Loperamide-COVID-19: Loperamide is a Potent inhibitor of SARS-cov-2, COVID-19 virus in vitro

[paracelsius]

Quite interesting Belgium-Dutch and Chinese studies:

de Wilde A, Jochmans D, Posthuma CC. et al. Screening of an FDA-Approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture. Antimicro Agents Chemother.2014; 58 ( 8 ): 4874-4884.

Abstract:..Registered therapeutics for the treatment of coronavirus infections are not avail able. Moreover, the pace of drug development and registration for human use is generally incompatible with strategies to combat emerging infectious diseases. Therefore, we have screened a library of 348 FDA-approved drugs for anti-MERS-CoV activity in cell culture. If such compounds proved sufficiently potent, their efficacy might be directly assessed in MERS patients. We identified four compounds (chloroquine, chlorpromazine, loperamide, and lopinavir) inhibiting MERS-CoV replication in the low micromolar range (50% effective concentrations [EC50s], 3 to 8 microM). Moreover, these compounds also inhibit the replication of SARS coronavirus and human coronavirus 229E. Although their protective activity (alone or in combination) remains to be assessed in animal models, our findings may offer a starting point for treatment of patients infected with zoonotic coronaviruses like MERS-CoV. Although they may not necessarily reduce viral replication to very low levels, a moderate viral load reduction may create a window during which to mount a protective immune response (cf txt for data on SARS-cov2 ie COVID-19).

Independently, this Chinese study also identified Chloroquine and Loperamide as potent anti-SARS-cov compounds in a screen of ~2000 approved drugs, confirming the Dutch study:

Shen L, Niu J,Wang C. et al High-Throughput Screening and Identification of Potent Broad-Spectrum Inhibitors of Coronaviruses. J Virology. 2019; 93(12): e00023-19.

Chloroquine is all over headlines news as being studied for COVID-19. Loperamide, an OTC antidiarrheal is as potent as chloroquine in the same in vitro assays: Its EC50 to block virus replication (SARS-cov) is about 5.9microM, in the same range as that of chloroquine (4.1microM). However, for Loperamide, the EC50 is well above the plasma concentration reached for a NORMAL maximum daily dose recommended (16mg) in humans to treat diarrhea (NOT FOR ITS CENTRAL OPIOID ACTION): Lope plasma concentration is roughly 50x lower than the antiviral EC50 reported by these authors. On the other hand, Chloroquine recommended dose (up to 500mg) and plasma concentration is within range of its antiviral EC50; but it is also within range of its lethal dose LD50!

Now, my question is: since lope is abused by some opiates users (100s mg/daily?!! way above its antiviral EC50), does that make them unwknowingly protecting themselves from SARS-COVID-19 infection? Would be interesting to see if heavy lope users get sick from COVID-19 or if they do, how do they handle the course of the infection?

NB: Please note, these are CELL CULTURE IN VITRO assays (doesn't mean Loperamide would work in vivo). Just like the jury is still out for Chloroquine (the real Scientific Jury not the "Know-it-all" "Doctor-in-Chief" claiming: "It works because I say so!!!"). I am just pointing out a potential alternative to Chloroquine to study for COVID-19 therapeutics, which incidentally turns out to be an abused...over-the-counter OPIOID!

 

[polymath]

Taking hundreds of mg:s of loperamide carries enough heart attack risk to negate any of that.

 

[paracelsius]

true. but also you can avoid taking the risk of heart attack and dropping dead chocking on your own lung collapse of COVID infection. It is a matter of TI for ALL drugs (not just Lope or Chloroquine!)

 

[evo4ever]

true. but also you can avoid taking the risk of heart attack and dropping dead chocking on your own lung collapse of COVID infection. It is a matter of TI for ALL drugs (not just Lope or Chloroquine!)

Theoretically yes Loperamide could potentially inhibit COVID-19 as Loperamide is a P-glycoprotein substrate so COVID-19 virions would bind to Loperamide instead of ACE2.

 

[Painful One]

Loperamide for the win!!

I am going to have to use it for a few days.
Besides keeping me out of morphine withdrawal hell, it actually helps with this virus!
WOO-HOO!!

Thank you for the fine information @paracelsius

 

[S.J.B.]

Moderators, please close this thread for being a dangerous unsubstantiated claim for a COVID-19 treatment. I will report this thread to closed. This is a novel coronavirus and any treatment for this coronavirus is so premature, and this one could be deadly.

I understand that people are scared and are looking for anything, but not now, and definitely do not suggest taking large amounts of loperamide. People could harm themselves listening to this nonsense!

A study is being discussed here. Nobody is suggesting anybody take anything.

Loperamide for the win!!

I am going to have to use it for a few days.
Besides keeping me out of morphine withdrawal hell, it actually helps with this virus!
WOO-HOO!!

Thank you for the fine information @paracelsius
❤

Please read the OP again, this is far from being evidence that loperamide can treat COVID-19 in humans.

 

[Painful One]

Well, I am going to have to use it for WITHDRAWAL for a few days anyway.
I am not expecting it to cure any virus.
But this study is an unexpected Bonus.

I am advising no one to use Loperamide.
it is dangerous and has a very bad withdrawal of its own if used for very long at high doses.

 

[paracelsius]

Moderators, please close this thread for being a dangerous unsubstantiated claim for a COVID-19 treatment. I will report this thread to closed. This is a novel coronavirus and any treatment for this coronavirus is so premature, and this one could be deadly.

I understand that people are scared and are looking for anything, but not now, and definitely do not suggest taking large amounts of loperamide. People could harm themselves listening to this nonsense!

—Wizard

amazing how the humans brain amygadala works: reactive rather than proactive. ever kin to pick and choose and made up stories to justify preconceived emotional studipidity and jump to conclusions: where exactly in the OP did it say "it is a treatment for this coronovirus"? you made that up! at the very least, read the tittle of the OP and the abstract of the studies: IN VITRO in cells assays.. (hope you understand what that means..else google it before spewing stupidities. OP cite two references with the EC50 IN VITRO aka in cells assay.. aka in test tube in a laboratory (google In Vitro, EC50, test tube, laboratory if you dont know what that mean).

Please note, these are CELL CULTURE IN VITRO assays (doesn't mean Loperamide would work in vivo)

Which part you don't understand?

Notice though you might not agree with the results of the 2 studies mentioned but it won't make an iota of a difference as to the numbers the authors published in peer-review journals.LOPERAMIDE INHIBITS MERS and SARS-cov VIRUS IN VITRO. If you disagree, do your experiments, get your data to show otherwise, submit them to peer-review and publish them..else, I'd suggest you try Psilocybin (it is good for shutting down the reactive, amygdala-dominated brain default mode network that makes people blind and see only what they want to see.. If you were to search and read the paper carefully and "see" with your pfc not the reptilian brain amygdala, you'd see that Loperamide is one among several drugs that were active: you might even come up with some suggestion for other Cov2 drugs among the list that may not have Lope or Chloroquine side-effects..but no: you choose to suggest to shut down the thread so people who might otherwise contribute positively from these studies will be silenced so your amygdala would make you feel better.. see how the default mode network (really try one of the Psilocybin psychedelic; it is incredible at overcoming the amygdala and opening peoples "eyes" so they can "see" what they're missing!!

 

[Nagelfar]

Interesting. (And for the record, I know it is slightly off topic, but in consequence to believing it is a little 'too much more' of a touchy subject for some than it need be; I had bowel movements every day on 200mg a day)

 

[sekio]

A good buddy of mine had a habit of eating stupid amounts of loperamide when in opioid w/d... from what he told me, he'd only get a half-hour or so of relief, but in return it screwed his bowels up bad (nothing like 45 minute shits that clog the toilet). In addition, the blue liquid-caps he took would stain his urine dark olive to black.

I can't imagine any of that was healthy for him. I never got any sort of useful effects out of lope.

 

[Painful One]

Interesting. (And for the record, I know it is slightly off topic, but in consequence to believing it is a little 'too much more' of a touchy subject for some than it need be; I had bowel movements every day on 200mg a day)

A good buddy of mine had a habit of eating stupid amounts of loperamide when in opioid w/d... from what he told me, he'd only get a half-hour or so of relief, but in return it screwed his bowels up bad (nothing like 45 minute shits that clog the toilet). In addition, the blue liquid-caps he took would stain his urine dark olive to black.

I can't imagine any of that was healthy for him. I never got any sort of useful effects out of lope.

I have no problem having a bowel movement when using Loperamide for morphine withdrawal.
It keeps things “normal” for me.
There is some strange synergy that allows me to use a moderate (way lower than most would think, not crazy stupid amounts)
amount of Loperamide as a “bridge” for 2-3 days until I get my next refill of morphine.
It is only when in dire straits. Serious emergency backup.
It is not healthy and can be very harmful, deadly even.

But for Me, with my high tolerance and if using just the right amount to keep me in “mild” withdrawal instead of severe withdrawal....
It works perfectly.
It seems to substitute for morphine particularly well.

I do not know how your buddy could only get a half hour relief taking stupid amounts when in withdrawal @sekio
Loperamide is long lasting and one dose will hold me out of morphine withdrawal for two days!
It lacks any feelings of being “high” so your friend was having psychological withdrawal not physical is my guess.
He must have been poisoning himself with crazy amounts to turn his urine dark....that is a sign of liver failure.
I can see why he was suffering. He is lucky he did not die a very painful death.

I am not advocating that anyone use Loperamide.
but if you are really in a bind, like I will be tomorrow, it is a lifesaver.
It is very strong and most can get by on 20 mg or less easily.
Never take Loperamide for more than 4-5 days MAX!

I had a fiasco with my medication over the holidays which has taken me months to straighten out.
This will be my last few days of using Loperamide as a “bridge “ until refill.
I am handing my prescription over to a family member to give me my daily dosage so I do not have this problem again!
It is retarded!!
It is just so hard to keep to the prescription instructions perfectly when one is suffering with severe chronic pain and injury.

 

[sekio]

Loperamide is long lasting and one dose will hold me out of morphine withdrawal for two days!

In my experience, there is a large interpersonal variance in how people respond to loperamide. I personally don't even bother with the stuff - I could consume whole boxes of the 2mg tablets and still be suffering, no lie. My friend at least reports a short-lived buzz and a few hours of relief, but from my perspective it didn't seem to be doing him very much good. Some lucky individuals can apparently even get high of lope... not me.

He must have been poisoning himself with crazy amounts to turn his urine dark....that is a sign of liver failure.

It turns out that the dark urine was from the dye included in the liquid gelcaps - it only ever occured immediately after dosing loperamide, and only when he used the liquid gels. Solid tablets or other formulations didn't cause the same dark pee.

 

[Xorkoth]

In my experience, there is a large interpersonal variance in how people respond to loperamide. I personally don't even bother with the stuff - I could consume whole boxes of the 2mg tablets and still be suffering, no lie. My friend at least reports a short-lived buzz and a few hours of relief, but from my perspective it didn't seem to be doing him very much good. Some lucky individuals can apparently even get high of lope... not me.

Interesting, for me, it blocks a lot of the opiate withdrawal effects, most notably the limb restlessness and pain, it makes me feel like a heavy blanket has been cast over me and I can relax in my own skin, which is the worst part of opiatte withdrawal, I used to suffer from horrid RLS as a kid so I think I'm particularly susceptible, I am utterly unable to sleep for the duration of acute withdrawal and the feeling of full-body RLS is not something I would wish on my worst enemy. Loperamide kills that in its tracks, it also helps some with the depression and anxiety but not as much with that. Also, it takes 3-4 hours to work, and then lasts about 36 hours, at least.

But, it also dries out my membranes much worse than any other opiate ever has, to the point it makes my esophagus and stomach hurt (quite severely) and absolutely no shitting for 4 days after a single large dose. Years back I used to take it often because I was yo-yoing in and out of opiate dependence when trying to get off of them. It had less side effects then, but they seem to have gotten worse. I relapsed on opiates last year and got off again recently... I used loperamide once, during the worst of it, and it did provide relief but the side effects were so severe it scared me and I just dealt with the w/d after that because even the relief wasn't worth it.

I'll also point out that we have a many years old thread in Trip Reports that started as a TR about using loperamide to get high, but over the years it collected a lot of replies and these included a number of BLers or loved ones of BLers reporting hospitalizations and even deaths from loperamide abuse, all involving heart damage.

 

[Skorpio]

I would be very conservative about using lope as a covid treatment due to the qt interval issues. These are an issue with chloroquine and could very well preclude one from safely doing both treatments.

Also for the non opioid dependent out there, I think it is quite a bad move to prophylactically dose lope and quite possibly come out of this quarantine with a habit because it has no data other than a reduction of viral load (not even complete cure) in cell culture. Combining the addiction liability (for opi naive folk) with the qt prolongation, lope has a lot of dark sides for a prophylactic or even curative treatment with very little indication that it has efficacy against the virus.

The most efficacious drugs are likely to be the vaccines and antibody treatments. Viruses dont have a lot of moving parts so antiviral small molecule drugs often have off target effects which makes them undesirable.

 

[LopeyInJax210]

A good buddy of mine had a habit of eating stupid amounts of loperamide when in opioid w/d... from what he told me, he'd only get a half-hour or so of relief, but in return it screwed his bowels up bad (nothing like 45 minute shits that clog the toilet). In addition, the blue liquid-caps he took would stain his urine dark olive to black.

I can't imagine any of that was healthy for him. I never got any sort of useful effects out of lope.

I believe the problem was that he was taking the blue liquid caps... Lope will last days. It's the little green tablets you have to take

 

[LandsUnknown]

Lope can build up in your system. So, if you're taking it daily, you can eventually reach an overdose threshold even if each individual dose was short of the OD threshold. That's what you need to watch out for with this stuff.

 

[SpaceWanderer]

I would like to share my experience with lope, quinine, and Covid19.
This is in the interest of science.

Everybody knows the dangers of loperamide: passing a dessicated pineapple out your butt that drags half your colon with it leaving it hanging out, long qt interval, torsoides de point, pacemaker, death. I post this with respect for the reader and assume he isn’t stupid and hoping he doesn’t have a death wish and has a sense of personal responsibility.

Beginning January two years ago I began a daily lope habit. 240 mg per day. For 2 years. Yes that long. I was getting a nice high off it. Then I quit.

Withdrawals were unbearable within 24 hours of my last 240 mg dose. Immediately went on 300 mg morphine sulfate per day and tapered to zero over a month.

I haven’t been sick those 2 years. Not even a cold.

So in January 2020 just days before confinement in Wuhan China and borders closed , my girlfriend flies back to my city. She touched the doors and railings of the Wuhan International Airport. She touched the grocery buggy handles and bathroom knobs at public places in that epicentre for covid.
She arrives and I meet her. I assumed she was exposed. She’s young and healthy. Low risk category.

3 days later I get a sore throat. Gargle salt water. Go run 10 miles. Sore throat gone. Not sick.

So after quitting lope and morphine I had my heart cheched. Doc said I have the heart of a marathon runner. In other words no damage . But I work out. Don't know about the people who burned out their hearts on lope.

I also asked for a covid test. The antibody test and the PCR test.

Doc says " You had covid. "

Yay. Best news of the day. It reminded me of how happy everybody was in a famous 25 year old AOL e-mail commercial.

I have tons of antibodies against it. Most likely I'm immune and will never get or the new strains. I assume I got it when I had that sore throat for an hour that daya year ago.

So while a lope fiend, I never got symptoms. I didn't get sick. Before taking up lope, I would get colds that kept me in bed for days. With lope, I have the immune system of a champion.

 

[allone]

IN VITRO. IF you want to challenge me, ill bring you 100 more natural elements that are IN VITRO against covid or any flu or cold out there. Its marketing, its SCIENCE@

to add to it, arent you guys ALL using vitamin d, vitamin c, zinc and elderberry by now

 

[SpaceWanderer]

IN VITRO. IF you want to challenge me, ill bring you 100 more natural elements that are IN VITRO against covid or any flu or cold out there. Its marketing, its SCIENCE@

to add to it, arent you guys ALL using vitamin d, vitamin c, zinc and elderberry by now

It would be interesting to see other people who were were exposed to covid19 while taking daily high doses of loperamide. Did they get sick ? Or were they asymptomatic like me ? If exposed did they develop antibodies which give them lifetime immunity ?
Several years before lope I took zinc and vitamins A and D and elderberry but they did nothing for me. Always got bad colds.

 

[MsDiz]

It would be interesting to see other people who were were exposed to covid19 while taking daily high doses of loperamide. Did they get sick ? Or were they asymptomatic like me ? If exposed did they develop antibodies which give them lifetime immunity ?
Several years before lope I took zinc and vitamins A and D and elderberry but they did nothing for me. Always got bad colds.

Antibodies from covid will not give you lifetime immunity. 3/6 months from what I’ve been reading. The vaccine will be a yearly thing.

High dose loperamide is so bad for your heart. Even, even, if it did help, getting Covid is nowhere remotely near as bad as taking loperamide at high doses.