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    Bioavailability/Half-life MEGA Thread 
    #1
    Bluelighter lyserg's Avatar
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    Alright guys our mission is to make an informative list of all chemicals, anything you came up with's bioavailability for oral, rectal, IV, IM and intranasal. Alright so lets all do some research and come back and collaborate on what info we have. Ill report back shortly!

    All bioavailabilies are relative to IV bioavailability (100% ). For those that do not know, the bioavailability of a substance is basically the percentage of the dose that gets absorbed. It changes drastically for each method of administration. A half-life is the amount of time it takes for your body to eliminate half of the substance that you took. There is a lot of conflicting data on the exact bioavailabilities of each substance so every thing thats listed here is the average.

    Opiates
    Methadone: Oral 84%. Elimination half-life:24-36 hours,
    Ketobemiodone: Oral 34% +/-10%; Rectal 44% +/- 9%. Elimination half-life: 2.25- 2.45 hours
    Meperidine: Rectal 55%, IM 80-85% Elimination half-life 3.0 h
    Buprenorphine: Oral 22%; Sublingual 30%; IM 90-100%. Elimination half-life: 12-44 hours
    Hydromorphone: Oral-30-35%; Intranasal 52.4%; Rectal 33%
    Dihydrocodeine: Oral 20%. Elimination halflife 4 hours
    Heroin: Oral 35%; IM 85%
    Fentanyl: Transdermal 92%; Sublingual and Buccal 50%; Intranasal 70%. Protein binding 80-85% Elimination half-life 3-12 hours
    Sufentanil: Intranasal 78%,
    Remifentanil: Protein binding 70%. Elimination half-life 1-20 minutes
    Alfentanil: 92% Protein binding. Elimination half-life is 1.5-2 hours
    Morphine: Oral 30%; Rectal 30%; Intranasal 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- 55-70%
    Hydrocodone: Oral bioavailability is not really known but it is around oxycodone bioavailability; Orally 70% of it is usually absorbed, half-life is 4-8 hours
    Oxymorphone: Intranasal 43%; Orals 10-20%; Rectal 10%
    BUTORPHANOL : Oral 5-17%
    Tramadol: Oral 68-72%; Rectal 77%: Eliminatio half-life 5-7 hours
    Codeine: Oral 90%; Rectal 90%
    Diphenoxylate: Protein binding 74-95%. Elimination half-life 12-14 hours
    Pethidine(meperidine): Oral 50-60%. 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: Oral 20%. Half-life 2 to 3 hours

    Opiate Antagonists
    Naloxone: Oral 2-4%. Elimination half-life 1-1.5 hours
    Naltrexone Oral 5-40%. Protein binding 21%, Half life-4 hours (naltrexone),
    and 13 hours (6-β-naltrexol) (metabolite)

    Benzodiazepines
    Alprazolam: Oral 80-90%. halflife 9-20 hours
    Bromazepam: Oral 84% half life 10-20 hours
    Cinolazepam: Oral 90-100%, Half life 9 hours
    Clobazam: Oral 90%. Elimination half-life 18 hour half life
    Clorazepate: Oral 91%. Elimination half-life 36-100 hours
    Chlordiazepoxide: Oral 100%; IM 90-95%. Elimination half-lives of its metabolites range from 14—100 hours
    Clonazepam: Oral 90%; IM 93%
    Diazepam: Oral 85-100%. Protein binding: 94% to 99%
    Estazolam: Oral 93%. Elimination half-life 10-24 hours
    Lorazepam: Oral 85-90%; Intranasal 78%
    Midazolam: Oral 36-40%; Intranasal 55%, IM 90%
    Flurazepam: Oral 83%. Elimination half-life is 40-250 hours
    Temazepam: Oral 96%. Elimination halflife is 8-20 hours
    Quazepam: Oral 29-35% Half life 39 hours


    Other GABA acting drugs/ analogs
    Gabapentin (Neurontin): Oral: lower doses absorb better at 60% for .9g daily dosing; 27% for 4.8g daily dose. Food increases absorbtion by 14%. Protein binding 3%. Elimination Half life 5-7 hours
    Pregablin (Lyrica): Bioavailability 90%. Elimination Half life 5–6.5 hours
    Vigabatrin: Oral 80-90%. Elimination half-life 5-8 hours in young adults, 12-13 hours in the elderly.

    Buspirone:Oral 5%. Elimination half-life 2-3h

    Stimulants
    Methylphenidate: Oral 11–52%; Rectal is significantly higher, however an exact figure is not currently known. Elimination half-life 2–4 hours
    Cocaine hcl: Oral 30%; Intranasal 40-60%. Elimination half-life .8-4 hours (depending on MOA)
    Methamphetamine: Oral 62.7%; Intranasal 79%; Smoked 90.3%; 62.7%
    Amphetamine: Oral 4L/kg; low binding to plasma proteins 20% Elimination half-life 10–13 hours
    Ephedrine: Oral 85%. Elimination half-life 3–6 hours
    Dextroamphetamine: Oral 75%. Elimination half-life 10-28 hours
    Bupropron (Wellbrutrin: Oral 5-30%. Elimination half-life is 20 hours

    Dissociatives/psychedelics
    PCP: Oral 65%; Smoked 50%
    Ketamine's: Oral 207%; IM 93%; Intranasal 25-50%; IV dose 96% and oral dose 207%. Ketamine is rapidly distributed into brain and other highly perfused tissues, and is 12% bound in plasma. The plasma half-life is 2.3 0.5 hours.
    MDMA: Elimnation half-life of the "S" isomer has a shorter half life (about 4 hours), whereas the "R" isomer has a much greater half life. (about 14hours)

    Anti-depressants
    Tianeptine: Oral 89 +/- 11%. Elimination half-life 2.5 hours
    Trazodone: Oral 89 to 95%.

    Muscle relaxants
    Carisoprodol(soma): Oral 65%. 60% protein binding. Elimination half-life 8 hours
    Meprobromate: Oral 60% protein binding. Elimination half-life is 10 hours
    Baclofen: Protein binding 30%. Elimination half-life 1.5 hours
    Dantrolene: Oral 70%

    Sleep aids
    Zolpidem: Oral 67%. 92% is bound in plasma
    Zaleplon: Oral 30%. Elimination half-life is 1.1 hours
    Diphenhydramine: Oral 86%. Protein binding 98 to 99%. Elimination half-life 1-4 hours
    Eszopiclone (Lunesta): Protein binding 52-59%. Elimination half-life 6 hours
    Zopiclone: Oral 52-59%. Bound to plasma protein. Elimination half-life 6 hours, and 9 hours for over 65


    Barbituates
    Hexobarbital: Oral 25%. Protein binding
    Methohexital: Rectal 17%. Elimination half-life is 5.6 hours
    Phenobarbital: Oral 95%. Protein binding 20-45%. Elimination half-life is 53 to 118 hours
    Primidone: Oral 90%. Protein binding 70%. Elimination half-life of Primidone 5-15 hours, active metabolite (Phenobarbital) Elimination half-life- 100 hours
    Last edited by Tripman; 24-03-2012 at 12:50.
     

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    #2
    Bluelighter jasoncrest's Avatar
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    BENZODIAZEPINES:

    Routes of administration:

    -Orally
    All benzodiazepines can be taken orally, and have a great bioavailabilty this way.
    (exemple: Diazepam oral bioavailability:85-100%, Protein binding: 94% to 99% )

    -Rectally
    All benzodiazepines except Chlordiazepoxide, Clorazepate (and surely Loflazepate too) can be taken rectally, and have a great bioavailabilty this way.

    -Intranasal (snorted)
    Only the following water-soluble benzos can be effectively snorted: Flurazepam, Midazolam, Loprazolam.

    -Injection (IV/IM)
    Unless you have ampoules for injection, only the following benzodiazepines can be prepared for injection with water only:
    Flurazepam, Midazolam, Loprazolam.

    *Note on Loprazolam: it is not completely soluble, but water-soluble enough to be effective when snorted or injected; this is also because you need a low dosage (1mg).

    *Note on the inactive water-soluble benzodiazepines:
    Chlordiazepoxide, Clorazepate Dipotassium (and Ethyl Loflazepate too I think) are water soluble, but they are inactive benzos, and need to be metabolized by some enzymes in your stomach into active benzos to give an effect. So these benzos can only be taken orally.
    If injectable preparations of Clorazepate exist, it's because they contain a substance that makes the Clorazepate active.
    Last edited by jasoncrest; 18-08-2006 at 07:06.
     

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    #3
    dihydrocodeine 21% oral;
    methadone 80% oral/ nasal; 76% rectal;
    morphine 20-32% oral/ rectal; 10% nasal (non chitosan solution) 10% nasal (non chitosan solution) (2)
    hydromorphone 50.7% +/- 29.8% oral; 33% +/- 22% rectal; 54.4% - 59.8% nasal
    heroin 5% oral; 52% smoked
    codeine 90% oral; 90% rectal
    oxycodone 60 - 87% oral; 45% nasal, 50 - 60% nasal (2), 46% (2567% ) nasal (3); widely varies nasally (notes on 50 - 60% study); rectal the same as oral
    bupenorphine 15% oral; 31% sublingual; 90- 100% IM
    meperidine 80% to 85% IM

    cocaine 30% oral; 30-60% Nasal 57% Nasal (2); ~71% smoked
    methylphenidate 1152% (Oral); rectal is higher, but can't find a source
    methamphetamine 79% nasal; 90.3% smoked; 62.7% oral; "67% of the estimated delivered dose or 37.4% of the absolute (pipe) dose after smoking. "
    dextroamphetamine ~25% oral

    alprazolam 80-90% oral
    diazepam 90% oral/rectal
    clonazepam 90% oral
    lorazepam 90% oral; 77.7% nasal; 80% rectal
    midazolam 75% oral; 55% nasal; 80 - 100% IM

    phenobarbital 70-90% oral; 90% rectal

    EDIT- If anyone disputes any of these that I didn't link to, let me know and I'll find the source. There shouldn't be any that are unbelievable though.
    Last edited by Pegasus; 29-10-2006 at 02:42.
     

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    #4
    Bluelighter jasoncrest's Avatar
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    Diazepam: 85-100% oral
    Diazepam: 90% rectal

    Lorazepam: 78% intranasal
    Lorazepam: 90% oral

    (all the interesting papers concerning the bioavailability of benzos can be read only if you pay...)
     

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    #5
    What is the source (reference) of methadone oral 80%? I don't suspect its validity, just want to know where it's from... just beginning to slide in...
     

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    #6
    Bluelighter
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    I think adding references to the numbers given in this thread is going to become a neccessity when people start trying to 'dispute' them with heresay information they believe to be correct.

    Jasoncrest: I have a paper that documents case reports of nasal abuse of benzos, specifically alprazolam and diazepam. A full text of the paper can be found here , but is annoyingly spliced with adds and page breaks.

    Just because a benzo isn't water soluble, doesn't mean it can't be used nasally. Check out this thread, and this thread.
    Last edited by raybeez; 18-08-2006 at 19:13.
     

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    #7
    Bluelighter Gaz_hmmmm's Avatar
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    Lyserg and JasonCrest, when you's say diazepam has a protein binding of 94% -99% what do you's mean?
     

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    #8
    Bluelighter the unknown's Avatar
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    Oxycodone-oral 60-87%
    oxycodone intranasal- 70%
    oxycodone 60 - 87% oral; 45% insuffulated(source for people who doubt);
    THOSE ARE VERY CONFLICTING . I dont care who did the study or whatever there is no way its 45% because i feel just as high as i do when i eat them. And i can say the same for almost everyone else. Why would so many people snort OCs, if the bioavailability its almost have that of oral, i think all those junkies would notice. I would def notice if i snorted 10mg and it only turned out to be 5mg or so. Whether i eat 10mg or snort 10mg of oxycodone it feels exactly the same th eonly difference is onset. Im sorry but the 45% is bullshit, i have to go with lyserg all day.
     

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    #9
    Bluelighter jasoncrest's Avatar
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    Quote Originally Posted by Gaz_hmmmm
    Lyserg and JasonCrest, when you's say diazepam has a protein binding of 94% -99% what do you's mean?
    I don't know exactly what it means, I just know that the protein binding % of a substance can indicate how fast and strong it kicks in.

    Quote Originally Posted by Canis aureus
    What is the source (reference) of methadone oral 80%? I don't suspect its validity, just want to know where it's from... just beginning to slide in...
    Why? You think it's higher than 80% or lower? Methadone has a very high oral bioavailability, that's all I know....
     

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    #10
    Quote Originally Posted by Canis aureus
    What is the source (reference) of methadone oral 80%? I don't suspect its validity, just want to know where it's from... just beginning to slide in...
    It's on there now. There are a ton of sources saying 80%

    Quote Originally Posted by the unknown
    THOSE ARE VERY CONFLICTING . I dont care who did the study or whatever there is no way its 45% because i feel just as high as i do when i eat them. And i can say the same for almost everyone else. Why would so many people snort OCs, if the bioavailability its almost have that of oral, i think all those junkies would notice. I would def notice if i snorted 10mg and it only turned out to be 5mg or so. Whether i eat 10mg or snort 10mg of oxycodone it feels exactly the same th eonly difference is onset. Im sorry but the 45% is bullshit, i have to go with lyserg all day.
    Yes, well nasal administration varies quite a bit. 45 - 60% vs 60 - 87% isn't a difference I think most people would pick up on, especially with the oxy kicking in quite a bit faster through the nasal route.

    I dont care who did the study or whatever there is no way its 45% because i feel just as high as i do when i eat them.
    That's not very solid reasoning...
     

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    #11
    Bluelighter
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    Quote Originally Posted by jasoncrest
    I don't know exactly what it means, I just know that the protein binding % of a substance can indicate how fast and strong it kicks in.
    Protein binding refers to the fact that some drugs form complexes with blood/plasma proteins, effectively "removing" the free drug from the blood. As the initial free drug is metabolised, and the plasma concentration of the drug begins to drop, the protein-drug complexes dissociate, releasing the drug back into the blood.

    What does this mean? Compared to drugs with low protein binding, drugs that are highly bound by plasma proteins have much longer half-lives/duration of action, but 'peak' at a lower blood concentration.
     

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    #12
    Bluelighter hussness's Avatar
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    Anyone have a figure for bioavailability of insufflated methylphenidate?
     

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    #13
    ^I can't find anything but oral methylphenidate bioavailability, but I'm looking. I really want to know, too.
     

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    #14
    Bluelighter the unknown's Avatar
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    That's not very solid reasoning...
    Your absolutely right, its not solid reasoning. Tell me how the vast majority of people who use OCs snort them and feel it being equal to Oral. If the bioavailability was really that low then im sure the thousands of thousands of people who snort OCs whould realize it and no one would do it any more. I never ever heard anyone complain that they cant feel it as much when they snort it, as apposed to Oral. I just cant believe that study, im sorry. I have to agree with llysergs original bioavailability, it just makes sense.
     

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    #15
    It feels about the same in oral or nasal, nasal comes just quicklier. (OXY)

    You think it's higher than 80% or lower? Methadone has a very high oral bioavailability, that's all I know....
    I believe that i've been reading it could be higher, indeed 90%. And it feels high, hahah.
     

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    #16
    Bluelighter jasoncrest's Avatar
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    Quote Originally Posted by the unknown
    Your absolutely right, its not solid reasoning. Tell me how the vast majority of people who use OCs snort them and feel it being equal to Oral. If the bioavailability was really that low then im sure the thousands of thousands of people who snort OCs whould realize it and no one would do it any more. I never ever heard anyone complain that they cant feel it as much when they snort it, as apposed to Oral. I just cant believe that study, im sorry. I have to agree with llysergs original bioavailability, it just makes sense.
    Oxycodone could have a 100% oral bioavailability, and a 50% intranasal bioavailability, some people would still snort it, because it kicks in quicker and stronger.
     

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    #17
    Yep,

    I'm sort of man who would wait that hour, hour or two, if better bioavailability; like I'm doing, LOL. Some wants it fast, some counts on numbers...

    What would you do? (Addressed to all, just think, no need to answer!) Let's get back to availability...
    Last edited by Canis aureus; 18-08-2006 at 21:51.
     

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    #18
    Bluelighter lyserg's Avatar
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    Carisoprodol(soma)-oral- 65% 60% protein binding
    The plasma binding of PCP is 65%, smoked is 50%
    Ketamines Bioavailability following an intramuscular dose is 93%, intranasal dose 25-50%, and oral dose 20±7%. Ketamine is rapidly distributed into brain and other highly perfused tissues, and is 12% bound in plasma. The plasma half-life is 2.3 ± 0.5 hours.
     

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    #19
    Methadone is a synthetic opioid with potent analgesic effects. Although it is associated commonly with the treatment of opioid addiction, it may be prescribed by licensed family physicians for analgesia. Methadone's unique pharmacokinetics and pharmacodynamics make it a valuable option in the management of cancer pain and other chronic pain, including neuropathic pain states.
    http://www.aafp.org/afp/20050401/1353.html

    that source seems to rank morpphine to 26% oral, pretty low.


    BollWeevil and all,

    cocaine would be better in oral availablity, if mixed with sodium or lime...(?) and chewed (like leaf)... Wouldn't it be as high as in snorted, or still higher? I'm thinking about that that several sources says that all oral coke should be absorbted via mouth mucouses and based.
     

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    #20
    lyserg, where did you get that 70% figure for oxycodone insuffulated?
     

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    #21
    Bluelighter lyserg's Avatar
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    Quote Originally Posted by BollWeevil
    lyserg, where did you get that 70% figure for oxycodone insuffulated?
    http://www.ncbi.nlm.nih.gov/entrez/q...=pubmed_docsum

    It says 'The intranasal bioavailability of oxycodone was 0.46 +/- 0.34.' So its anywhere from 46%-80% so 70s somewhere in the middle.
     

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    #22
    ^That means its 46% + or - 34%... 46 is right in the middle.

    I posted a few sources that put it at 45 - 46% too.

    Just FYI.
     

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    #23
    Bluelighter lyserg's Avatar
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    Quote Originally Posted by BollWeevil
    ^That means its 46% + or - 34%... 46 is right in the middle.

    I posted a few sources that put it at 45 - 46% too.

    Just FYI.
    Yes but those sources are wrong. The effect people get from intranasal oxycodone speaks for itself. Its 60-70%. Anyway anything anyone adds im gonna add them to my 2nd post in the thread along with everyone on there now. Please take your time and try to make it accurate. After we get all the bioaavailabilities down im gonna do halflife for all of them also but you guys dont gotta do that, just keep finding percentages of bioavailability and this thread will turn into a very successful sticky at the top of the page
     

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    #24
    Bluelighter the unknown's Avatar
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    The effect people get from intranasal oxycodone speaks for itself.
    Thank you, if it was really that low, everyone would notice. And since theres so many junkies out there, and the vast majority insuffulate crushed oxycodone ER, the effects speak for itself.

    There is no way in hell i would not notice, that low bio. Its like insuffulating 20mg would only feel like 10mg. And i would notice that, since i do take IR pills, i know what 10mg feels like and what 20mg feels like.

    Oxycodone could have a 100% oral bioavailability, and a 50% intranasal bioavailability, some people would still snort it, because it kicks in quicker and stronger.
    I dont get it, if its stronger that would mean that it would have a high bioavailability. Or could that just mean it feels stronger but for a shorter duration of time, so the bioavailability could be lower, but the "high" feels the same or stronger because its compacted into a shorter amount of time.
    I still however do feel euphoric from 45-60 minutes whether its nasal or PO.
    But that would make sense if im right.

    Can you explain JasonCrest

    Thanks buddy, that post got me to think
    Last edited by Captain.Heroin; 29-11-2010 at 13:35.
     

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    #25
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    40-50 percent rectal admin bioavailablity for Oxycodone? Thats bullshit, it should be 90-100 percent, its 30 percent more bio then oral route. As stated in the 2006 PDR.
     

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