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Opioids tramadol and white grapefruit juice

R

real142

Bluelighter
Joined
Nov 1, 2012
Messages
73
does this weaken the Tramadol or does it potentate it i have looked around with mixed views wat do u think? also when was ultram/tramadol avaliable on the US market?
 
It may slightly potentiate it but not extensively. Its been available in the US for 20 years or so.
 
Well gfj inhibits CYP3A4 mostly. Tramadol is metabolized to an inactive metabolite by this enzyme but I do not think it would be a vastly noticeably difference than if you took it on its own.
 
Kittycat5 said:
Well gfj inhibits CYP3A4 mostly. Tramadol is metabolized to an inactive metabolite by this enzyme
Click to expand...

Huh, isn't it metabolized to the much more µ-affinitive O-Desmethyltramadol? Which inactive metabolite are you talking about?
 
2D6 metabolizes tramadol into O-desmethyltramadol. GFJ does not inhibit this as far as I can tell. 3A4 is responsible for metabolizing tramadol into N-desmethyltramadol which is not active, so perhaps it may provide some potentiation via GFJ (I have read anectodal reports as saying so) but not convinced how much it would be worth it unless you have low tolerance.
 
well what does it do CYP3A4..if it blocks it up than that would mean more tramadol would be converted via 2d6 right therefore a increase and this would be good for taking 25mg every 30 min at that rate it would take 16 doses to reach the 400mg limit... which u probably wouldn't reach because of the bio-avaliabilty increase as more is taken and the enzyme blocked up the metabolizes it into the undesirable N-desmethyltramadol ....correct?
 
That is the theory most people put forth. But I have not seen proof of it to satisfy why I feel it is nothing more than wishful thinking. Have you tried it? If so, what is your opinion on the matter.
 
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