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    Antacids and opioids (percocet) 
    #1
    As a pain patient who has started to develop a tolerance to my 10/325 percocets (every 6 hours), I have a few questions.

    Other than CYP3A4 inhibitors (cimetidine and grape fruit seed extract, which I take 45mins before dosing), I am looking for another potentiator. Now, what is the pharmacological/physiological reason for taking antacids, and does it apply to Percocet in particular?

    It's my understanding that oxycodone is in the form of a hydrochloride salt. What effect would antacids have other than lowering the ph of the stomach? If I'm correct, very little (if any) of medications can be absorbed in the stomach itself, so is the idea to 'protect' the drug from acidic PHs? I can't find any information that acids harm oxycodone...

    I mean, after all, oxycodone is combined with an acid.


    Also, isn't cimetidine an antacid itself? If I'm taking that (400-600mg every 6 hrs) then why take tums?

    Thanks!
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    #2
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    An anta-acid is just a property of a drug not a classifcation, just like saying sedative, or anxiolytic, anti-convulsant, etc. So you need to be more precise in that respect.

    Cimetidine stops acid secretion by binding to H2 receptors in the stomach, much like ranitidine. Both can be classified as H2 antagonists.

    Tums is calcium carbonate. When calcium carbonate interacts with stomach acid, it neutralizes the acid and balances the pH in the stomach by increasing alkalinity.

    How neutralizing stomach acid could affect opioid metabolism I don't know, but if anything I would guess they would slightly decrease absorption since these drugs maybe somewhat dependent on non-neutral ph to be broken down.
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    #3
    Quote Originally Posted by Chromophobia View Post
    An anta-acid is just a property of a drug not a classifcation, just like saying sedative, or anxiolytic, anti-convulsant, etc. So you need to be more precise in that respect.

    Cimetidine stops acid secretion by binding to H2 receptors in the stomach, much like ranitidine. Both can be classified as H2 antagonists.

    Tums is calcium carbonate. When calcium carbonate interacts with stomach acid, it neutralizes the acid and balances the pH in the stomach by increasing alkalinity.

    How neutralizing stomach acid could affect opioid metabolism I don't know, but if anything I would guess they would slightly decrease absorption since these drugs maybe somewhat dependent on non-neutral ph to be broken down.
    I understand that they have different mechanisms of action for the same effect, which is why I was wondering if something like calcium carbonate or magnesium carbonate (ie. Tums) would be of any benefit and if so, why/how since I'm already taking an antacid in the form of an H2 antagonist
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    Bluelighter Swimmingdancer's Avatar
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    Quote Originally Posted by Chromophobia View Post
    Tums is calcium carbonate. When calcium carbonate interacts with stomach acid, it neutralizes the acid and balances the pH in the stomach by increasing alkalinity.

    How neutralizing stomach acid could affect opioid metabolism I don't know, but if anything I would guess they would slightly decrease absorption since these drugs maybe somewhat dependent on non-neutral ph to be broken down.
    It's my understanding that it's the reverse, that opioids are better absorbed in a less acidic stomach, so calcium should help, but it might depend on the opioid. I will try to find some sources, I'm sure I read that somewhere science-y
    Last edited by Swimmingdancer; 03-02-2013 at 00:33. Reason: meant to say "less", not "more less" lol
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    #5
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    ^ Honestly I was just as guessing as I said. Opioids themselves raise gastric pH. Also that many extended release preparations are pH dependent/independent. Which means they're specifically designed (particular to the drug of course) to bypass the stomach and disintegrate in the liver vice-versa.

    Opioids are absorbed by the stomach and chiefly metabolized by the liver which has high pH of ~6.8 as opposed to a pH of between 1-2.0 for the stomach. So this is what I was going by.

    I found this to back up what your saying though so my guess is seemingly wrong:

    In the acidic environment of stomach, opioids are highly ionized and therefore poorly absorbed.
    http://update.anaesthesiologists.org...armacology.pdf

    In essence antacids such as calcium carbonate raise stomach pH therefore lowering acidity. So going by this, antacids should actually increase absorption, to which degree I have not been able to find.
    Last edited by baooozs; 02-02-2013 at 22:39.
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    Bluelighter laCster's Avatar
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    In my honest opinion and experience, adding Tums or anything else to raise the ph of the stomach to produce a higher BA is a hoax. I have tried and never notice a difference to be honest. On the other hand, I can definitely feel more pronounced effects on tagamet which coincides with the theory of potentiation via inhibition of hepatic enzymes.
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    #7
    Quote Originally Posted by laCster View Post
    In my honest opinion and experience, adding Tums or anything else to raise the ph of the stomach to produce a higher BA is a hoax. I have tried and never notice a difference to be honest. On the other hand, I can definitely feel more pronounced effects on tagamet which coincides with the theory of potentiation via inhibition of hepatic enzymes.
    I figured as much, especially considering that my stomach should be pretty basic an hour after taking 600mg of cimetidine.

    I am wondering though, is it beneficial to take cimetidine after dosing the opioid (say an hour after the effects come on)? I read that the half-life of cimetidine is only 2 hours but is the enzyme inhibition only that long? I read GFJ can inhibit 3A4 for up to 72 hrs and I'd imagine that the bergamottin doesn;t actually stay in the body that long...?
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    #8
    Bluelighter laCster's Avatar
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    You want to inhibit the liver enzymes inhibited before you take the oxycodone so that when you take a drug orally and passes through first pass metabolism, metaboliztion of oxycodone into inactive metabolites is inhibited thus increase the efficacy of the most oxycodone to reach your brain, higher plasma levels, and a duration of effects. So in order to achieve this, you need to take the tagamet 30-60minutes before dosing your oxy. Howeverx I have taken tagamet an hour after oxycodone and I definitely noticed potentiation, not as effective as doing before, but it still worked.



    Although tagamet is weaker at inhibiting 3A4 than grapefruit juice, tagamet acts as a blanket inhibitor of multiple hepatic functions and enzyme. For example, tagamet inhibits 3A4, 2E1, 2C9, 2D6, and many other enZymes including inhibiting UTG2B7 which is the main glucuronadizer of opiates and benZos which also increase the effects. Grapefruit juice is a moderate-strong inhibitor of 3A4, but only affects two or 3 other 450 enZymes ans that's it.

    I would expand, but g2g pce


    Also, that is only.a rumour that gfj can inhibited.the enzymes for 72+ hrs. That is false.

    It works in.the same.time tagnaet does. It lasts for 2-4 hours after ward's which means you would have to constantly be drinking grapefruit juice to make it last that long
    Last edited by laCster; 03-02-2013 at 17:45.
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    #9
    Bluelighter hefe1313's Avatar
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    I notice a bump in the high if i take 3-4 tums before i dose
    I'm pretty sure to make Heroin you have to add calcium carbonate. so im pretty sure tums helps.
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    #10
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    Quote Originally Posted by hefe1313 View Post
    I'm pretty sure to make Heroin you have to add calcium carbonate. so im pretty sure tums helps.
    It's used in the process of extracting morphine from opium, if that's what you are referring to, but that has no bearing whatsoever on why taking calcium with oral opioids increases absorption.
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    #11
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    If it's used to extract morphine from opium, wouldn't it help to take some tums if you're taking somthing like poppy seed tea? i'm thinking the tums would help extract the morphine in your system, no?


    Quote Originally Posted by Swimmingdancer View Post
    It's used in the process of extracting morphine from opium, if that's what you are referring to, but that has no bearing whatsoever on why taking calcium with oral opioids increases absorption.
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    #12
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    Quote Originally Posted by hefe1313 View Post
    If it's used to extract morphine from opium, wouldn't it help to take some tums if you're taking somthing like poppy seed tea? i'm thinking the tums would help extract the morphine in your system, no?
    No, without getting into how one extracts morphine from opium and how one's body metabolizes opium, suffice it to say I don't think it's that simple. Calcium just helps with absorption of opioids from the digestive tract by making the stomach less acidic.
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