11–20 of 104 posts
A point of interest, not mentioned in the article, is that loperamide is actually an opioid. All opioids cause some degree of constipation, hence why loperamide helps with diarrhea. Loperamide is unusual, in that it doesn't cross the blood-brain barrier, hence why taking it doesn't get you high.
Sooo, opiates have an anti-diarrhea action by slowing down the intestines/Bowel movements, which is why they cause constipation. Loperamide is an opiate that acts locally (and probably via the bloodstream too) on the intestines, but doesn’t get into the brain, so you get the anti-diarrhea effects without pain relief/getting high/slow breathing of opiates. Some randos on the internet believe that you could consume a b…
If a drug is metabolized in the liver then instead of ingesting a bottle of pills (most likely not safe, certainly not recommended), the way to bypass the liver is to use suppositories. Again, safety-wise it is not a sensible thing to do.
Sooo, opiates have an anti-diarrhea action by slowing down the intestines/Bowel movements, which is why they cause constipation. Loperamide is an opiate that acts locally (and probably via the bloodstream too) on the intestines, but doesn’t get into the brain, so you get the anti-diarrhea effects without pain relief/getting high/slow breathing of opiates. Some randos on the internet believe that you could consume a b…
Sooo, opiates have an anti-diarrhea action by slowing down the intestines/Bowel movements, which is why they cause constipation. Loperamide is an opiate that acts locally (and probably via the bloodstream too) on the intestines, but doesn’t get into the brain, so you get the anti-diarrhea effects without pain relief/getting high/slow breathing of opiates. Some randos on the internet believe that you could consume a b…
> Some randos on the internet believe that you could consume a bottle of loperamide and overcome that inability to get into the brain. In theory that’s true (since the brain barrier is actively pumping it back out and there’s gotta be a limit to that rejection), but I don’t think it’s worked out in practice other than causing massive constipation. It's a medication that gets stolen by drug users which is a bit frustr…
Sooo, opiates have an anti-diarrhea action by slowing down the intestines/Bowel movements, which is why they cause constipation. Loperamide is an opiate that acts locally (and probably via the bloodstream too) on the intestines, but doesn’t get into the brain, so you get the anti-diarrhea effects without pain relief/getting high/slow breathing of opiates. Some randos on the internet believe that you could consume a b…
Re getting loperamide in the bloodstream If a drug is metabolized in the liver then instead of ingesting a bottle of pills (most likely not safe, certainly not recommended), the way to bypass the liver is to use suppositories. Again, safety-wise it is not a sensible thing to do.
Or transdermal or intranasal or sublingual or through the lungs or ...
But I think the issue here is that the blood-brain barrier is actively pumping it back out, not immediate liver metabolism.
I’ve updated my post a bit. I probably shouldn’t have said “locally” since it gets into the bloodstream and should have an effect from the other side too.
Several classes of opioids have been shown to cause neuronal degeneration via ATF4 activation. So, key points: 1. Loperamide is not unique. I don't know why these researchers have singled it out. Is it because they heard there's an opioid that doesn't get you high? It only avoids getting you high because it doesn't get into the brain. IF you deliver it to the brain to treat a brain tumor, it will get you high. 2. Pat…
> ...several studies have shown the induction of autophagic cell death (ACD) by natural compounds or Food and Drug Administration-approved drugs in multiple cancer cell lines. Among these, glioblastomas seem to be particularly vulnerable to the induction of ACD, thus highlighting ACD induction in the context of glioblastoma as an attractive therapeutic strategy to selectively trigger cancer cell death.
Glioblastoma [2], "also known as glioblastoma multiforme (GBM), is the most aggressive type of cancer that begins within the brain." Autophagy [3] "is the natural, regulated mechanism of the cell that removes unnecessary or dysfunctional components."
[1] https://www.tandfonline.com/doi/full/10.1080/15548627.2020.1...
Consider that new drugs cost 1 to 2 billion to come to market, needing extensive tests in petri dishes, cells, animals, young male human volunteers, and then mass drug trials. It is very slow and challenging work to find new drug molecules that are both safe and effective.
But, there are hundreds of disorders, we can't test all safe drugs for effective actions against all disorders. If we have great repurposing, probably through mass automation of tests and computer modeling, then we can make a gold mine of already existing gold nuggets.
This was true of dexamethasone for covid, seems true of loperamide, and could be true for dozens of other compounds already in our pharmacy and medicine cabinet. This is the biggest opportunity in drug development, and HN has technical, computational talent, so consider this area!!!