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Thread: Low dose buprenorphine to POTENTIATE opiate agonists

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    Low dose buprenorphine to POTENTIATE opiate agonists 
    #1
    Bluelighter
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    Hey fellas, I wasnt sure if this belonged in BDD or ADD so mods feel free to move this wherever. I believe I originally saw a post for this in ADD but I cannot find it now so work with me fellas, or link me if you find it

    Anyways guys you all wanna know the question now, right? i recently saw a post on this and was reading an interesting paper on the topic, and the question is:

    Can low doses of buprenorphine potentiate full opiate agonists?

    Basically, the jist of it was this:

    since buprenorphine acts as much as an agonist as it can in lower doses, typically observed to be the "ceiling" of agonist effects is around 2mg, (possibly 4?), it is exhibiting very low antagonistic action, if any, at these doses. So then if one were then to take a very small dose (I believe the article was doing 100-500 micrograms, or .1-.5 mg of buprenorphine) before taking one's agonist, the buprenorphine will be exhibiting almost agonistic activity.

    since the bupe will be acting as an agonist (a strong one at that) as much as possible (at these doses), it will be activating those receptors akin to any other agonist; since the dosage of buprenorphine is so low that it will not fully saturate one's opiate receptors, it thereby leaves many open; since these receptors are all open and the buprenorphine is not acting as an antagonist (or if it is, in VERY VERY minute amounts) but rather an agonist, would it then be possible to ingest another opiate (an agonist) and fill up these empty receptors?

    Since the buprenorphine is in ones system before hand, it has already taken up as many receptors as it can and NOT stripped them of any agonists: since the buprenorphine is totally absorbed but not occupying all receptors, is it then possible to fill up the rest of them, and well get one "high"? And, to boot, "higher" (relatively speaking) than one would have been w/o the buprenorphine, because there are more receptor sites being occupied (by agonists).

    no precipitated withdrawals because the sub is not knocking things off the sites, rather already there.

    naloxone is ineffective orally and sublingually; if this is a concern however one could wait for most of the naloxone to be eliminatd since it is done so fairly quickly, and VERY quickly relative to buprenorphine (which stays in ya system for ages). one could wait a few hours for the naloxone to go, and the buprenorphine will still be there, despite it being a small amount, it will definitely be there for quite awhile

    Interesting thinking...if anyone can find me any information on this further (the thread on bluelight would be good, as well as the paper which I had been reading), it'd be great. Sorry I didnt talk in very precise chemical terms, I was just trying to convey the concepts so that many could understand and contribute their thoughts. Any thoughts and input are still input

    Hope this gets a good discussion going; or I can be pointed in the right direction of an already good discussion
    Last edited by DooMMooD; 03-04-2011 at 11:42. Reason: fixed some stuff; added a few things
     

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    #2
    Bluelighter Codones's Avatar
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    Good stuff. This was just posted by Captain Heroin in the NMI forum in the social thread.

    Quote:
    Originally Posted by muvolution
    Do you do this also? I mean, my girl knows I fuck around with opiates, but I do the exact same thing... Bedtime for you, alone time for me, everyone is happy.

    Hey Cap'n - I posted this several weeks ago in the opie potentiation thread, but never got a response - can you give me some insight?
    Buprenorphine isn't a classical full antagonist (like naloxone or naltrexone), however you can do this. Once you use buprenorphine, you can use full agonist opiates again, but not the other way around (without waiting an adequate amount of time).

    The buprenorphine can help boost the effects of the full agonist like this...

    Let's say you have 100 mu-opioid receptors, and you normally get 60% of them covered by a full agonist. To potentiate this dose with buprenorphine, take the buprenorphine first, at a dosage where it wouldn't "hold you" but it isn't unnoticeable, aka a baseline dosage. For some people this could mean 1mg sublingual, for me it might mean 0.05mg IV'd.

    After you feel it a little but not adequately, then you can take your regular full agonist dosage.

    This way, the buprenorphine will occupy 10%, the regular dose occupying 60%, meaning the buprenorphine won't block the full agonist, just potentiate it.

    Just be careful not to use too much buprenorphine otherwise you'll not potentiate it but diminish the desirable effects.
     

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    #3
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    I agree 100% with you said. EXACTLY what I was saying man. Glad to hear another person chime in on this theory (or is it fact now, have people proven it?).

    As I stated and you agreed, 2 things are crucial to this idea:

    1) bupe in a small enough amount so that it does not fully saturate your receptors is key to this,

    2) taking the buprenorphine beforehand. although I am sure that if you took such a low dosage it might not be the worst Precip w/d, im very confident that the bupe would still outcompete agonists already at the receptor sites, as well as bind to open ones. That is to say, I do not believe that bupe would immediately "go for" the unopen ones, and would just go for any receptor, whether occupied or open, if it is taken afterwards. I do not believe it would discriminate in such a way as to only go to "open sites".

    I have not tried it, nor do I desire to until I hear some concrete facts, concrete dosage limits, etc.

    Although I (obviously, I hope) have a great idea of what these dosage limits and such are, I have no desire to attempt and waste some of my little opiates (and thereby $) on a shot in the dark, especially gambling something as awesome as oyxmorphone against something as bleh as buprenorphine. not saying bupe has not helped me tremendously, when I was doing MAT it was a godsend, and still is, I believe it has the power to stop addiction, I am simply talking "bleh" in terms of high. Comeon, how can bupe which makes me "normal" compare to oxymorphone, which makes me feel amazing and normal heh)

    Anyway thanks for givin some input Codones. If you could find a link to the other thread or links to any relevant studies that'd be great. Thanks again for the contribution man, hopefully we get some other people up in here to give their .02$ as well
    Last edited by DooMMooD; 03-04-2011 at 12:14. Reason: fixed up a bit
     

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    #4
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    Hey fellas, I wasnt sure if this belonged in BDD or ADD so mods feel free to move this wherever. I believe I originally saw a post for this in ADD but I cannot find it now so work with me fellas, or link me if you find it
    I feel this would work better in ADD, so I'll move it there for ya

    BDD - > ADD

    BDD Guidelines! - BLUA - BL Search! - Conversions for Opiates & Benzos - Save Your Liver Do a CWE
     

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    #5
    I remember reading a study where they found no antagonistic activity at doses below 2mg, and that at such doses it could be combined positively with other opioids. I believe this was at least part of the reason suboxone comes in such high doses.
     

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    #6
    Bluelight Crew negrogesic's Avatar
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    Additive maybe, potentiate, not sure. Certainly doesnt mimic ULD-antagonist .
     

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    #7
    Isn't buprenorphine a partial agonist (50? There is no reason, save that it's tied up all the MOR receptors, that it would seriously interfere with other full agonists. It seems to me that norbuprenorphine might have more euphoric potential & it isn't hard to convince the body to N-dealkylate the drug fairly efficiently.
     

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    #8
    Bluelighter amanitadine's Avatar
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    ^^^ By first pass metabolism? One would think......but oral buprenorphine just doesn't result in much. Not quite nothing, but certainly an order of magnitude less going on than alternate ROAs...
     

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    #9
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    You brought up oral ingestion as being a poor choice for this, but what about sublingual or nasal ingestion?

    Specifically curious about sublingual ingestion, since this is how it is intended to be ingested, and how I ingest my suboxone.
     

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    #10
    Snorting suboxone is a popular past time for some. On an occasion or two I've engaged in this past time when I was running low.

    Even these new strips can be insufflated, and quite effectively, I've found, at least for low doses. 1 to 1.5mg (half to 3/4 a single 2mg strip), placed onto the very front of a normal sized spoon, has very hot water dripped onto it (not too hot, since you would dip your finger into the water, and then direct the small drops that come off of it onto the strip on the spoon, repeating until there's just enough water to cover the strip effectively. You'll need to hold the spoon such that the water is pooling at the very front of the spoon without dripping off. Hold it this way for a minute or two. The strip should pull up and sort of bubble as it dissolves. Then take a knife or perhaps a large pin and carefully stir the water around so that you have a fairly homogeneous mixture. Waiting until the strip is starting to dissolve is important so that the wet 'melting' strip doesn't stick to your implement when you're stirring.

    Once you're completed, carefully put it up to your nose and sniff it into your sinuses. It has the benefit of not hurting at all. Alternate nostrils between sniffs. You'll probably find that there's a little bit of orange on the tip of the spoon despite not being able to get anything else in. Add one small drip here and and stir it (stirring is a bit of an exaggeration, you can't really stir it, just mix it up a bit) and then do it again. You probably still can't get it all, so lick the spoon clean for good measure.

    You brought up oral ingestion as being a poor choice for this, but what about sublingual or nasal ingestion?

    Specifically curious about sublingual ingestion, since this is how it is intended to be ingested, and how I ingest my suboxone.
    It can be of no surprise that sublingual is a pretty good way to administer the drug. It has a bioavailability through this route of about 33%, and I believe insufflation jumps to 50-75%.

    I don't know what you want to know exactly. Yeah, you can use it at low doses to potentiate other opiates.
     

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    #11
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    Not asking about bioavailability. I know the differences between oral, insufflated, IV, etc bioavailability.

    I was referring to bupe undergoing first past metabolism via sublingual/nasal vs bupe undergoing first past via oral.

    They said that orally it barely undergoes this; how does the first past sublingually/nasally compare?

    Edit: also i have no desire to insufflate these strips heh. I know how it can be done and have seen it done, but I have 0 desire to put that liquid cum consistency concoction up my nose lol.
     

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    #12
    So what is the consensus on this? This all makes sense in writing, how about in practice? I took a small dose, maybe 1.5 mg,(usually I need at least 8mg for any relief) of Suboxone around 4 hours ago(9:10 EST, it is now 1:12 EST), which was enough to feel slight effects and allow me to sleep a few hours since I tossed and turned all night and got not a fucking wink....withdrawing from a 300mg a day oxy habit, you see(I know for the sake of harm reduction you guys are gonna want to say to just kick it, but I have no more suboxone and nothing will change my mind about continuing on for now, so kindly save it :-) ). Anyway, as I said I took 1.5 mgs 4 hours ago, and am on the way to get 9 oxy ir, will I experience a poteniation effect, or a diminished blockade effects on the oxy? Response would be much appreciated, but either way I'll post back with my experience for the sake of information on this(very interesting, and, frankly, very exciting) topic.
     

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    #13
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    If this is even possible wouldn’t it only work in someone with No opiate tolerance, and no other opiates in their system?

    I know at least for myself even the smallest amount of sub will put me into PW if I do not wait long enough, and my normal dose is just at or under 2mg.

    If you are using bupe for maintenance even if you are using less than 2mg a day wouldn’t you have more than 2mg built up in your system?

    In theory if you have no tolerance and you take a very small dose of bupe and then a larger dose of some other full agonist maybe it would have some stacking effect but I think with something like bupe things become way more complicated than I think most if anyone even knows.
     

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    #14
    ULD dupe has been used by a handful of chronic pain patients as a potentiator.....similar to ULD naltrexone. I'll see if I can get any of the patients to post here on BL....
     

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    #15
    Bluelighter lenses's Avatar
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    You should research ULD naloxone as well, seems like BUPE could be doing the same thing... it seems to be like an "up-regulation" process of the opiate receptors by every day ultra low dose naloxone , from what the research is suggesting. People were dosed ULD naloxone everyday for a perioid of time, and it was found that their opiate tolerance was reset, even lowered from baseline, and there was some increase in the amount of receptors as well, from what I can remember.

    Point being, same process may be going on with naloxone as with BUPE. Would be interesting to see a comparative study of them in regards to this, as bupe has mixed antagonism/agonism while naloxone is straight antagonist . Would BUPE work in the same way?

    -lenses
     

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    #16
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    Suboxy, i wish you'd post back.

    OnAndOff, we're talking about sub FIRST then agonists, so no PWD. Your idea of the amount "building up" when on maintenance is on point though; my thoughts are aimed at once dosing, and not someone who is on maintenance (when i was on my 2mg/day this definitely would not have worked). I'm talking about like just taking less than 2mg one day, not everyday.

    I'm kinda hestitant to experiment with this too much, for the sake of it wasting sub that i need when i detox (or wasting precious opiates).

    BUT, tbh one of the few times ive done this, i took like 1.25mg sub maybe, and railed an opana later and honestly i was high as balls. This was awhile back so my memory is not the clearest but i remember being WAY HIGHER than i thought i'd be....it seemed slightly different though, not the same as usual. but i was high nonetheless. Anecdotal evidence at best, but better than no input.

    EDIT: BTW mods, do you think this would get more traffic in OD or BDD? Its more advanced than that but not quite ADD material now that i think about it. And i'm less worried about the label as i am with gettin a lotta traffic and input regarding this.
     

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    Sometimes i can be very fuckin stupid.. 
    #17
    Bluelighter MartinFn's Avatar
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    ^^^Suboxy, post back, give us your lights man! I'm a CP patient and i take fentanyl for 8 years(the 100 ones,i change every 48 h. I try subutex(without naloxone) 2 times in my life.The first time, i had my patch stuck on me as always, and i cook(boil, not just dissolve the pill,i made it like i make heroin for IV). So,it was an 8 mg pill and i took it (IV) to take me high, as i had hear from some guys. Fuck, i will never forget it,it was maybe the worst thing in my life.I thought that i will die,it was a very bad situation. It was like my soul was out of my body, i had a really bad pain, and i slept and woke every 5 minutes. I'm sure that i would die,but God save me, maybe for my children. The second time(how much idiot i am, i took one again,do you believe it,a totally fool and idiot person) i took an 8mg pill, this time sublingual. A patch was stuck on my chest as always, so this time the things were shit again(but not so strong as the first try).I lied on my bed in fuckin terrible pain, i took some clonazepam that helped me,and my wife lied next to me and treated me like a baby, i wasn't think that i will die, and the only situation was not as bad as the first time, but still it was fuckin shit..So that's my experience with buprenorphine, i know that it's a very useful med to take off, it helped a lot of people, but as a drug to take you high..But of course i know that it was my mistake to take it with fent patches together,it would be totally different to take it alone..

    MartinFn
     

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    #18
    I have 2mg sublingual tablet of subutex (no naloxone) i have a rather high tolerance for opiates. Say I took the 2mg sub sublingually, how long in theory would i have to wait to take a full agonist such as methadone for a decent effect? i have a full 40mg wafer, but its the kind you can dissolve in water and take as a shot. since i have a tolerance (high), would the pure bupe be enough to potentiate the dose of methadone I choose to take? I dont want to take the whole wafer since I have never mixed these two before, but maybe a quarter to half. would the full agonist (methadone) be blocked entirely by the bupe? I do not take bupe daily and the most i ever take in a day is 2mg. Just curious about the potentiation
     

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    #19
    im interested in this topic as well. I take 1.5 mg subutex per day and was thinking about trying out some hydrocodone on top of it. Anyone tried this out yet? how much stronger was it? im paranoid about
    oding.
     

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    #20
    I have the same problem with the od fear like, I know I have a decent tolerance, ive been on opes for 6 years, but i just dont wanna take to much bupe and have the other ope nto effective at all or od ya know?
     

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    #21
    ^^

    im 99% sure we wouldnt od at reasonable doses and im very confident that at 1-1.5mg sub doses we would get high using opies on top. I just want to get someone to test it first so we kno for sure. ive seen mmany many
    anecdotal reports it works fine.
     

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    #22
    Yea same here, id rather have someone else test it first, cuz i took sub sublingual2mg about 4 hours ago and i have FST kratom and the wafer. i just dont wanna waste either you know? but ive heard if you have a tolerance you have more receptors therefore the bupe can be a potentiator
     

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    #23
    If no one else tries by tomorrow ill try taking 1mg of sub and mixing it with like 30 drops of the FST Kratom. usually works well

    Id rather try the FST than the full agonist strength of methadone
    Last edited by GeisterxFahrer; 05-08-2011 at 03:51.
     

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    #24
    Quote Originally Posted by GeisterxFahrer View Post
    If no one else tries by tomorrow ill try taking 1mg of sub and mixing it with like 30 drops of the FST Kratom. usually works well

    Id rather try the FST than the full agonist strength of methadone
    id try the methadone cuz then youd kno for sure whats going to happen for future reference, cant really say with something like kratom.
     

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    #25
    Bluelighter Nagelfar's Avatar
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    I've taken someone out of a serious OD with suboxone crushed into powder and put in small amounts under his tongue until he awoke, and said it was the highest/best-feeling he had ever been once coming to. I crushed it to use titration so that he didn't go into WD, but I needed to use about half. Came to in 15 seconds after.

    Since then, I have had the very unsafe, non-HR idea of putting a suboxone strip under my tongue, and shooting way more than my tolerance, so that I'd get a huge rush, go out in a dangerous way, and be immediately 'brought back' by the slow release of the suboxone with just enough to feel wonderful, and remove the suboxone just as I became again functional. Something along the lines of a "lazarus shot". I don't think I'd try it without extra suboxone on hand and a sitter though.
     

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