Opiate Bioavailabilities

Discussion in 'Opiates & Opioids' started by Forthesevenlakes, Sep 14, 2006.

  1. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    The bioavailability of a drug is the percentage of the drug that makes it from the route of administration into the bloodstream. Intravenous administration of a drug means that all of the drug is put directly into the blood, so the bioavailibility of IV is always 100%. With other routes (oral, insufflated/snorting, rectal, etc.), less of the drug reaches the blood due to incomplete absorption, metabolism in the liver before reaching the blood, etc. By knowing the route of administration You plans to use for a drug, and its dosage, You can estimate about how much of it will make it into the blood, and thus be available for the brain.

    This thread will be a place to post bioavailabilities of opiates through different routes. Please cite sources when you contribute to this thread, and as I re-find the sources I used to make this I'll add them as links to the percentages!

    Buprenorphine
    Oral: 15%
    Sublingual: 30%-50%
    Intramuscular: 68%

    Codeine
    Oral: 60-90%
    Rectal: about 90%

    Dihydrocodeine
    Oral: 20%

    Fentanyl
    Oral: 30%
    Buccal: 50% (absorbed through the mouth lining, not swallowed)
    Transdermal: 92%

    Heroin
    Oral: 35%
    Smoked: 52%
    Intramuscular: 85%

    Hydrocodone
    Oral: 50-60%

    Hydromorphone

    Oral: around 51.35%, some reports say 10-65% but this range is awfully wide.
    Intranasal: 54.4%
    Rectal: 36.33, up to 60% in the source I used.

    Meperidine
    Oral: 50-55%
    Rectal: 55%
    Intramuscular: 80-85%

    Methadone
    Oral: 70%-80%

    Morphine

    Oral: 40%
    Insufflated: 10% alone, 60% with a chitosan solution. But I think this number should be higher. Can anyone find any articles that give alternative measures?
    Intramuscular: 70-70% estimated
    Rectal: 70-90% One study says 27% in a parental solution, however!
    Subcutaneous: 60%

    Oxycodone

    Oral: 60-87% (due to low first-pass metabolism).
    Insufflated: One study says 45%. However anecdotal evidence says that it may be higher than this number.
    Rectal: 61.6% in one study.

    Oxymorphone
    Oral: 10-20%
    Insufflated: ~40%

    Pentazocine
    Oral: 20%

    Propoxyphene
    Oral: 30-70% (This is quite a wide range. SWIM suspects its closer to 30% but has no other sources at the moment to confirm this.)

    Tramadol
    Oral:70%

    more to come later, please contribute if you have any info! Also keep in mind that everyone's body is different, and may metabolize and absorb drugs in different ways. These numbers are averages, so your milage may vary.
     
    Last edited by a moderator: Mar 31, 2011
  2. bob78

    bob78 Silver Member

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    I would say Morphine's bioavailibility is quite high when insufflated, I think there is quite a difference compared to being taken orally.
     
  3. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    yes, I has heard that it can increase the bioavailability of it from 3 to 6 times that of oral. chitosan, a type of polysaccharide, can apparently potentiate this but i dont have a source to confirm this at the moment.

    I am interested in finding bioavailabilities for heroin through the insufflation and smoking routes. can anyone find these?

    also if you swims out there know any bioavailabilities for opiates i dont have up there, please help out and post them here!
     
  4. Riconoen {UGC}

    Riconoen {UGC} Newbie

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    I am pretty sure the bioavailability of hydrocodone through insuffulation is damn near zero but this is from personal experience. swim wiull try to find some sources erowid may have some.
     
  5. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    snorting vicodin is not very efficacious because of the huge amounts of acetaminophen and fillers in them, if thats what You has tried. pure hydrocodone, as obtained from a CWE and evaporating the water at the end, may have better bioavailability. or that bioavailability figure might only be for a certain salt of hydrocodone, and You had a different form of it. thanks for looking for others, post them if You finds any!
     
  6. DrMuffy

    DrMuffy Silver Member

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    I found a legitimate site which posted the bioavailability for rectal morphine doses, and the bioavailability is are somewhere between 70-90% Its because in your anal cavity or whatever u call it, has 1000 of veins to suck up the Morph, compared to hundred in your nose. I hope i helped
     
  7. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    This logic makes sense. Absorption does tend to be better in the anal cavity for most drugs. I am going to change the rectal bioavailability accordingly and look up that source for himself. His initial search yielded the 10-30% which did sound too low. Thanks!!
     
  8. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    What other bioavailabilities should be included? Also, I am having trouble locating bioavailibilities for non-oral routes of administration for hydrocodone and tramadol. If anyone could help, itd be much appreciated!
     
  9. Sklander

    Sklander Silver Member

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    I think the bioavailability of Hydromorphone via rectal administration is higher than 36%... Probably in the 70% - 90% range, I would imagine.

    Anything taken rectally is going to have a substantially higher percentage of absorbtion compared to oral ingestion.
     
  10. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    So true, swiSklander. I am honestly wondering why he's getting such low numbers for the rectal route on his searches. Later today he'll look for another source to confirm swiy's report, and he'll add in this number right now. Thank you!
     
  11. Fantasian

    Fantasian Gold Member

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    IM morphine is slightly less than that of IM Diamorphine.

    SWIF would estimate at 70-77%
     
  12. pokeymcsmot421

    pokeymcsmot421 Newbie

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  13. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    I think its came from people using the chitosan solution. But other things I've read state that its always about 6 times more bioavailable nasally than orally. Certainly the nasal route should be higher than the oral route. I'm starting to think its somewhere around 30%, but not sure. I want to find a non-chitosan paper that gives its bioavaliability.
     
  14. pokeymcsmot421

    pokeymcsmot421 Newbie

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    i think it would also be interesting to see what peoples first hand opinion/experiences are.

    I has done morphine both orally and insufflated many manny times and it always works better when he insufflates, beyond placebo. But data is data.

    also Swim thinks oxy insufflated works far better than oral and the data goes against that.

    swim seems to feel theres some conflict between what should get someone more fuckd up and what actually does.

    time of onset and intensity both could be major factors, as could placebo and ritual.

    p.s. props for puttin a bioavailability thing together, good shit man.
     
  15. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    it should more be said that "some data goes against that"...different studies could show that the nasal data is correct, and the oral data is too high. I am wondering what it is about chitosan that could increase the insufflated bioavailability by six times though, thats impressive.

    and the nature of the opiate itself, as well of time of onset and intensity could all contribute to what SHOULD work and what DOES work. set and setting play a huge role in this too.
     
  16. Citizen Kane

    Citizen Kane Newbie

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    @Forthesevenlakes: Very interesting pieces of information. Thanks for those. What are your sources if I may ask?
     
  17. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    all types of research papers. I was using google alot. I hope to get an actual chart with many different types from some kind of publication, but so far I've just had to search drug by drug.
     
  18. Fantasian

    Fantasian Gold Member

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    FTSL - Im sure that the bioavailablity for Buprenorphine isnt correct. I have no idea on the exact bioavailablities but there is definately a bigger margin from swallowed buprenorphine to sublingually taken buprenorphine.
     
  19. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    I just work with what the research papers give me...I believe you, certainly, so if anyone can come up with a more realistic figure let me know.
     
  20. allyourbase

    allyourbase Palladium Member

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    I am not sure about the scientific figures of bioavailability regarding morphine. SWIM can tell you this much. 90% is lost orally we all know this, one can eat a gram of opium and its ~ 8-9 mg of morphine on the brain. enough to feel, not enough to enjoy so much. now I know from my experience that one can take two thirds this, ingest it sublingually (again as latex) and it feels ~ like eating a gram. I have snorted MS contins. I had to snort 60 mg (!) to feel it at all. now by this "60% insufflated bioaivalability" qoute given above thats approx 24 mg on the brain. sure as HELL didnt feel like it, so SWIM must agree to disagree with those figures. these rascally ultra tertiary opiates. theyve been identified too long by our bodies as a poison and weve as a genetic whole built up this enzymatic tolerance to them. perhaps the best answer is to block the mitochrondrial enzymes destroying yous morphine in the first place???? ahh forgot to read the base topic. I do find that insufflation of dilaudid (that is hydromorphone bitartrate[[email protected] tartrate]) is approximately 1.25 times as effective as swallowing the pills.
     
    Last edited: Oct 7, 2006