Loperamide; intranasal administration possible?

[IkBenDeMan]

I was a member of the long discussion of the thread Loperamide: the sudafed of opiates? until it got moved to the chemistry forum. I just found this article about by-passing the blood-brain-barrier, y'all should check it out:

http://www.drugdeliverytech.com/cgi-...i?idArticle=61

SWIM may have to experiment...

[Nicaine]

SWIM tried an experiment this morning (same conversation happening on another forum). He took three 2-mg loperamide tablets and dissolved in isopropyl alcohol (loperamide is freely soluble in alcohol, only slightly in H2O).

After doing a "cold alcohol extraction" he evaporated the results. He can safely say this removed 95% or better of the pill material. Snorted recently, and waiting on effects. Other than bitter drip at back of throat, SWIM notices what could be a mild opiated feeling... he's going to wait awhile to help eliminate placebo effects, but he thinks he feels something. If present, it's nothing dramatic (yet anyway)...

P.S. others may want to try the alcohol extraction technique. Simply crush the tablets and dissolve in 91-99% isopropyl, then place in refrigerator for about an hour and allow pill contents to settle to bottom. Siphon off alcohol with eye dropper onto an evaporation surface and evaporate the alcohol. Scrape up contents and insufflate. SWIM recommends no more than about 8mg to avoid the possibility of severe diarrhea and/or nausea+vomiting.

[Nicaine]

SWIM is sure enough he feels something that he's gonna hit the store & pick up some more loperamide tablets. Next time he's in kratom withdrawal will be the best time to experiment -- if it has the ability both to block withdrawal symptoms and actually produce a bit of a nod, SWIM will pronounce the experiment a definite success.

[Benga]

is there no risk of severe constipation ? loperamide - in its traditional use- is one thing swim has been staying away from for quite sometime as it is much too strong. Here it is sold in geltabs, and went from OTC to prescription to OTC again...

[Nicaine]

Probably more of a risk taking it orally, as it hits the gut directly that way (of course, intranasal intake often ends up in the stomach). But I don't see why the risk of constipation would be more severe than with opiates in general, unless an unusually high dose were taken.

[IkBenDeMan]

SWIM is fairly certain he felt something with an experiment last night too... SWINicaine and SWIM need to work on this.

[DrMuffy]

SWIdr is very interested in loperamide and has also followed the "Loperamide, sudafed of opiates" thread. He just happens to have a bottle of them, and will give this method a try tonight, sounds promising....

[DrMuffy]

UPDATE: SWIdr used the method SWInicaine mentioned above with 6 mgs of loperamide. He was left with about 10 percent of the origional pill matter (not his best extraction). He snorted two lines of the now approx. 6mgs of loperamide one after the other. He began to feel a slight buzz 10 minutes after ingestion. The effects then increased for about 20 minutes after that, and the plateau seemed to last for about 15 minutes. The effects then slowely decreased until he was back to baseline approx. 2 hours after injestion.
Overall, this experience was much like a small dose of oxycontin insufflated. SWIdr is definatly going to do some more experimenting with different methods and doses with loperamide.

[IkBenDeMan]

SWIM experienced somewhat of a ditto of SWIDr

[IkBenDeMan]

It's proven. It can't be proven that SWIM can get high from it... but thinking it must have been placebo SWIM drank tonight. SWIM usually drinks 15 beers before he's drunk. SWIM felt drunk at 5-6 as if he had taken a low dose of opiates as well (which he does often when he drinks)... something is possible here he believes, though as far as a replacement he is still skeptical...

[paranoid_android]

One thing to consider is that there is very little information on the bioavailability of loperamide HCI for insufflation. The primary mechanism by which it enters the brain is remnants of the olfactory system. However, it's worth noting that not all of the drug may be absorbed this way. This doesn't mean that only a small portion of the drug is absorbed intranasally. It is certainly possible that some enters the brain, but the majority is absorbed into the bloodstream without crossing the blood-brain barrier.

The disturbing implication of this line of logic is that the method outlined above for intranasal administration, when using around twice the theraputic dose, may cause severe constipation, especially if done often.

Still, I don't think it's a total loss. Like IkBenDeMan said, it could be very useful for potentiating other respiratory depressents such as alcohol, benzos, and other opiates. SwiPA would be very cautious about such potentiation, though. Potentiating benzos could cause dangerous respiratory depression, as could potentiating with alcohol. Opiate potentiation carries the added risk of severe constipation if my hypothesis is correct, moreso than using either alone.

[IkBenDeMan]

Originally Posted by paranoid_android

One thing to consider is that there is very little information on the bioavailability of loperamide HCI for insufflation. The primary mechanism by which it enters the brain is remnants of the olfactory system. However, it's worth noting that not all of the drug may be absorbed this way. This doesn't mean that only a small portion of the drug is absorbed intranasally. It is certainly possible that some enters the brain, but the majority is absorbed into the bloodstream without crossing the blood-brain barrier.

The disturbing implication of this line of logic is that the method outlined above for intranasal administration, when using around twice the theraputic dose, may cause severe constipation, especially if done often.

Still, I don't think it's a total loss. Like IkBenDeMan said, it could be very useful for potentiating other respiratory depressents such as alcohol, benzos, and other opiates. SwiPA would be very cautious about such potentiation, though. Potentiating benzos could cause dangerous respiratory depression, as could potentiating with alcohol. Opiate potentiation carries the added risk of severe constipation if my hypothesis is correct, moreso than using either alone.

Agreed. I'm also starting to think that the amount of the drug one would have to sniff would have to be such a high dosage that the PNS would be affected by much higher concentrations of the drug than the CNS, which would be terribly damaging to one's bowels.

[Benga]

Originally Posted by paranoid_android

One thing to consider is that there is very little information on the bioavailability of loperamide HCI for insufflation. The primary mechanism by which it enters the brain is remnants of the olfactory system. However, it's worth noting that not all of the drug may be absorbed this way. This doesn't mean that only a small portion of the drug is absorbed intranasally. It is certainly possible that some enters the brain, but the majority is absorbed into the bloodstream without crossing the blood-brain barrier.

The disturbing implication of this line of logic is that the method outlined above for intranasal administration, when using around twice the theraputic dose, may cause severe constipation, especially if done often.

Still, I don't think it's a total loss. Like IkBenDeMan said, it could be very useful for potentiating other respiratory depressents such as alcohol, benzos, and other opiates. SwiPA would be very cautious about such potentiation, though. Potentiating benzos could cause dangerous respiratory depression, as could potentiating with alcohol. Opiate potentiation carries the added risk of severe constipation if my hypothesis is correct, moreso than using either alone.

this constipation issue is quite bothering indeed... without going into details one loperamide gel can constipate swim for over 2 days... which could cause problems if more than one gel is insufflated and a significant amount ends up in swim's gi tract... ha maybe swim is a sissy but he'll stay hanging on to this thread a bit more before chopping up his imodiums

b

[Nicaine]

SWIM performed another "cold alcohol extraction" (of 8 or 10mg, forgot which) and ended up with a very small amount of highly bitter powder which in fact probably weighs what the loperamide does. In other words, he thinks this method yields nearly pure loperamide... probably 95%+ purity. For those looking to do this, just let the pill matter settle out for an hour or more... it seems only loperamide and the blue-green coloring are alcohol-soluble.

SWIM also believes he again got something of a high from it. It's on top of kratom this time, but feels significantly more potent than the kratom by itself (and the buzz feels somewhat different too, in a way difficult to describe). This is a very expensive way to merely "catch a buzz" but could really come in handy for opiate withdrawals or whatever.

Edit -- SWIM just noticed pinpoint pupils as well... he just hopes crossing with kratom won't result in any nausea/vomiting...

[Nicaine]

SWIM has not encountered any severe issues in the past few days, after insufflating loperamide a couple times. He wouldn't do it on any regular basis (or in larger amounts) and his bowels are probably a bit slower than usual, but he hasn't encountered anything really nasty like serious bloating, painful defecation or anything.

This issue is of course a valid concern, and anyone considering taking loperamide for reasons other than diarrhea should be cautious about it. Having laxatives available in case constipation occurs is probably a good idea. SWIM does not think it's anything dangerous though, unless dosage/frequency of use go well above recommended amounts. Maybe he'll end up eating his words though (and unable to poop them out? ).

[darkglobe]

Originally Posted by Nicaine

Maybe he'll end up eating his words though (and unable to poop them out? ).

Lovely! Just what one wants to read whilst eating (what was very nice) chocolate mousse.

I'm not childish at alll.... Wheeeeeeeeee.... bonk.

I've read somewhere (I forget where, apologies) that Loperamide cannot cross the blood-brain barrier as the molecule is too big (sorry chem ain't my thing) and there is a possibility of reducing it to something else. I shall try to find where I read this and post.

[paranoid_android]

Anyone considering experimenting with insufflation of loperamide would do well to heed posts about extraction. I don't know what binders are in those little pills, but SwiPA crushed about 8 mg worth and snorted it straight. In about a minute he experienced what he could only describe as a feeling of "two thousand microscopic crabs pinching the flesh on the inside of my nose".

Don't be a 'tard like SwiPA was.

[IkBenDeMan]

I like the intra-nasal thing, but would an MAOI have any affect on the passing of this drug?

[ironmics]

Originally Posted by IkBenDeMan

I like the intra-nasal thing, but would an MAOI have any affect on the passing of this drug?

No, an MAOI would definitely not help. MAOI's only work with drugs that can't enter the brain because they are broken down before they can reach it. Loperamide is not reaching the brain because it is very large, not lipid soluble, and dones't look like a precurssor. The lipid solubility is the main thing though. This is why heroin provides a much bigger rush compared to morphine since it all enters your brain at once almost and it then converted to morphine, but morphine just slowly crosses this barrier.

Anyway my point for posting is because swim tried this last night and told me about it. He took 25 mg of doxlamine because he wasn't tired and needed to be up early. About 5 minutes later he decided to tried the loperamide he extracted a couple weeks ago. He got kinda tired from the doxlamine, but then bam! opiate feelings. Whether or not it was a placebo will be found out tomorrow, but doxlamine by itself sure doesn't provide even the slightest hint of happiness and warmth he had. He tried to keep himself awake for awhile longer and succeeded for about an hour and still felt something. He just discovered benzedrex today because of this forum too! You guys are ruining him!! haha good thing he has a pretty low addiction potentional(he's gone through opiates and benzos never escalating and never needing them). He'll report back tomorrow if he tries it. Oh forgot to say but it was about the experience, swim took a perfectly healthy poop today around 2, so theres definitely no days on end of no pooping but he probably only got a few mg because his extraction stuck together somewhat.

Reputation Comments on this post:

good detailed post and some hopeful info :)

[DrMuffy]

Once again SWIdr decided to give loperamide another try. He used SWInicaines method (above) with 20 mgs of loperamide. He ended up with an approx. 70% pure batch of loperamide. He snorted about four small lines of the stuff (Approx. 8 mgs loperamide). He didn't feel much after 20 minutes so he snorted another approx. 8 mgs of loperamide and waited. He began to feel opiate-like effects within 5 minutes after the second round of lines, and the experience was moderatly short in duration. SWIdr experienced a bit of euphoria, but he did become very relaxed. Overall, this experience resembled a light/moderate dose of hydrocodone. The only bad part was that SWIdr did not have a bowl movement for almost a week afterwards (but a laxative should relieve that side-effect).

[ironmics]

I don't see why this method of ingestion should cause anymore constipation than normal opiates, since I assume it shouldn't be binding to anything other than the mu's just like normal. The mu's are reponsible for the constipation correct? Someone I know is thinking about trying it, since he's getting pretty opiate naive again. He'll have me report after he's done.

Also there is loperamide liquid, so it seems like an extraction of this would be even easier except that it might have some menthol in it afterwards.

[csharpprogrammer]

Originally Posted by Nicaine

SWIM recently mixed a couple loperamide tablets with water, then added one drop of isopropyl alcohol to help extract and disperse the loperamide throughout the solution. He would have used grain alcohol if he'd had it, but one drop of isopropyl is not enough to cause any harm. He then added this to a nasal spray bottle and snorted it.

Very minor effects, if any... SWIM is still not sure whether it's placebo or not, but he thinks it is. Stuff that doesn't cross the BBB doesn't have any CNS effects, period, end of story. Sorry guys, sort of a biological law of nature.

I'm unconvinced as well of the notion that snorting bypasses the BBB; maybe a little bit of substance could end up in cerebrospinal fluid or brain tissues, but probably not much. Perhaps a little bit getting through could help with severe opiate withdrawal, but one thing SWIM can say for sure: loperamide has no recreational value, none, zilch, zero. If SWIM felt anything, he can confidently say that 7-8 grams of kratom has perhaps a hundred times more CNS potency.

SWIM loves the idea of a legal OTC opiate probably even more than most, and the notion of getting something over on the DEA is irresistable... unfortunately, with Loperamide there's just no "there" there.

Is SWIY certain that these effects were placebo? SWIdr reports effects:

Originally Posted by DrMuffy

Once again SWIdr decided to give loperamide another try. He used SWInicaines method (above) with 20 mgs of loperamide. He ended up with an approx. 70% pure batch of loperamide. He snorted about four small lines of the stuff (Approx. 8 mgs loperamide). He didn't feel much after 20 minutes so he snorted another approx. 8 mgs of loperamide and waited. He began to feel opiate-like effects within 5 minutes after the second round of lines, and the experience was moderatly short in duration. SWIdr experienced a bit of euphoria, but he did become very relaxed. Overall, this experience resembled a light/moderate dose of hydrocodone. The only bad part was that SWIdr did not have a bowl movement for almost a week afterwards (but a laxative should relieve that side-effect).

[Nicaine]

SWIM has tried this a couple more times in small amounts, with varying effects... now he's beginning to suspect placebo (because of the variability). Unfortunately there's nothing scientific about this kind of experiment.

Loperamide has been tested pretty extensively over the years and is still sold OTC, so chances of placebo effect here are good .

[ironmics]

http://en.wikipedia.org/wiki/Loperamide
Look at the routes listing on there: Possible Insufflation. Looks like this may have been tested by others out there. Also what's wrong with placebo effects Any effects are still effects.

[Zaprenz]

Anyone interested in loperamides effects on the CNS might be interested in this publication, can't seem to attach it at the moment but the link provides pdf download.

http://www3.interscience.wiley.com/c...70150/ABSTRACT

Two studies [Niemegeers et al., 1979; Wuester and Herz, 19781 have examined the action of loperamide on the CNS upon intravenous rather than oral administration. The two studies are consistent in showing that intravenous loperamide is capable of producing opiate-like CNS activity, although the activity occurred only at doses that are equal to or only slightly lower than the lethal dose.

^Its enough to put SWIM off the idea.