• N&PD Moderators: Skorpio | thegreenhand

Getting loperamide across the blood-brain barrier

This needs to go to Best of Bluelight, tbh. Slamming a mixture of superglue, insulin and loperamide is right up there in the greats like faxing acid.

This poster said it best: "hai guise can I slam diarreah pills with insulin and get hii?" . I lol'ed, hard.

Props to the OP for creativity, but not for posting it in a place where people might just try it.
Interesting theory with the whole protein-mediated passage across the BBB, but please, try it on some test animals first or something.
 
Well I couldn't find any superglue so I used Elmer's. The insulin dissolved pretty well but the glue was kind of a problem, I had to cook it a long time before it finally melted enough to get it into the syringe. I shook it really hard to make sure all the particles were coated, and I decided to shoot it into an artery because I heard that is more of a rush. Well, that was 10 minutes ago and it didn't work. :( I didn't feel anything... oh wait, I am getting a pain in my
 
I can understand the polymer nanoparticles (although I doubt just chucking some loperamide tablets and some superglue in 2M hydrochloric acid is going to be all that productive), but where the fuck does the insulin come into play, Mr. McGuyver? I think loperamide might be active if taken with a highly poten p-glycoprotein efflux transporter inhibitor. It would have to be taken orally, as it is absolutely insoluble in water. I bet it would feel a lot like diphenoxylate or its slightly better active metabolite. Still, the urban myth that is loperamide continues. And nothing can be funnier than faxing acid ;).
 
OK, let's look at this from a scientific perspective. I have quite a bit of experience making aqueous acrylate based polymer systems, and this whole concept is based on someone putting together different pieces of information available on the web with no understanding of what that information actually means.

Yes it is true that nano-particle suspensions of poly(i-butylcyanoacrylate) coated with polysorbate-80 and loperamide have been shown by some studies to pass the BBB.

That is about the beginning and the end of any validity of what is proposed.

Here is why the rest is pure bullshit.

1) Making a suspension of nano-particles of cyanoacrylates is not a trivial process. There are two basic techniques, destructive and constructive routes.

The destructive route: You can mill larger particles of polyalkylcyanoacrylate to reduce the particle size.

The constructive route: You can make a nano-suspension of polyalkylcyanoacrylate by interfacial polymerization of the monomer as a water-in-oil microemulsion.

Both techniques require equipment and skills *way* outside of the scope of what the layman is capable of.

2) Having successfully prepared a nanosuspension ( which you will not) there is additional considerable art and technology required to coat the particles with the drug and surfactant and still maintain a stable suspension. Not that you could do step 1, but even if you did, you can pretty much forget accomplishing this part especially in light of all the additional binders etc you would find in what would be your likely drug source, i.e the starches and other formulation stuff in a typical pill.

3) The whole insulin deal just indicates how bogus this is. Preparations containing insulin have been widely described, but not because it has dick to do with making a basic nanosuspension, but rather because there has been a lot of research in this new technology where the target drug of interest was - yes you guessed it - insulin.

The addition of insulin - unlike how it is described here - in fact has absolutely nothing to do with the preparation of the *delivery system* itself. Rather it is the payload of interest in many studies.

The notion that a layman can do this with some superglue, Tween-80, water, immodium pills, and a diabetic friend is just that - a notion.

To summarize, what is described is a bunch of horseshit.
 
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hfrs said:
I think I'm going to send this over to ADD and let them tackle the flaws in the presented protocol.

*** this is not something that you should be screwing around with unless you really know your chem and pharm. As presented there are quite a few flaws and holes and i would hate to think of anyone even thinking about sticking this in a syringe or anywhere near a body ***

F&B - do with it what you like....


I think the time has come to put this thread out of it's misery...
 
Loperamide and Crossing the Blood Brain Barrier

I apologize for contributing to the excessive threads about loperamide but I had a specific question. I'm not someone who 'swears' by this drug but I think it's helpful for W/Ds.

I've read a few reports and a couple BL threads where quercetin is mentioned in combination with loperamide to helping it cross the BBB. One person on here said it gave him a "dirty high".

Is there any truth to this? Does ingesting quercetin prior to loperamide help it cross the BBB or is this just speculation?
 
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AFAIK, quercetin isn't a P-gp inhibitor (would make loperamide cross the BBB). So, probably speculation.

It is a potent inhibitor of some enzymes though, so it might be a good potentiator. Well, according to wiki, I'll check the sources when I feel like using my crappy internet with journal access.
 
lopramide and prilosec - an otc opiate combo???

wikipedia says you need a protein-pump inhibitor to make loperamide
cross the BBB and become a recreational opiate - prilosec is a PPI...

so $20 could buy you a good time???? 8o8o8o
 
Well, messing with P-gp (what the proton pump inhibitor actually affects to make loperamide centrally active) is a terrible idea. Not to mention the fact that most people have reported not liking the loperamide high.

So yes, you could. And you could also use $20 to buy 5 boxes of diphenhydramine 8)

edit: And are proton pump inhibitors actually P-gp inhibitors? I saw that sentence on wiki, but it didn't have a citation. I have a list of some P-gp modulators, but I don't think it's a complete list.
 
Well, obviously taking Omeprazole doesn't have serious consequences. Omeprazole + Loperamide might, however.

Just look at the toxicity seen when loperamide is administered to children without formed BBB.
 
Well, messing with P-gp (what the proton pump inhibitor actually affects to make loperamide centrally active) is a terrible idea. Not to mention the fact that most people have reported not liking the loperamide high.

So yes, you could. And you could also use $20 to buy 5 boxes of diphenhydramine 8)

ugh...diph makes me sick. dextromorphthan is better:)
 
So it is. Quercetin does seem a little strange. Although I'm mostly interested in the mitochondrial strengthening property.

Apparently there was a study done in humans which should be written up sometime this year. So far it has seemed to work pretty well for the mice, and it's quite cheap.
 
I have tried every otc substance that helps stuff cross the BBB, including quercetin and vitamin C both in high doses. I haven't noticed much of a difference from taking immodium alone. All i get is peripheral effects, but no significant euphoria. Quercetin however has some good synergy with opioids, by acting as anti-histamine and anti-nociceptive.
 
meh, i dont know....i prefer chemicals which exist:D

perhaps he means dextromethorphan. I think I would take 7-hydroxymtragynine if I were lookin for a cheap legal opiatesque high. I would much prefer it to DXM. OTC meds in America make baby jesus cry.
 
Well, I decided to be the test dummy and give this combo a shot just to see. I didn't expect anything which was good because I took 80mgs of prilosec then the loperamide about 45 mins after.
Results:
Nada.... just the same.
I'm giving up on any thoughts that the loperamide may cross the BBB. I think it's a reality we'll all just need to accept.
 
perhaps he means dextromethorphan. I think I would take 7-hydroxymtragynine if I were lookin for a cheap legal opiatesque high. I would much prefer it to DXM. OTC meds in America make baby jesus cry.

legal and opiatesque....yes
cheap......HELL NO

if u are indeed talking about pure 7 hydroxymitragynine and not kratom in general, it is prohibitively expensive. u can get a decent opioid-like experience from plain old bali leaf for a low cost, but once u start with the pure isolates and extracts. kratom becomes absurdly expensive.

Additionally, despite the current prevailing opinion that 7-OHM is the alkaloid responsible for the majority of kratom's effects, my experience and the experience of many others is that pure 7-OHM provides a very incomplete and tame kratom experience. Even large doses of 7-OHM are not nearly as opioid like as just moderate doses of plain leaf.
It seems that even though on paper, 7-OHM SHOULD provide an opioid like experience, clearly the many other alkaloids in kratom leaf make for a much more opioid like effect then when dealing with 7-OHM alone.
 
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