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Thread: Spitting out suboxone, SUPERIOR results.

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    Spitting out suboxone, SUPERIOR results. 
    #1
    Greenlighter Chemgineer's Avatar
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    (This is anecdotal stuff that I feel could shed light on the metabolic
    characteristics of bupe. )


    Although we have a plethora of science available to us
    concerning our favorite chemicals, there is still a factor x that we do not know
    about given chemicals. In my Taking of them I take this into account.


    Well with my suboxone I had a hunch.

    I've always wondered what happened to the bupe when taken via the oral
    route. From my experience inducing cyp450/3A4 with bupe I am a believer that
    norbupe crosses the BBB and has an effect. An effect exactly as described in
    the literature. (ie; more agonist than bupe but not quite as affintive. If that's a word)

    Well I wondered "well why don't I just swallow my whole dose, if orally more would be turned into norbuprenorphine?"

    Well that is where I was wrong.

    I had read that Bupe-glucruonide was more antagonist than bupe. But as with norbupe there was still plenty that wasn't known.

    I wondered recently if upon swallowing the spit that's probably filled with 30-40% of the total dose that I took (or more) that most of it was turned not into norbupe but bupe-g (and norbupe-g).

    So I stopped swallowing my suboxone.

    And suddenly I am pinned like I wasn't before, I am itchy like I want before.
    Well no, I feel like I usually feel the first hour after my daily dose, but all day. Meaning, that it seems by swallowing my bupe I was ending whatever warmth I was feeling.(and I did feel it foR 30-45 min after dosing).

    Now that I don't swallow, I feel all day what I used to feel for 30 min.

    That is, much more classic agonist.

    There is not much science to prove what I am saying. There may even be science to go agaisnt it, I don't know. But my pin point pupils don't lie. They aren't being placeboed. And my wife suddenly thinks I'm taking something. I look high now.

    I am on 32mg of bupe a day. I know there is a wisdom that says low dose bupe is best. And that may be.

    But to get the most of my dose, I now am strictly not swallowing.(ha ha, yeah yeah)

    I have been on it for 4 years and for me to suddenly be getting this effect is not usual.
    I still induce my 3A4 and still take p-gp inhibitors even though norbupe hasn't been
    Id'd as a substrate of p-gp(as far as I know). I find vitamin a(retinyl, dry vitamin a) to be helpful. It reduces expression of p-gp.
    And garlic to induce. (I will soon be trying tergretol and primidone for 3A4 and verampril for p-gp. Will let you know. I likely will shy away from the primidone, who wants to be perpetually tired. But low dose tegretol should induce.

    Anyway, just wanted to let folks know of what I found.

    Like I said, I always assume that there will be some science that is wrong and quite a bit that isn't yet known. Acting according to that belief led me to this pleasant discovery. Don't swallow your suboxone spit. It may be turning into too much bupe-g and norbupe-g.

    (now, the bupe that makes it in sublingually will STILL have some conversion to bupe/norbupe-g. I think the receptors are not flooded with it like they are if the oral route works on the bupe. )

    It's more alchemy than science, more gut than proof.

    But the proof for me is in the pins.

    Oh I forgot to mention last month I took lots of sub throughout a day. I kept swallowing it quickly just to see what would happened. I basically swallowed 48 mg without much tounge time. At the end of the day I had the shits for the first time in year and was mildly sick.
    I didn't connect it then, but thinkng back on it now, If my theory that oral bupe turns largely And principly to bupe-g(more antagonist than not) than I basically went into withdrawl from swallowing my doses instead of sublingual route. (and It wasn't the level, I take 5 or 6 quite frequently and never feel like I did that Night. )

    just thought that this was anecdotal stuff that is important to our understanding of bupe metabolism.
    Last edited by Chemgineer; 03-01-2010 at 08:43.
     

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    #2
    Bluelighter dread's Avatar
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    I never noticed any difference in spitting vs. swallowing, except if I swallow it works as a laxative...
     

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    #3
    Spit or swallow? lol!
     

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    #4
    Greenlighter Chemgineer's Avatar
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    It's been a huge difference for me. Maybe the fact that I am inducing 3A4 plays a part. I haven't tried it without inducing 3A4 plus use p-gp inhibitors, but that's because it's way better when I induce. (again, I don't believe norbupe has been proven to be a substrate of p-glycoprotein, so that may or may not be involved. )

    Spit or swallow, I knew This thread would generate that.

    Like I said I approach chemical taking with the premise that:

    1) There is going to be some science that is going to be wrong about some of a given chemicals
    Characteristics.

    2) There is going to be even more that we just haven't discovered about a given chemicals pharmodynamics.

    Approaching with this has allowed, over the years for many personal discoveries. Many of Which are eventually borne out in the science, more which have not been.

    Why approach it assuming all is known, that there is no chance for an improved response?

    I like to approach all of them with the assumption that they are all still frontiers, some more mapped than others.
     

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    #5
    I guess I feel this way too. I still enjoy it after all these years, and I only swallowed it a few times.
     

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    #6
    I have always spit, my logic was always that you were spitting out the naloxone and that the bupe had been mostly absorbed already. I do keep the spit in my mouth for a couple minutes though.
     

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    #7
    If your theory is correct that spitting out the left-over sub instead of swallowing it gets you a 'better feeling' then how do you describe the effects of insufflated suboxone? B/c when you snort sub it seems to be a hell of lot stronger in the simple fact that your absorbing more of the bupe and it also kicks in way faster..like 10-15mins compared to like 1 or 2 hours with sublingual administration..
     

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    #8
    Greenlighter Chemgineer's Avatar
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    I've never snorted it. My dose is too big, and I regardless of how people have reported the nalaxone to have no effect, I've always done all I could to make sure my brain stayed free of antagonists like naloxone. Maybe it's old superstition..


    You probably get such a good effect because most gets absorbed nasally and there isn't much bupe in the drip to get converted into the bupe-g.

    Bupe-g is a stronger antagonist from what i have read.

    It's my suspicion that swallowing bupe results in most of that bupe going straight to glucuronide.

    If it went to norbuprenorphine, I believe it would be a stronger experience. (regardless of the questions remaining about norbupes ability to cross the bbb, inducing 3A4 for me gives better results. )

    But since orally I don't get that feeling I get when I induce norbupe production above the natural rate, then I suspect it's turning into bupe-g. (and norbupe-g)

    Most studies involving sublingual administration have the people swallowing their dose. So the recovered dose of bupe in their urine is showing what happens when some bupe is swallowed)

    Anyway, I am getting some 3A4 inducers today, so I'll be able to report if they affect things at all.

    Snorting it probably gives a feeling similar to, but a bit better than, what I feel now that I have stopped swallowing it.
     

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    #9
    I've always held it under my tongue for at least an hour, sometimes a bit over two hours if I'm engaged in something.

    I snort 3mg, put 4 under my tongue.
     

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    #10
    Bluelighter
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    Dude it's still an opiate. It miight make your eyes more pinpoint, maybe your expecting that. Maybe it's been extra sunny, maybe a thousand things. Opiates do the same things to your body every time. Except withouth receptors being downregulated, you don't have tolerance. But does constipation go away-NO. Naloxne is one oxygen atom from OXYMORPHONE. They both attach to the same receptors. Loperamide or Immodium is an opiate that doesnt pass the BBB. Maybe the naloxone is now being abosorbed more and causing slightly different effects to the autonomic nervous system. There are too many confounds to know for sure.
     

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    #11
    Bluelighter dread's Avatar
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    Naloxne is one oxygen atom from OXYMORPHONE.
    False. Naloxone is N-allyl-nor-oxymorphone. That is, oxymorphone with n-methyl changed to n-allyl.

    And oral naloxone has laxative effects, due to antagonizing mu-receptors in the gut.
     

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    #12
    Bluelighter lolwhatzdrugs's Avatar
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    Quote Originally Posted by dread View Post
    False. Naloxone is N-allyl-nor-oxymorphone. That is, oxymorphone with n-methyl changed to n-allyl.

    And oral naloxone has laxative effects, due to antagonizing mu-receptors in the gut.
    I don't understand this at all. Naloxone has a 2 percent oral bio-availability. Is this significant enough to antagonize mu receptors (assuming we're talking about 8mg suboxone)?

    If it is, then why is it not crossing the blood brain barrier out-competing buprenorphine?
     

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    #13
    Bluelighter dread's Avatar
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    As far as I know, it binds to receptors in the gut, but first-pass metabolism then destroys it before it can enter the blood. The BBB doesn't even enter the equation here.
     

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    #14
    Bluelighter lolwhatzdrugs's Avatar
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    Quote Originally Posted by dread View Post
    As far as I know, it binds to receptors in the gut, but first-pass metabolism then destroys it before it can enter the blood. The BBB doesn't even enter the equation here.
    Ah, gotcha. That makes sense, it effects those cell's receptors directly, but never enters central circulation.
     

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    #15
    Bluelighter dread's Avatar
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    Besides that, naloxone would not compete with buprenorphine even if it did enter the bloodstream (ie. when you IV suboxone). Since buprenorphine has higher binding affinity to mu-receptors than naloxone, the naloxone will have no central effects when administered with buprenorphine.
     

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    #16
    Bluelighter lolwhatzdrugs's Avatar
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    Quote Originally Posted by dread View Post
    Besides that, naloxone would not compete with buprenorphine even if it did enter the bloodstream (ie. when you IV suboxone). Since buprenorphine has higher binding affinity to mu-receptors than naloxone, the naloxone will have no central effects when administered with buprenorphine.
    Per my understanding from another post, I'm starting to get the feeling that that's not completely true.
     

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    #17
    Bluelighter dread's Avatar
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    Quote Originally Posted by lolwhatzdrugs View Post
    Per my understanding from another post, I'm starting to get the feeling that that's not completely true.
    That post is wrong. Naloxone does not compete with buprenorphine and that's a fact.
     

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    #18
    Bluelighter lolwhatzdrugs's Avatar
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    Quote Originally Posted by dread View Post
    That post is wrong. Naloxone does not compete with buprenorphine and that's a fact.
    I have seen no definitive proof of anything. Do you have source I can check out? I'm not saying your wrong, just would like some further reading as I obviously lack understanding about buprenorphine overdose treatment.
     

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    #19
    Bluelighter dread's Avatar
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    Google it.
     

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    #20
    Quote Originally Posted by dread View Post
    That post is wrong. Naloxone does not compete with buprenorphine and that's a fact.
    That's absolutely false! If you have overdosed on bupe and are brought into the ER the treatment will be an IV infusion of naloxone and ventil;ation to maintain breathing. Naloxone will knock any opiate off the receptors, it's only the dose that will change.

    It's a very basic pharmacology principle: an antagonist will shift the dose response curve to the right.

    Naloxone won't outcompete bupe in Suboxone but that's b/c the oral BA is so low. IM/IV naloxone has 100% BA.
     

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    #21
    I just want to add that the longer you keep Suboxone under your tongue, it gives you a much stronger effect. They say to keep it under there for 5-10 minutes, just until the pill dissolves. If you let it absorb until the saliva goes from orange to clear (about 30 minutes for 8mg, less for lower doses), you get far more of an effect. Whenever I was with someone in the morning who didn't know I took Suboxone and only had 5-10 minutes to take my Sub in the shower I only felt 2/3rds of the effect. Everyone bitches about the taste but I like it.
     

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    #22
    Bluelighter lolwhatzdrugs's Avatar
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    Quote Originally Posted by WSB15 View Post
    Everyone bitches about the taste but I like it.
    Do you really like the taste, or do you like the subtle feeling associated with the taste?

     

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    #23
    Bluelighter dread's Avatar
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    That's absolutely false! If you have overdosed on bupe and are brought into the ER the treatment will be an IV infusion of naloxone and ventil;ation to maintain breathing. Naloxone will knock any opiate off the receptors, it's only the dose that will change.

    It's a very basic pharmacology principle: an antagonist will shift the dose response curve to the right.

    Naloxone won't outcompete bupe in Suboxone but that's b/c the oral BA is so low. IM/IV naloxone has 100% BA.
    That's absolute drivel. BA has nothing to do with this, naloxone's receptor affinity is lower than buprenorphine's therefore bupre kicks naloxone out of the receptors.

    Besides if we're talking of BA, bupre has 0% oral BA. It is used sublingually.

    Bupre overdoses are not treated with naloxone, at least around here. Naltrexone might be used, I'm not sure... but not naloxone, since it has no effect on bupre overdose patients.

    If naloxone would compete with buprenorphine, then how do you explain IV suboxone working just as well as IV subutex?
     

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    #24
    Quote Originally Posted by lolwhatzdrugs View Post
    Do you really like the taste, or do you like the subtle feeling associated with the taste?

    Haha I'm sure it's the latter. There's a strong Pavlovian element to it. Now every time I eat a citrus fruit, I'm like "Oh yeah, I'm gonna get hiiiiigh off this shit...oh wait, no I'm not."
     

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    #25
    Bluelighter lolwhatzdrugs's Avatar
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    Quote Originally Posted by WSB15 View Post
    Haha I'm sure it's the latter. There's a strong Pavlovian element to it. Now every time I eat a citrus fruit, I'm like "Oh yeah, I'm gonna get hiiiiigh off this shit...oh wait, no I'm not."

    That would be fucking awesome if they dosed suboxone patients with oranges laced with buprenorphine! Try shooting that shit!

    Hah, you must be getting some awesome fucking suboxone if you think it tastes like a citrus fruit.
     

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