loperamide 48mg/gabapentin 600mg/omeprazole 60mg - Experienced: will this work?

[Vexanize]

Hi, I have done many tests with drugs before, so myself doing something this far out there doesn't surprise me. so I was wondering since Loperamide cannot cross the blood brain barrier unless taken in insane dosages, if gabapentin, a potentiate of opiates, would help allow this non-psychoactive opiate to cross the blood brain barrier. Will this work? All answers are appreciated, I understand if you want to call bs, but I've seen many promising studies on this combining this potentiates of opiods. Most reports I have read up on use omeprazole by itself, and they say that has proven ineffective.

 

[truenamebrand]

Do you have a pharmacological basis for gabapentin being a potentiator of opioids, and therefore a tool in enabling the lope to better penetrate the BBB? Because gabapentin potentiating opioids is purely subjective as far as I know, and for me personally, it actually blocks the effects of opioids.

 

[Lorne???]

No, gabapentin isn't going to help lope penetrate the CNS, by any mechanism I've came across - and honestly, you don't really want lope crossing the BBB, certainly not
in large enough amounts to linger

As far as potentiating, cimetidine snfar superior, and grapefruit juice and cimetidine is the best combo- Tgis will pretty much exponentially increase the amount of loperamide absorbed from GI tract into blood stream; we are talking, as a random(yet realistic) number) 10-15x plasma levels.

Lope is it be be played with. An addict who is desperate can take reasonable doses to help WD; the fact you have gapapentin, well known for treating RLS, and good for opioid wd in general (usually (m) should be enough, with a bit of lope to take the edge off

If your trying to get a buzz from a neurotoxic drug, that the body goes through great measures to keep out of the CNS(even if small amounts enter, they are pushed back by pgp; it would take a moderate-large amount, not to mention without a decent 3A4 inhibitor(s), the BA% is atrocious, less than ~5% average (less than 1% according to some sources, though that would make it undetectable, pretty much) OP, if this is an ill advised experiment, or are you in wd? Answer knowing that the consuqences of casually playing with this stuff are far worse than one would imagine. Note that gabapentin is hit or miss, though would stick with that, if it works for you. An answer would be useful, though in any case, please be careful, and MAKE NO ATTEMPT TO CATCH A BUZZ FROM LOPERAMIDE; it won't work unless you know what you are doing, it isn't worth it, and it's dangerous, and even lethal- H is risky, trying Loperamide just because is absurd (using a procedure to treat opioid wd is a bit different) And again, forget Omeprazole, Cimetidine is superior, though Pure Grapefruit Juice (preferably white) is best- also experimenting with gabapentin has to be done in a certain way, because of BA% issues and also what effects it may or may not have on you

Thats a lot of info, though necessary IMO

 

[truenamebrand]

^ Well said.

 

[Lorne???]

^ Thank You

 

[Vexanize]

i just took shrooms and ketamine last night instead, i dont even remember much but extreme hallucinations and dissociation, time distortion, everything was so euphoric, i felt like i was falling infinitely. It was the best trip ive ever had. psilocybin is probably my new favorite drug besides LSD

 

[Vexanize]

it enhances almost everything for me, especially hallucinogens

 

[GQ_chill]

Loperamide Possibility

Loperamide is a substrate (underlying layer or substance) for P-glycoprotein, the efflux membrane transporter in the blood-brain-barrier (bbb). Even though Loperamide is a potent mu-opioid receptor agonist and is highly lipophilic (combines with or dissolves in lipids &/or fats) it is actively excluded from the CNS.
P-glycoprotein (P-gp) is THE important protein of the human cell membrane vis-a-vis Loperamide. Why? 2 important reasons:
1. It pumps many foreign substances like Loperamide (hence the reason why Loperamide is a substrate of P-gp) out of cells.
a) In Liver cells, P-gp pumps toxins and/or drugs into bile ducts.
b) In the relevant cells of the Kidney, P-gp pumps Loperamide into the urinary filtrate of said cells (proximal tubule cells).
c) In the interior Capillary cells that interface with circulating blood and the cells of the bbb, P-gp pumps Loperamide back into the capillaries.
2. P-gp is extensively distributed in the intestinal epithelium, only a fraction of ingested Loperamide reaches the GI tract. Here, Loperamide is pumped right back into the intestinal lumen (the inside space of a tube) by P-gp. Thus, when Loperamide reaches the intestinal wall, it is in an infinite absorption and extraction cycle and Loperamide it has no where else to go once it reaches the gut wall.

As a result, Loperamide is almost completely extracted and metabolized as explained in 1. a)-c) above and acts only peripherally.

Because Gabapentin crosses the bbb and enters the CNS you have the right idea. Because Gaba has a low lipophilcity (poor ability to dissolve in fats & lipids), it requires active transport across the bbb. The large neutral amino acid transporter (LAT1) absorbs Gaba in the intestines & actively transports it across to the brain.

If only Loperamide was prevalent in the GI tract, had a high lipophilcity, and needed a way around the efflux pump of G-pg . . . Wait! What!?