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Thread: Suboxone/Buprenorphine Mega Thread and FAQ v16.0

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    Greenlighter
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    Yeah I have a friend who got prescribed 2 tablets a day.
     

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    Seems like there's a lot of discussion going on here at the same time, I'd leave it but I'm afraid it's coming and I want to know something beforehand... I hope it's alright, I'm new, never tried any forums, so I'm finding it hard to navigate it...

    I'm on the suboxone program.
    It's a large dose, and I'll explain after how I'm aware there's very little explanation for it if anyone really wants it afterwards!

    I forgot to renew my script, and my doctor isn't answering his after-hours number. I wouldn't call if it's just one day... but it's the weekend; about 3am, Saturday. So I've got potential issues.
    I dosed Thursday, 24mg. I've come down from 32mg(!), not a big drop. Been on it 3 months after switching from Methadone after 2 years
    So tomorrow will hit 48hrs at 5pm, I have a lot of people counting on me for something beforehand. Most people feel very much from 36-48hrs? What about after only 3-4 months on it?
    I have to be active, very active in that space of time tomorrow... any chance I'll be operating reasonably well?

    If it helps, when I switched from 50mg Methadone I was flushed, at 32mg, after just under 36hours from last dose, and I spent 4 hours of complete hell as I felt the 'done being knocked off the receptors, then a few lag days... enough in the system you think to get me to 48 hours alright?

    Afterwards is easy... I'm going to hospital for symptoms if real bad mentally. The detox clinic is closed on weekends and I can't kick at home... get 'quite'(?) suicidal.
     

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    Oh and I wasn't calling the doc at 3am hehe, called last at 5pm Friday
     

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    Quote Originally Posted by Captain.Heroin View Post
    Yeah oh man I think I am smart enough I hope.

    EDIT

    BACK ON BUPE

    I had to. It feels too good to avoid.

    Something about that "oomph" yeah. To each his own but I want to be on bupe for life. Let's see how illogical my plans are as time goes on.
    hey captain. I've been on subutex for 2 months now and my psychiatrist and I planned that I will need this medicine for the rest of my life.

    I have noticed it is a great anti-depressant for me and gives me energy to actually do things. Before I was fed SSRI's for my depression/social anxiety but they did nothing. Subutex really helps, is there anything wrong using it indefinitely? I don't really see a problem.
     

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    If I can add my 2 cents, I had issues my whole life with depression, and on Maehadone it was no different. Now on bupe I feel a lot more stable, still with a natural anxiety I've always had, but back to the point before the depression set in. There are a couple of minor health issues I think, but nothing worse than the teeth, if you're dissolving it in your mouth. I don't know of anything severe... which doesn't mean there isn't I guess.

    My only issue is that my senses are dimmed. I know I can't smell and perceive things around me in as much emotional clarity, and my creativity sort of drags along on the same level. I'm a writer, and I can't get to the same extremes I could before. But having said that, when I wasn't on it, at worst, which was often, I was so down I couldn't pick up a pen or turn on the computer. I couldn't focus enough to finish anything. To me it's a straight swap; a catch 22. I feel good, but I want to get off it; I'm missing out on life a bit. But only when I feel ready. My guess is most people get sick of it at some stage.
     

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    Oh why it's a straight swap/catch 22 is I can sit down and write all night without any ideas.
     

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    Senior Moderator
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    Quote Originally Posted by Cassepipe View Post
    Seems like there's a lot of discussion going on here at the same time, I'd leave it but I'm afraid it's coming and I want to know something beforehand... I hope it's alright, I'm new, never tried any forums, so I'm finding it hard to navigate it...

    I'm on the suboxone program.
    It's a large dose, and I'll explain after how I'm aware there's very little explanation for it if anyone really wants it afterwards!

    I forgot to renew my script, and my doctor isn't answering his after-hours number. I wouldn't call if it's just one day... but it's the weekend; about 3am, Saturday. So I've got potential issues.
    I dosed Thursday, 24mg. I've come down from 32mg(!), not a big drop. Been on it 3 months after switching from Methadone after 2 years
    So tomorrow will hit 48hrs at 5pm, I have a lot of people counting on me for something beforehand. Most people feel very much from 36-48hrs? What about after only 3-4 months on it?
    I have to be active, very active in that space of time tomorrow... any chance I'll be operating reasonably well?

    If it helps, when I switched from 50mg Methadone I was flushed, at 32mg, after just under 36hours from last dose, and I spent 4 hours of complete hell as I felt the 'done being knocked off the receptors, then a few lag days... enough in the system you think to get me to 48 hours alright?

    Afterwards is easy... I'm going to hospital for symptoms if real bad mentally. The detox clinic is closed on weekends and I can't kick at home... get 'quite'(?) suicidal.
    At that dose you should be fine at the 36 hour mark and starting to feel sick at the 48 hour mark. Try not to think about it and you should be alright.
     

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    Bluelighter mydrugbuddy's Avatar
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    Ive been down to 0.25 for a few days. I tried to jump off at that dose a a few days ago. It was worse than i was expecting, my stomach felt like it had a cat scratching around in it and also so exhausted as if id walked a thousand miles. I didnt last any longer than mid afternoon, before giving in. Its a lot harder to quit when you still have a few pills left. Maybe when i next try to quit i should flush any pills that i might have left. I'll have to go through with it then.

    Although I'd imagine Kratom will probably help a bit, is it worth bothering with ? Wont it just be prolonging the misery by just holding off w/ds a bit longer ? Or could it allow a further gradual taper, as im reaching the stage now where i cant really cut my bupe pills any smaller than 0.25mg. I beleive Kratom works on exactly the same receptors as opiates ?
     

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    Hey i'm curious. I either snort or plug around 1mg of sub a day. If i want to taper off, can i continue snorting? I mean obviously i can.. but should i make the switch to SL administration? Also, when people talk about their sub dose, please include the ROA (route of administration) because 1mg IV is very different from 1mg sublingual..

    Also to the previous poster, why can't you cut your dosage? Or spread it apart further.
     

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    Bluelighter mydrugbuddy's Avatar
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    i get 2mg pills, im allready cutting them into eight pieces. These pieces are fuckin tiny, and id jsut be left with dust if i tried to cut them further. I take them SL. Im not sure, but i suspect the effect lasts longer this way than insuffllating it.

    I could spread the doses apart further, thats true.
     

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    I just remembered, remember a couple years back i tappered of the subs. I ended up putting them in capsules numberedsomething like 1-30. Started with 2mg chunks.. then 1mg.. then Imade a small pile that weighed contained about 1mg of sub and make smaller and smaller amounts to put into each capsule for the last 10 or so. Must have been doing around .1 at a time or less at the end. I would open the capsule and snort. Sometimes i iv'd. Was able to stop completely, but I believe i started doing H again a couple months later.
     

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    Greenlighter
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    hey bruv.sub normaly cancels out the opiate unless its a high dose,but everyones different iv noticed from friends.i have can only get high if iv taken no sub that day...its a case of try and see,youl know after...
     

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    Bluelighter Slum Survivor's Avatar
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    wow... i just got back from an argument with the idiot woman at the pharmacy counter at walgreens that brought me nearly to tears

    fuck these IDIOTS who dont understand that naloxone has absolutely no effect on your opiate receptors over bupe.

    she also argued with me that there are NO generics for either suboxone or subutex until one subutex one JUST came out this month. i quickly corrected her but she refused to listen, and laughed at me. like im just an idiot junkie there to get my script who thinks im gonna talk them ino giving me subutex or something...

    i had only brought the subject up by saying that its rediculous that dr's wont prescribe subutex, after she had sympathized with the cost fo my suboxone and told me i can get a minimum of 14 to use the $50 off card each month.
    She laughed and said OH NO, hahahaha. subutex is something different. people can get high off of that. <--wow....

    so i sat there and explained to her that i know how the receptors work, and that bupe always beats out naloxone. She said, no, its still effective.... omg.

    she said: "You need to quit listening to stuff u read on the internet." that threw me into a rage.

    i said excuse me... do u know who Dr. Junig is? have u ever heard of the NAABT?? she kinda blushed and tried to tell me she knew who those were.... ya fucking right.

    im tempted to go back up there with a nice stack of stuff for her to read. or get her ass fired for sending me into a panic attack and all out rage after i left.

    i even told her that i used to get my subutex at this same walgreens from a different dr.... she acted like i was nuts and didnt even check it. stupid idiot.

    can u guys believe this crap... i wanna go and just flip out on those people now.
     

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    Sorry to hear.

    Even if they were completely different drugs, and you could get "High", that should be of no concern to her. Sounds like she was trying to be your Mom and not your pharmacist.

    As far as the naloxone..

    If it has no effect, then why do people report adverse effects?

    (Im not saying it does anything but I do question its effects or lack thereof)
     

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    Bluelighter Slum Survivor's Avatar
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    well she was saying that it has other medicinal properties... her words were: its there for somethign else. which i think she meant that after u take your sub u cant go get high... which we all know is form the bupe.

    plus she thinks that the naloxone prevents people from getting high on the bupe... she certainly is wrong.

    i believe that naloxone has almost no effects on the average person unless purposely dosed in effective ways.

    thats different that a little bit of it causing side effects. but yeah i know what u mean Zerrr. i spit out my sub to avoid any furhter possible naloxone absorption.

    only thing i think it may compete with, and i could be wrong on this one, is the Nor-bupe. and im not sure on that one. but maybe thats why the naloxone causes side effects for some folks who arent even on very high doses of bupe. idk. i think alot of side efffects come from the nor-bupe being antagonized by the bupe at higher doses...
     

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    I don't have the background to prove anything..yet. So back to the pharmacist.

    Yea, thats absurd. It seems like a conversation that would be semi insulting even behind closed doors with your P.C.P.

    Not surprising tho, most of us on sub experience some form of misguided discrimination. I went to the ER a while ago because I was worried about a tooth infection. To be taken seriously, I have to make it completely obvious that I am there for antibiotics and don't even want the p.k's.

    Guess it would save time if I brought a sign with me that says "Not looking for pain pills"...might cover up the "junky" tag I have acquired without my permission.
     

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    I am really excited right now!!!
    I posted a few question this past month about the effects of Naloxone on Bupe (Suboxone). I was always skeptical of the general opinion that Naloxone has no effect on the Bupe. Very skeptical. I know many people on BL are very educated and experienced with Suboxone and I was not discounting their educated opinions and the information they generously share. Rather, I had a hard time believing that the pharmaceutical company B&R would seriously put Naloxone in the Suboxone if it doesnt have any effect. I am stubborn and I wanted some facts or studies or whatever that could prove this either way.
    So here it is. And Its pretty cool what the results of this study are and the information that is given. Granted, this is one study, one conclusion. But I am still very excited to read this and I thought I would share.

    http://dailymed.nlm.nih.gov/dailymed...6-b6d3cb3d04aa

    I hope someone else is excited and maybe this information can help someone some how. I hope you are all well. And no matter what anyone says, YOU are the only person that can decide what is best for YOU. Do not let judgmental, biased, cynical, argumentative people question what you feel is best for you. Until we find a way to literally walk in another's shoes, let's try to be more understanding and empathetic. We all struggle, we all hurt, and we all could use some help and compassion.

    Peace. Scarlet
     

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    Bluelighter Slum Survivor's Avatar
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    can u plz explain further??? im lost on that one.

    the naloxone has no effect on BUPE itself. i know that for a fact. it took me a couple years to even understand that.

    and if u look into it... there is no other reason they added it except for reasons that have been debunked for the most part. it was just a way to push it thru the FDA and get $$$ FUCK R&B and FUCK that stupid idiot at the pharmacy. shes lucky i have anxiety meds i was able to take to calm down... i was really planning on going up there and telling her whats up with a little paperwork to back it up.

    i plan on discussing this with my DR as well, i mean i pay him. not the other way around. he needs to at least listen to me and give me a better explanation than , o thats a different med... no its not. ive been on it before and ive shot both subutex and suboxone Iv there isnt a damn bit of difference... ugh i get a little mad about this now.

    people like her and my Dr make america look stupid as all hell... and greedy.
     

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    Yea sorry about the link, it works for me but I'm sorry it doesn't for you. Here is the part I was speaking of. It comes from a more reputable source than say, a Suboxone "patient information" site. But it is still the internet. It was just nice to see the results of a non partial parties study on the topic of the effects of Naloxone on Bupe.
    I know this won't work but ill past the link to "site" my source.

    http://dailymed.nlm.nih.gov/dailymed...6-b6d3cb3d04aa
    Last edited by .Scarlet.; 28-10-2013 at 03:12. Reason: Deleted the huge paragraph I didn't mean to post.
     

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    Dang. Please disregard the above text I copied- I didn't copy the correct paragraph. Really sorry folks that was stupid!! Ok here is the paragraph I was talking about.

    Physiologic and subjective effects following acute sublingual administration of SUBOXONE and SUBUTEX tablets were similar at equivalent dose levels of buprenorphine. Naloxone, in the SUBOXONE formulation, had no clinically significant effect when administered by the sublingual route, although blood levels of the drug were measurable. SUBOXONE, when administered sublingually even to an opioid-dependent population, was recognized as an opioid agonist, whereas when administered intramuscularly, combinations of buprenorphine with naloxone produced opioid antagonist actions similar to naloxone. In methadone-maintained patients and heroin-dependent subjects, intravenous administration of buprenorphine/naloxone combinations precipitated opioid withdrawal and was perceived as unpleasant and dysphoric. In morphine-stabilized subjects, intravenously administered combinations of buprenorphine with naloxone produced opioid antagonist and withdrawal effects that were ratio-dependent; the most intense withdrawal effects were produced by 2:1 and 4:1 ratios, less intense by an 8:1 ratio. SUBOXONE tablets contain buprenorphine with naloxone at a ratio of 4:1.
     

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    Bluelighter
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    Well, fuck. I need some advice.

    First things first, I'm on 10mg a day of Suboxone, scripting for ORT. I have a very fast metabolism, and the 10mg lasts until I'm asleep.

    I'm travelling, and have lost most of one dose somewhere. Thankfully it's just 8mg, so I've got 2mg left. I'll be flying though, and am not looking forward to being in withdrawals on the plane...

    I also have 600mg of pure (no APAP or Ibuprofen) Codeine, in pill form. Now, I want to stress that my body clears Suboxone out quickly (it's made life difficult when I was trying to stabilise a year and a half ago); for example, if I don't make sure I keep the subs in my mouth for long enough and spit out undissolved strips, I'm in withdrawals within about 8 hours or so.

    I took my last dose of 10mg at 12pm today. This should hold me until late tomorrow morning, but I'd rather not spend my flight in withdrawals.

    I want to stress that I don't want to get high -- I just want to hold myself over on the flight until I can get home and go to bed, then go to clinic as usual tomorrow morning.

    What is my best course of action here? I was thinking I'll take the codeine tomorrow morning (unsure of dose, I just want to not be in withdrawals if I can help it as I'm seeing and ex-girlfriend when I get back!), then once that has worn off and the WD's start tomorrow eveninig I'll take the 2mg (possibly snort it? or would orally be better here) to tide me over and let me sleep.

    Or is it better to try and reverse that? The only issue is I really don't want to take the codeine out of the country if I can help it; I have a letter for customs for my Suboxone, but not the codeine.

    Any help is greatly appreciated!
     

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    Interesting read, thank you! Its cool to see bupe in action.

    Naloxone did not affect the pharmacokinetics of buprenorphine and both SUBUTEX and SUBOXONE deliver similar plasma concentrations of buprenorphine. The levels of naloxone were too low to assess dose-proportionality. At the three naloxone doses of 1 mg, 2 mg, and 4 mg, levels above the limit of quantitation (0.05 ng/mL) were not detected beyond 2 hours in seven of eight subjects. In one individual, at the 4mg dose, the last measurable concentration was at 8 hours. Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose. Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.
    Naloxone did not affect the pharmacokinetics of buprenorphine and both SUBUTEX and SUBOXONE deliver similar plasma concentrations of buprenorphine.
    So, naloxone did not affect the Absorption of buprenorphine in either drug.

    Since they didn't ask about euphoria or side effects, this doesn't help us figure out what is going on in the receptors though, correct? I was told the receptors are invisible. (by an M.D)

    Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.
    It does help me understand how much naloxone is being absorbed in the bloodstream.

    Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose.
    As expected naloxone was detected in at least 7 of the 8 patients and the levels increased with dosage.

    RECEPTORVILLE WALL THEORY

    Quote Originally Posted by High Anxiety View Post
    The bupe/norbupe reaches the receptors first, therefore making the naloxone ineffective. So, bupe wins the race to receptorville and builds a wall that the naloxone cannot penetrate.
    UNIQUE OVERRIDE THEORY

    Quote Originally Posted by High Anxiety View Post
    I am starting to think the override theory might be more accurate. Meaning the naloxone does get to the receptors but the bupe whips its ass so fast its hard to notice. How fast the bupe does this would be dependent on the dose, person, and the bupe/naloxone ratio in the bloodstream.
    The higher % of naloxone vs bupe, the harder it would be to override.

    speculation ofc..
    The study seems to add credence to the idea that the naloxone would become more difficult to override for some people depending on the dose and the bupe vs naloxone ratio in the bloodstream. Therefore unique override theory is still a possibility...(I Hope)
    Last edited by Zerrr; 28-10-2013 at 11:04. Reason: fixed quote and 200th post!
     

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    Senior Moderator
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    Quote Originally Posted by C_Tripper View Post
    UNIQUE OVERRIDE THEORY



    The study seems to add credence to the idea that the naloxone would become more difficult to override for some people depending on the bupe/naloxone ratio. Therefore unique override theory is still a possibility..
    What part of the article did you get that from. I saw the ratio thing mentioned, but I interpreted it differently.

    In morphine-stabilized subjects, intravenously administered combinations of buprenorphine with naloxone produced opioid antagonist and withdrawal effects that were ratio-dependent; the most intense withdrawal effects were produced by 2:1 and 4:1 ratios, less intense by an 8:1 ratio. SUBOXONE tablets contain buprenorphine with naloxone at a ratio of 4:1 (source).



    Here they are talking about precipitated withdrawals and how different bupe/naloxone ratios effected it. I wish that they said what the doses were instead of just the ratios, because we don't know if the bupe doses were increased while the naloxone dosage remained the same, or vice versa. If think it's the former, and the withdrawals may not have been as intense at the higher dose since the bupe is able to fill the receptors after ripping the other opiate off, compared to lower doses that may just be enough to rip the other opiates off but not enough to take their place to relive the withdrawals.

    That's my interpretation of it. I still don't think the naloxone does anything in that case, and probably only would if the ratios were reversed. That's seen in cases of bupe overdoses when 4-8x the normal dose of naloxone is needed to remove the bupe from the receptors.
     

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    Here is more of that article. It is really interesting information- its also great to find information like this. Like I said above this group is not associated with the brand Suboxone. I know this is long but since my link didnt work here it is. Thanks for dissecting some of this! The chart at the bottom didnt copy correctly so FYI (im sure you all can figure it out but just in case) the dosing goes information is in increasing order.

    CLINICAL PHARMACOLOGY
    Subjective Effects:
    Comparisons of buprenorphine with full agonists such as methadone and hydromorphone suggest that sublingual buprenorphine produces typical opioid agonist effects which are limited by a ceiling effect.
    In non-dependent subjects, acute sublingual doses of SUBOXONE tablets produced opioid agonist effects, which reached a maximum between doses of 8 mg and 16mg of SUBUTEX. The effects of 16mg SUBOXONE were similar to those produced by 16mg SUBUTEX (buprenorphine alone).
    Opioid agonist ceiling effects were also observed in a double-blind, parallel group, dose ranging comparison of single doses of buprenorphine sublingual solution (1, 2, 4, 8, 16, or 32 mg), placebo, and a full agonist control at various doses. The treatments were given in ascending dose order at intervals of at least one week to 16 opioid-experienced, non-dependent subjects. Both drugs produced typical opioid agonist effects. For all the measures for which the drugs produced an effect, buprenorphine produced a dose-related response but, in each case, there was a dose that produced no further effect. In contrast, the highest dose of the full agonist control always produced the greatest effects. Agonist objective rating scores remained elevated for the higher doses of buprenorphine (8-32 mg) longer than for the lower doses and did not return to baseline until 48 hours after drug administrations. The onset of effects appeared more rapidly with buprenorphine than with the full agonist control, with most doses nearing peak effect after 100 minutes for buprenorphine compared to 150 minutes for the full agonist control.
    Physiologic Effects:
    Buprenorphine in intravenous (2mg, 4mg, 8mg, 12mg and 16 mg) and sublingual (12mg) doses has been administered to non-dependent subjects to examine cardiovascular, respiratory and subjective effects at doses comparable to those used for treatment of opioid dependence. Compared with placebo, there were no statistically significant differences among any of the treatment conditions for blood pressure, heart rate, respiratory rate, O2 saturation or skin temperature across time. Systolic BP was higher in the 8 mg group than placebo (3 hour AUC values). Minimum and maximum effects were similar across all treatments. Subjects remained responsive to low voice and responded to computer prompts. Some subjects showed irritability, but no other changes were observed.
    The respiratory effects of sublingual buprenorphine were compared with the effects of methadone in a double-blind, parallel group, dose ranging comparison of single doses of buprenorphine sublingual solution (1, 2, 4, 8, 16, or 32 mg) and oral methadone (15, 30, 45, or 60 mg) in non-dependent, opioid-experienced volunteers. In this study, hypoventilation not requiring medical intervention was reported more frequently after buprenorphine doses of 4 mg and higher than after methadone. Both drugs decreased O2 saturation to the same degree.
    Effect of Naloxone:
    Physiologic and subjective effects following acute sublingual administration of SUBOXONE and SUBUTEX tablets were similar at equivalent dose levels of buprenorphine. Naloxone, in the SUBOXONE formulation, had no clinically significant effect when administered by the sublingual route, although blood levels of the drug were measurable. SUBOXONE, when administered sublingually even to an opioid-dependent population, was recognized as an opioid agonist, whereas when administered intramuscularly, combinations of buprenorphine with naloxone produced opioid antagonist actions similar to naloxone. In methadone-maintained patients and heroin-dependent subjects, intravenous administration of buprenorphine/naloxone combinations precipitated opioid withdrawal and was perceived as unpleasant and dysphoric. In morphine-stabilized subjects, intravenously administered combinations of buprenorphine with naloxone produced opioid antagonist and withdrawal effects that were ratio-dependent; the most intense withdrawal effects were produced by 2:1 and 4:1 ratios, less intense by an 8:1 ratio. SUBOXONE tablets contain buprenorphine with naloxone at a ratio of 4:1.
    Pharmacokinetics:Absorption:
    Plasma levels of buprenorphine increased with the sublingual dose of SUBUTEX and SUBOXONE, and plasma levels of naloxone increased with the sublingual dose of SUBOXONE (Table 1). There was a wide inter-patient variability in the sublingual absorption of buprenorphine and naloxone, but within subjects the variability was low. Both Cmax and AUC of buprenorphine increased in a linear fashion with the increase in dose (in the range of 4 to 16 mg), although the increase was not directly dose-proportional.
    Naloxone did not affect the pharmacokinetics of buprenorphine and both SUBUTEX and SUBOXONE deliver similar plasma concentrations of buprenorphine. The levels of naloxone were too low to assess dose-proportionality. At the three naloxone doses of 1 mg, 2 mg, and 4 mg, levels above the limit of quantitation (0.05 ng/mL) were not detected beyond 2 hours in seven of eight subjects. In one individual, at the 4mg dose, the last measurable concentration was at 8 hours. Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose. Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.
    Table 1. Pharmacokinetic parameters of buprenorphine after the administration of 4 mg, 8mg, and 16 mg Suboxone® doses and 16mg Subutex® dose (mean (%CV)).
    Pharmacokinetic Parameter Suboxone®
    4 mg Suboxone®
    8 mg Suboxone®
    16 mg Subutex®
    16 mg
    Cmax, ng/mL 1.84(39) 3.0(51) 5.95(38 ) 5.47(23)
    AUC0-48,
    hour. ng/mL 12.52(35) 20.22 (43) 34.89 (33) 32.63 (25)
     

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    Naloxone did not affect the pharmacokinetics of buprenorphine and both SUBUTEX and SUBOXONE deliver similar plasma concentrations of buprenorphine. The levels of naloxone were too low to assess dose-proportionality. At the three naloxone doses of 1 mg, 2 mg, and 4 mg, levels above the limit of quantitation (0.05 ng/mL) were not detected beyond 2 hours in seven of eight subjects. In one individual, at the 4mg dose, the last measurable concentration was at 8 hours. Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose. Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.
    This shows that the naloxone had a very minimal impact on 7 of the 8 subjects.

    In one individual, at the 4mg dose, the last measurable concentration was at 8 hours.
    I assumed if he still had naloxone in his system after 8 hours, a higher concentration must have entered his system.

    Even if its a slow metabolism thing, this shows the naloxone effects some people very differently.

    So in this instance the bupe/naloxone ratio would be dependent on the individual and not the numbers on the package.

    Within each subject (for most of the subjects), across the doses there was a trend toward an increase in naloxone concentrations with increase in dose. Mean peak naloxone levels ranged from 0.11 to 0.28ng/mL in the dsose range of 1-4 mg.
    Its logical that an increase in dose would cause a higher concentration of naloxone in the blood, which is seemingly supported here.

    My overall conclusion would be:

    95-99% of people experience the receptorville theory (Theory #1)
    (or the "override" happens so fast you wouldn't really notice)

    People have reported a delayed onset from IV suboxone vs IV subutex.

    1-5% of people are very sensitive to naloxone and might react in a way closer to the Override Theory (Theory #2)

    Resulting in a longer duration before the bupe infiltrates and saturates all the receptors.

    This is entirely based on my own experience, others experience, and info I have access to.
    (grain of salt perhaps)

    Its a work in progress..

    EDIT:
    (I might have missed this part)

    Naloxone, in the SUBOXONE formulation, had no clinically significant effect when administered by the sublingual route, although blood levels of the drug were measurable. SUBOXONE, when administered sublingually even to an opioid-dependent population, was recognized as an opioid agonist, whereas when administered intramuscularly, combinations of buprenorphine with naloxone produced opioid antagonist actions similar to naloxone
    SL roa = recognized as an opioid agonist

    IM roa = produced opioid antagonist actions similar to naloxone

    In methadone-maintained patients and heroin-dependent subjects, intravenous administration of buprenorphine/naloxone combinations precipitated opioid withdrawal and was perceived as unpleasant and dysphoric. In morphine-stabilized subjects, intravenously administered combinations of buprenorphine with naloxone produced opioid antagonist and withdrawal effects that were ratio-dependent; the most intense withdrawal effects were produced by 2:1 and 4:1 ratios, less intense by an 8:1 ratio. SUBOXONE tablets contain buprenorphine with naloxone at a ratio of 4:1.
    IV roa = produced opioid antagonist and withdrawal effects that were ratio-dependent

    Last edited by Zerrr; 28-10-2013 at 11:21. Reason: ill get back to this SOT..
     

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