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Opioids Loperamide intranasal versus oral bioavailibility

M

mistman23

Greenlighter
Joined
Dec 14, 2009
Messages
19
My apologies is this has been asked and answered before...but this could prevent loperamide overdoses. What is the INTRANASAL bioavailibility of loperamide? Wikipedia reports that it is only 0.3% bioavailable orally. One would assume the nasal bioavailibility to be MUCH higher than that of oral due to by-passing first pass metabolism. Thoughts?
 
If the nasal bioavailability was just 10% it would mean snorting one pill would be like eating 30 pills...wonder if most of the OD deaths are intranasal because many people don't understand routes of administration effect bioavailability so greatly
 
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Just Don't... You will have a bowel obstruction well before you get high. Lope can cross the BBB, but it's P-Glycoprotein that pumps it out almost instantly. Therefore, only a very very very minimal amount of lope will bind with the opioid receptors in the nucleus accumbens This is why some people feel some effects from large doses, but they aren't pronounced. The only way to even possibly get high off lope is if you take a potent dose of a PGP inhibitor; doing so will also open your brain up to a world of crap too, so don't do it. I just thought that I needed to explain this so you actually know that it won't work and why it won't work from a objective scientific position.

A higher serum level of lope will cause more to cross the BBB and have more effects, but they'll still be minimal; the dose required to produce a high or something of the sort would also likely cause ileus or a bowel obstruction which is a serious issue and will cause you a ton of pain for you're below average buzz. Overall, if you're this desperate, it's time to either quit or score... Paralytic ileus can kill, there have been several deaths caused by loperamide induced paralytic ileus.

The risk is very high and the reward is minimal, this is equatable to jumping off a tall building in order to get a rush from those 3 seconds of flight only to splat on the ground.
 
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Just don't...yea I get it. Hey, I agree with everything wrote above.

BUT FOR HARM REDUCTIONS SAKE SOME PEOPLE NEED TO KNOW JUST HOW MUCH WORSE SNORTING 20 PILLS IS FOR THEM VERSUS SWALLOWING 20 PILLS!!!

10X, 20X, 70X...I have know clue exactly how much but I know damn well people are going to snort these and they need to know how many times stronger they are snorted.

Believe it or not there are people out there who will snort these thinking it will just get rid of there WDs faster than just swallowing (if it helps at all) and not even consider the bioavailibility change.
 
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Considering how toxic lope is I can not in good faith answer this question. If you can not find the information on google, then it likely doesn't exist. Stop with the lope. Shit is cardio-toxic.
 
There is another thread pointing out how lope use will disrupt your heart rythem leaving you dead without explination without knowing one was using large ammounts of lope.

Just Don't........
 
mistman23 said:
Just don't...yea I get it. Hey, I agree with everything wrote above.

BUT FOR HARM REDUCTIONS SAKE SOME PEOPLE NEED TO KNOW JUST HOW MUCH WORSE SNORTING 20 PILLS IS FOR THEM VERSUS SWALLOWING 20 PILLS!!!

10X, 20X, 70X...I have know clue exactly how much but I know damn well people are going to snort these and they need to know how many times stronger they are snorted.

Believe it or not there are people out there who will snort these thinking it will just get rid of there WDs faster than just swallowing (if it helps at all) and not even consider the bioavailibility change.
Click to expand...

No one snorts lope dude, you would be snorting 500mgs of binder, that 2mg of lope would likely drip down your throat and into your stomache.
 
I disagree pbuilder, people do. I've seen it.

People snort all kinds of pills that have a very small amount of active ingredient and a large amount of pill binder all the time...e.g. Opana IR 10mg- low bioavailibility oral (around 10 percent) and quite a bit higher nasal (40-50 percent)
 
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mistman23 said:
I disagree pbuilder, people do. I've seen it.

People snort all kinds of pills that have a very small amount of active ingredient and a large amount of pill binder all the time...e.g. Opana IR 10mg- low bioavailibility oral (around 10%) and quite a bit higher nasal (40-50%)
Click to expand...

Snorting opana is entirely different then snorting loperamide.

And snorting loperamide isn't going to do shit, it's not active because of the fact that it doesn't cross the blood brain barrier very well. It's got nothing to do with oral vs nasal having different bioavailabilities. Thats why 2mg of it can constitpate you, because its active at opiate receptors in the body itself, but not in the brain, or the cns. Unless you take mega doses, which is cardiotoxic and will likely lead to you dropping dead from sudden cardiac death.
 
Pbuilder, I am not advocating anyone snort loperamide. I know the dangers and am aware trying to get high off it is pointless! People out there need JUST need to know how much worse SNORTING them is than swallowing them! Especially if the nasal bioavailibility is MUCH, MUCH higher than the 0.3 percent ORALLY which I strongly suspect.

And it does have to do with the different bioavailibilities...20 pills oral could cause no harm, while 20 pills intranasal could kill you.
 
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mistman23 said:
Pbuilder, I am not advocating anyone snort loperamide. I know the dangers and am aware trying to get high off it is pointless! People out there need JUST need to know how much worse SNORTING them is than swallowing them! Especially if the nasal bioavailibility is MUCH, MUCH higher than the 0.3 percent ORALLY which I strongly suspect.
Click to expand...

Honestly, sounds to me like your strongly suspect it because you've been snorting loperamide...
 
No, perfectly content with my Opana script...if I'm in WD's I go to Subs.

I strongly suspect it because other opiates such as fentanyl have ultra low oral bioavailibility and much higher bioavailibility by just about any other intake method.
 
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mistman23 said:
No, perfectly content with my Opana script...if I'm in WD's I go to Subs.

I strongly suspect it because other opiates such as fentanyl have ultra low oral bioavailibility and much higher bioavailibility by just about any other intake method.
Click to expand...

But fentanyl and loperamide are completely different. Fentanyl is reasonably active orally as well. With loperamide, it's got nothing to do with bioavailability. Loperamide isn't active in the CNS because it can't cross the blood brain barrier, which I already stated. Or it can, but only in very high doses, but that doesn't change the fact that it cannot cross the blood brain barrier well at all. The route of administration won't change this.
 
mistman23 said:
I disagree pbuilder, people do. I've seen it.

People snort all kinds of pills that have a very small amount of active ingredient and a large amount of pill binder all the time...e.g. Opana IR 10mg- low bioavailibility oral (around 10 percent) and quite a bit higher nasal (40-50 percent)
Click to expand...

LOL @ comparing intranasal opana 10ir to railing a nice line of lope. Don't worry I understood your point but still lol.

Threads like this are becoming more and more annoying. Someone needs to sticky that average doc thread that just went up.
 
It's 2015 and Bluelight still has loperamide threads.
 
Loperamide has no place as a recreational substance. The effects are cardiotoxic and using it in any way other than as it's intended is asking to fuck up your body. Sure, people are going to do it anyways, but I would hope by now they at least know they're literally killing themselves by causing long term damage.

Need something legal to help with withdrawal? Buy some kratom. Buy some poppy seeds. Just please, don't ruin your organs overdosing on an anti-shit drug.
 
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