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Loperamide Insufflation

antbanks99 said:
Don't fucking snort the stuff. Seriously I'm not one to jump on anyone for asking a question, but what the fuck are you thinking Private Pyle? Its an anti-diarrheal medicine...ya let's snort it dude...we snort everything else right? crack, coke, muscle relaxers, hell ya! remember that one time we snorted a BC powder and it felt like our nose caught on fire....FUCKING AWESOME DUDE!

Anyways, can we please end this thread IMMEDIATELY!

who the fuck cares if its an anti-diarrhea med, to many people hate on it becuz of this, Lomotil is an anti-diarrhea med and its a schedule V drug, it is in the same class of drugs as Imodium (loperamide) and Fentanyl. When Imodium was being developed it was meant to be A strong pain med, but since it didnt cross the BBB in any significant amount they couldnt use it as a pain medication so instead of it going to waste they market it as a shit pill, since all opiates will stop you up. Loperamide is an opiate how ever weak it may be, and people can get high off it, no matter what you say, that doesnt mean you or I could but certian cemicals can help it cross the BBB and also some people bodies are different and some chemicals can cross their BBB while for most people this isnt possible.
 
yeah alot of its making alot more sense to me now. its got a LOT to do with genetics, in my mind. because, i didnt know this, but a few nights back my mom told me when she cant sleep at night, she takes some immodium and it makes her way drowsy and can go to sleep. so obviously its in my genes.....loperamide has effects on me, and my family. i think that for ANYONE it SHOULD be a miracle for wd. also i start to get slightly itchy when i dose up on it, so i belive that not only am i getting peripheral effects, i beLIEve that in small amounts it is crossing my bbb
namaste
 
thats right, even opium tinctures and heroin were once viewed as "anti-diarrheal meds" and obviously, they are, and work great, but even though thats how they were labled, they still get you high as fuck. if someones unwillingly to belive somethign works becasue its otc, then where teh fuck have you been????? ever heard of dextromethorphan or doxylamine or diphenhydramine or propylhexedrine or ephedrine or the fucking list goes on and on........?
 
PcChip said:
I was coming off of 100mg per day habit of Hydrocodone for 2-3 months, I'd call that "medium" or so I suppose

First let me say: comparing habits is about the dumbest thing you can do, worse than comparing dicks and a lot less fun than a literal pissing contest. That said, that is a very small habit, not a medium one. This is not an insult to your manhood, so don't get all bitchy. Doctors say to take it every four hours, and an addict would be taking it at least that often, meaning approx 4-5 times a day. Lots of non-tolerant high-seekers easily take 10-30mg of hydrocodone (maybe more) for recreational purposes.

Sounds to me you had little, if anything at all, of a habit over what I would call a baseline addiction. Baseline addiction being defined as an addiction acquired using close to a standard recreational dose for a period long enough to become addicted, but not long enough (or with the dosing patterns) to ramp up either dosage tolerance (need more to get same effects) or time tolerance (the tolerant-adjusted dose provides shorter effects than originally). Furthermore, medium- to long-term addicts and researchers agree that the length of addiction is more important than how high of a dose, though that isn't particularly relevant in regards to loperamide dosages.

I often think of opiate tolerance in terms of a multiplier- lots of opiate addicts are taking 2x, 5x, 10x or maybe even more- researchers have documented folks using as high has 100 times the amount of heroin in a day than they did when they began at the baseline addiction. My tolerance multiplier when I was last using opiate was 6x, that is, I originally was using a quarter cup of pod grounds daily when I started, but before I quit it was at a cup and a half of grounds, 6 times the dose, to get to the same place. For a short period it was as high as 12x, but for the last 5 years of my 10 year addiction it was 10x (two cups of grounds made into tea). These numbers represent a single dose, but only taken every 24 hours.

I wanted to pop in to say that loperamide does indeed kinda sorta get you high. However, I want to reiterate the point already made: it's pretty dumb to take enough loperamide with the intent to get high, whether tolerant to opiates or not, though sometimes getting slightly buzzed is a side effect of maintenance.

However, loperamide is a veritable wonder drug when it comes to maintenance and withdrawal. It is a flexible drug, and can be used either between bouts of regular addiction with another opiate, it can be used to bring down that tolerance to make using cheaper, it can be used for as a long term replacement for maintenance *and* as a drug to taper with. A pharmacist friend of a friend has called it the "poor man's methadone." It's cheaper, more accessible (doesn't require a clinic or Rx), and has a TON less abuse potential than methadone. Because of the scored 2mg pills it is a TON easier to taper down as fast or slow as you want from the original maintenance dose, so much easier than trying to taper down on something like poppy pods or heroin. A dose lasts about 24 hours for me, but while I had a high dose tolerance, I had a small time tolerance to the pods- I still only used once a day, and was totally high and unsick for 24 hours- if you're using pods (for instance) twice a day, ever day, you will probably need to dose loperamide twice a day as well.

I am on an 80 mg (40 pills) daily dose of loperamide, which has been very slowly tapered down with no WDs or any discomfort from 96 mg (48 pills) a day. I've gone on loperamide dozens of times over 10 years, most times only for a couple weeks. Even when I was still using, I'd switch to maintaining on loperamide if I was going to be on vacation for more than 2-3 days, because using 2 cups of grounds made into tea each day isn't that much work per se, but it's a lot of work to keep it from being obvious to everyone.

When going from use to maintenence, I used the the process outlined below. PLEASE NOTE these dosages are for someone with a high, long-term tolerance. I am not a doctor and I am not giving medical advise. You can use the dose multiplier idea to find the right dose, but start lower than what the math would tell you to do.

1. At the point where you're starting the smallest WD symptoms, where you would usually re-dose your usual drug, take the loperamide. For me, when I was using a cup (4x my original dose) or a cup and a half (6x) of grounds I'd take 96 mg.

2. Repeat the following for 2 days, taking the dose 24 hours after the first dose, and from now on dosing at that time daily. These 2 days aren't fun, but they aren't hell. No shits, but bumping stuff hurts, I get an upper backache, I feel cold, and a few other smaller WD symptoms, but nothing like where you'd be after 2-3 days of a real pod WD. I could sleep fine, but usually only for 6 hours. It wasn't like the usual opiate WD sleeping problems- I'd wake up awake and pretty refreshed, but it's a bit jarring in a way to go from sleeping 8-12 hours a night (opiates, yea) to 6 at first.

You've get a lot of anxious energy during this adjustment phase. In these 2-3 days I found that Xanax or Valium worked wonders for the anxiety and mental symptoms. I personally don't see any recreational value to benzos and had no problem using them to control WD symptoms for a couple of days and stopping, but people who are prone to benzo abuse might want to avoid it. Kava kava works too, but avoid valerian, it just makes you feel shittier somehow during this phase. I usually also take ibruprofen during this phase because I get an upper backache that the IB removes, and the IB also helps with the opiate bump-pain during this adjustment phase.

I think this adjustment phase of very light WD symptoms is why a lot of people with opiate addiction assume loperamide doesn't work. They are using super low doses compared to their tolerance level- if you need 100mg of oxycodone (at once, not an OC) to get high taking 2-10mg loperamide isn't going to help you any more than 5-10 mg of oxycodone will, while those doses are completely effective for non-tolerant folks. Another note for skeptics- this 2-3 day adjustment phase is not just completing a WD. Even a couple of months into a loperamide maintenance/taper if one has to wait a few hours past the time where they'd usually take their loperamide dose WD symptoms start. Taking loperamide eliminates the oncoming WDs. Similarily, taking another opiate in the appropriate dose as the WDs come on of someone who is only on loperamide also elimates WD symptoms. The WD symptoms of loperamide use are the same as any other opiate. One note along these lines- abruptly stopping loperamide if you are maintaining on a dose like this is just as bad as an idea as stopping methadone randomly. Loperamide WD is more like methadone WD than a heroin WD because of the longer time of effect. The bulk of a heroin WD lasts like 3 days, while the bulk of a methadone or loperamide WD lasts more like 10-20 days and can be just as intense. So, if you get off something else using loperamide, don't assume you've been "cured" of your addiction and just stop- taper down. Thanks to the low dose of each pill tapering is easy as it gets.

3. On the third day, I'd take 48 mg (24 pills) and see how well it worked. If it didn't work well, I'd take another 48 mg. The adjustment phase lasted 2 days for me at first, but over the years it became longer, 3 and sometimes 4 days where I'd be taking the 96 mg dose, and then cut it.

If the 48 mg (24 pills) worked, I would maintain on that indefinately until resupply, or start tapering from there. I'm not sure why it works that way- I've got some theories about the BBB learning to allow it in, or a build up that saturates the reverse pumps, etc. Loperamide *does* cross the BBB, it just gets pumped back out. Folks have put forward quercetin as a means to saturate the pumps that push loperamide back out through the BBB (more info on this), but I can tell you that it doesn't work any batter than loperamide by itself.

One note is that if you are already a day into WDs, the loperamide worked immediately for me, no adjustment phase required. That is, I not only had no shits, but I also was completely free of WDs, feeling content but not high. If you can suffer through a day of full on, long term addiction WDs easily, I'd do so instead of taking the double dose for the first few days, it's probably better for you in a handful of ways.

Up until I quit using opiates recreationally, most of my loperamide maint periods were a couple of weeks. I got into the habit of having a loperamide maint week every 8 weeks or so to keep my tolerance down. Early on, going on loperamide for a few days cut my tolerance in half and brought back the euphoria of the honeymoon period, but toward the end of my addiction it didn't cut the tolerance all that much, but it did continue (though not as effectively) bringing back the euphoria. It was also very useful for cutting time tolerance, and the effectiveness to produce that never was diminished. That is, if I started to depend upon 2 doses a day, which means I didn't take 2 for "fun" on Fridays, but rather the 10 AM dose wore off and I was getting sick at 6 PM, requiring redose or WDs. After I started using loperamide to maintain, I've never had to dose on the tea more than once a day because I was back to being high all day long off of one dose.

Also, when I'm maintaining I still shit. Back in the day I would shit every morning before taking my loperamide dose. These days I shit whenever I need to, even if the loperamide is going full strength. I believe my ENS has a different level of tolerance to loperamide than my CNS, because only a portion of the loperamide actually makes it into my brain, but all of it is going wild on the opiate receptors in my GI tract. I shit like a normal person, once or twice a day. I still tend to take a dump in the morning before dose, but it is common for me to take on in the afternoon, even while the slight loperamide buzz is still felt and is still working. I don't ever get the runs though, even after eating/drinking something that might otherwise give me or a non-tolerant person some trouble.

There are a few other observations I've made over the years that I'll relate, but of which I never consistently tested for enough to make a scientific hypothesis about.

1. Avoid taking loperamide as a potentiator or otherwise with your usual opiate. To decrease the total amount of time I spent in the adjustment phase (which is kinda shitty, but by no means anywhere near how you feel during WD) I tried phasing in loperamide. I did this for a few times, and while the transition from morphine+loperamide to just loperamide was easier, the total usefulness of the loperamide was diminished a TON. That is, when using morphine one day and using loperamide the next I'd have a few shitty days but then be like a normal person. But when I did a mixed dose for a couple days to a week before switching to only loperamide I started off on the first day with no morphine feeling OK compared to a first day off as I outlined above, but it took A LOT longer to get to the point where I had no WD symptoms and the slight loperamide buzz, usually 10-14 days.

Furthermore, a mixed loperamide+other opiate daily regimen greatly increases your ENS (GI tract) tolerance to opiates. When I mixed them with the intent to transition to loperamide, but maybe ran out of loperamide and took just a full dose of morphine (e.g. enough to get my high) I often got the runs. Who knew, the shits on morphine? In a way this is good and bad, depending on your intention. For someone who is actually going to quit using opiates for fun it isn't a bad thing- like I said, I'm able to pass a BM even on loperamide, but in the couple of times I've run into something and used it instead of the loperamide I got diahrea a couple of times. If you are planning on staying a 'real' opiate addict, I'd avoid mixing them.

2. I've noticed too that ramping up (taking part of the dose every 15 minutes) has worked well. It's how I first noticed that it worked, actually. Doing so might help especially in the first 2-3 days in the program I outlined above, though I never conclusively determine if it did or not. I take my dose all at once and it is effective, the slight buzz included.

Side Effects: These days, I don't have any sort of side effects from the long term loperamide maintenance. I've had blood work done and everything is still healthy. Not that there might not be other long term side effects, but as with any medication it's good only to use them as long as you need it- if you are at the point where you can taper off rather than just maintain, do it. If you feel you will always need something, it might be worth your while to look into methadone just in case.

However, earlier on I did have a side effect on some of the loperamide cycles I went on, though not every time- an empty feeling in the pit of my stomach. Eating didn't resolve this. For me, it went away every time after a few days of maintenance. I never had any other sort of cramps or pain, twisting or otherwise.

The buzz? In case anyone is still wondering, the 'buzz' form loperamide is very opiate like, but way more in my head than in my body. It has a more stimulant-feeling effect than any other opiate I've used does, though my heart rate and blood pressure doesn't go up. That said, if I am tired as the dose comes off and doze off I can often fall sleep for a few hours in a nice opiated way, rather than a more usual .5-1 hour naps I would take. Sometimes when I've started a loperamide cycle I might only sleep 6 hours a night, but if daily doses are timed in a way such that I need to take it in the middle of sleep (like at 2 AM, long story), I often can't sleep well before that time, but when I take it and it comes on sleep comes back very, very easily. That said, during the day I don't feel sedated and lazy in the way that morphine or methadone makes me feel.

In conclusion...
Sorry about the long post, but I'd hate to see some kids hard up for a high taking a TON of loperamide, and either achieving that high but fucking up their digestive systems in the process. If you are someone without a signifigant tolerance and take a massive you will get constipated, maybe for 1-4 days. But taking a single huge dose will not constipate you for weeks, months, or years. You will likely get stomache cramps, but other than that you'll probably be fine, but like I said, it really isn't worth it. Abusing loperamide is the best way to get it taken off the shelves, and those of us who are using it as a methadone-like maint drug will be screwed. Do us all a favor and buy some kratom or something.

The other reason for this long post is that just as bad would be for folks with opiate addiction to miss out on one of the best ways to manage your addiction and remove it from your life when you get to that point. If it weren't for loperamide I wouldn't be off the real opiates like I am now.
 
oxycont1n said:
"When loperamide is taken by itself, it cannot readily cross the blood-brain barrier; however, when loperamide-containing nanoparticles are coated with polysorbate 80 and injected," - wikipedia.org

has anyone done this??? i would like to know how effective that is!!
yeah, i tried it.

i induced metal to thermal plasma in my underground lab, nanoparticles ere formed upon cooling while exiting the plasma region, i used a metal that binds efficiently with polysorbate 80. the loperamide was already in the metal solution before creating the nanoparticles

after injection, i felt an immediate rush, similar to hydromorphone
 
thank god malfunkshun posted in here to bring some ACTUAL FIRST HAND EXPERIENCE to this flame war. I have tried the same method he has (hell i gave him the method i was trying) and i had similar effects. GREAT for moderate wd's, not so good for getting you high. I maxed out at 100mg in one shot (by shot, i mean line). I have also read that .04% of loperamide DOES cross the BBB. I wish i had the article that stated it, but i cant locate it. It was a medical journal of some sort though.

oh yeah, stop being a retard enoughorangejuice. I know you know more than the average joe about drugs, but god. you are no better than InTheEyesOfGod in this thread. Turn off your computer, take a benzo, and when it kicks in, turn your comp back on. Stop raging cause you are dope sick or whatever
 
Even IF loperamide gets through the BBB, it won't get you high. I've read the papers and the SARs show that it's just Sooooo weak. Try lopping of that chlorine with NaBH4 then esterifying the bare -OH group. Good, now you have something about 1/5 the potency of codeine.

Folks, this stuff is OTC for a reason. A LOT of time was spent ensuring that it was NOT abusable.

If your going to go to all that trouble, you would be much better to spend your time and effort looking at other OTC stuff because there IS stuff out there that can be made fairly good...
 
^^^+1
did i ever mention that i'm a fan of Haribo1? I like his chemistry knowledge and that he is actually contributing to the topic. No sarcasm here. I wish more people would appreciate it!
 
well the problem with that, dear sir, is that hes completely full of shit, has no first hand experience with it, and is just going off his opinion. "even if it crossed the blood brain barrier it would cause effects" ?!?!?!??! what the fuck are you talking about? firstly, it does cross the bbb. secondly, it does cause effects, i belive both peripheraly and centeraly. it is documented ahs having weak mu, delta, and kapp agonism. welp, THERE you have it. oh well if its weak activity, its still there, so if you dose up enough, your going to get something. i know because i use the stuff. yesterday i ran out of my lortabs early in the day so i popped 30 mg lope. that evening i was likee "Wwiat a minute these vics are SURE lasting a long ass fukcign time and sedating the fuck out of me".............."oh wait the lope!" i was high as fuck, itching, nodding, and i know it wasnt from the 30 mg of hydro i took in the morning. t he stuff takes about 5 hours to peak, and then lasts a while. hey, if it had NO activity, then tell me why the fuck EVERYONE on this board will swear to you it eliminates wds?
i dont know everyhitn about this chemical, but i know more than you, simply because ive actualy tried it.............many times. keep up the lope discussion, this is some good shit, and very interesting.
also, "spent alot of time making sure it wasnt abusable" BULLSHIT. they were trying to make a POWERFUL opiode agonist similar to fent. it turned out that per dose this drug was jsut too weak to market as an analgesisc, and through it on the shelves as an anti-diareahl. just like opium and morphine tinctures used to be. they dont take time to make sure otc shit wont get you hihg. ever heard of robo jellies? or benzedrex inhalers? or primatines? the list goes on and on.
peace
 
But crossing the BBB but not as much as we want is what we are talking about. For some people it does cross the BBB from others, it doesn't. All we are doing is trying to get more of it to cross the bbb
 
Okay, been weening myself off of the percs, today I'm trying to go cold turkey. Am taking between 12mg and 26mg of loperamide day, keeps the sick off. I do miss the feeling of being high all the time... but I guess I'll just deal with it.
 
more experience with loperamide:

i have been off of opiates now for about 2 weeks. all of my withdrawals are completely over with. even my depression is starting to abate. i'm pretty much back to 'normal'.

now, i am a junkie. i need (want) my opiates. if it has to be loperamide, then so be it. so, lately, i've been eating it like candy. the other day i ate 100 loperamide pills, 2 mg each, all at once. 200 mg.

the effects were VERY opiate like. no euphoria yet, but by got it feels exactly like being on a medium dose of morphine. its almost the way it was when i first started doing poppy seed tea, before i crossed the 'euphoria threshold'. you have to do morphine for a few weeks before you actually get high on it.

this is what the lope feels like at such a high dose. i don't get sick at all, no stomach twisty yuckiness or anything. it is definitely 'almost' maybe RIGHT ON THE VERGE of being a good ole opiate high. i have the rubber legs, i have a feeling of lethargy but without a lack of energy or motivation. i am definitely in a better mood. my heart rate might be a little higher. i am more alert generally. in all ways 'normal', i feel fine.

now, i haven't eaten more than a hundred pills at a time. yet. i'm just wondering that if i eat enough of this, will the .04% that crosses the BBB ever actually give me a euphoric buzz. probably not but thats not going to stop me from finding out.

oh yeah. i had a helluva hard time sleeping that night too, just like when i'm on a really good dose of poppy seed tea.

this is just how it effects me personally. i don't have any trouble going to the bathroom, i dunno why, but lope basically doesn't do anything to me in that regard... well, i might go a day or two between dumps but when i do go its normal, not dry and hard or anything, just normal.

so there's an account of an extremely high dose of loperamide and what i think are its potentials. my opinion is that enough of this shit eventually WILL get you high, but its probably not a good idea for the average joe to take more than i have. i'll probably double the dose eventually and report back on that, as long as i'm not getting sick or anything... why not.
 
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haribo1 said:
Even IF loperamide gets through the BBB, it won't get you high. I've read the papers and the SARs show that it's just Sooooo weak. Try lopping of that chlorine with NaBH4 then esterifying the bare -OH group. Good, now you have something about 1/5 the potency of codeine.

Most reports of people who managed to get some Loperamide through the BBB seem to confirm what haribo1 said here:
On the alt.drugs.* message boards, there are many reports of people who managed to get some Loperamide through their BBB by:
1. taking huge amounts
2. associating with a p-gp inhibitor (there's a report of the use of Quinine for this purpose, another one with Quercetin, and a few other ones)

These people report effects similar to a very weak dose of Codeine (60mg)....
Not worth IMO...

--------

Loperamide is pumped out of the BBB by P-glycoprotein, so in order to get some Loperamide through the BBB should:
-take a few p-gp inhibitor
-AVOID p-gp ACTIVATORS!!

There are many easy to get p-gp inhibitors:
-Tangeretin, Heptamethoxyflavone, Nobiletin (all present in orange juice)
-Bergamottin (found in grapefruit juice)
-Gluconate salts (buy Magnesium, Ptassium or Calcium Gluconate)
-Quinine
-Lecithin
Most other p-gp inhibitors/substrates are RX only (Amitriptyline, antibiotics....)
Here's a complete list of them:
http://bigfoot.med.unc.edu/watkinsLab/website/intesinfo.htm

So you can inhibit p-gp by drinking a lot of orange juice, associated with lots of grapefruit juice, Quinine, Lecithin, Magnesium Gluconate +a few other p-gp inhibitors.
(be careful, inhibiting p-glycoprotein may be dangerous)

But if you want to get some Loperamide to your brain through the BBB, you absolutely have to avoid taking p-gp ACTIVATORS.
P-gp activators include:
Dexamethasone
Phenothiazines (Thorazine, Promethazine...)
St John’s Wort
Progesterone
Here's a complete list of them:
http://bigfoot.med.unc.edu/watkinsLab/website/intesinfo.htm

--------

I'm sure that:
-by taking an over-therapeutic dose of Loperamide (above 10mg-20mg)
-and by snorting it
-and by associating it with a few p-gp inhibitors
-and by avoiding p-gp activators
-and by maybe taking Cimetidine with it,
people WILL get some Loperamide through their BBB, up to their brains;
and then they might get a weak Codeine high... (which is still enjoyable, and addictive)

(I would definitely experiment this during withdrawal, if OTC Codeine wasn't so cheap, and Loperamide so expansive by comparison.....)
 
ive been off oxy for 3 weeks now just using loperamide, im down to about 20mgs a day, one thing that is underated is tagamet, ive been using that but i ran out a few days ago and now i have to take a dose every 16-18 hours instead of 24 hours.

Also I tried to stop using loperamide a few days ago since it had been 18 days since my last "real" opiate and it did cause withdrawals, all physical, not metal, this was from 25mgs of lope so im just gonna keep decreasing by 1mg a day till I can stop taking it and I deff gotta pick up some more tagamet and mabye some poppy seeds to get a nice little buzz, treat myself for making it 3 weeks.

If it werent for imodium id still be sniffin 400mgs of OC every day. Lifesaver.

edit: Jason- I used a p-gp inhibitor along with loperamide (80mgs oral and 20mgs snorted) along with cimetidine (1 gram), i forget the name of the p-gp inhibitor but it is used to help a certain HIV med cross the BBB, i took 4x the normal dose of this inhibitor but this combo did nothing to increase the effects or anything, I felt the same as if I had taken 100mgs of loperamide, i didnt take any of those p-gp activators either. So either the p-gp inhibitor was not good enough or mabye the amount that crossed was so weak I couldnt notice it ( which is very possible since i was in day 2 of withdrawals from a 4 year stint on 400+mgs of OC)

one thing I wonder about is how loperamide actually effects the brain, since it was developed to be a strong drug like fentanyl and is somewhat similar in structure to it some have suggested that if it did cross the BBB It could be very powerfull, so either this isnt true or noone has found a way to get it across in any significant amount, I think its also important to note that anyone trying this most likey already has an opiate tolerance so this could be a factor in how strong the drug is perceived to be.

very interesting stuff, I hope one day we will unlock the mysteries of loperamide heh.
 
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jasoncrest said:
I would definitely experiment this during withdrawal, if OTC Codeine wasn't so cheap, and Loperamide so expansive by comparison.....

otc codeine. yeah fuckin right. not here in the U.S. hell i'd never even fuck with loperamide if codeine was otc.

i'm working in alaska right now, maybe i'll make a trip over to canada and try out this miraculous nurofen
 
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