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Opioids Loperamide and P-glycoprotein modulator (omeprazole) in opioid detoxification

saiconoclast said:
Interesting and very promising case study using loperamide and omeprazole in opiate WD.

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Lansoprazole (Works the same way as omeprazole aka is a proton pump inhibito.) is also a P-glycoprotein modulator and I assume pantoprazole is too.

I read the study but it doesn't say when to take the loperamide, if you should take it at the exact same time as the PPI or if you should or can take it later.

Also I'm regards to the scores regarding the withdrawal severity, I'd assume loperamide by itself would lower withdrawal a little such as stopping diarrhoea, especially at the very small doses used in the study.
 
Gaz_hmmmm said:
Lansoprazole (Works the same way as omeprazole aka is a proton pump inhibito.) is also a P-glycoprotein modulator and I assume pantoprazole is too.

I read the study but it doesn't say when to take the loperamide, if you should take it at the exact same time as the PPI or if you should or can take it later.

Also I'm regards to the scores regarding the withdrawal severity, I'd assume loperamide by itself would lower withdrawal a little such as stopping diarrhoea, especially at the very small doses used in the study.
Click to expand...
I take from the conclusion where it says some like '[the two] taken together allows lope to cross the BBB.' that they should be taken together. I'm on day 2 of this test myself. Will report.
 
Loperamide is a P-glycoprotein substrate, which is a cheap, widely available, over-the-counter drug that acts primarily in the gastrointestinal tissues to treat diarrhoea. It was reported that if used in larger than recommended doses it can penetrate the blood brain barrier and have methadone-like effect. Furthermore, it has been reported that loperamide has been used among users of opioids to manage opioids discontinuation symptoms.8 Loperamide is a phenylpiperidine derivative and μ-opioid receptor agonist, does not readily cross the blood-brain barrier and thus has minimal impact on the central nervous system. As it is a P-glycoprotein substrate, co-administering it with a P-glycoprotein inhibitor such as omeprazole (a proton pump inhibitor) would support breaching this barrier, converting it from a peripherally-acting μ-opioid receptor agonist to treat diarrhoea to a central-acting opioid agonist that reduces the full spectrum of opioid withdrawal manifestations.9
 
Update.

Took 410mg codeine Tuesday afternoon, it's now Monday morning. Been on 30mg lanzo and 2mg lope three times a day (6mg lope the first two doses). Withdrawal nothing like I've had before. Almost nothing. Sleep isn't great, but no diarrhea, no nose running, almost no rls at night. Mentally much better than previous WD.

Try it.
 
At interpreting the chart, am i correct the combo of:

Loperamide & Omeprazole with add-on 200 mg Quetiapine
C.O.W.S. 2-1-1 and,
Loperamide & Omeprazole with add-on 200 mg Quetiapine & Escitralopam
C.O.W.S. 3-1-0

These two seem most effective, if i interpret it correct ?
 
I have pantoprazole and will buy loperamide and try it.

I reduced my doses rapidly, with help of pregabaline, alprazolam, modafinil and sometimes mirtazapine.
 
emkee_reinvented said:
At interpreting the chart, am i correct the combo of:

Loperamide & Omeprazole with add-on 200 mg Quetiapine
C.O.W.S. 2-1-1 and,
Loperamide & Omeprazole with add-on 200 mg Quetiapine & Escitralopam
C.O.W.S. 3-1-0

These two seem most effective, if i interpret it correct ?
Click to expand...
I'd say.

My sleep is the only aspect really that isn't being made good.
 
Yes this all pretty much lines up with what we know about Loperamide (Immodium) and its use with P-Glycoprotein Modulators like Omeprazole (Prilosec). We used to talk with much greater frequency regarding Loperamide here on the forums. It was years ago now that it came into clear focus that the drug's usage in high dosages is inherently cardiotoxic. We started seeing deaths in scenarios that at first seemed random but with time became clear; people dead with no apparent cause, Loperamide present at site of death or in the blood of the deceased etc. (Loperamide is dangerous without using PGP inhibitors, I want to make that completely clear).

For this reason, we have taken to advising against Loperamide's usage in this fashion completely. We understand people will do it. If you need to, use this once or twice in your life to bail you out of some serious shit. It's the ones who decide that Loperamide is now going to be their daily fix that are at highest risk. Please be careful guys.
 
Keif' Richards said:
Yes this all pretty much lines up with what we know about Loperamide (Immodium) and its use with P-Glycoprotein Modulators like Omeprazole (Prilosec). We used to talk with much greater frequency regarding Loperamide here on the forums. It was years ago now that it came into clear focus that the drug's usage in high dosages is inherently cardiotoxic. We started seeing deaths in scenarios that at first seemed random but with time became clear; people dead with no apparent cause, Loperamide present at site of death or in the blood of the deceased etc. (Loperamide is dangerous without using PGP inhibitors, I want to make that completely clear).

For this reason, we have taken to advising against Loperamide's usage in this fashion completely. We understand people will do it. If you need to, use this once or twice in your life to bail you out of some serious shit. It's the ones who decide that Loperamide is now going to be their daily fix that are at highest risk. Please be careful guys.
Click to expand...

What does cardiotoxic actually mean? Does it irreversibly damage the heart muscles or does it just make it pump incorrectly?
 
saiconoclast said:
Interesting and very promising case study using loperamide and omeprazole in opiate WD.

Click to expand...
Honestly that paper is really suspicious.
Their protocol is 3X daily loperamide 2 mg and 1 20 mg omeprazole per day. Doesn’t seem like a lot.

More worrying are the drug doses of the case study patients. The people who were addicted to heroin all were reported to be doing >1 gram per day. The people who were addicted to morphine were reported to be doing 0.5-5 mg per day.

None of the patients were reported to have a severe withdrawal score, and everybody had very much stabilized by the end of the week or treatment. This seems an outsized effect for the amount of loperamide used.

All taken together (and including the niche journal I’ve never heard of publishing it), I really don’t trust the findings in this paper.

evo4ever said:
What does cardiotoxic actually mean? Does it irreversibly damage the heart muscles or does it just make it pump incorrectly?
Click to expand...
It blocks a cardiac potassium channel known as the hERG channel at high doses. This can throw the heart into a type of ventricular tachycardia called torsades de pointes, where the heart muscle quivers rapidly but doesn’t fully contract enough to pump blood. This often develops into cardiac arrest, but can also cause damage from starving the heart muscle of oxygenated blood.
 
I know about the high dosage danger of Lope. Under 10mg a day isn't a high dose.

I was sceptical. I understand the dosage seems small, but I wasn't as heavy a user as those claimed in the study. I was on holiday with no opi access and CT'd ~400mg a day codeine following the study regimen, and apart from pretty shitty sleep, had next to none of the usual WD. YMMV. It worked on around a 8.5/10 rating for me.
 
Skorpio said:
Honestly that paper is really suspicious.
Their protocol is 3X daily loperamide 2 mg and 1 20 mg omeprazole per day. Doesn’t seem like a lot.

More worrying are the drug doses of the case study patients. The people who were addicted to heroin all were reported to be doing >1 gram per day. The people who were addicted to morphine were reported to be doing 0.5-5 mg per day.

None of the patients were reported to have a severe withdrawal score, and everybody had very much stabilized by the end of the week or treatment. This seems an outsized effect for the amount of loperamide used.

All taken together (and including the niche journal I’ve never heard of publishing it), I really don’t trust the findings in this paper.


It blocks a cardiac potassium channel known as the hERG channel at high doses. This can throw the heart into a type of ventricular tachycardia called torsades de pointes, where the heart muscle quivers rapidly but doesn’t fully contract enough to pump blood. This often develops into cardiac arrest, but can also cause damage from starving the heart muscle of oxygenated blood.
Click to expand...

When this happens can you feel it? Or do you just drop dead without knowing?
 
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