Just read in another thread that Omeprazole (Prilosec) inhibits CYP3A4 metabolism of other drugs. Could the reason that my tramadol hasn't been effective for me be due to the fact that it's inhibiting my CYP3A4 enzyme? I've just read that tramadol is only effective by metabolizing into the M1 (O-DMT) metabolite by path of the 3A4 enzyme.
-
BDD Moderators: Keif’ Richards
Proton Pump Inhibitors and CYP3A4 Metabolism of Tramadol
- Thread starter Jktm
- Start date
nope, tramadol is o-desmethylated to M1 through 2D6 and is metabolized to inactive metabolites through 3A4. prilosec could do the trick at boosting the amount converted into M1 unless it also inhibits 2D6 which then would be sorto f counter-productive IMO
http://www.ncbi.nlm.nih.gov/pubmed/15258107
So apparently 2D6 is also effected by all 5 of those in a minor amount at least, so maybe that has something to do with my inability to get relief from tramadol. I'll be contacting my doc about this either way.
So apparently 2D6 is also effected by all 5 of those in a minor amount at least, so maybe that has something to do with my inability to get relief from tramadol. I'll be contacting my doc about this either way.
doctors usually don't like when you know more about drugs than they do lol, especially when you are asking about potentiation. the most likely response from your doctor will be, "why do you need to potentiate tramadol? do you plan on using it recreationally?"
besides most common physicians stupid enough to prescribed tramadol for whatever reason will be highly unlikely to know about all its modes of actions, its pharmocology, ect..
besides most common physicians stupid enough to prescribed tramadol for whatever reason will be highly unlikely to know about all its modes of actions, its pharmocology, ect..
Swimmingdancer
Bluelight Crew
You might also be naturally deficient of the enzyme that mainly metabolizes Tramadol. Tramadol, hydrocodone and codeine don't work for me but other opioids work just fine.
true JK, very true...
@swimming
hydrocodone has been proven to provide more effects itself rather than relying on it's main metabolites like other prodrugs. in addition, research has been done on whether codeine relies on morphine for its opiate effects or its other metabolite codeine-6-glucuronide
@swimming
hydrocodone has been proven to provide more effects itself rather than relying on it's main metabolites like other prodrugs. in addition, research has been done on whether codeine relies on morphine for its opiate effects or its other metabolite codeine-6-glucuronide
Swimmingdancer
Bluelight Crew
I just know those particular drugs do very little for me (although I still get the side effects), whereas some other opioids seem to work better for me.
Anyway, the reason I mentioned enzymes is because with Tramadol, around 1 in 10 of people have an excess of CYP2D6 activity, and around 1 in 10 have decreased CYP2D6, (although I have read different sources saying anywhere from 4%-15%, but you get the basic idea) so I figured it was worth considering. For some people Tramadol just doesn't work very well.
This is an interesting study which found that people with low CYP2D6 who took analgesics metabolized by CYP2D6 (such as tramadol, codeine, hydrocodone, oxycodone, methadone) are more likely to experience side effects and therapeutic failure for agents requiring CYP2D6 metabolism to be converted to an active metabolite. About 6% of the people they studied reported high adverse effects and/or low desirable effects for a drug and 80% of those were "poor metabolizers" with impaired CYP2D6 metabolism, while only 20% of those with these adverse drug reactions had other cofactors such as drug-drug interactions. I wish I could read the whole study and see the results for each specific drug.
I did hear that with codeine the morphine was responsible for much of the euphoria and some of the analgesia, whereas the codeine-6-glucuronide was now believed to be responsible for some (or even much) of the analgesia, since not that much codeine is actually metabolized into morphine. Codeine is metabolized by UGT2B7 to c-6-g, so perhaps I am low in that enzyme, but you'd think if it was a UGT2B7 issue that I'd have problems with morphine too, I haven't used morphine much so I'm not too sure...
For hydrocodone Wikipedia says:
Methadone (which is also affected by CYP2D6 and a bunch of other CYPs) lasts for a very short time for me, but at least methadone has some effect for a period of time if I take enough of it and doesn't give me major side effects like codeine etc. I dunno, maybe I'm just a crappy metabolizer with a lot of drugs, lol.
Perhaps I have a lot of the enzyme(s) that metabolize these drugs into their inactive metabolites? Would that have a similar effect or just shorten the duration?
TL;DR Basically how exactly the enzymes affect the effects (or lack of effects) one gets from a drug is complex and not completely understood, I just thought that since no one seems to know of a contrindication with omeprazole and Tramadol, aside from perhaps potentiation, that one's unique metabolism was something to consider
