Myth about Tramadol potentiation

[oxyaddict05]

I was doing a little research on the CYP2D6 liver enzyme which converts Tramadol into O-desmethyltramadol (the good stuff that gets you high). Now I have read in many posts here that antihistamines (specifically diphenhydramine) can potentiate a Tramadol high, but I just read something in Wikipedia that contradicts this. If you follow this link, http://en.wikipedia.org/wiki/CYP2D6 you will see that antihistamines (like diphenhydramine) are actually an inhibitor of the CYP2D6 enzyme. Shouldn't this mean that taking antihistamines would actually decrease the effetcs of Tramadol, because less of it is converted into O-desmethyltramadol? Some input would be appreciated. This is only an educated guess.


Sources: http://en.wikipedia.org/wiki/CYP2D6

[oxyaddict05]

However, SWIM does find that antihistamines can potentiate or "bring back" the high many hours after the tramadol was taken. SWIM just took 25mg diphenhydramine and it is slightly bringing back the buzz from the tramadol SWIM took 5-7 hours ago. =)

[Orchid_Suspiria]

Swim doesn't know too much about tramadol but swim can tell you that diphenhydramine does indeed potentate methadone,oxycontin,and heroin.Swim can't give you any indepth,scientific reason why but swim knows what he has experienced.

[Bajeda]

If you want to potentiate Tramadol, grapefruit juice is a much better alternative to research.

[fiveleggedrat]

Swim has been using antihistamines since day one for potentiating. Recently he experimented with higher doses (50mg dyphenhydramine and 20mg loratidine). He did not feel the effects of his basic 150mg tramadol starting dose, which is unusual. He has absolutely no physical addiction or built-up tolerance. He will experiment further with this.

[BoxStar]

As far as SWIM knows, antihistamines in particular diphenhydramine, to which SWIM has had access to use in IV form, potentiate the subjective effects of opioids, including Tramadol by their action on the CNS, its known that certain antihistamines enhance the analgesia and reduce the itching which at recreational doses can become quite annoying.

As it has been said diphenhydramine inhibits the enzyme responsible for the metabolism of Tramadol and Codeine so taking it at the same time it’s a bad idea and most likely will reduce the effects, however taking it just after the opioid effects peak can in fact enhance and prolong the euphoria.

In SWIM experience with IV diphenhydramine injecting 50mg when the opioid peaks (this applies to every opioid SWIM has tried so far, indifferent of administration route) causes a marked “rush” that lasts for about 5-15 minutes and a long-lasting potentiation of effects, unfortunately side-effects such as drowsiness, urinary retention and “extra strength” constipation are also potentiated and it also causes dry mouth, nose, throat and eyes.

Same effects are obtained by oral administration but with a much slower onset.

[y0ssarianlives]

http://en.wikipedia.org/wiki/Pyribenzamine

interesting bit at the bottom in regards to this first generation antihistamine