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Opioids Counteracting opioid induced constipation with naloxone?

Artificial Emotion

Artificial Emotion

Bluelighter
Joined
Jan 19, 2009
Messages
5,314
If naloxone is ingested can it counteract some of the constipation caused by opioids by antagonizing the opioid receptors in the gut? It has a very negligible bioavailability so it would allow your regular opioids to continue to work centrally while the drug works peripherally on the GI tract. There's a drug called methylnaltrexone that's injected subcutaneously which works in a similar way but the cost is prohibitive and it's mainly used for palliative care from what I gather, and where conventional laxatives have failed. Naloxone is cheap though, so would it work and would it be feasible?
 
If you inject it sure, but it will also stop the desired effects. Swallowing naloxone wont stop either the desired or adverse effects precisely because it has poor bioavailability. In order to reach the gut, it would still have to reach the systemic circulation first, so poor absorption will prevent this.

Methylnatrexone works because it does not penetrate into the CNS and can exert its effects peripherally, in this case the gut.
 
I keep seeing stupid pharmaceutical ads for this https://en.m.wikipedia.org/wiki/Naloxegol , I've always just figured if u do a lot of opioids and are backed up you could wait a couple extra hours before taking ur next dose and I'm sure after long enough u will not be backed up anymore...
 
It's a crying (sometimes screaming) shame that we who are in 24/7 pain, have to endure tx-resistant constipation...when we take our pain meds.

NOTHING...and I MEAN NOTHING is working for me towards relieving OIC constipation, as IBS with constipation was pre-existing. I'm miserable with the lack of pain relief, and the pelvic inflammation. The bloating, cramping of inability to move bowels makes all matters worse.

I was in such misery this weekend, I took a Toradol (anti-inflammatory). Those would help me if I could take regularly, but I'm told I can't. Lord, take me now...in my sleep tonight. I don't wanna do this any more!
 
Ryno91 said:
I keep seeing stupid pharmaceutical ads for this https://en.m.wikipedia.org/wiki/Naloxegol , I've always just figured if u do a lot of opioids and are backed up you could wait a couple extra hours before taking ur next dose and I'm sure after long enough u will not be backed up anymore...
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It depends on how much and how frequent you use. If you take opioids several times a day, in relatively high doses, pain may return or withdrawal symptomps start before bowel function returns to normal.

And I does seem oral naloxone despite poor bioavailability, may help decrease constipation from opioids with limited (but not necessarily none) effects on analgesia. So I stand corrected.
 
I have wondered about this, too. I think it may have helped me somewhat when I used to swallow my saliva after letting my Suboxone dissolve. But it would also cause me to feel nauseated for an hour or two, so I began spitting it out and that has been less of an issue. For constipation, I drink Milk of Magnesia every night and it works pretty good. I don't think there's anything especially dangerous about this, at least not compared to taking a stimulant laxative long term, and I've found that it doesn't require larger doses to keep working. Usually between half a tablespoon and 2 tablespoons works for me.
 
DixiChik said:
It's a crying (sometimes screaming) shame that we who are in 24/7 pain, have to endure tx-resistant constipation...when we take our pain meds.

NOTHING...and I MEAN NOTHING is working for me towards relieving OIC constipation, as IBS with constipation was pre-existing. I'm miserable with the lack of pain relief, and the pelvic inflammation. The bloating, cramping of inability to move bowels makes all matters worse.

I was in such misery this weekend, I took a Toradol (anti-inflammatory). Those would help me if I could take regularly, but I'm told I can't. Lord, take me now...in my sleep tonight. I don't wanna do this any more!
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Get miralax, which is safe to use regularly, and probiotic suppliments or else increase your yogurt consumption to at least one a day.
 
Yep. Use an osmotic laxative, polyethylene glycol 3350 by Perrigo does the job, I dose every 3rd day.
 
I always had good results with waiting on my dose, and taking milk of magnesia, senna, and lots of water. Yes it will still hurt, yes you may have blood in the toilet due to your asshole tearing just a bit...but this is peanuts compared to having an impacted colon.
 
Kittycat5 said:
If you inject it sure, but it will also stop the desired effects. Swallowing naloxone wont stop either the desired or adverse effects precisely because it has poor bioavailability. In order to reach the gut, it would still have to reach the systemic circulation first, so poor absorption will prevent this.

Methylnatrexone works because it does not penetrate into the CNS and can exert its effects peripherally, in this case the gut.
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Hey there, with respect I think you've got a couple of things confused. It can reach the gut easily when it's ingested (swallowed), so that isn't a problem. Unlike methylnaltrexone, when injected it does cross into the blood brain barrier and acts centrally on the brain and also peripherally on the the GI tract. To get around this problem I am suggesting we could take advantage of the fact that it has an extremely low bioavailability when swallowed as opposed to when it is injected, so instead of being distributed all around the body it will act on the opioid receptors in the GI tract and not in the brain as well.

I found this small study online when I did a google search. Small, not exactly a comprehensive drug trial but it's still noteworthy and interesting and I think it gets to the points I'm making above. I suspect it does work but the question is whether it is feasible or whether there are cheaper options that do the job just as well. It looks like a good candidate because of the fact that it's so cheap and when ingested it's pretty safe and also because it acts directly at the root of the problem instead of masking the constipation which conventional constipation treatments do.

Oral naloxone reverses opioid-associated constipation.

Meissner W1, Schmidt U, Hartmann M, Kath R, Reinhart K.

Opioid-related constipation is one of the most frequent side effects of chronic pain treatment. Enteral administration of naloxone blocks opioid action at the intestinal receptor level but has low systemic bioavailability due to marked hepatic first-pass metabolism. The aim of this study was to examine the effects of oral naloxone on opioid-associated constipation in an intraindividually controlled manner. Twenty-two chronic pain patients with oral opioid treatment and constipation were enrolled in this study. Constipation was defined as lack of laxation and/or necessity of laxative therapy in at least 3 out of 6 days. Laxation and laxative use were monitored for the first 6 days without intervention ('control period'). Then, oral naloxone was started and titrated individually between 3x3 to 3x12 mg/day depending on laxation and withdrawal symptoms. After the 4-day titration period, patients were observed for further 6 days ('naloxone period'). The Wilcoxon signed rank test was used to compare number of days with laxation and laxative therapy in the two study periods. Of the 22 patients studied, five patients did not reach the 'naloxone period' due to death, operation, systemic opioid withdrawal symptoms, or therapy-resistant vomiting. In the 6 day 'naloxone' compared to the 'control period', the mean number of days with laxation increased from 2.1 to 3.5 (P<0.01) and the number of days with laxative medication decreased from 6 to 3.8 (P<0.01). The mean naloxone dose in the 'naloxone period' was 17.5 mg/day. The mean pain intensity did not differ between these two periods. Moderate side effects of short duration were observed in four patients following naloxone single dose administrations between 6 and 20 mg, resulting in yawning, sweating, and shivering. Most of the patients reported mild or moderate abdominal propulsions and/or abdominal cramps shortly after naloxone administration. All side effects terminated after 0.5-6 h. This controlled study demonstrates that orally administered naloxone improves symptoms of opioid associated constipation and reduces laxative use. To prevent systemic withdrawal signs, therapy should be started with low doses and patients carefully monitored during titration.
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source here

One of the most troubling side effect I get from my methadone use and recently my tapentadol is huge shits. It wouldn't be so much of a problem if they made toilets that could handle the size but imagine every single time you took a shit you would block the toilet and the only way to deal with it is to stick your hand with a rubber glove down to get the blockage moving again if the plunger doesn't work. It's disgusting and having to do it on a regular basis is shitty (pun intended). It's not good for the healthy of your colon and intestines to have shits that large. My anal sphincter is now very week according to my doctor and I suspect opiate use has played a role in this. Also chronic constipation increases your risk of colon cancer so it really is not healthy and you should address the issue if you can.

As well as my regular lactulose I've been put on a drug called lubiprostone (Amitiza) which according to the manufacturers has been authorized for use specifically for opioid induced constipation. They haven't tested it with methadone though, they warn, however it seems to be working quite well for me when combined with the lactulose.
 
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Theres a prescription drug called relistor that is naloxone but with a tweaked molecule so it doesn't cross the blood brain barrier. I hear it relieves opiate induced constipation like magic.
 
Yeah, I think that's the methylnaltrexone that I was talking about. It seems like the best option but the only problem is the prohibitive cost. I asked my doctors to prescribe it and she said the NHS won't even authorize her to prescribe it even if she wanted to because it would be hugely expensive (we're talking hundreds of £ GBP per month just for a constipation drug). If it wasn't so expensive I would take it but because it is I was wondering about naloxone instead.
 
Artificial Emotion, yes I spoke before I checked. There is also an earlier study with similar conclusions. I corrected myself in my later post. My wording sucked too because yes it gets through the GI but high first pass metabolism prevents large amounts of reaching systemic circulation.
 
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Yes, I take Miralax daily (twice) as per doctor. I also take Senna daily. Last night I took Dulcolax along with those, but was afraid to go to sleep (without a diaper :X). I awakened at 5:00 with cramping and explosive BM...I know, TMI...but at least I woke up in time!

I rarely fully evacuate, and don't recall ever having a daily movement. Well...wait...Post bariatric surgery, I was 24/7 diarrhea. It was so bad that I had to take (then prescribed) Lomotil to prevent soiling myself. Common sense tells me that wasn't healthy to take for YEARS, but that's all the doctor could do. Once the diarrhea ceased the constipation began.

AGAIN...Constipation for me is partly anatomical, with surgery to remove disease PLUS a crimped colon in my left side, which even the cancer surgeon would not TOUCH 21 years ago. I avoided opiate therapy for decades because I KNEW my GI would REBEL. It has. It is. I've done (am doing) everything I possibly can. As AE said, these fucking meds for OIC are FAR TOO EXPENSIVE. Yes, there's Amitiza, Linzess, Movantik...but they cost $200-$400 per month. Who the fuck can afford that out of pocket for BMs?

It's not that simple...If it were, I could figure this out. Believe me.
 
Kittycat5 said:
Artificial Emotion, yes I spoke before I checked. There is also an earlier study with similar conclusions. I corrected myself in my later post. My wording sucked too because yes it gets through the GI but high first pass metabolism prevents large amounts of reaching systemic circulation.
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No biggie, easiliy done ;)

Dixiechik you have my sympathies! I don't know how you manage with problems as severe as that and it sounds like a living nightmare.
 
Artificial Emotion said:
Yeah, I think that's the methylnaltrexone that I was talking about. It seems like the best option but the only problem is the prohibitive cost. I asked my doctors to prescribe it and she said the NHS won't even authorize her to prescribe it even if she wanted to because it would be hugely expensive (we're talking hundreds of £ GBP per month just for a constipation drug). If it wasn't so expensive I would take it but because it is I was wondering about naloxone instead.
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Yeah the cost is high and its only been studied for end of life use. So no one knows the long term consequences.
 
Its been studied, at least by the drug company for OIC in patients with non-cancer chronic pain and has that indication. Think others are investigating it orally for the same reason as well.
 
Do not overdo the ducolax or senna. If you use them too much your intestine will be too weak to pass stools although I think this is only true for ducolax, but senna also should not be used regularly. Just stop all the laxitives besides the miralax, which might lead to discomfort at first, but should regulate once it strengthens
 
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