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  #1  
Old 16-01-2012, 05:19
iamamangod iamamangod is offline
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Loperamide Report

my interest in the opiate potential of loperamide was piqued on a vyvanse-induced research spree, and i decided to use swim's body for the sake of recreational research lol.

This is my experience (repeated three times in the past week or so)

two boxes 18-count loperamide 2mg tabs (only $2.18 at the mini-mart near my house) so thats 72mg. I did not consume any other drugs that day. i even abstained from my prescribed klonopin and vyvanse. I swallowed one box on an empty stomach, made some chicken and piled on the black pepper (for notations sake i also added loads of garlic, lemon pepper, and hot sauce).
The importance of this is that black pepper makes loperamide pass through the blood brain barrier. after eating the chicken i swallowed the other box's worth and about 45 minutes after i was in awe. it felt like the first time i had ever abused painkillers.
The high was comparable imho to taking about 3 oxy op 30mgs which i did about a month ago, that's the closest thing i can compare it to bc of the duration/intensity. It turned into a dope high though after about 6 hours and i was surprised at this added bonus i began nodding. All three times i have done this in similar doses, it follows the same pattern two highs-in-one, amazing painkiller high for a long long time, followed by a dope high and nodding out. I always took the loperamide on an empty stomach followed by lots of black pepper on a small meal of chicken with the other added ingredients (my eating habits are very routine lol) i would also heat soup broth and add more black pepper just to make sure i was maximizing the ability of the loperamide to cross the bbb, and i would drink this broth.

so, that's my experience. I was surprised, but loperamide impressed me.

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intriguing and detailed experience report, could use some citations
  #2  
Old 16-01-2012, 07:20
TurboGolf TurboGolf is offline
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Re: Loperamide Report

holy shit.. thats insane!! I never heard abou that before . i heard people tried loperamine to avoid withdrawals but i didn't know there was an actual way for it to pass the BBB and to gain full potentiation.. would you say if my tolerance was very good.. cuz 3 OP 30s are nothing, the OPs are very weak and I use to swallow 4 of the OP 80s to feel barely good , would you advise swallowing 2 of the packages? and there is no OD possibilities of it right?

TurboGolf added 23 Minutes and 45 Seconds later...

actuallly edit.. i think i'll just stay away from this lOl.. nvm , thanks tho

Last edited by TurboGolf; 16-01-2012 at 07:20. Reason: Automerged Doublepost
  #3  
Old 16-01-2012, 08:03
eisenheim eisenheim is offline
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Re: Loperamide Report

Anyone knows LD50 of loperamide for humans?
  #4  
Old 19-01-2012, 23:31
chibi curmudgeon Gold member chibi curmudgeon is offline
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Re: Loperamide Report

Quote:
Originally Posted by iamamangod View Post
The importance of this is that black pepper makes loperamide pass through the blood brain barrier.
I find this very hard to believe. Citation needed.
  #5  
Old 23-01-2012, 05:01
iamamangod iamamangod is offline
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Re: Loperamide Report

Quote:
Originally Posted by TurboGolf View Post
holy shit.. thats insane!! I never heard abou that before . i heard people tried loperamine to avoid withdrawals but i didn't know there was an actual way for it to pass the BBB and to gain full potentiation.. would you say if my tolerance was very good.. cuz 3 OP 30s are nothing, the OPs are very weak and I use to swallow 4 of the OP 80s to feel barely good , would you advise swallowing 2 of the packages? and there is no OD possibilities of it right?

TurboGolf added 23 Minutes and 45 Seconds later...

actuallly edit.. i think i'll just stay away from this lOl.. nvm , thanks tho
I had some tolerance I suppose, I had been hanging out with my dope fiend friends so we were iv'ing a lot, but I compared it to the ops because when I did those a few months ago I had zero tolerance for opiates. As for the ld50 and black pepper info it's all on wikipedia. also it may have been possible that I had also purchased Hylands pharms leg cramp pm OTC tablets which contain quinine I can't recall my dope friend took me on a shopping spee so we bought random things. You'll read on the wiki that quinine greatly alters loperamides ability to pass through the bbb.
  #6  
Old 23-01-2012, 18:40
chibi curmudgeon Gold member chibi curmudgeon is offline
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Re: Loperamide Report

Quote:
Originally Posted by iamamangod View Post
As for the ld50 and black pepper info it's all on wikipedia.
You didn't say exactly how much pepper you ate, but some studies I saw used 20 mg/kg of pure piperine. For the average person, that's at least 15 g of pepper, and it probably needs to be fresh.

Quote:
Originally Posted by iamamangod View Post
also it may have been possible that I had also purchased Hylands pharms leg cramp pm OTC tablets which contain quinine I can't recall my dope friend took me on a shopping spee so we bought random things. You'll read on the wiki that quinine greatly alters loperamides ability to pass through the bbb.
I would NOT play around with quinine, it can cause heart arrhythmias in significant doses.

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sound safety advice
  #7  
Old 24-01-2012, 00:32
Mindless Mindless is offline
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Re: Loperamide Report

Piperine is a human p-glycoprotein inhibitor. P-glycoprotein serves as a drug transporter and also removes or keeps out unwanted matter from the brain. Since loperamide is a substrate of p-glycoprotein, it may be that piperine could prevent or slow down it's efflux.

Quote:
Originally Posted by iamamangod View Post
. You'll read on the wiki that quinine greatly alters loperamides ability to pass through the bbb.

This is not what wikipedia actually says. The text says that drugs such as quinine or piperine could '
potentially allow loperamide to cross the blood-brain barrier' i.e. be active in the brain for long enough to work before the p-glycoprotein efflux pump removes them. Wikipedia can be a useful source of further reading, but merely saying that something is true because it's on wiki is not a valid argument. If you do see data somewhere that helps make your point, then it's better to post it (with sources) rather than saying 'look it up'. I'm more intersted your experience, what you've read, and what your opinion is based on both of these.

As far as I am aware only one drug, quinidine, has been demonstrated to permit loperamide to have any CNS effects such as respiratory depression. Piperine, taken as plain dietary black pepper, has been shown to increase the plasma concentrations of some p-glycoprotein substrates such as phenytoin, at doses as low as one gram. However, increased plasma concentrations of the p-glycoprotein substrate in question do not necessarily equate with Central Nervous System or brain activity. If I see any studies showing respiratory depression as a result of co-administration of black pepper and loperamide, I would change my opinion.
The experience of iamamangod is intriguing, but my feeling is that one report does not make a case for the effects attributed to piperine or black pepper in combination with loperamide.

If an individual were to find a drug combination that allows loperamide to exert typical opioid effects, there would be no dosing guidelines and a fatal overdose could ensue. It should also be noted that P-glycoprotein helps protect our brain and central nervous system from infection and toxicity. Inhibiting this protection could be quite risky.


I thought this thread might also be of interest.

Sources:
Increased drug delivery to the brain by P-glycoprotein inhibition
. The full document can be seen here.

Piperine, a Major Constituent of Black Pepper, Inhibits Human P-glycoprotein and CYP3A4
Rajinder K et al 2002:

http://jpet.aspetjournals.org/content/302/2/645.full


Mindless added 63 Minutes and 2 Seconds later...


Quote:
Originally Posted by eisenheim View Post
Anyone knows LD50 of loperamide for humans?

I don't think LD50 testing is applied to humans, given that LD50 means the amount required to kill 50% of the test population. I believe the LD50 of loperamide in rats has been reported at 249mg/kilo
(Pharmacological studies of loperamide, an anti-diarrheal agent. I. Effects on diarrhea induced by castor oil and prostaglandin E).

Out of 216 poison reports for loperamide there were no life-threatening symptoms and no fatalities. The range was 0.03 to 0.94 mg/kg. It should also be noted that while loperamide itself rarely causes dangerous adverse reactions, there have still been isolated deaths. Those most at risk are children, and those with hepatic impairment (who are at risk of increased toxicity due to deficits in first-pass metabolism). Signs of overdose can include sleepiness, slow breathing, drowsiness, stomach cramps, bloating and vomiting. Mega-doses of loperamide would probably increase the risk of serious adverse reactions, with or without p-glycoprotein inhibitors.

Source:
Surveillance of loperamide ingestions: an analysis of 216 poison center reports. Litovitz T et al 1997 PMID:9022646

Mindless added 106 Minutes and 23 Seconds later...

Quote:
Originally Posted by chibi curmudgeon View Post
You didn't say exactly how much pepper you ate, but some studies I saw used 20 mg/kg of pure piperine. For the average person, that's at least 15 g of pepper, and it probably needs to be fresh.
.
I'd be most grateful if you could point me in the direction of these studies. What was the effect on plasma levels, and what CNS effects were detected of the loperamide/piperine combination, including any respiratory depression?

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As ever, meticulously backed up with actual citations and evidence. Well done, Mindless!
You just saved me a load of work. Great research.

Last edited by Mindless; 31-01-2012 at 16:20. Reason: Automerged Doublepost
  #8  
Old 24-01-2012, 18:16
chibi curmudgeon Gold member chibi curmudgeon is offline
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Re: Loperamide Report

Quote:
Originally Posted by Mindless View Post
I'd be most grateful if you could point me in the direction of these studies. What was the effect on plasma levels, and what CNS effects were detected of the loperamide/piperine combination, including any respiratory depression?
I searched PubMed for some of the articles cited in the piperine wiki and looked around the related articles for others, and I vaguely recall there was some evidence of respiratory depression, albeit mild, from loperamide, with huge doses of piperine. PK effects were kind of mixed and not always significant, so....hard to extrapolate the possibility of getting high off loperamide. High doses of piperine are, however, definitely safer than quinine or quinidine.

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useful pointers on finding extra information
  #9  
Old 31-01-2012, 13:19
Mindless Mindless is offline
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Re: Loperamide Report

Thanks Chibi. I had a look at the piperine wiki and read some of the documents in the bibliography. I note that Bioperine is also available as a dietary supplement, in one case as 10mg capsules. I still can't find any citations for central nervous system effects such as respiratory depression when piperine and loperamide are used in combination, but there is anecdotal evidence of CNS effects on DF and various drug-use websites. I came across this:

These studies demonstrated that piperine is a nonspecific inhibitor of drug metabolism which shows little discrimination between different cytochrome P-450 forms (these enzymes are active in drug metabolism). Oral administration of piperine in rats strongly inhibited the hepatic AHH and UDP-glucuronyltransferase activities (both involved in the liver's metabolism of drugs). The maximal inhibition of AHH observed within 1 hr restored to normal value in 6 hr. Pretreatment with piperine prolonged hexobarbital sleeping time and zoxazolamine paralysis time in mice at half the dose of SKF-525A. These results demonstrate that piperine is a potent inhibitor of drug metabolism.”

Source: Biochemical basis of enhanced drug bioavailability by piperine: evidence that piperine is a potent inhibitor of drug metabolism. J Pharmacol Exp Ther January 1985 232:258-262

So piperine is a nonspecific inhibitor, and doesn't discriminate between cytochrome P-450 enzymes used in metabolism. It also inhibits the hepatic metabolism of drugs. I think this means that the metabolism of many drugs is inhibited by piperine. Also, piperine acts as a cytochrome inhibitor as well as a P-glycoprotein inhibitor.


Here are some quotes on the use of piperine as a bioenhancer, from a paper which contains some useful possible explanations of the pharmacokinetics involved:


A bioenhancer is an agent capable of enhancing bioavailability and bioefficacy of a particular drug with which it is combined, without any typical pharmacological activity of its own at the dose used,”

Piperine was found to increase bioavailability of different drugs ranging from 30 to 200%. Subsequent research has shown that it increases curcumin bioavailability by almost ten-fold.However it was also noted that piperine did not increase bioavailability of all drugs, while with some drugs the effect was found to be inconsistent.”

The aim of this technology is to target expensive, toxic and scarce drugs or drugs that exhibit poor bioavailability. It is interesting to note that Piperine is added in a dose of 10 mg in all formulations, irrespective of the dose of active combination.”

Piperine is derived from pepper, which has been used since time immemorial as a food condiment and which as such is a very safe food item. However, since Piperine can influence drug levels of a number of drugs, care should be taken when using with other drugs whose levels are influenced by it. It can potentiate the efficacy of drugs hence, dose reduction is required to prevent toxicity. The list is still being researched and updated.”

Pharmacokinetics

“Different mechanisms for the bioenhancer activity of piperine have been proposed including DNA receptor binding, modulation of cell signal transduction and inhibition of drug efflux pump. In general, it inhibits drug metabolizing enzymes, stimulates absorption by stimulating gut amino acid transporters, inhibits the cell pump responsible for drug elimination from cells and inhibits intestinal production of glucuronic acid, thus permitting a more active form of drug to enter the body.”

So piperine can increase the availability as well as the efficacy of some drugs, although the effects can be inconsistent with others. It can influence a number of drugs, necessitating reduction in dose to prevent toxicity. In formulations that combine piperine with other drugs, 10mg seems to be the standard dose, here's one example:

"The formulation named Risorine containing 200 mg of rifampicin, 300 mg of isoniazid (INH) and 10 mg of Piperine has already been launched in India by Cadila Pharma in November 2009. Piperine is the first and most potent bioenhancer to this date. Piperine increases bioavailability of rifampicin by about 60%. Therefore adding bioenhancer ‘Piperine’ reduces the dose of rifampicin from 450 to 200 mg. This reduces dosage, cost and toxicity of rifampicin.
"

Source: Bioenhancers: Revolutionary concept to market Navin Atal and K. L. Bedi1 J Ayurveda Integr Med. 2010 Apr-Jun; 1(2): 96–99.

There's more on the pros and cons of altering the action of p-glycoprotein here:

Inhibition or induction of P-gp by coadministered drugs or food as well as herbal constituents may result in pharmacokinetic interactions leading to unexpected toxicities or undertreatment. On the other hand, modulation of P-gp expression and/or activity may be a useful strategy to improve the pharmacological profile of anticancer P-gp substrate drugs.”

Source: Concise Review: Clinical Relevance of Drug–Drug and Herb–Drug Interactions Mediated by the ABC Transporter ABCB1 (MDR1, P-glycoprotein) Marchetti S, Mazzanti R, Beijnen JH


Piperine can be used to reduce the dose of toxic drugs while maintaining or improving the therapeutic effects. Piperine may inhibit the metabolism of loperamide (a P-glycoprotein substrate), as well as it's removal from the central nervous system and brain by P-glycoprotein efflux. There remains a potential for overdose or toxicity from loperamide if piperine is co-administered. Poly drug use or polypharmacy can lead additional risks. Many of us use more than one prescribed or recreational drug, and piperine can have a dramatic effect on some these as well. The list of drugs which may be potentiated by piperine is not complete, so there may be unknown potential adverse drug interactions.

There may be an interaction between PD-450 cytochrome inhibitors such as piperine, and Venlafaxine. Cytochrome PD-4502D6 is responsible for the metabolism of both tramadol and venlafaxine. Anyone taking venlafaxine may be more likely to experience adverse effects when combining this drug with cytochrome PD450 inhibitors.

"
there could be a potential drug–drug interaction with other medications that are metabolized via CYP450–3A4 when coadministered with venlafaxine."

Sources: Venlafaxine induces P-glycoprotein in human Caco-2 cells, M.J. Ehret, G.M. Levin, M.Narasimhan, A.Rathinavelu 2006, and Examining the Use of Tramadol Hydrochloride as an Antidepressant. The document can be seen here.


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Yet another excellent addition to the thread, as always, and meticulously backed up with evidence.
awesome findings, well formulated and backed up with sources

Last edited by Mindless; 05-02-2012 at 20:30. Reason: extra info
  #10  
Old 03-02-2012, 13:46
iamamangod iamamangod is offline
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Re: Loperamide Report

Good information here, thank you for posting everyone especially Mindless. Well I repeated the loperamide experience again, two boxes of 180count 2mg tablets, with broth that was essentially 99% black pepper and hot sauce.\
The high was similar but differed in a few ways.
1) It was extended about 1.5x the length of the previous highs, totalling about 16 hours from start to finish. ---this was most likely due bc I was not manorexic and starved like the other times, I have gained some weight with a steady habit of eating a lot of food but with less black pepper in my daily diet (which in general i use in everything bc of it's own effects but anyways)
2.) The high was not nearly as strong....it was noticeable but since I was that poor and bored/whatever, for my money, I would have grabbed dxm gel caps for 5 bucks instead if i could relive it lol. Anywhosie no quinine this time for sure. Could be a contributing factor. Will experiment when i get a)bored b)quinine and loperamide from the grocery store. And we shall see. Although I could just get some Prilosec, apparently that works too. but 'thats jkust according to wiki which as we all know is untrustworthy even though we use it for everything ' )

iamamangod added 0 Minutes and 49 Seconds later...

18-count *******
-_- lolsrybye

Last edited by iamamangod; 03-02-2012 at 13:46. Reason: Automerged Doublepost
  #11  
Old 03-02-2012, 23:34
Munnsmoke Munnsmoke is offline
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Re: Loperamide Report

Allright first time poster long time reader. I happened to have some loperamide and quinine and was interested in this thread. I was, after some searching, unable to find my bottle of hylands but did find just 2 pills of it. Each pill contains 3xHPUS of quinine. I just combined those 2 pills with 12ct of 2mg loperamide pills. I know its a smaller dosage than the 2 18ct's but thats all i had and my tolerance for opiates is fairly low. Not to mention i dont want to do any damage. Anyways ill post back with the effects, if any. just thought i'd try this out without the black pepper and sub in some quinine.
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Old 06-02-2012, 09:20
Mindless Mindless is offline
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Re: Loperamide Report

Quote:
Originally Posted by Munnsmoke View Post
2 pills of it. Each pill contains 3xHPUS of quinine. I just combined those 2 pills with 12ct of 2mg loperamide pills. I know its a smaller dosage than the 2 18ct's but thats all i had and my tolerance for opiates is fairly low. Not to mention i dont want to do any damage. Anyways ill post back with the effects, if any. just thought i'd try this out without the black pepper and sub in some quinine.
What was the total dose of quinine, and what was the total dose of loperamide, in milligrams(mg)? I'm not saying that this experiment is well-advised or safe, but I can't work out actual doses from the information above, am still curious about the outcome and hope the experience is not unpleasant or hazardous.

I have serious reservations regarding the safety of self-experimentation that involves modifying the way our bodies metabolise drugs. There is the potential for overdose and increased toxicity. This may apply to piperine, but as chibi curmudgeon says, piperine has much less potential to do harm than quinine. I'm glad you only found the two tablets. Quinine can have some unpleasant effects at best, and is highly toxic in overdose. Side effects include:

"tinnitus, hearing impairment, vertigo, headache, nausea, vomiting, abdominal pain, diarrhoea, visual disturbances (including temporary blindness), confusion; cardiovascular effects, dyspnoea; hypersensitivity reactions including angioedema, rashes, hot and flushed skin; hypoglycaemia, blood disorders, muscle weakness, and renal failure."

Loperamide is also not without adverse effects, and taking large doses increases the risk of these. At high doses it is more likely to cause gastro-intestinal problems, dizziness, skin reactions and drowsiness.

Source: British National Formulary 62 September 2011.

Mindless added 791 Minutes and 40 Seconds later...

Quote:
Originally Posted by iamamangod View Post
Although I could just get some Prilosec, apparently that works too. but 'thats jkust according to wiki which as we all know is untrustworthy even though we use it for everything'
Just a couple of points here. Prilosec (generic name Omeprazole) is mentioned in wikipedia as a p-glycoprotein inhibitor. Wikipedia does not appear to say that this drug has the potential to allow loperamide to exert Central Nervous System (CNS) effects. The fact that a drug may act as a p-glycoprotein inhibitor does not necessarily imply that it will allow the drug to have a CNS effect. I take omeprazole every day at a prescribed dose for medical reasons, and sometimes take loperamide for diarrhoea, usually just the initial dose indicated of 4mg. I have taken up to 16mg in one day. I have not felt any CNS effects, and don't fancy taking mega-doses of omeprazole to see if that works. As a proton-pump inhibitor it can have some adverse effects, including various types of gastrointestinal disturbance and headaches.

Less common problems include sleep disturbance, hepatitis, sensitivity reactions including anaphylaxis, depression, confusion, kidney disorders, and an increased potential for gastro-intestinal infections, blood disorders, hair loss, and toxic dermal necrolysis (a life-threatening skin disease). Omeprazole can also cause agitation and impotence. At low doses which have medical indications the chance of these adverse effects is probably minimal. At high doses the risk will be greatly increased.

Wikipedia is a useful source of further reading, and often helps me arrive at a preliminary and basic understanding of ideas that are new to me. It is often misinterpreted and requires careful reading like any text. I do prefer to verify and expand on what I pick up on in wikipedia. Wikipedia is not a safe way to determine usage and dosage of drugs.

Source: British National Formulary 62 September 2011

Last edited by Mindless; 06-02-2012 at 09:34. Reason: Automerged Doublepost
  #13  
Old 13-02-2012, 00:11
kenkon kenkon is offline
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Re: Loperamide Report

I don't post very often, but I performed a personal bio-assay using various doses of loperamide HCL and found the effects to be most profound following continuous low doses. The first time I ever noticed any sort of analgesia indicative of CNS depression was during Buprenorphine detox. I had tapered down from 16 to .25mgs over several months, but withdrawals were interfering with my studies. The result was what felt like an amplification at the time, producing mild opiate effects. This sparked my interest and prompted research. The second time was a massive dose of 80 mg based on anecdotal recommendations. The effects were much stronger, with a duration of almost 24 hrs. My interest now peaked, I decided to give it one more attempt, however this time I built it up in my system at doses of roughly 16 mgs/day. After 2 weeks I took a massive dose, again at 80 mg, and felt what I can only describe as a mix of vicodin and methadone. The strength of the effect was clear, powerful, and very, very long, lasting roughly 36 hours. Keep in mind I had absolutely no other opiates for several months, but also no outside influences like pgp/polysorbate 80 prep or other medications. This was a definitive experience for me, especially considering 400 2mg pills are easily purchased for $6 where I live. Just food for thought, but I think having an accumulation in the body, combined with a massive dose, allows enough to cross the BBB. I was ridiculously high.

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interesting experience report
  #14  
Old 13-02-2012, 11:18
Mindless Mindless is offline
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Re: Loperamide Report

Taking any drug at a dose which is 25 times greater than the maximum daily dose greatly increases the risk of adverse effects. The adverse effects of loperamide include:

"abdominal cramps, dizziness, drowsiness, and skin reactions including urticaria (skin rash); paralytic ileus (intestinal obstructions) and abdominal bloating also reported."

Source: British National Formulary 62 September 2011.

Last edited by Mindless; 13-02-2012 at 11:18. Reason: spacing
  #15  
Old 14-02-2012, 04:42
kenkon kenkon is offline
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Re: Loperamide Report

@Mindless, uhhhh, yeah, you posted that already. The reason I shared my experience was with regards to certain people questioning the efficacy of Loperamide HCL as a recreational drug. It works, granted there are certain prerequisites, but I simply wanted to share the information I accumulated. The effect was identical to opiate intoxication. There's a huge difference between feeling dizzy/drowsy and feeling an opiate high, all of which I am well versed. I hope you're not trying to imply that I don't know what I'm talking about. Other than a warning for those who won't read a meter-long paragraph, why the re-post? My dose was 8 mg less than the OP's, but administered under different circumstances.
  #16  
Old 14-02-2012, 15:44
Mindless Mindless is offline
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Re: Loperamide Report

Quote:
Originally Posted by kenkon View Post
@Mindless, uhhhh, yeah, you posted that already.
Apologies for the repetition, I didn't realise that I'd just put something similar in my last post. I read your report with great interest, but felt obliged to point out the risk involved in the spirit of harm reduction. I would hope that others would do the same for me if I were taking such a risk. What I have not posted yet is that loperamide should not be taken for more than five consecutive days. Taking it for longer periods also increases the chance of adverse effects.

Quote:
Originally Posted by kenkon View Post
I hope you're not trying to imply that I don't know what I'm talking about.
I did not make any comment about the validity of your experience report. How did you manage to infer that I was saying you don't know what you are talking about? My post was about the adverse effects of loperamide, nothing else was mentioned. It wasn't my intention to spark off an argument during this thread. If you're still feeling aggrieved please PM me, a thread is not the place to resolve grievances.

Thank you for your reference to polysorbate 80, which is something I've not read about. Apart from being an emulsifier and food additive, it has also been investigated for it's potential to allow loperamide to have central nervous system effects. A solution of polysorbate 80 and loperamide did produce "a much less pronounced and very short analgesia", but this was administered intravenously (to mice). If the solution were ingested, I wonder what impact the process of digestion would have? The only effective intravenous solution was formulated by incorporating loperamide into PBCA (poly(butyl cyanoacrylate) nanoparticles:

"Polysorbate 80-coated PBCA nanoparticles loaded with loperamide enabled the transport of loperamide to the brain.
"

Source: Delivery of loperamide across the blood-brain barrier with polysorbate 80-coated polybutylcyanoacrylate nanoparticles. Alyautdin RN et al 1997. PMID:9098875

Last edited by Mindless; 15-02-2012 at 23:09. Reason: extra information
  #17  
Old 17-02-2012, 23:04
Cooe Cooe is offline
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Re: Loperamide Report

SWIM's been lurking round these part's for many years now, but only now has felt the strong need to post. To all those out there who don't believe that loperamide isn't centrally active, let SWIY assure you it is, it caused SWIM to go into overdose twice, the second of which SWIM stopped breathing. SWIM's dreadful tale begins before work one day with two 48ct boxs of 2mg loperamide pills (SWIM had taken one in the past before to no ill effect), a couple tagamet (cimetidine) for liver enzyme inhibition (of pathways which lope does use), some dxm (45mg), and a few benadryl (100mg); so pretty much your standard opiate potentiators. About 3 hours later SWIM begins to feel all the tell tale signs of an opiate high coming on, and slowly but surely they do, and it just keeps building and building to the point that he's passed out in the break room, and has to have his mom come pick him up from work cause he's so fucked up (SWIM was living back at his parents house for the summer at the time). He try's to convince his mom he just took too many sleeping pills, and somehow made it down to his room and passed out. Next thing SWIM knows is he's being dragged out of bed, and forced into the car by his parents to get taken to the hospital, and he can't walk very well, can't see straight at all, is having serious communication issues, and keeps passing out. At the hospital the doctors immediately recognize that swim was in an critical opiate overdose and gave him a nice big shot of Narcan, which managed to bring him back to reality with a vengeance. Now in withdrawl and puking his guts out but alive, SWIM explains to the docs what he had done, who think that he is lying to them, saying that what he did was impossible, probably thinking he was trying to cover up heroin use or something. After an hour or so they send SWIM home, and tell his parents to keep an eye on him. After they get home, and they all go to bed, hat happens next is nothing short of a miracle. Loperamide's half-life is about 10 hours, but with the tagamet SWIY took it was much longer which meant that it was still there chilling in his system as he slept, and slowly through the night the Narcan wore off essentially causing him to "re"overdose. At the exact moment SWIM stops breathing, his mom wakes up (this is at around 4:20a.m) with the feeling that something is wrong and that she needs to go check on SWIM. She finds him blue and limp in his bed, not breathing, she then gave him mouth to mouth and calls the paramedics, whilst his dad pounded on his chest to keep his heart going till they got there and gave him another shot of Narcan and epinephrine. SWIM was in the ICU for 5 days, 4 of those on assisted breathing, it's a miracle he has no permanent brain damage, and is in fact, perfectly healthy. But the myth of loperamide having no central activity. That's busted.

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detailed and instructive post which demonstrates the risks
  #18  
Old 18-02-2012, 00:41
Mindless Mindless is offline
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Re: Loperamide Report

Hello Cooe and welcome to DF. That's a great first post, scary but highly informative.

I don't doubt that loperamide can have central nervous system effects when combined with drugs which inhibit it's metabolism or alter its pharmacokinetics. When combined with other CNS depressants, these effects would be multiplied, as would the risk of adverse reactions. Despite it's removal from the central nervous system by p-glycoprotein efflux, loperamide does appear to exert central effects in very large doses. When taken at recommended doses, loperamide does not seem to have have any central effect. Respiratory depression and failure are possible as a result of overdose. It would appear that some doctors are not aware that it is possible to overdose on loperamide, although Naloxone is a recognised treatment for loperamide overdose.

Quote:
Originally Posted by Cooe View Post
SWIM explains to the docs what he had done, who think that he is lying to them, saying that what he did was impossible, probably thinking he was trying to cover up heroin use or something.
The problem with using loperamide to achieve recreational results is that it is a potent opioid. If an individual does manage to obtain a central effect through taking mega doses, or by tweaking loperamide's pharmacokinetics, then there is a chance this could be fatal.

Quote:
Originally Posted by Cooe View Post
She finds him blue and limp in his bed, not breathing,


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Very good points. Thank you for expanding on the con's of the substance. Also your last quote that you highlighted shows the reality of the danger. Thank you for pointing that out.

Last edited by Mindless; 18-02-2012 at 13:58. Reason: spelling
  #19  
Old 22-02-2012, 06:59
kenkon kenkon is offline
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Re: Loperamide Report

@Mindless: I appreciate your objective and informative reply. You make a valid point regarding harm reduction and I misunderstood the intent of the re-post. Initially I thought you were implying the symptoms I experienced were not opiate-related, but rather an exacerbation of common side effects associated with such a large dose. I apologize for my antagonism/condescension.

On Topic: @Cooe: Thank you for sharing such a harrowing experience with the forum. This singular post underscores the efficacy of the various loperamide HCL potentiation methods I've yet to try. As it stands now, I don't think I'll ever dare.
  #20  
Old 02-03-2012, 15:14
purplereign purplereign is offline
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Re: Loperamide Report

SWIM absolutely had to try the method described using loperamide and black pepper after reading that it could produce such profound effects. SWIM must report however that there is nothing here having started at 10mg and worked up to a max of 30mg in 4 separate dosing schedules of 6-8 hours apart taken orally. SWIM followed each dose with 1g black pepper in a orange and lemon juice mixture. SWIM can only say that with the max dose SWIM experienced a light sedation followed by joint stiffness that SWIM can only compare to come down from a low dose of morphine. SWIM would advise anyone trying to do this that stomach cramps followed about 8 hrs after last ingestion lasting for 24-36 hours.

SWIM also tried the "alcohol extraction" technique of taking 30 mg of loperamide and mixing with Everclear, refrigerated and strained off, then evaporated. SWIM then mixed with 1g black pepper in a orange and lemon juice mixture. SWIM combined this with cinchona officinalis which is a homopathic form of quinine at 30mg taken orally as suggested by some. SWIM must report that this too was a bust producing no noticeable effects except the cramping about 8 hrs after last ingestion and lasting 24-36 hours.

In closing, SWIM would advise anyone thinking of trying this that the cramping is not worth the effort or the time, however without further research at higher doses SWIM cannot absolutely say this would not produce some sort of effect comparable to morphine but, as SWIM has tried all manner of opiates, SWIM understands why someone would want to "be in the know".

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good experience report
  #21  
Old 02-03-2012, 21:55
kailey_elise Gold member kailey_elise is offline
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Re: Loperamide Report

I do wonder if some people have stronger reactions to tweaking things to be able to feel lope due to, um, chromosomal differences? I don't know if it is "chromosomes" specifically, but some people don't react to, say, codeine because they lack certain liver enzymes that are commonly needed to process drugs like codeine.

Perhaps some people have too MUCH of these enzymes? That, plus inhibitors, make for stronger reactions?

Anyway, I believe I've read that, if loperamide WERE to cross the BBB, that it would be pretty fucking potent. It is most definitely best to err on the side of caution when it comes to screwing with lope recreationally - and it's not a good idea to do so at ALL.

~Kailey

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relevant safety oriented advice
  #22  
Old 18-11-2012, 00:21
c4nucKsens8tioN c4nucKsens8tioN is offline
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Re: Loperamide Report

About My Friend:

My friend is a 25y/o 150 lbs male who has extensive experience with opiates since the age 14. When my friend was 14 half of his middle finger got caught in a press brake machine while working for his father in a metal shop during summers off from school. Since then my friend has been completely consumed by opiates until my hamster was about 21-22. My friends habit got to the point of 5 30mg Roxi's a day snorted at times but would take any opiate swim could find. Hydro's, percs, tramadol, morphine, opanna, etc. At that point my friend had an expired green card (originally from Canada, living in SC) and was not allowed to work legally for almost 2 years until the government finally approved him for a new one (Thanks 9/11 terrorists for making it that much harder for the good people to get citizenship). Was probably one of the best things for my friend regardless of all the hard times, starvation, and homlessness because it got him clean. So far my friend has been clean from opiates for just over two years. He likes to have fun with Kratom when he can. At times a daily habit, others a few times a week habit. Dosages of kratom would range anywhere between 5g - 25g depending on where swim's tolerance was at.

I know this is off topic from a Lope experience but I would just like to say that Kratom can definately be a double edged sword. It helped keep me clean by keep my opiate receptors busy and allowing me to say no to perscription opiates. But with daily use you will most definately withdrawal, no doubt about it. While the withdrawals aren't nearly as bad as roxi's or tramadol per say, but any withdrawals are a bitch to deal with no matter how light or hard they are, weather your working 80 hours a week, or an "at home parent". Any addict will agree with that.

My "Lope" Experience:

One day while not being able to purchase any kratom and after reading extensive forums about Lope and actually using it myself a few years back to help with opiate withdrawals has decided to give it a shot with next to no opiate tolerance. (Yes I know kratom is similar but swim has not done any perscription opiates in almost 2 years). So my friend went out and purchased a bottle of generic lope (48 count for $3) and a box of Tagment (6 count for $2). Here is what has followed.

2:00pm - Ingested 900mg of Tagment with approximately 12 ounces of Welches Grapefruit Juice.

3:00pm - Ingested 44 2mg Lope tabs in one gulp (88mg's Total), also washed down with approximately 12 ounces of Welches Grapefruit Juice.

3:30pm - Definately feel something that isn't placebo. I repeat, NOT placebo, but I can't quite put my finger on how to explain it. Almost like someone who's taken too many tramadol in too little of a time trying to achieve a high multiple times a day. My friend most definately notice his breathing has slowed substantially. He waits a little longer...

4:15pm - My friend still feels the same as he did in the previous update. Nothing new to report. Just a feeling of disassociation and surrealness (if that's a word)


6:00pm - My friend went outside to take a walk around the neighborhood as he was tired of sitting in front of the computer for most of the day. About half way around the neighborhood my friend noticed that nice warm feeling in his stomach associated with a low-medium dose of hydrocodone. Also feeling a small amount of euphoria and mood lift.



7:16pm - Still feeling the effects, although they have somewhat tapered, they are still VERY noticeable. Very surprised by this.


Conclusion:


Very surprised by the results. As this is something that my friend doesn't suggest doing on a regular basis it is definitely a nice compromise if one was to really want an opiate experience but is unable to obtain any opiates or kratom. I will edit my post tomorrow to show how long the effects have lasted through the night.


Hope this was informative to any and all wondering about Loperamide. Stay safe everyone!

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