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Old 02-14-2012, 11:59 PM
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Default How much Black Pepper to potentiate Loperamide

I remember a while back there was a thread about potentiating loperamide, and someone said that Piperine would break down some enzyme, allowing it to cross the blood brain barrier. Someone also suggested an OTC medication that would do the same. Reading this, I ran out, picked up some loperamide, as well as a handful of potentiators. Unfortunately, I was unable to find the most crucial one that broke down the enzyme, so I experienced little. I just starting breaking open a bunch of melatonin gel caps, and was planning to do some loperamide tomorrow, but just wanted to know how many of the caps I should fill with black pepper. Also, it'd be nice to have an idea how much it would potentiate the loperamide, since I don't feel like taking an unintentionally heroic dose and waking up in the ICU.
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Old 02-15-2012, 12:15 AM
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Default Re: How much Black Pepper to potentiate Loperamide

I don't know enough about biochem to know if this metabolite dosen't cross the BBB by the same virtue as Lope, or whether or not it would if you ate alot of black pepper. However, I doubt you do either, so I suggest you cease and desist.

Quote:
Identification of an N-methyl-4-phenylpyridinium-like metabolite of the antidiarrheal agent loperamide in human liver microsomes: underlying reason(s) for the lack of neurotoxicity despite the bioactivation event.
Kalgutkar AS, Nguyen HT.
SourceDiscovery Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Global Research and Development, Groton, CT 06340, USA. amit_kalgutkar@groton.pfizer.com

Abstract
In contrast with the Parkinson's-like effects associated with the mitochondrial neurotoxin N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and the neuroleptic agent haloperidol, there exist no reports on adverse central nervous system (CNS) effects with the structurally related N-substituted-4-arylpiperidin-4-ol derivative and antidiarrheal agent loperamide. Although this difference can be attributed to loperamide's P-glycoprotein substrate properties that prevent it from accessing the brain, an alternative possibility is that loperamide metabolism in humans is different from that of MPTP and haloperidol and does not involve bioactivation to a neurotoxic pyridinium species. In the current study, loperamide bioactivation was examined with particular focus on identification of pyridinium metabolites. A NADPH-dependent disappearance of loperamide was observed in both rat and human liver microsomes (human t(1/2) = 13 min; rat t(1/2) = 22 min). Loperamide metabolism was similar in human and rat and involved N-dealkylation to N-desmethylloperamide (M3) as the principal metabolic fate. Other routes of loperamide biotransformation included N- and C-hydroxylation to the loperamide-N-oxide (M4) and carbinolamide (M2) metabolites, respectively. Furthermore, the formation of an additional metabolite (M5) was also discernible in human and rat liver microsomes. The structure of M5 was assigned to the pyridinium species (LPP(+)) based on comparison of the liquid chromatography/tandem mass spectrometry characteristics to the pyridinium obtained from loperamide via a chemical reaction. Loperamide metabolism in human microsomes was sensitive to ketoconazole and bupropion treatment, suggesting P4503A4 and -2B6 involvement. Recombinant P4503A4 catalyzed all of the loperamide biotransformation pathways in human liver microsomes, whereas P4502B6 was only responsible for N-dealkylation and N-oxidation routes. The wide safety margin of loperamide (compared with MPTP and haloperidol) despite metabolism to a potentially neurotoxic pyridinium species likely stems from a combination of factors that include a therapeutic regimen normally restricted to a few days and the fact that loperamide and perhaps LPP(+) are P-glycoprotein substrates and are denied entry into the CNS. The differences in safety profile of haloperidol and loperamide despite a common bioactivation event supports the notion that not all compounds undergoing bioactivation in vitro will necessarily elicit a toxicological response in vivo.
http://www.ncbi.nlm.nih.gov/pubmed/15319335

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Old 02-15-2012, 02:48 AM
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Default Re: How much Black Pepper to potentiate Loperamide

I've got a better idea. Let's go surfing on a rainbow.
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  #4  
Old 02-18-2012, 02:43 AM
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Default Re: How much Black Pepper to potentiate Loperamide

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Originally Posted by Kipohippo View Post
I tried this once. I call it the week of no shits.
I hear that.
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Old 02-18-2012, 03:07 AM
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Default Re: How much Black Pepper to potentiate Loperamide

yep why not just buy kratom since itl work better and you can shit ??
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Old 02-18-2012, 03:11 AM
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Default Re: How much Black Pepper to potentiate Loperamide

two words; bowel obstruction
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Old 02-18-2012, 05:13 AM
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Default Re: How much Black Pepper to potentiate Loperamide

Actually went through with this a few days ago. Ate like 7 capsules of black pepper, then an hour later 54 mg of loperamide. An hour after that, I got burning stomach pains on and off for a half hour, and around the time they subsided, I began to notice sedation and a small, but noticeable mood boost, which is all I've ever really obtained from opiates, unless mixed with DXM. It persisted for the rest of the day, and I noted pupil constriction as well.
Despite eating 27 anti shit pills, the next morning, I shat 4 times in the hour before I left home, and shat my pants later that day. Fucking Irritable Bowel Syndrome, bro.
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  #8  
Old 02-18-2012, 05:16 AM
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Default Re: How much Black Pepper to potentiate Loperamide

I tried it with raw piperidine/piperine, and even with massive doses only got very mild effects. Not worth the trouble.
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Old 02-18-2012, 05:28 AM
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Smile Re: How much Black Pepper to potentiate Loperamide

Thanks for your noble experimentation. I heard "a tablespoon" given as a starting amount to try, once, but I have no idea how reliable that is. It seems like it fucks with your stomach a bit, though, so probably not worth it in any case.

I attained some effects from a large dose of loperamide by itself - it does cross the BBB, just in very small amounts. Unfortunately, I didn't even notice a mood boost; just sedation.
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Old 02-18-2012, 08:23 PM
Hydroponichronic Hydroponichronic is offline
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Default Re: How much Black Pepper to potentiate Loperamide

I think OP might be confused. A while back I made a thread on black pepper and phenol-ether opiates (codeine type, with a methyl group on the aromatic ring). The idea was that the piperine would stimulate the enzyme that hydrolysed that ether bond resulting in faster, higher in-vivo conversion to the resulting morphine-type opiate. I then go on to test the idea in that thread with DXM (a codeine-type NMDA antagonist) and found no effects whatsoever. It is possible that piperidine could work for this process, but piperine is no good, and only produces bowel issues.
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Old 02-19-2012, 02:50 AM
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Arrow Re: How much Black Pepper to potentiate Loperamide

That's pretty interesting it itself, but I think what the OP is basing this on is one of these. It's a fairly common hypothesis on drug forums; whether the concept is valid or not, I don't know. If you're too busy to look around yourself, I can try to find a link that describes the theory (flawed or otherwise) behind the idea and you can see what you think.

Edit: Everyone here who tried it reports fantastic results. I'm still skeptical; I took a bit more than a third what these people took, and without pre-loading or black pepper etc. (but so did some of those in the thread IIRC - just with larger doses than I), but even so I felt CNS effects... and there was no euphoria or opioid-like feeling. I'm thinking maybe it's possibly worth another try now, though. Crowbar seems to have had some success; maybe he would have achieved more of a mood boost with a higher dose (and perhaps so much black pepper isn't needed).

I'm leery about taking so much loperamide, though. All indications seem to be that it's safe - as far as I can find; the only scary thing, an article about loperamide overdose possibly causing pancreatitis, appears to be a false alarm - it's just a bit... unnerving to know you're taking 40x the recommended dose. Even if you can read many reports online of people taking as much or more (I think 120mg at once is the most I've seen reported).

I wouldn't recommend it, but I also wouldn't bet that it's dangerous - if I had to gamble. Am I willing to try it myself? ...not yet. But the evidence looks enticing; nearly every report* I can find seems to indicate that it gets you high to some extent. *Excepting those of people addicted to something else and using loperamide to avoid withdrawal.
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Last edited by AdMech; 02-19-2012 at 03:26 AM.
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  #12  
Old 02-19-2012, 03:13 AM
Hydroponichronic Hydroponichronic is offline
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Default Re: How much Black Pepper to potentiate Loperamide

Now that I think of it, there was another thread in which I found polysorbate 80 could be co-admin'd to assist BBB crossing. The easiest source of which is probably ice cream. Though I doubt it works orally, but it might be worth a shot.
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Old 02-19-2012, 03:16 AM
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Default Re: How much Black Pepper to potentiate Loperamide

Yeah. I slam ice cream and anti-diarrhea medication. Sowut?
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  #14  
Old 02-19-2012, 03:21 AM
AdMech AdMech is offline
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Grin Re: How much Black Pepper to potentiate Loperamide

Haha, ice cream contains polysorbate-80? I'll be damned. But I think you must coat the loperamide in polysorbate-80 nanoparticles; that's the method used in the only article citing this technique that I'm aware of, at least.

Check out my edited post's link, or just Google around. I want to believe it truly is "the poor man's methadone".

Btw, I can at least vouch for the fact that the constipatory action hits a limit fairly quickly; I had no problem shitting after 30mg or so. Really, it's more the nausea I'm worried about. (And apparently, loperamide dependence/withdrawal is pretty awful.)
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Old 02-19-2012, 03:21 AM
Hydroponichronic Hydroponichronic is offline
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Default Re: How much Black Pepper to potentiate Loperamide

Quote:
Originally Posted by iMagiNation View Post
Yeah. I slam ice cream and anti-diarrhea medication. Sowut?
Do it for science!
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Old 02-19-2012, 03:22 AM
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Grin Re: How much Black Pepper to potentiate Loperamide

Stop replying so quickly, Hydro; I don't know if you can see that the thread has been updated with my posts.
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Old 02-19-2012, 03:34 AM
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Default Re: How much Black Pepper to potentiate Loperamide

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Last edited by 1337; 07-30-2012 at 10:07 PM.
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Old 02-19-2012, 03:47 AM
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Hypno-HAI Re: How much Black Pepper to potentiate Loperamide

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Originally Posted by 1337 View Post
Quinine (not concentrated enough in tonic water) is also used to aid in loperamide passing through the BBB. Also, mannitol (a sugar substitute) will theoretically work.
Yeah, but why and how
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Old 02-19-2012, 03:57 AM
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Default Re: How much Black Pepper to potentiate Loperamide

Those pills are so cheap, you can get them in bulk online, I always wanted to try this out as well but I am very skeptical it works or is worth it, euphoria is a must, anything can make u tired, and that is just boring
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Old 02-19-2012, 04:01 AM
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Default Re: How much Black Pepper to potentiate Loperamide

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Last edited by 1337; 07-30-2012 at 10:07 PM.
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  #21  
Old 02-19-2012, 04:11 AM
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Mad Re: How much Black Pepper to potentiate Loperamide

Everyone read this and/or Google for more, dammit. I once dismissed loperamide entirely, due in part to my own experience, but I've now re-convinced myself it might be worth a shot. Thoughts?
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Old 02-19-2012, 04:18 AM
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Default Re: How much Black Pepper to potentiate Loperamide

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Originally Posted by AdMech View Post
Stop replying so quickly, Hydro; I don't know if you can see that the thread has been updated with my posts.
*checks*

well I'll be damned
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Old 02-19-2012, 04:19 AM
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Default Re: How much Black Pepper to potentiate Loperamide

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Last edited by 1337; 07-30-2012 at 10:07 PM.
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Old 02-19-2012, 04:25 AM
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Default Re: How much Black Pepper to potentiate Loperamide

I think black pepper inhibits certain enzymes initially, but after some hours it induces them.
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Old 02-19-2012, 06:58 AM
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Thumbs Up Re: How much Black Pepper to potentiate Loperamide

Quote:
Originally Posted by 1337 View Post
Not sure if serious, but mannitol temporarily shrinks the endothelial cells that form tight junctions at the BBB. From the introduction of IV mannitol, the endothelial cells will shrink after 5 minutes and stay shrunk for 30 minutes. The tight junctions open and theoretically anything in the bloodstream can enter the brain.
Honestly didn't know that, but it makes sense.
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Old 05-15-2013, 08:53 AM
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Grin Re: How much Black Pepper to potentiate Loperamide

Quote:
Originally Posted by iMagiNation View Post
Yeah. I slam ice cream and anti-diarrhea medication. Sowut?
Quote:
Thanks: Hydroponichronic (Yesterday)
well at least you didn't necrobump it!...oops
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Old 05-15-2013, 09:45 AM
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Default Re: How much Black Pepper to potentiate Loperamide

Godamn. Sometimes I forget how truly insane life can be.
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Old 05-15-2013, 09:52 AM
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Default Re: How much Black Pepper to potentiate Loperamide

Enzyme inhibition won't potentiate shit if loperamide can't cross the BBB in significant amounts.
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Old 05-15-2013, 03:16 PM
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Default Re: How much Black Pepper to potentiate Loperamide

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well at least you didn't necrobump it!...oops
I was reading over this thread (found it looking for that compilation post) and then saw your post. I thanked it thinking "There's no way he'll ever see this in a thread this old." Joke's on me.
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  #30  
Old 05-15-2013, 03:40 PM
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Grin Re: How much Black Pepper to potentiate Loperamide

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Originally Posted by Hydroponichronic View Post
I was reading over this thread (found it looking for that compilation post) and then saw your post. I thanked it thinking "There's no way he'll ever see this in a thread this old." Joke's on me.


someone doesn't obsessively check every thank they've gotten.
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