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Opioids Loperamide - OTC Opioid for Recreational and Withdrawal tapering purposes? My initial research forays.

opiateconnect369

Greenlighter
Joined
Oct 4, 2022
Messages
6
Apparently, there is an OTC opioid that just has shitty permeability into the CNS. I didn't even know.

Loperamide Potentiation - Increasing BBB and Intestinal Wall Absorption


Efflux via P-glycoprotein can be inhibited. MDR1 inhibitors (MDR1 is a gene relevant to P-glycoprotein expression) have a stub section on the P-glycoprotein wikipedia article. However, above it a section contains this:

Some common pharmacological inhibitors of P-glycoprotein include: amiodarone, clarithromycin, ciclosporin, colchicine, diltiazem, erythromycin, felodipine, ketoconazole,[32] lansoprazole, omeprazole and other proton-pump inhibitors, nifedipine, paroxetine, reserpine,[33] saquinavir,[32] sertraline, quinidine, tamoxifen, verapamil,[34] and duloxetine.[35] Elacridar and CP 100356 are other common[citation needed] P-gp inhibitors. Zosuquidar and tariquidar were also developed with this in mind.[clarification needed] Lastly, valspodar and reversan are other examples of such agents. ABCB1 is linked to the daily dose of warfarin required to maintain the INR to a target of 2.5. Patients with the GT or TT genotypes of the 2677G>T SNP require around 20% more warfarin daily.[36] Concurrent administration of P-glycoprotein inhibitors such as quinidine potentially allows loperamide to cross the blood–brain barrier and produce central morphine-like effects. Loperamide taken with quinidine was found to produce respiratory depression, indicative of central opioid action.[37]
So, Lansprazole and omeprazole would be the go-to potentiators. These are "proton pump inhibitors", so they come with some side effects of their own. But, all three of these are available OTC in just about every pharmacy in America.

DANGERS - Cardiotoxicity, Arrythmia, Neurotoxicity?


High doses may result in heart problems such as abnormal heart rhythms.[18] Loperamide metabolizes into an MPTP-like compound, but is unlikely to exert neurotoxicity.[34] Since 2015, several reports of sometimes-fatal cardiotoxicity due to high-dose loperamide abuse have been published.[68][69]

Maybe lower doses, facilitated with potentiation via PPIs, could avoid these scary side effects?

Conversion to Fentanyl?


Is it possible to easily convert this substance using kitchen chemistry? It seems pretty similar.
 
Oh, I just realized this is well-covered elsewhere in the forum. Sorry. Im just going to keep this up for my own personal notes if that is OK
 
Here's what you need to read

There are others you can search for. You most likely are going to get a wealth of responses telling you this is a horrible idea and for good reason. It's extremely cardiotoxic - people literally drop dead without warning from fatal heart arrhythmias. The physical dependence it causes makes withdrawal from other drugs look like a walk in the park and it'll sneak up on you real quick. The 'high', such as it is, is more akin to a dirty tramadol buzz than anything. You shouldn't be fucking around with the BBB - there's a reason we have one and the dose response curve is biphasic with loperamide, not to mention extremely steep when you hit the second curve. It skyrockets tolerance to all opioids pretty quickly and it will dehydrate the hell out of you

All in all it's really not something that's worth messing around with. Even using it for WDs can be dangerous and should be used at the lowest effective dose (just accept you're going to be a little uncomfortable from WDs instead of going for obliterating them) for the smallest amount of time possible
 
I have not found any recreational effect even at 250mg and it makes you feel like your stomach is being ripped apart. what is weird is got a euphoric sensation in my legs but no where else for a few hours on that dose but no mental effects. I doubt you could safely convert it to anything with home chemistry
 
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