It's a medication that gets stolen by drug users which is a bit frustrating if it's not working for them.
BNF and Department of Health (England) don't describe addiction to loperamide, but do describe its use as an adjunctive treatment for people trying to come off opioids, which suggests it's not that problematic: https://bnf.nice.org.uk/treatment-summary/substance-dependen...
https://assets.publishing.service.gov.uk/government/uploads/...
> Prescribing symptomatically can reduce some of the physical effects of withdrawal. There is no systematic evidence that any of these medicines work to improve outcome but they may be useful for the clinician in situations where it is not possible to prescribe effective opioid substitution. Particular care is needed concerning the risks of polypharmacy and ensuring appropriate supervision and support in such cases.
> •Diarrhoea – loperamide 4mg immediately followed by 2mg after each loose stool for up to five days; usual dose 6-8mg daily, maximum 16mg daily.
As someone who suffers from IBS and takes loperamide regularly, while its not necessarily an addiction, I see forums of people (especially on /r/ibs) saying that it causes a dependency. I saw posts where people kept upping the dose until it got to a point where it doesnt work anymore and you would have to increasingly take larger amounts to have the same effect. Heck some take as many as 3 after every meal. I cant imagine doing that.
I try to avoid doing this and luckily I can get away with one every few days but I dread the day I have to be in that situation.
One thing I noticed is that - it gives me incredible mental boost a day after taking it. It just makes me feel normal and that to me is a 'boost'.
I've read that loperamide doesn't just quell bowel problems with opioid withdrawal, but that it lessens cognitive symptoms, as well.
Sounds like there might be some active metabolites, or that peripheral opioid receptor activation can affect cognition.
I'm not sure why this happened, but my suspicion is that while hospitalized I was infected by MRSA, and to try to get rid of it they were dumping some of the more toxic anti-bacterials into me to get rid of the MRSA (which took a year and a half to get rid of.)
Honestly the whole thing about people abusing it and FDA clamping down works against normal people who are genuinely using it.
40, 38, 36, ... -> freedom
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.
Blood-brain barrier is another obstacle to cross. Quinidine taken with loperamide blocks transport protein P-glycoprotein and causing loperamide to have opioid like effects in the brain.
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 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.
The article touches on this:
> In future studies it has to be explored, for example, how loperamide can be transported into the brain and cross the blood-brain barrier. > Nanoparticles might be a feasible option.
But it remains to be seen what opiate-like effects it would have on the brain if it got through.
For a short-term treatment, this could be managed/mitigated. Mechanically (this machine will breathe for you while we knock out your drive to breathe) or chemically: an opiate-antagonist (naloxone infusion or naltrexone tablets). Whether this would counteract the effect of loperamide remains to be seen.
I also wonder what made loperamide special or if opiates in general would have the same effect. It would be interesting to see if long-term opiate users get this particular tumour less.