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Opioids Loperamide (Immodium) Megathread: We have now lost at least 2 of our own from Lope

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Loperamide is an opioid-receptor agonist and acts on the μ-opioid receptors in **the myenteric plexus **large intestines**; **by itself it does not affect the central nervous system like other opioids.**

It works by decreasing the activity of the myenteric plexus, which, like morphine, decreases the tone of the longitudinal smooth muscles but increases tone of circular smooth muscles (anal sphincter) of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.[4]

Loperamide molecules do not cross the blood-brain barrier in significant amounts, and, thus, it has no analgesic or euphoric properties. Any that do cross the blood-brain barrier are quickly exported from the brain by P-glycoprotein (Pgp), also known as multidrug resistance protein (MDR1). Tolerance in response to long-term use has not been reported.

However, loperamide has been shown to cause a mild physical dependence during preclinical studies, specifically in mice, rats, and rhesus monkeys. **Symptoms of mild opiate withdrawal have been specifically following abrupt discontinuation of long-term therapy with loperamide.[5][6]**
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interesting what wikipedia has to say .... .... seems like loperamide is addictive ... if its addictive SOME of it must cross the bbb......
 
Free_Man** said:
interesting what wikipedia has to say .... .... seems like loperamide is addictive ... if its addictive SOME of it must cross the bbb......
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well by addictive they may mean physical dependency. and if thats the case, yes, the mu-opioid receptors in the gut can become physically dependent upon it. for example, if you're taking a ton of loperamide for coming off heroin, even after the main withdrawal symptoms subside, when you stop taking the loperamide, you'll eventually have to take that explosive crap thats been building up forever.
 
Free_Man** said:
interesting what wikipedia has to say .... .... seems like loperamide is addictive ... if its addictive SOME of it must cross the bbb......
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PHYSICAL DEPENDENCE does not equal ADDICTION. You can be physically dependent on lots of drugs that are not recreational/addictive... 2 commonly cited examples are oxymetazoline, an OTC nasal spray commonly sold as Afrin that you can develop physical dependence to within 3 days of maximum use, as well as beta blockers for hypertension.

Addiction is a biopsychosocial disease meaning it affects people physically, mentally and socially. Physical Dependence is 1 criteria for addiction (to make things confusing they use *specific drug* then dependence in the DSM-IV-TR in place of 'addiction') but a drug can fail to cause physical dependence and still be addictive and a drug can cause physical dependence and not be addictive.

Furthermore, people who take 'addictive drugs' appropriately can develop physical dependence and not be addicts. Chronic pain patients for example can take stable doses of narcotics for years and be very physically dependent but would not meet criteria for addiction... to be an opiate addict you have to meet 3 of the following criteria within a 12 month period.

-Tolerance (marked increase in amount; marked decrease in effect)
-Characteristic withdrawal symptoms; substance taken to relieve withdrawal
-Substance taken in larger amount and for longer period than intended
-Persistent desire or repeated unsuccessful attempt to quit
-Much time/activity to obtain, use, recover
-Important social, occupational, or recreational activities given up or reduced
-Use continues despite knowledge of adverse consequences (e.g., failure to fulfill role obligation, use when physically hazardous)
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I see people confuse physical dependence and addiction a lot so I wanted to clarify.
 
pallidamors said:
well by addictive they may mean physical dependency. and if thats the case, yes, the mu-opioid receptors in the gut can become physically dependent upon it. for example, if you're taking a ton of loperamide for coming off heroin, even after the main withdrawal symptoms subside, when you stop taking the loperamide, you'll eventually have to take that explosive crap thats been building up forever.
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lolz well yeah , but a lot of people (including wiki) seem to be referring to more than just that?...... i personally think taking loperamide for a high is a waste of time

but...... i still think its interesting listening to what people have to say ..... i try to stay open minded - even tho im a stubborn and opinionated MF

;)
 
Nothing in that wiki piece indicates more than straight physical dependence in the myenteric plexus. You are reading that into it.
 
Cane2theLeft said:
PHYSICAL DEPENDENCE does not equal ADDICTION. You can be physically dependent on lots of drugs that are not recreational/addictive... 2 commonly cited examples are oxymetazoline, an OTC nasal spray commonly sold as Afrin that you can develop physical dependence to within 3 days of maximum use, as well as beta blockers for hypertension.

Addiction is a biopsychosocial disease meaning it affects people physically, mentally and socially. Physical Dependence is 1 criteria for addiction (to make things confusing they use *specific drug* then dependence in the DSM-IV-TR in place of 'addiction') but a drug can fail to cause physical dependence and still be addictive and a drug can cause physical dependence and not be addictive.

Furthermore, people who take 'addictive drugs' appropriately can develop physical dependence and not be addicts. Chronic pain patients for example can take stable doses of narcotics for years and be very physically dependent but would not meet criteria for addiction... to be an opiate addict you have to meet 3 of the following criteria within a 12 month period.



I see people confuse physical dependence and addiction a lot so I wanted to clarify.
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thanks for clarifying - man ... i am aware of the difference between physicall dependence and addiction though - im just observing the possibilities at the moment
 
Cane2theLeft said:
Possibilities of what?
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the possibility that the people on here , who say that loperamide offers some relief from opiate withdrawal (i think one person even mentioned psychological relief) could be telling the truth

i mean why would they lie ? im sure they are being honest about what they say - even if it is just a subjective experience - its probably still accurate

i give them that much credit....
 
pallidamors said:
because theyre shills for whoever makes imodium?
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whats a shill please ? that one is not in urban dictionary ... its hard work keeping up with u yanks .

im guessign u mean they are trying to make immodium seem amazing - when it isnt ...
 
He meant shill as in "A person paid to endorse a product favourably, while pretending to be impartial."

I assume he was joking.

I've used loperamide for opiate withdrawal in doses that far exceed the daily maximum labeled on the box and I think it does help some beyond just the GI effects, but if it has any recreational potential that is extremely limited.

I am pretty sure the studies wikipedia mentioned weren't testing it in ridiculously high doses like some take for withdrawal and at regular doses a limited amount of physical dependence can develop and naturally the reverse of that upon cessation.
 
Cane2theLeft said:
He meant shill as in "A person paid to endorse a product favourably, while pretending to be impartial."

I assume he was joking.

I've used loperamide for opiate withdrawal in doses that far exceed the daily maximum labeled on the box and I think it does help some beyond just the GI effects, but if it has any recreational potential that is extremely limited.

I am pretty sure the studies wikipedia mentioned weren't testing it in ridiculously high doses like some take for withdrawal and at regular doses a limited amount of physical dependence can develop and naturally the reverse of that upon cessation.
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im with you on this Cane. well put. this sounds true and accurate to me. not that i ever tried loperamide as recreation - or ever used to alleviate withdrawal - except to stop dioarhea after DHC cessation... i didnt notice it stop any of the pain in my legs - or the the overwhelming depression - which made me wanna cry...
 
You have to use it in real HIGH doses to really hault WD.

Problem is then you risk getting serious side-effects, like massive stomch pain and vomiting.
 
I used to feel wd relief at even low doses. Now I believe at least part of that wad placebo. Even after taking 20mg (my highest and most desperate dose) the cramp like pain in my gut just wasn't worth it. I have heard others talk of the same experience and I can imagine how bad it could've been had I taken 100mg. In short I do not recommend anyone take more than the recommended dose.

Free man, isn't codeine and dhc OTC in the UK? If I had the option I would much rather use those if anything OTC.
 
Johnny blue said:
I used to feel wd relief at even low doses. Now I believe at least part of that wad placebo. Even after taking 20mg (my highest and most desperate dose) the cramp like pain in my gut just wasn't worth it. I have heard others talk of the same experience and I can imagine how bad it could've been had I taken 100mg. In short I do not recommend anyone take more than the recommended dose.

Free man, isn't codeine and dhc OTC in the UK? If I had the option I would much rather use those if anything OTC.
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yes dude they are OTC but only in strengths that are very low 12.8mg codeine (with 500mg apap , 200mg ibuprofen) 7.46mg for DHC (with 500mg apap)

besides i was trying to get off DHC not get back on it lol

my doc gave me loperamide to help with the shits .....
 
Free_Man** said:
the possibility that the people on here , who say that loperamide offers some relief from opiate withdrawal (i think one person even mentioned psychological relief) could be telling the truth

i mean why would they lie ? im sure they are being honest about what they say - even if it is just a subjective experience - its probably still accurate

i give them that much credit....
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I used Loperamide to successfully taper off of Suboxone a year ago. I used it for about 2 months, tapering down gradually from 48mg to 2mg, and experienced no withdrawal symptoms what-so-ever. It's nice that they come in 2mg pills because it makes it very very easy to taper down slowly and in small increments.

Would I lie about that? What would I have to gain from lying about that?

You aren't the one doubting it, but to those who are, don't judge it till you've tried it for yourself. You can read as much as you want about it, but until you see it for yourself, you won't know. It DOES work as a withdrawal aid, and it works well. As for getting high off it, it does provide some weird effects at higher doses (96mg and above). Whether you consider that a high or not is totally subjective. For me, I don't think it's a high because it's not very pleasurable, and in fact is quite uncomfortable.
 
6/7 how was the constipation from 48mg dosing compared to suboxone or your DOC before that?
 
Johnny blue said:
I used to feel wd relief at even low doses. Now I believe at least part of that wad placebo. Even after taking 20mg (my highest and most desperate dose) the cramp like pain in my gut just wasn't worth it. I have heard others talk of the same experience and I can imagine how bad it could've been had I taken 100mg. In short I do not recommend anyone take more than the recommended dose..
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I did 200mg - and that made me think my organs were failing it hurt so bad :|
 
lollerskater said:
6/7 how was the constipation from 48mg dosing compared to suboxone or your DOC before that?
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A bit more intense. Without getting too detailed, I will say that with Suboxone or my DOC (heroin) I was able to go around 18 hours after dosing, or if I had to, could mange to get some out if I put effort into it. With loperamide, the constipation was much more intense (harder to force yourself to go if need be) and lasted quite a while longer.

That said, it wasn't terrible. I was going maybe once every 36 hours (as opposed to 12 - 18 hours with Sub/Heroin), but wasn't getting much out when I did go. When I finally got down low enough, I was going more frequently. It took a few weeks to become regular again, but it did happen eventually.
 
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