Forcing Loperamide through the BBB

[izo]

not wanted to read through the whole thread, how much loperamide does an opiate naive person need for full effects?

 

[plumbus-nine]

Would say it'd be irresponsible to give you concrete dosage advice as this will be very variable between individuals. I for example tolerated, when opioid-naive, full 30mg of methadone - somebody else might have been killed by that.
It'll be a multitude of regular dosage, people have survived crazy high dosages, but others have died from less...

 

[Gaffy]

.... ... ... ..

Liperamide on its own is a bit like desmethoxy carf, not that strong. What Frenchies do is boil it in a mixture of 1/26th citric acid with 25/26 liperamide in pure methanol or just pharma grade desnaturalised alcohol. It becomes BBB passing and fcked up strong. Like 1/500 of a pill is a good nod

 

[prince_igor]

There's a thread by TheTripDoctor on Loperamide in Other Drugs, it seems that he found the way to enjoy Loperamide....

In the thread, it has been said that the way to feel an effect from Loperamide is to take a very large amount of it (just like GABA doesn't cross the BBB, but is taken in 1 to 5 grams doses, so a part of it goes through the BBB)

I would like to read an advanced drug discussion on this subject.

#Is it true that if you take a very large amount of a substance that doesn't cross the BBB, some of it will cross the BBB.

#If this is true, is it possible to know how many mgs Loperamide will cross the BBB if you eat 10 grams of Loperamide?

(If there's no answer to this question, do we know how many mgs GABA cross the BBB when someone eat 10 grams of GABA powder?)

Any input, info?

loperamide is a bad idea but not what I am interested in.

now gaba is this real.

well im about to drop 5g but I really think its a load of bull to be honest.

why would everyone take GHB if gaba did the trick.

personaly I think its way to polar to cross the BBB in any volume.

anyway bottoms up.

also if you want to play with loperamide acetylate it.

you would never get me to take a high dose of loperamide like some do here its crazy and is really proof that the person needs some kind of

drug canceling.

please forgive me but this is meant to be a drug harm reduction site and loperamide is the exact opposite,

Its dangerous and should not be promoted.

 

[prince_igor]

50 minutes in and I have had a slight warm flush (did not expect it) I took 5g +-10mg

warm flush is slowly leaving the body though this does not mean it crossed the BBB as it could just be the receptors in my stomach reacting with it.

not the same as GHB infact the hot flush was not the nicest though not the worst either.

will report back in a couple of hours.

 

[prince_igor]

nope warmth gone its just a reaction with the stomach I think.

no cerebral high noticed at all.

not interested in trying again its a waist of gaba.

 

[plumbus-nine]

not the same as GHB infact the hot flush was not the nicest though not the worst either.

Even with GABA entering the brain in significant amounts you wouldn't get anything like GHB because that has, besides activativating GABA-B (had to look it up, at least wiki really tells it isn't active at GABA-A. Weird.) its own glutamatergic-excitatory GHB receptor. The other pharm to activate it is an antipsychotic, ami/sulpride. They say that one in low doses enhances dopaminergic transmission because preferably hitting autoreceptors yet this might be wrong, there was little known about GHBr back then.

To get an impression of what GABA's like you could use the Sowjet pharm picamilon. It's a precursor to GABA a bit like 5-htp to 5-ht, found one pill (50mg maybe) to be relaxing, not really euphoric but I tend not to find GABAergics euphoric in general so YMMV.

Gut receptors are weirda on their own. It has been proven effective to block just peripheral NMDAr's to avoid central opioid tolerance, and proglumide also does something in the gut which reverses tolerance.

 

[prince_igor]

that makes sense.

wanted to see if it did anything and got mild effect but I do not think it really crosses the BBB.

biochem way not my thing

thankyou for looking into this and replying plumbus-nine.

 

[Xorkoth]

50 minutes in and I have had a slight warm flush (did not expect it) I took 5g +-10mg

warm flush is slowly leaving the body though this does not mean it crossed the BBB as it could just be the receptors in my stomach reacting with it.

not the same as GHB infact the hot flush was not the nicest though not the worst either.

will report back in a couple of hours.

I get a really nasty hot flash and almost like a skin rash or hives from ingesting GABA. I got a big tub, thinking it might be a mild calming thing, but it paradoxically makes my heart beat hard and fast and feels really uncomfortable.

 

[prince_igor]

thats the exact same thing I got.

its not crossing the BBB

 

[plumbus-nine]

There are feedback loops connecting the peripheral and central nervous system - maybe the body reacts to a big amount of artificial GABA with a reduction of secretion of it's own?

 

[prince_igor]

that makes sense most drugs we like to take create a change in the production of the bodies own chemicals.

I don't like it one bit though and im 100% with Xorkoth nasty hot flush I guess that would make a good name for it

hot flush.

 

[sekio]

boil it in a mixture of 1/26th citric acid with 25/26 liperamide in pure methanol or just pharma grade desnaturalised alcohol. It becomes BBB passing and fcked up strong.

loperamide would not react under those conditions, at best you might form loperamide citrate but that's still loperamide.

 

[simstim]

I read a synthesis and bioessay thread on an old synthesis forum about the acetyl ester of loperamide. The guy who synthed it and tested it claimed that the potency, high, and duration were similar to methadone. This guy died not very long after this of a stroke. Of course no one can say how much he was using acetyl-lope or if it for sure contributed to his death, but the fact that smart people have said it could be potentially neuro-toxic or form toxic metabolites make me think that esters of loperamide may not be safe enough for use. I used to fantasize about trying other esters due to acetic anhydride being watched. Theoretically other esters should retain activity. Having access to other more commonly used opioids makes the idea of something untested and potentially damaging like loperamide esters a lot less attractive.

 

[Xorkoth]

Loperamide is sketchy, it certainly works to diminish opioid withdrawal symptoms, peripherally, but in high doses it causes long QT syndrome and chronic usage can cause life-threatening problems (as is evidenced by a classic thread in Trip Reports that went on for years in which several members either died or almost died, or reported loved ones as having done so). I don't think trying to get it to cross the BBB is a good idea at all. As it stands, it's good for preventing diarrhea, or in larger doses of 40mg or so, suppressing a good portion of opioid withdrawal for ~24 hours. I have used it for that quite a lot of times over the years, and I hesitate to do so because of how intensely it dries my mucous membranes/insides, it reliably gives me pain in my esophagus when swallowing that is very unpleasant and even alarming at times.

Loperamide is not a good candidate for getting high. It is an option for short-term withdrawal relief, and that's it. Or, of course, what it is sold for.

 

[prince_igor]

for sure Xorkoth.

its discussion should be put in the im drinking bleach section of this place.

oh ye we don't promote that shit so why lop is is beyond me.

edit:

I am talking about getting the mind effects of the drug through high dosage not using it to help you ease the stomach and bum problems of withdrawal.

but even for withdrawing it should only be used to stop these body problems and not the actual withdrawal.

its just too dangerous as when you are in pain and you do use it and it works you will up the dose in seconds as your desperate.

viscous circle.

 

[Gaz_hmmmm]

Let's pretend it passed the BBB in small doses, like in certain breeds of dogs.
Would it be worse health wise using it long-term than using long-term at the same doses as it is for IBS?

 

[izo]

I read that around 80mg are needed for an opioid naive person but I doubt it’s worth it.

 

[Skorpio]

Let's pretend it passed the BBB in small doses, like in certain breeds of dogs.
Would it be worse health wise using it long-term than using long-term at the same doses as it is for IBS?

Likely not. The two big risks of loperamide are its hERG channel inhibition (which becomes more and more deadly as the dose increases), and its dose response curve, which is very shallow until PGP is overwhelmed, then becomes as steep as any other similar full agonist. Because nobody knows where that inflection point is for them (and it likely varies with the concentration of other PGP substrates floating around), dosing a "sweet spot" is quite difficult.

If PGP were fully unable to pump out lope, the dose response curve would only have the steep portion allowing for simpler titration. The overdose risk would be comparable to demerol or methadone

 

[negrogesic]

Unfortunately, I have tried doing this various times, with 500-750mg quinine and 60-100mg loperamide, as well as 300mg and 450mg quinidine (quinidex ) with 80mg and 70mg of loperamide respectively. Bottom line: i felt very little, and what I did (the 450mg quinidine + 70mg loperamide was most noticable) was extremely shitty in quality. This is incredibly stupid, and anways, when loperamide is forced across, the effects are very dirty.

Well this was a blast from the past (was made over a decade ago).

I was just speaking to someone the other day who ordered something like a kilogram of loperamide from india to use as an opioid maintenance drug, they said they fill an OO sized capsule with it and consume it every other day. Terrible idea.

Once again, loperamide at very high doses has a high but it isn't a good one. Closest I could describe it is a very long lasting meperidine.