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  • Trip Reports Moderator: Xorkoth

(Loperamide/96 mgs) Experienced: YES, I'm high.

Here is a link to PubMed government website, which clearly notes some major complications from high dose usage, including opiate tapering.
https://www.ncbi.nlm.nih.gov/pubmed/28506439.

This substance is useful and relatively safe in therapeutic dosages usually taken for diarrhea,2-4 mg. Very high dosages causes problems that may not show up for awhile.

This is truely a substance not to play with.
 
Kind of proves my point. Every specific case pointed to in the articles connected to that link are either short term doses of 300 mg daily or more, or doses of 200 mg daily for a year or longer.
The authors speak generally about the toxicity. Then cite the actual numbers of deaths and hospitalizations(which are maybe 10% of other OTC drugs like Tylenol/APAP). Then point to specific cases of those hurt by long term high dose Loperamide.
There is a feeling shared by most people researching Loperamide that anything more than what the box says to take will certainly destroy your heart. Every case where a patient was made ill from lope use involved recless long term use in amounts that are 2 to 10 times more than what is generally believed to be toxic. And in most cases, the symptoms go away within a few days of stopping its use.

I have read several case studys where the patient was sneaking lope into the hospital. The symptoms would subside after 24 or 48 hours after the patient was admitted and then return without warning (because he/she had snuck out and ingested 200 or 400 mg) The story always ends with the patient coming clean about their use and going to counseling.

Please make no mistake. I am not advocating for the harmlessness of Loperamide. I am only pointing out that the danger doesnt lie at the 100 mg per day for a month range. Also that there is no Loperamide epidemic on the horizon, as the US FDA would have us all believe. I just want people to understand that more deaths worldwide are attributed to stampeding elephants than to Loperamide misuse. And that it is probably safe to use at a level necessary to overcome opiate withdrawals.
 
Maybe all of the nasty side effects of high dose lope come from all the clay filler in the little green pills??????
 
Here's an interesting paper on Loperamide and the hERG channel (this is actually a misnomer as the hERG gene only codes for a subunit of a potassium ion channel, but people use the term all the time)
BACKGROUND:
Loperamide (Immodium?) is indicated for symptomatic control of diarrhea. It is a μ-opioid receptor agonist, and recently has been associated with misuse and abuse. At therapeutic doses loperamide has not been associated with cardiotoxicity. However, loperamide overdose is associated with proarrhythmia and death - two effects that are likely attributable to its block of cardiac ion channels that are critical for generating action potentials. In this study, we defined loperamide-hERG channel interaction characteristics, and used a ventricular myocyte action potential model to compare loperamide's proarrhythmia propensity to twelve drugs with defined levels of clinical risk.

METHODS AND RESULTS:
Whole-cell voltage-clamp recordings were performed at 37?C on a HEK293 cell line stably expressing the hERG channel proteins, and loperamide was bath-applied to assess its effects on hERG current. Loperamide suppressed hERG current in a use- and voltage-dependent but frequency-independent manner, with a half-maximal inhibitory concentration <90nM. The onset of current suppression was concentration-dependent and appeared to follow a first-order reaction. Loperamide also altered the voltage-dependence of steady state hERG current properties. Electrophysiological data were integrated into a myocyte model that simulated dynamic drug-hERG channel interaction to estimate Torsade de Pointes risk through comparisons with reference drugs with defined clinical risk. In the context of overdose that would result in loperamide levels far exceeding those produced by therapeutic doses, loperamide is placed in the high risk category, alongside quinidine, bepridil, dofetilide, and sotalol.

CONCLUSIONS:
The combined in vitro and in silico approach provides mechanistic insight regarding the potential for loperamide to generate cardiotoxicity in overdose situations. This strategy holds promise for improving cardiac safety assessment.
https://www.ncbi.nlm.nih.gov/pubmed/28830713

So what this study tells us is, that loperamide blocks a certain channel in your heart, that's important for repolarization. Blocking this channel can result in long QT-syndrome and an arrhythmia called Torsade-de-pointes, this arrhythmia can degenerate into ventricular fibrillation and this can cause sudden death.
Moral of the story, don't use more than a few milligram.
 
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