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Thread: Enzymes (eg CYP2D6/CYP3A4) and Inhibitors/Inducers

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    #26
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    if you take Quercetin (CYP3A4 inhibitor)
    would that render contraceptive pill useless? considering the pill requires that enzyme to metabolise?

    also what will happen to the high of MDMA when taken with CYP3A4 inhibitor?
    Last edited by Advanc3d; 11-08-2008 at 07:31.
     

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    #27
    ^
    Yup, I remember the Ki values@MOR for bupe is 0.7nM and for nor-bupe, 0.8nM
     

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    #28
    Quote Originally Posted by Advanc3d
    also what will happen to the high of MDMA when taken with CYP3A4 inhibitor?

    MDMA is first metabolized by CYP3A4 (N-demethylation) to MDA.
    Both are then metabolized by CYP2D6.

    There are other enzymes involved in this, although 2D6 is the primary enzyme for metabolizing MDMA. I suspect taking MDMA with a 3A4 inhibitor may not make that much of a difference.
     

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    #29
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    Quote Originally Posted by aj1976
    MDMA is first metabolized by CYP3A4 (N-demethylation) to MDA.
    Both are then metabolized by CYP2D6.

    There are other enzymes involved in this, although 2D6 is the primary enzyme for metabolizing MDMA. I suspect taking MDMA with a 3A4 inhibitor may not make that much of a difference.
    MDA is neurotoxic metabolite of MDMA though, guessing inhibiting its production is a plus?
    i would i thought CYP3A4 inhibitation with MDMA will make the high last longer


    actually, i just picked this up from wikipedia

    Because the enzyme CYP2D6 is deficient or totally absent in some people[80], it was once hypothesized that these people might have elevated risk when taking MDMA. However, there is still no evidence for this theory and available evidence argues against it.[81] It is now thought that the contribution of CYP2D6 to MDMA metabolism in humans is less than 30% of the metabolism. Indeed, an individual lacking CYP2D6 was given MDMA in a controlled clinical setting and a larger study gave MDMA to healthy volunteers after inhibiting CYP2D6 with paroxetine. Lack of the enzyme caused a modest increase in drug exposure and decreases in some metabolites, but physical effects did not appear appreciably elevated. While there is little or no evidence that low CYP2D6 activity increases risks from MDMA, it is likely that MDMA-induced CYP2D inhibition will increase risk of those prescription drugs that are metabolized by this enzyme. MDMA-induced CYP2D inhibition appears to last for up to a week after MDMA exposure
    Last edited by Advanc3d; 12-08-2008 at 03:42.
     

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    #30
    Quote Originally Posted by Advanc3d
    if you take Quercetin (CYP3A4 inhibitor)
    would that render contraceptive pill useless? considering the pill requires that enzyme to metabolise?
    I don't know if oral contraceptives are metabolized through this pathway but IF SO, then:
    The contraceptive pill wouldn't be totally useless. But the possibility of a failure of protection is increased. The term "to render it useless" implies for me the total failure with the majority of affected women. This is not the case here. It is rather like a higher percentage of pregnancies occur when taking respective CAP-inhibitors.

    In my place, Hypericum perforatum (ENG: St. John's wort; GER: Johanniskraut; FR: Millepertuis perforé) is a light OTC-antidepressant with exactly this side-effect. Ouch!

    Peace! Murphy
     

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    #31
    ^^Hypericum perforatum is a CYP3A4 inducer not inhibitor, no?

    Peace
    J
     

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    #32
    Indeed it is. This means the contraceptive's half life is significantly reduced, so plasma level of it are decreased, and contraceptive reliability falls. If however it were a prodrug then yeah we'd be concerned with inhibition more.
     

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    #33
    Thought so, as a long term user of Xanax for panic disorder i started to use St. John's wort to se if it would help. Nope, had to increase my Xanax dose by 50%.
    J
     

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    #34
    Oh!! Of course. Sorry for the confusion!
     

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    umm??? 
    #35
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    guys so i have cilostazon and chlorpramazine i wanna do it wit suboxone ??? so what one do i use to make it stronger?? im confused
     

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    #36
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    cilostazol
     

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    #37
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    no one will prob ever look at this but ne way the cilostazol is for poor blood circulation kk and the promazine is a old drug from the 50s so how are there gonna do ne thingf to suboxone? or any opiate for that matter???? pls teach me how lol
     

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    #38
    A molecule can act as both an inhibitor and modification product for an enzyme if it has a strong binding capacity for the binding pocket, but a reduced ability to undergo the reaction mechanism the enzyme catalyzes. Hence it is an inhibitor because it is slow to react with the enzyme compared to other substrates, and this can be readily detected in vitro with or without sufficiently detailed analysis to figure out what is truly going on.

    I believe the OP was asking about this as well? I don't know of any other way for it to happen, although I am not directly familiar with the data for codeine and other molecules on this issue. It is an interesting concept however...
     

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    #39
    I'm on Metronidazole as of today for an infected wisdom tooth, taking it three times a day, but I would like to drop 1 or 2 pills at a rave this Saturday...

    Could anyone explain the risks involved for me? Would it have a serious effect on my treatment if I didn't take any doses for all of Saturday day, but start again on sunday morning / when coming down?

    Lets say I take my last dose at 6 - 7 PM on the Friday, and drop pills at the rave at say 1 - 2 am, and have Sunday's first dose of Metronidazole at 8am?
     

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    #40
    [B]BUMP BUMP BUMP//// Now i was hoping that people could talk to me about how all this information relates to suboxone does anyone have any information of BUPE and how to increase the level Of NOR BUPE and if this is safe extra for someone who is on a mataince of bupe and takes it daily tryin to cop a free high ???
    Last edited by vecktor; 21-10-2010 at 23:11.
     

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    #41
    So no one has any clue about this topic is what i m guessing ????
    Last edited by vecktor; 21-10-2010 at 23:12. Reason: color doesn't show up very well on my CGA monitor
     

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    #42
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    I've read plenty on these forums re: "since bupe metabolizes to norbupe which is a full vs. partial mu agonist would it be viable to induce bupe with the goal of increasing the high?" The wall, so to speak, is that the affinity of bupe is SO high it would negate increasing norbupe... if it weren't so high, IV Suboxone would have the effects the manufacturer advertised, whereas we all know any ROA works.

    Then there's the issue that you're on maintenance, as someone who's also been on Sub maint for the last 22 mos, if you're taking 16mg SL then considering the ceiling dosage is 32mg chances of getting high are almost nill, anything that you do achieve will be negligable as with bupe, truly "less is more"...
    I've both plugged and IV'ed enough to intentionally hit that ceiling; one must be on a lower dose to feel anything resembling an opioid high (e.g. my first 6 mos on maint [I snorted it to increase BA and onset as although I'd figured out a great alcohol SL method b/f ever seeing one on here, said method lacked the subjectivly quick onset] I'd take 4mg day 1, next day 8mg, then none, repeat cycle with the longest number of days on Sub being 4 and detox periods up to 48+hrs). However, until recently I could go up to 72 hours abstinent- I begin W/Ds at hr 36- then either dose a full agonist which would get me high or dose bupe: Despite the amount or the ROA, all the bupe did for me after all that time was alleviate W/Ds, and not even the alleviation with euphoria that I used to experience after a mere 36 hr detox during that 1st 6 mos of maint. Only reason it's different now is that I've tapered down

    The above is almost tangential/a sidenote, my actual response is:
    Go do an Advanced Search and restrict it to the Other Drugs forum, the answer will likely be in the Suboxone/Buprenorphine Megathread and FAQ v9.0
    That way you need not read every page, although skimming through it will likely prove both informative and enjoyable, plus CH did an excellent job: info is highly accessible with JC's BA contingent on ROA being one of the first things you see, the FAQ, and the Mega Thread Directory which links to great stuff
    http://www.bluelight.ru/vb/showthread.php?t=524458

    Actually, I just looked at the thread and I guess you did search or find it sitting near the top of OD as you're the first post after CH's initial 4, hehe
     

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    #43
    Quote Originally Posted by MattPsy View Post
    Really? Hmmmmmmm. Thanks. I'll look more into that.
    I apologize but you're incorrect about grapefruit juice being a CYP3A4 inducer. Might want to check even common knowledge before you post something like that on here and spread misinformation. This is a harm prevention board and the spread of misinformation in a place like this is downright dangerous. It obviously isn't so much that your specific response was dangerous, but that an incorrect response, or heck even the right response, taken out of context, can be dangerous or even lethal.

    Let's keep harm prevention in mind here guys. Thanks.
     

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    #44
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    Quote Originally Posted by JASS92 View Post
    I apologize but you're incorrect about grapefruit juice being a CYP3A4 inducer. Might want to check even common knowledge before you post something like that on here and spread misinformation. This is a harm prevention board and the spread of misinformation in a place like this is downright dangerous. It obviously isn't so much that your specific response was dangerous, but that an incorrect response, or heck even the right response, taken out of context, can be dangerous or even lethal.

    Let's keep harm prevention in mind here guys. Thanks.
    Oh ffs and I've already downed a liter of pink grapefruit juice now. shouldve kept reading... (im entirely serious btw lol)
     

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    #45
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    So would cimetidine make hydromorphone last longer or feel stronger?I think i felt like it brung the nod back for me.but im not sure if it lasted longer or not.
     

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    #46
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    It might make it last longer, but probably won't make it feel any better - hydromorphone is already very active and has active metabolites.
    Guidelines for OD ||| OD Standards ||| OD Directory Read Me First! ||| NPD Rules
    Please read the links above or PM me if I lock your post. R.I.P. F28
     

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