-opioid receptor sites in his/her CNS/brain are completely saturated and antagonized (deactivated) by IV naloxone (Narcan), no amount of any μ-opioid full agonist drug (e.g. morphine, methadone, hydromorphone, heroin/diacetylmorphine, etc.) will be able to break through that because the naloxone (Narcan) possesses a higher binding affinity for μ-opioid receptors.

AFAIK, due to the relatively short half-life of naloxone (Narcan), a patient who has been given a dose of a prescription opioid (such as hydromorphone aka Dilaudid) via any route and is not experiencing any relief of pain and/or discomfort should theoretically be able to begin to feel relief over time as his or her body metabolizes (breaks down) the naloxone into inactive compounds via the liver. This is assuming that no more subsequent dosages of naloxone (Narcan) are given at a later time, and also that the patient's liver is functioning normally.

To answer your question, the MD may be using very small dosages of naloxone (Narcan) to counteract the morphine. The dosages may be so small that there is simply not enough of the drug available to fully saturate (or occupy) the patient's μ-opioid receptor sites. So In other words, I cannot say for certain whether he's right or wrong, because I'm not entirely sure how much naloxone (Narcan) he used in total, and how he spaced it out (among other things).

I seriously need an XL ice cold Mountain Dew.

 

[pmoseman]

That is absolutely what the site is implying.

if too much narcan is given can more of the narcotic be given immediately to prevent withdrawal symptoms.

 

[neversickanymore]

No. here is some good information Naltrexone Implants for Opiates

I realize this is for an implant.. but the premise of the implant is to provide a continuous dose of the short half lived naltrexone thus preventing the ability of a person to receive and effects if they administer other opiates.

Naltrexone is a pure narcotic antagonist. That is, it attaches to the endorphin or opiate receptors in the brain and completely blocks them. This means that if someone tries to use any kind of opiate while they are on Naltrexone, they feel no effect because all of the receptors are completely blocked. While Naltrexone is in the body, it is virtually impossible to relapse.

From the link above.

 

[BlueHues]

I will say this:

The amount of naloxone given, is supposed to be proportional to the amount of opiates used...

Despite naloxone or naltrexone having a higher binding affinity than say...morphine, enough morphine will override the antagonist. Although, I've never heard of someone being administered more opiates to counteract the withdrawal brought upon by an antagonist...

although, that's not quite true...There's someone in one of the buprenorphine threads that's being given naltrexone shots and buprenorphine at the same time...but that's the first I've ever heard of such a thing...

Edit: so, to be fair here...The idea that opioid antagonists can't be overridden by a high enough dose of opiates is completely false...sorry...I've witnessed it...Some people overdosing need only one mg of Narcan, some people need more...Naloxone has a higher binding affinity, but won't block a massive dose of heroin...

Now, there may be a dose of naloxone that will block "everything", but that's not a dose that's typically given...

 

[pmoseman]

Are there drugs that can prevent narcan from working?
Depends
Not to my knowledge. however a large enough dose of narcotics may overwhelm a given amount of narcan

Dr. Gary Ritholz
Anesthesiology , Board Certified
New York, NY

...
also received a response from a retired RN.

If too much Narcan is given can more of the narcotic be given immediately to prevent withdrawal?
kaismama
No. Narcan is going to bring on withdrawal , that's just the way it is.

I have the strangest feeling opi8 is going to coming around soon...

 

[opi8]

Are you saying the MD is wrong? Believe me, I want nothing more than to edit my earlier statement and shoot an angry email off to that Hospice website. I just don't know enough about it.

You have no problem editing your posts after people have replied. In fact, you have changed your post completely, sometimes to actually hold a position that was almost opposite of your original post. That is, if nobody quotes you. I don't understand why you are still here, I think you should have been perma-banned for being a troll a long time ago. You have no interest in the subjects of this board except to incite anger and simply to disagree with everybody for the sake of disagreement. I don't think you even have your mind made up about the crap you spout, you just want to disagree with whoever is posting at the time.

 

[opi8]

No. here is some good information Naltrexone Implants for Opiates

I realize this is for an implant.. but the premise of the implant is to provide a continuous dose of the short half lived naltrexone thus preventing the ability of a person to receive and effects if they administer other opiates.



From the link above.

No, Naltrexone is not Naloxone. Naltrexone has a very long half life, it is not used for overdoses. Naloxone has a short half life, Narcan is used for overdoses however sometimes, in extreme cases, more than one dose of the short acting naloxone must be used, as it is possible that it could wear off, then once there are receptors open for the opiod agonists, such as heroin, there may still be dangerous depression of the CNS.

Naloxone != Naltrexone.

Naltrexone is used in the implants which are extremely dangerous and with no real clinical trials done (in Australia) except for human guinea pigs. I've read some horrible things, I know people who have had them and they were surprisingly happy with them, but the facts on a large scale show that they are dangerous and they are often not done responsibly.

 

[nthron]

I'm just going to chime in here and say that naltrexone implants website set off my Microsoft security essentials. I suggest not clicking on it.

 

[23536]

I'm just going to chime in here and say that naltrexone implants website set off my Microsoft security essentials. I suggest not clicking on it.

Perhaps your machine is a heroin user.

Stupid joke aside: a youtube video set it off? I suggest you get a better antivirus program than MSE. There are many free options that are superior.

 

[neversickanymore]

Woops.. Thanks for clearing that up. I was thought it was just naloxone under a different brand name. (neads embarrassed smiley)

I spoke with a physician and a pharmD and they both said that the addition of the vast majority of opiates will have no effect until the naloxone drops off. There are a few partials and some really strong agonists which have similar or greater affinities and can compete with the naloxone.

Isn't there also a naltrexone injection that prohibits use for around two weeks?

 

[ro4eva]

I will say this:

The amount of naloxone given, is supposed to be proportional to the amount of opiates used...

Despite naloxone or naltrexone having a higher binding affinity than say...morphine, enough morphine will override the antagonist. Although, I've never heard of someone being administered more opiates to counteract the withdrawal brought upon by an antagonist...

Neither have I, until my discussion yesterday with pmoseman.

It sounds rather risky, but I didn't wanna say anything.

Now, there may be a dose of naloxone that will block "everything", but that's not a dose that's typically given...

If such a dose is administered, does that not mean (commonly used, weaker affinity) μ-opioid agonists cannot override a 'high enough' dosage of naloxone - at least until enough of the antagonist is broken down into inactive compounds that μ-opioid receptor sites throughout the CNS/brain are not completely saturated?

----------------

I sincerely apologize in advance if I'm coming across as a smartass (I'm genuinely curious about naloxone's limits as an antidote, and I'm not confident that my understanding is correct).

I was actually injected once with Narcan, back in 2006 because I had OD'd on a combination of booze and OxyContin. Upon regaining consciousness, I was extremely agitated, and I felt like I was experiencing a 'mini' panic attack, followed by intense muscular pain in my legs, and profuse sweating around my forehead, chest and lower back - very consistent with typical acute opiate withdrawal symptoms, only a very short version (2 hours later, I was stoned again, but not enough to nod). All in all, a very unpleasant experience - and that was back when my opioid habit consisted of about only 60mg of oxycodone daily (a small amount compared to how much I was using 3 years later).

 

[pmoseman]

This is perhaps all getting a bit too extraneous. I just wanted to see if there was a safety net for hard withdrawal. If such a net exists, it is not a very safe one.

Isn't there also a naltrexone injection that prohibits use for around two weeks?

the facts about NALTREXONE for Treatment of Opioid Addiction

ReVia® and Depade® = pill every 1 to 3 days
Vivitrol® = injection once a month

If you are taking naltrexone, you cannot get high from
other opioids because the medication blocks the effects.
Sometimes people take large amounts of opioids to try
to overcome this block. Do NOT do this! It is VERY
dangerous and can cause overdose or death.

You have no problem editing your posts after people have replied. In fact, you have changed your post completely, sometimes to actually hold a position that was almost opposite of your original post. That is, if nobody quotes you. I don't understand why you are still here, I think you should have been perma-banned for being a troll a long time ago. You have no interest in the subjects of this board except to incite anger and simply to disagree with everybody for the sake of disagreement. I don't think you even have your mind made up about the crap you spout, you just want to disagree with whoever is posting at the time.

Ar! I would have gotten away with it too.

 

[BlueHues]

Neither have I, until my discussion yesterday with pmoseman.

It sounds rather risky, but I didn't wanna say anything.



If such a dose is administered, does that not mean (commonly used, weaker affinity) μ-opioid agonists cannot override a 'high enough' dosage of naloxone - at least until enough of the antagonist is broken down into inactive compounds that μ-opioid receptor sites throughout the CNS/brain are not completely saturated?

----------------

I sincerely apologize in advance if I'm coming across as a smartass (I'm genuinely curious about naloxone's limits as an antidote, and I'm not confident that my understanding is correct).

I was actually injected once with Narcan, back in 2006 because I had OD'd on a combination of booze and OxyContin. Upon regaining consciousness, I was extremely agitated, and I felt like I was experiencing a 'mini' panic attack, followed by intense muscular pain in my legs, and profuse sweating around my forehead, chest and lower back - very consistent with typical acute opiate withdrawal symptoms, only a very short version (2 hours later, I was stoned again, but not enough to nod). All in all, a very unpleasant experience - and that was back when my opioid habit consisted of about only 60mg of oxycodone daily (a small amount compared to how much I was using 3 years later).

All I really know is that even a weaker full agonist opioid is capable of "breaking through" a naltrexone or naloxone blockade if a high enough dose is used. I don't know why this is, and it seems to somewhat contradict the basic concept of the way opioid antagonists are supposed to work. That is to say, they're supposed to have a stronger affinity for the mu receptors, bind strongly to them, and nothing with a weaker affinity is supposed to have any chance of getting through.

This could be because not all of the receptors are being "used" by the antagonist, and that's leaving "room" for other opioids to bind to some of them, but that really doesn't explain it adequately IMO. If there were some mu receptors still available, even a low dose of any opioid should be able to bind to them, and if most of the receptors were still being taken up by the antagonsit, the effects should be almost nil...In reality, when the antagonist is overwhelmed, the full effects of the opioid take hold..

It seems to me like, even something with a weaker binding affinity can still "push off" something stronger if there's enough of it present in the bloodstream...I'm not a scientist with a degree that's studied these things, but I've read plenty about it on my own and had it explained to me enough times by people who were... and it seems like the way the whole "binding/blocking receptor" thing works isn't perfectly understood and is more complicated and less black and white than the way it's routinely explained...

Of course, maybe there is a dose of naloxone or naltrexone that completely negates any and all opioids with a weaker binding affinity, and as it stands it requires very high doses to override even the standard amounts usually given people.