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Thread: Loperamide and Crossing the Blood Brain Barrier

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    Loperamide and Crossing the Blood Brain Barrier 
    #1
    Bluelighter sweethome's Avatar
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    I apologize for contributing to the excessive threads about loperamide but I had a specific question. I'm not someone who 'swears' by this drug but I think it's helpful for W/Ds.

    I've read a few reports and a couple BL threads where quercetin is mentioned in combination with loperamide to helping it cross the BBB. One person on here said it gave him a "dirty high".

    Is there any truth to this? Does ingesting quercetin prior to loperamide help it cross the BBB or is this just speculation?
    Last edited by nuke; 15-04-2009 at 17:45.
     

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    #2
    AFAIK, quercetin isn't a P-gp inhibitor (would make loperamide cross the BBB). So, probably speculation.

    It is a potent inhibitor of some enzymes though, so it might be a good potentiator. Well, according to wiki, I'll check the sources when I feel like using my crappy internet with journal access.
     

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    #3
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    protein-pump inhibitors like prilosec are good to use too
     

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    lopramide and prilosec - an otc opiate combo??? 
    #4
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    Question
    wikipedia says you need a protein-pump inhibitor to make loperamide
    cross the BBB and become a recreational opiate - prilosec is a PPI...

    so $20 could buy you a good time????
     

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    #5
    Well, messing with P-gp (what the proton pump inhibitor actually affects to make loperamide centrally active) is a terrible idea. Not to mention the fact that most people have reported not liking the loperamide high.

    So yes, you could. And you could also use $20 to buy 5 boxes of diphenhydramine

    edit: And are proton pump inhibitors actually P-gp inhibitors? I saw that sentence on wiki, but it didn't have a citation. I have a list of some P-gp modulators, but I don't think it's a complete list.
     

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    #6
    Well, obviously taking Omeprazole doesn't have serious consequences. Omeprazole + Loperamide might, however.

    Just look at the toxicity seen when loperamide is administered to children without formed BBB.
     

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    #7
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    Quote Originally Posted by Sturnam View Post
    Well, messing with P-gp (what the proton pump inhibitor actually affects to make loperamide centrally active) is a terrible idea. Not to mention the fact that most people have reported not liking the loperamide high.

    So yes, you could. And you could also use $20 to buy 5 boxes of diphenhydramine
    ugh...diph makes me sick. dextromorphthan is better
     

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    #9
    Quote Originally Posted by robcypher View Post
    ugh...diph makes me sick. dextromorphthan is better
    meh, i dont know....i prefer chemicals which exist
     

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    #10
    So it is. Quercetin does seem a little strange. Although I'm mostly interested in the mitochondrial strengthening property.

    Apparently there was a study done in humans which should be written up sometime this year. So far it has seemed to work pretty well for the mice, and it's quite cheap.
     

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    #11
    Bluelighter Tsukasa's Avatar
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    I have tried every otc substance that helps stuff cross the BBB, including quercetin and vitamin C both in high doses. I haven't noticed much of a difference from taking immodium alone. All i get is peripheral effects, but no significant euphoria. Quercetin however has some good synergy with opioids, by acting as anti-histamine and anti-nociceptive.
     

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    #12
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    Quote Originally Posted by daddysgone View Post
    meh, i dont know....i prefer chemicals which exist
    perhaps he means dextromethorphan. I think I would take 7-hydroxymtragynine if I were lookin for a cheap legal opiatesque high. I would much prefer it to DXM. OTC meds in America make baby jesus cry.
     

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    #13
    Bluelighter sweethome's Avatar
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    Well, I decided to be the test dummy and give this combo a shot just to see. I didn't expect anything which was good because I took 80mgs of prilosec then the loperamide about 45 mins after.
    Results:
    Nada.... just the same.
    I'm giving up on any thoughts that the loperamide may cross the BBB. I think it's a reality we'll all just need to accept.
     

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    #14
    Quote Originally Posted by robatussin View Post
    perhaps he means dextromethorphan. I think I would take 7-hydroxymtragynine if I were lookin for a cheap legal opiatesque high. I would much prefer it to DXM. OTC meds in America make baby jesus cry.
    legal and opiatesque....yes
    cheap......HELL NO

    if u are indeed talking about pure 7 hydroxymitragynine and not kratom in general, it is prohibitively expensive. u can get a decent opioid-like experience from plain old bali leaf for a low cost, but once u start with the pure isolates and extracts. kratom becomes absurdly expensive.

    Additionally, despite the current prevailing opinion that 7-OHM is the alkaloid responsible for the majority of kratom's effects, my experience and the experience of many others is that pure 7-OHM provides a very incomplete and tame kratom experience. Even large doses of 7-OHM are not nearly as opioid like as just moderate doses of plain leaf.
    It seems that even though on paper, 7-OHM SHOULD provide an opioid like experience, clearly the many other alkaloids in kratom leaf make for a much more opioid like effect then when dealing with 7-OHM alone.
     

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    #15
    ...this was discussed to death.

    In short, my 2 cents on this topic:

    Trying to make loperamide cross the BBB is not worth the effort. First, most experiments in this direction simply fail. Second, loperamide is suspected to get metabolized in MPP+-like derivatives; something you definitively don't want in your brain. Third, disabling pGP is a baaad idea. The BBB serves a well defined purpose and turning off this said purpose is downright stupid...

    - Murphy
     

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    #16
    Bluelighter Tsukasa's Avatar
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    polysorbate 80, a common ingredient in icecream is supposed to make loperamide cross the BBB. Forgot to mentioon that.
     

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    #17
    Yeah, mix your loperamide with icecream and get high. Another retarded thread on ADD. Mods, please move to BDD.
     

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    #18
    Quote Originally Posted by Tsukasa View Post
    polysorbate 80, a common ingredient in icecream is supposed to make loperamide cross the BBB. Forgot to mentioon that.
    Talk about a total misunderstanding.

    Polysorbate 80 coated PBCA nanoparticles allow it to get into the brain. Uncoated particles do not get through.

    Polysorbate 80-Loperamide solution results in very weak and very short duration analgesia.

    So, yeah, IVing a loperamide-polysorbate 80 solution may have benefits in completely drug naive people, but it's awfully unlikely to be of any use for 99% of the population who would consider doing such a thing (unless you're a total newb who wants to go straight to IVing drugs).

    This will not work for oral administration, so I dunno what the hell the icecream reference matters. You'd have to be narutokun to IV an icecream loperamide solution for fuck's sake.
     

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    #19
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    OMG, When will this EVER end???
     

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    #20
    I think I'm going to just merge all the other threads about this into one when I get a chance. There are a lot. Depending if most of it lies within OD, I may send it there.
     

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    #21
    Bluelighter Tsukasa's Avatar
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    Quote Originally Posted by Hammilton View Post
    Talk about a total misunderstanding.

    Polysorbate 80 coated PBCA nanoparticles allow it to get into the brain. Uncoated particles do not get through.

    Polysorbate 80-Loperamide solution results in very weak and very short duration analgesia.

    So, yeah, IVing a loperamide-polysorbate 80 solution may have benefits in completely drug naive people, but it's awfully unlikely to be of any use for 99% of the population who would consider doing such a thing (unless you're a total newb who wants to go straight to IVing drugs).

    This will not work for oral administration, so I dunno what the hell the icecream reference matters. You'd have to be narutokun to IV an icecream loperamide solution for fuck's sake.
    The icecream i thought i'd just add as an interesting fact. but yea, I know both drugs would have to be IV'd to work.

    btw i've heard of some people adding large doses of loperamide (around 100mg's a day) with their narcotic analgesic regimen for extra analgesia for a while. If it really does work for them, then maybe if IV'd with polysorbate 80, it would reduce their required dose to a more affordable amount. Many people also report

    A personal experience of mine. One evening I found a bunch of immodium. Tried a small amount along with some vitamin C, quercetin, and gingko biloba, which supposedly help a little with drugs crossing BBB. I didn't feel anything... until the next morning. I woke up, went outside to take out the trash and noticed I had a mild opiate buzz going, which was totally unexpected. It wasn't even a large dose. Was only like 4mg's. Not something i'd try again unless it was free though and I had nothing better. It was pretty weak (but very noticeable), and the severe constipation was a bitch.

    I'll also give you a quote from that opiate potentiation site:

    Loperamide (Immodium): This drug is related to meperidine/pethidine (Demerol) but does not cross the blood-brain barrier in sufficient quantities to cause euphoria. However, the consumption of doses of 150-300% of the therapeutic dose when mixed with high doses of codeine or meprobamate have been reported to produce a weak Darvon-like buzz aside from the effects of the other drugs.
     

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    #22
    thankyou all for your contributions,
    but lopermide discussion is not going anywhere, it always becomes the same (lack of) shit each time it is dicussed.

    from now on perhaps any thread with loperamide and BBB in it needs to be really good to survive.
     

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