RoboRobot
Bluelighter
[Mod note: taking large doses of loperamide, especially in combination with potentiating agents, can be fatal and is strongly discouraged - several Bluelighters have died this way.]
Alright, so in fear, (or actual complete confidence) of sounding like an idiot kid drug-chaser (which Im not!
), I attempted to get CNS effects from Loperamide (Imodium, anti-diarrheal).
The methadone clinic was full for intake today, and feeling completely sick and w'ding from opiates (H, etc),
I purchased a bottle of 72 generic Loperamide as I heard they help, and they slightly helped me once, though I took methadone soon after so I wasnt entirely sure how much they helped.
I knew it was going to bind to my GI tract receptors, atleast, though.
Anyway, I ingested 18 of them (36mg).
I was reading more extensively on them afterwards, when I was still experiencing withdrawal symptoms, and was seeing if it was safe to dose any higher. I, of course, stumbled upon the many, many plethora of "forcing Loperamide across the BBB," threads which I was already aware that it didn't.
As I had no other means to get well, couldn't even get to the store to get poppies (and Im completely SICK of this OTC bs, I just wish I was back at the methadone clinic and/or had more money
)
Anyway, there were the thoughts that the polar area made it difficult to cross into the BBB. In further research though, it seems it DOES cross the Blood-Brain-Barrier but is then IMMEDIATELY forced out by P-GP (P-glycoprotein) , a protective function for the brain that forces out toxins among other things.
Wanting to get a CNS effect and actually get well so I can go out and get a job, I started trying to foolishly alter my BBB and inhibit my P-GP function for a certain amount of time.
Ive read quite a few experiences now of people doing that, combined with a mega-dose of Loperamide, or just a mega-dose by itself, which seemed less plausible.
As I didnt have Quinidine which is proven to inhibit P-GP, I read that Paxil (paroxetine) is a moderately strong P-GP inhibitor. I don't take paroxetine anymore, but I had some left, so I ingested 30mg of that.
To inhibit the proper liver enzymes, I injested grapefruit juice (didnt have any cimetidine/tagament). Sadly is was Ruby Red and not white.
Garlic also inhibits some of those enzymes, so I injested 3 caps of that.
Parachuted Black Pepper as that is ALSO a P-GP inhibitor.
and to top it off, and try to offset any possible nausea from untolerated use of paroxetine, I took a dose of Promethazine (which also happened to be a DXM solution, which DXM also potentiates and prevents tolerance from opiates.)
So, I thought I had a pretty good cocktail, if anything, to get this to work.
I also, of course, injested many Tums to offset the acidic-ness of the grapefruit juice as a decent amount of loperamide is destroyed in an acidic environment and more readily absorbed in a higher PH.
about 30-40 minutes later I injested 37 loperamide, equaling 74mg. If you count the earlier dose of 36mg (which was between 3-4 hours prior), I was at a total of 110mg. Though, Im guessing, to actually get CNS activity, if possible, larger doses should probably be taken together in a wishful attempt to flood the BBB more adequately.
Now, I do NOT like being a guinea pig these days, but I was so sick and had appointments today and couldnt just be w/d'ing all day.
After reading enough reports where I felt that I would be okay (and a cross of the fingers to not induce Parkinson's), and testing a moderately high dose of loperamide before hand to make sure I dont have any allergic reactions to it, I did it, in an attempt to get well.
I also know about the potential neurotoxic side-effects from loperamide, leading all the way to possible Parkinson's, as mentioned.
That would SUCK and I am not a risk-taker anymore (this doesnt count!
), but I felt the need to go ahead after reading enough reports and feeling so crappy.
It definitely DID help with my muscle cramps. I was surprised. I have/had a warm body feeling after injesting it as well. seemed like slight CNS activity. Was a world different from how I felt earlier.
BUT, I then also got very tired with a weird slight headache after 10 minutes of onset. The drowsiness Im guessing was another sign?
it wasnt a nice drowsiness though like some opiates. Anyways, I slept like 3 hours the night before, which had to be contributing to it, as well as the promethazine.
I went and laid down, and fell asleep easier than I have been while going through w/d's.
When I woke up about 3 hours later though, I felt nauseous in a weird sense, and had a headache with a spacey feeling.
Took me a little bit to recuperate and feel better, which Im feeling fine now, and not dope sick which is great.
my tolerance to opiates HAS dropped considerably though, as these last couple weeks Ive been barely scrapin' by remaining well, I know lower doses do a lot more than they used to for me.
THIS was the weird side-effect, though: After waking up and feeling crappy (but not dope sick), I had DIARRHEA.
I heard of people taking a stool softener later after taking megadoses, so I wasn't expecting this.
But yet, 3 hours after come-up, my "stool" was water. I was pretty surprised.
I mean, I know my body has adapted to opiate constipation and same with the old, "hard to pee," feeling.
Still, after eating 100mg+ of an anti-diarrheal, I didnt expect diarrhea so soon, especially because it hasnt plagued my actual wd's as fast and as bad as it usually does.
So, what do you think the diarrhea was from? Also, the crappy feeling?
Im guessing it was the big cocktail of herbs and pharmaceuticals that caused it.
probably the 30mg of paroxetine as well, for having no tolerance to it?
I assumed black pepper at first, but its actually very healthy for you.
sorry for another lope thread, I hate it too, but I thought this was worth noting as it was a weird side-effect.
As well, I guess, of confirmation of p-gp inhibitors and loperamide actually doing SOMETHING, though I dont think inhibiting p-gp all the time purposefully is a good idea and needs more clinical study and trial.
Guess you can mark me off as an unregulated trial :D
Thanks for reading and I apologize about the lengthy post and explanation!
Alright, so in fear, (or actual complete confidence) of sounding like an idiot kid drug-chaser (which Im not!

The methadone clinic was full for intake today, and feeling completely sick and w'ding from opiates (H, etc),
I purchased a bottle of 72 generic Loperamide as I heard they help, and they slightly helped me once, though I took methadone soon after so I wasnt entirely sure how much they helped.
I knew it was going to bind to my GI tract receptors, atleast, though.
Anyway, I ingested 18 of them (36mg).
I was reading more extensively on them afterwards, when I was still experiencing withdrawal symptoms, and was seeing if it was safe to dose any higher. I, of course, stumbled upon the many, many plethora of "forcing Loperamide across the BBB," threads which I was already aware that it didn't.
As I had no other means to get well, couldn't even get to the store to get poppies (and Im completely SICK of this OTC bs, I just wish I was back at the methadone clinic and/or had more money

Anyway, there were the thoughts that the polar area made it difficult to cross into the BBB. In further research though, it seems it DOES cross the Blood-Brain-Barrier but is then IMMEDIATELY forced out by P-GP (P-glycoprotein) , a protective function for the brain that forces out toxins among other things.
Wanting to get a CNS effect and actually get well so I can go out and get a job, I started trying to foolishly alter my BBB and inhibit my P-GP function for a certain amount of time.
Ive read quite a few experiences now of people doing that, combined with a mega-dose of Loperamide, or just a mega-dose by itself, which seemed less plausible.
As I didnt have Quinidine which is proven to inhibit P-GP, I read that Paxil (paroxetine) is a moderately strong P-GP inhibitor. I don't take paroxetine anymore, but I had some left, so I ingested 30mg of that.
To inhibit the proper liver enzymes, I injested grapefruit juice (didnt have any cimetidine/tagament). Sadly is was Ruby Red and not white.
Garlic also inhibits some of those enzymes, so I injested 3 caps of that.
Parachuted Black Pepper as that is ALSO a P-GP inhibitor.
and to top it off, and try to offset any possible nausea from untolerated use of paroxetine, I took a dose of Promethazine (which also happened to be a DXM solution, which DXM also potentiates and prevents tolerance from opiates.)
So, I thought I had a pretty good cocktail, if anything, to get this to work.
I also, of course, injested many Tums to offset the acidic-ness of the grapefruit juice as a decent amount of loperamide is destroyed in an acidic environment and more readily absorbed in a higher PH.
about 30-40 minutes later I injested 37 loperamide, equaling 74mg. If you count the earlier dose of 36mg (which was between 3-4 hours prior), I was at a total of 110mg. Though, Im guessing, to actually get CNS activity, if possible, larger doses should probably be taken together in a wishful attempt to flood the BBB more adequately.
Now, I do NOT like being a guinea pig these days, but I was so sick and had appointments today and couldnt just be w/d'ing all day.
After reading enough reports where I felt that I would be okay (and a cross of the fingers to not induce Parkinson's), and testing a moderately high dose of loperamide before hand to make sure I dont have any allergic reactions to it, I did it, in an attempt to get well.
I also know about the potential neurotoxic side-effects from loperamide, leading all the way to possible Parkinson's, as mentioned.
That would SUCK and I am not a risk-taker anymore (this doesnt count!

It definitely DID help with my muscle cramps. I was surprised. I have/had a warm body feeling after injesting it as well. seemed like slight CNS activity. Was a world different from how I felt earlier.
BUT, I then also got very tired with a weird slight headache after 10 minutes of onset. The drowsiness Im guessing was another sign?
it wasnt a nice drowsiness though like some opiates. Anyways, I slept like 3 hours the night before, which had to be contributing to it, as well as the promethazine.
I went and laid down, and fell asleep easier than I have been while going through w/d's.
When I woke up about 3 hours later though, I felt nauseous in a weird sense, and had a headache with a spacey feeling.
Took me a little bit to recuperate and feel better, which Im feeling fine now, and not dope sick which is great.
my tolerance to opiates HAS dropped considerably though, as these last couple weeks Ive been barely scrapin' by remaining well, I know lower doses do a lot more than they used to for me.
THIS was the weird side-effect, though: After waking up and feeling crappy (but not dope sick), I had DIARRHEA.
I heard of people taking a stool softener later after taking megadoses, so I wasn't expecting this.
But yet, 3 hours after come-up, my "stool" was water. I was pretty surprised.
I mean, I know my body has adapted to opiate constipation and same with the old, "hard to pee," feeling.
Still, after eating 100mg+ of an anti-diarrheal, I didnt expect diarrhea so soon, especially because it hasnt plagued my actual wd's as fast and as bad as it usually does.
So, what do you think the diarrhea was from? Also, the crappy feeling?
Im guessing it was the big cocktail of herbs and pharmaceuticals that caused it.
probably the 30mg of paroxetine as well, for having no tolerance to it?
I assumed black pepper at first, but its actually very healthy for you.
sorry for another lope thread, I hate it too, but I thought this was worth noting as it was a weird side-effect.
As well, I guess, of confirmation of p-gp inhibitors and loperamide actually doing SOMETHING, though I dont think inhibiting p-gp all the time purposefully is a good idea and needs more clinical study and trial.
Guess you can mark me off as an unregulated trial :D
Thanks for reading and I apologize about the lengthy post and explanation!
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