Imodium (loperamide) a Cortisol Blocker?

MAxximal

MAxximal

Well-known member
Cortisol Blocking Supplements & Drugs
October 5th, 2007 by Paul Johnson

Sometimes bodybuilding supplement science comes from the most unusual places. A few days ago, someone wrote me asking about Imodium (an over the counter anti-diarrhea drug) as a potential cortisol blocker. At first I thought it was a joke, but I actually started searching around and was surprised at what I found.

What is Loperamide?

Loperamide is the active ingredient in the over the counter product Imodium(and a few other brand names). Loperamide is part of the class of opioid receptor agonists. There is no potential for drug dependance or CNS overdose as it only acts on the intestines. However, it can cause dependance and even euphoria at high doses, so caution should be taken.

Why would loperamide be applicable to bodybuilding?

During my research, I discovered study after study where loperamide reduced cortisol levels. Blocking cortisol has become a new fad in the bodybuilding and supplement industry. Cortisol is a nasty hormone and excessive levels cause muscle loss, fat gain(visceral fat), overtraining, and health problems.

Here is the summary of just one study of loperamide on cortisol levels from the Journal of Clinical Endocrinology & Metabolism in 1992.


So what does this mean in laymans terms? For most people, loperamide will lower body cortisol levels significantly. However, it won't help if you have the excessive cortisol levels due to disease cushing's disease or other medical problems of your pituitary.


Final thoughts on loperamide:

Loperamide seems to give the impression of being a potential miracle supplement for bodybuilders. But there are some serious things that will stop it from ever catching on for widespread use. The biggest problem with imodium AD is it can cause dependance and slowing down waste removal in the colon. Slowing the flow of the colon long term, by using something like imodium, would lead to increased risk of colon cancer(a very fast spreading deadly cancer) and other diseases. Not to mention it would be a very uncomfortable experience being more susceptible to constipation.

I don’t see imodium AD(loperamide) as a useful cortisol blocker for bodybuilders, at least not for consistent long term use. If it is to be used, it should only be done in recommended dosages for very short periods of time, once in a great while. Of course, also make sure you take plenty of fiber supplements during it’s use.


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This article should get around just because it will make buying imodium less embarrassing. If you buy Pepto you can tell people it's for indigestion, but Imodium is only for diarrhea, until now, "No I don't have the squirts, I'm suppressing cortisol, incidentaly I need to use the bathroom now..."
 
Its not effective ive been reading into it just to be a guinea pig for a 2 week test run... and all ive read is that it wont lower ACTH levels for a normal male...
 
Even if it were this would be a TERRIBLE idea. The fact that it causes dependence (tachyphylaxis) has bad idea written all over it. So picture having diarrhea and you treat it with an opioid and slow GI motility. Downregulating these receptors is going to have a rebound effect if using long term and guess what that means? ;)

It isn't worth blocking cortisol with these types of drugs. Cortisol can be a problem if dysregulated but it isn't typically a huge issue. SSRI's do a better job if you truly do have a dysregulated cortisol negative feedback system. But if you did you would probably be depressed and need the SSRI anyways.
 
I call Vicodin ES Immodium AD b/c either way it is like shoving a cork up your @$$ for 3 days or so.

I thought that tachyphlaxis meant tolerance, not dependence, two separate phenomena (or is it a multi-use term)? For example, lidocaine transdermal patches cause tachyphlaxis if used for more than 12 hours in a 24 hour period (I used to use them). I know that local anaesthetics are completely unrelated to opioids (including loperamide), but would you say that I was dependent on lidocaine patches if they lost their effectiveness (for some period of time) due to wearing one for too long?

I may just be mincing words, but tolerance, physical dependence, and psychological dependence are all distinct phenomena in the context of opioids (I know, you know this). Tolerance to the pain relieving effects of opioids is thought to be rare (a shock to some doctors) once an effective dose is obtained in clinical use. Further need to increase the dose usually reflects a worsening of the underlying painful condition. But physical dependence is very common with opioids (and to be expected) but not necessarily accompanied by tolerance or psychological dependence. Even at a steady-state dosage of 30-40mg of oxycodone a day for several months, which I thought was not that much, I quit taking it for 5 days (no taper...whoops) and spent the next month in physical withdrawal (wow that sucked, but I lived), even after I resumed taking it at the maximum dose every day. I tapered off slowly over the next month as my pain was minimal by then and the WD syndrome faded away.

Technically, since loperamide is an opioid, one should be able to taper off of it if they become dependent on it and not have to deal with withdrawal symptoms (like crapping 5 times a day), right? I still don't think using it would be a good idea, I am just speculating.

Also, depending on how much similarity there is between loperamide and the opioids that are more prone to cause euphoria and pain relief (like mu-agonists such as oxycodone, morphine, etc), I do know that opioids have been associated with decreased testosterone levels when used chronically. So if that holds true for loperamide, then all that theoretical cortisol suppression isn't going to do much good for you anyway.
 
dumbhick3 said:
I call Vicodin ES Immodium AD b/c either way it is like shoving a cork up your @$$ for 3 days or so.

I thought that tachyphlaxis meant tolerance, not dependence, two separate phenomena (or is it a multi-use term)? For example, lidocaine transdermal patches cause tachyphlaxis if used for more than 12 hours in a 24 hour period (I used to use them). I know that local anaesthetics are completely unrelated to opioids (including loperamide), but would you say that I was dependent on lidocaine patches if they lost their effectiveness (for some period of time) due to wearing one for too long?

I may just be mincing words, but tolerance, physical dependence, and psychological dependence are all distinct phenomena in the context of opioids (I know, you know this). Tolerance to the pain relieving effects of opioids is thought to be rare (a shock to some doctors) once an effective dose is obtained in clinical use. Further need to increase the dose usually reflects a worsening of the underlying painful condition. But physical dependence is very common with opioids (and to be expected) but not necessarily accompanied by tolerance or psychological dependence. Even at a steady-state dosage of 30-40mg of oxycodone a day for several months, which I thought was not that much, I quit taking it for 5 days (no taper...whoops) and spent the next month in physical withdrawal (wow that sucked, but I lived), even after I resumed taking it at the maximum dose every day. I tapered off slowly over the next month as my pain was minimal by then and the WD syndrome faded away.

Technically, since loperamide is an opioid, one should be able to taper off of it if they become dependent on it and not have to deal with withdrawal symptoms (like crapping 5 times a day), right? I still don't think using it would be a good idea, I am just speculating.

Also, depending on how much similarity there is between loperamide and the opioids that are more prone to cause euphoria and pain relief (like mu-agonists such as oxycodone, morphine, etc), I do know that opioids have been associated with decreased testosterone levels when used chronically. So if that holds true for loperamide, then all that theoretical cortisol suppression isn't going to do much good for you anyway.
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From a definition standpoint you are absolutely correct :). But in this case there is "more than likely" tachyphylaxis. I have seen articles both ways saying that tolerance is not an issue but it is conflicting and I just think it would be a bad idea long term using any sort of opioid.

You could taper it for sure and it is definitely recommended to but there are better ways to achieve the goals you are trying to achieve haha. I agree with dumbhick's first sentence. Also, this could be a bad idea if you develop a GI infection that you become unaware of as you would almost certainly develop problems much faster than normal as you are decreasing motility.
 
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