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Thread: Opiates and Opioids Bioavailability and Half-life Thread

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    Opiates and Opioids Bioavailability and Half-life Thread

    on a quick search I noticed there wasn't a bioavailability thread for opiates and opioids, which I believe should be a sticky. if anyone has different information, additional information, or wants to correct something they should post it here. I've taken this info from bluelight but have corrected a few things.
    Methadone-oral 80-90%, halflife- 24-36 hours, rectal 76%
    Ketobemiodone oral was 34% +/-10%, rectally 44% +/- 9%, half-life is 2.25- 2.45 hours
    Meperidine rectal bioavailability is approximately 55%, 80% to 85% IM, elimination half-life 3.0 h
    Buprenorphine highly protein bound 96%, sublingual bioavailability is approximately 30%, oral is 15-22%, 90-100% IM, elimination half-life is 12-44 hours
    Hydromorphone-- 5-8 times as potent as morphine, intranasal- 52.4%, Rectal administration 33% ,Oral-30-35%, (also reported as 50.7% +/- 29.8% oral; 33% +/- 22% rectal; 54.4% - 59.8% nasal)
    Dihydrocodeine oral-20-21% halflife 4 hours
    Heroin oral ~35% IV- 100% IM-85% Smoked (or vaporized?) 52-55% vaporized Semisynthetic derivative, Intranasal 44-61%
    Fentanyl- Bioavailability 92% (transdermal), 50% (sublingual/ buccal (against cheek), Protein binding 80-85%, half-life 3-12 hours
    Sufentanil intranasal bio- 78%,
    Remifentanil Protein binding 70% (bound to plasma proteins) Half life 1-20 minutes
    Alfentanil- IV ~100%, 92% protein binding, half life is 1.5-2 hours
    Morphine ~32% oral/rectal, insuffulated- 15-20%, Chitosan(a linear polysaccharide that helps absorb drugs better) has been shown to increase nasal bioavailability of morphine from around 10-20% to over 60%, SC-60%, protein binding 30-40%, half-life is 2-3 hours
    Oxycodone-oral 60-87% intranasal- widely varies 45-70%
    Hydrocodone- oral bioavailability is not really known but it is around oxycodone bioavailability, ~70% of it is usually absorbed, half-life is 4-8 hours
    Oxymorphone nasal bioavailabilty [43%] orals low 10-20%
    Butorphanol -oral 5-17% due to high first pass metabolism
    Tramadol- the absolute bioavailability of rectally admistered tramadol in the suppositories was 77.0%, Oral-68-72% (Increases with repeated dosing) Half life 5-7 hours
    Codeine- following rectal or oral administration with a systemic availability of about 90%; in one study clearance varied 4-fold and systemic availability after oral dosage was between 50 and 84%
    Diphenoxylate Protein binding 74-95% Half life 12-14 hours used for diarrhea, (does not appreciably cross the blood-brain barrier)
    Pethidine(meperidine) Absorption Oral bioavailability is 50-60% in patients with normal hepatic function. IM 80-85%, Protein Binding 65-75%, Half Life 3-5 hours
    Normeperidine is about half as potent as meperidine, but it has twice the CNS stimulation effects.
    Pentazocine- Bioavailability ~20% orally, Half-life 2 to 3 hours

    Opiate Antagonists
    Naloxone oral- 2-4% (90% absorption but high first-pass metabolism), Half life 1-1.5 hours
    Naltrexone Oral Bioavailability 5-40%, Protein binding 21%, Half life-4 hours (naltrexone),
    and 13 hours (6-β-naltrexol) (metabolite)
    Last edited by JonnyM; 09-02-2009 at 10:39 PM.
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    OpioNoMo dalottafun is a total asshat.
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    Default Re: Opiates and Opioids Bioavailability Thread

    very noice - props i can really use this thank you

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    Default Re: Opiates and Opioids Bioavailability Thread

    This is a very useful thread. I agree if should be a sticky.

    Thanks for the info.

    1der

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    Default Re: Opiates and Opioids Bioavailability Thread

    Is it just me or was all this stolen from bluelight lmao
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    Default Re: Opiates and Opioids Bioavailability Thread

    did you not read
    I've taken this info from bluelight but have corrected a few things.
    ?

    also it would be cool if a moderator could change the thread title to Opiates and Opioids Bioavailability and Half-life Thread.
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    Default Re: Opiates and Opioids Bioavailability Thread

    For noobs like me, you may want to consider adding "pure" to the list...for, as I understand it, bioavailability is a different game when considering pills made for oral use, etc.

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    Default Re: Opiates and Opioids Bioavailability & Half-life

    Dude wonderful thread.....long time user first time writer! Does anyone know where I can find the comparison chart for all the the different opiates. It uses a 1mg shot of IV Morphine as a base for comparison......any use would be helpful. Please don't consider this a thread jack.
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    Default Re: Opiates and Opioids Bioavailability & Half-life

    Quote Originally Posted by shag1233 View Post
    Dude wonderful thread.....long time user first time writer! Does anyone know where I can find the comparison chart for all the the different opiates. It uses a 1mg shot of IV Morphine as a base for comparison......any use would be helpful. Please don't consider this a thread jack.

    I believe such a thread is on the site. Where? Got me, ya gotta search.
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    Default Re: Opiates and Opioids Bioavailability & Half-life

    Does anyone know where I can find the comparison chart for all the the different opiates.
    The opiate dose converter I use is:
    http://www.globalrph.com/narcotic.cgi

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    Default Re: Opiates and Opioids Bioavailability & Half-life

    Sentinel Fit Rate

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    Default Re: Opiates and Opioids Bioavailability & Half-life

    Rectal bioavailability is low in people who are not cleared out down there before the dose is plugged. In people who are cleared out down there, rectal bioavailbility is most often almost as good as IM injections.

    Most likely the 8 people on the rectal hydromorphone bioavailability study weren't all cleared out when they were given their dose.

    Also even though that study found the average oral hydromorphone bioavailability was 51.35%, the range was +/- 29.29%. This meant that one person had an oral bioavailibility of 80.64%, and another had an oral bioavailibility of 22.06%.

    The figures on that study for rectal hydromorphone bioavailability was 36.33%, the range was +/- 29.60%. This meant that one person had an rectal bioavailibility of 65.93%, and another had an rectal bioavailibility of 6.73%. The 6.73% figure was so low, because the vast majority of the drug was soaked up into feces.

    So you can't just read oral bioavailibility = 51.35% and rectal bioavailibility = 36.33% and think that that's the figure for everyone, every single time they take it.

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    Icon6 Re: Opiates and Opioids Bioavailability & Half-life

    This thread is a god-send. I'm stickying it to my favorites bar on all my browsers! Nice job!
    with that, I would like to contribute one item if I may:

    Tapentadol Bioavailability
    (as taken from various google sources by sourcecod)
    (feel free to append/correct as needed)

    • IV: 100%
    • Nasal: No Data yet (burns)
    • Buccal: 0% (?really?)
    • Oral: 32% to 42%, half life: 4.5 hours
      31.9 6.8% (wiki for oral)
    • Plugging: No Data yet
    Side Notes:
    • Don't take more than 700mg EVER! :eek:
    • Avoid snorting, the burn is horrible.
    • 100mg is enough to feel decently fucked up by a noob.
    • 200mg is enough to feel decently fucked up by a regular opiophile.
    • People have reported seizure like shit as low as 300mg and up
    • also Xanax allegedly helps with preventing falling out or doing the "fish dance" on the floor. :cool:
    • Street prices seem to be about ten cents per milligram MAX. anything more is highway robbery. :wink: (Less is preferable)

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