Possible Grapefruit Juice Potential for Greater Tramadol Experience

[Bajeda]

Originally Posted by Paracelsus

And SWIM is immune to placebo.

I seriously doubt that anyone is completely immune to placebo. If you are aware of what you are doing and approach new combinations or substances that hold promise a bit incredulously I think there is a lesser chance of encountering the placebo effect. I still don't think you can discount it entirely though.

Anyways, on to swim's report....




Swim currently weighs one hundred and sixty pounds. He had been using Tramadol fairly regularly for about a month but took a break recently so he has little to no tolerance, and the SSRI effects should have worn off in the meantime. The diminished tolerance swim has may make it more difficult to evaluate the specific impact of grapefruit juice potentiation on the Tramadol experience, but he feels that his memory of previous Tramadol experiences without tolerance is good enough to allow for some judgement. Swim also wanted to smoke cannabis throughout the experiment, so that could throw him off a bit, but he has smoked cannabis on un-potentiated Tramadol before so he may be able to notice a difference between the effects.


12:30... Swim ingested 150mg 'Tamolan' generic Tramadol along with 350ml of grapefruit juice. Grapefruit juice isn't really swim's thing, so his stomach felt queasy after drinking the glass.

12:50... Swim begins eating a nice plate of pasta for lunch. He wanted to have a beer with the meal but thought he better not.

13:15... Swim is feeling good all-around. The mood lift is much more prominent than swim remembers from before, as is the body buzz. Things are looking good.

13:40... Swim starts to smoke a fat hash-filled joint. After only a few puffs all the jitters from the Tramadol disappear.

13:55... Swim has finished smoking. He feels a very mellow yet trippy high. Not really any anxiety or rapid tangential thought processes to fend off. Sensory perceptions are heightened more than they usually would be from just smoking cannabis by itself.

14:15... Swim took a shower. Afterwards he need some water to quench his thirst, as he feels a bit 'heated'. He is still very cheery and basking in euphoria, though his mental state has calmed considerably as he turned off the music to help him chill out.

14:45... Swim is debating whether or not to take another 50mg of Tramadol. I think he will wait a bit and decide then. Swim is feeling very 'up' and happy right now, and his body is light and full of energy. Cognition is slowed somewhat, but swim is more able to focus on single trains of thought better than when he smokes cannabis alone or with a bit of tramadol normally.

14:55... Now swim is chatting with himself in the chat room. This is interesting... He is having too much fun to really think about it though, his mind is pretty erratic at the moment, but he is still very cheerful.

15:05... Swim takes another 50mg with only a swig of grapefruit juice.

15:10... Swim could really go out and dance at this point. Instead, he cranks up the music and just goes nuts in his room. This feels almost like a good first plateau DXM trip, except less trippy as the cannabis high is wearing off. Swim is very euphoric, giddy, energetic, almost speedy.

15:20... There is a greatly enhanced level of auditory input for swim. It makes him want to smoke sinicuichi to add to it and maybe distort the hearing more. This is great for music though, at the moment it sounds even better than when swim is stoned. Swim feels he may want to smoke another joint soon though, as the previous high isn't as strong and he is getting a bit on the speedy and jittery side.

17:35... Swim smoked another moderately sized joint. He is feeling a heavy stoning effect and is tripped out, though he is still experiencing a good deal of euphoria. Some slight visual distortions, such as when he looks at paintings and his vision is a bit fuzzy so he sees movement. Nothing especially intense, but still cool nonetheless. Swim's mind doesn't feel as clouded, though its difficult to perform some not too complicated tasks, and swim's motor-control isn't functioning at its best!

18:50... Swim washed down another 50mg Tramadol with some grapefruit juice. He is feeling a bit jittery, but pretty good on the whole. Swim is feeling heated again, but its most likely due to the air conditioning being off at the moment.

20:15... Swim smoked another medium size joint. He is feeling less trippy effects this time around, but pleasant euphoria and mellowness. Swim made a mixed drink with about two shots or so of alcohol. He isn't going to go over that amount, and knows mixing alcohol with Tramadol is an additional risk. He wants to see how the alcohol synergizes with the potentiated Tramadol and cannabis. Swim waited until this point as he doesn't feel the very strong effects he was feeling earlier, but still fairly pleasant ones.

20:50... Swim feels 'weighty' in the limbs. If he stops concentrating on anything its like he goes directly in a Zen state. Great euphoria and level mindset shortly after finishing the drink. Very enjoyable.

22:00... Smoked another joint. Swim is feeling very blazed right now. There is still euphoria present, but the energy is a bit lacking by this time. Swim is trying to concentrate on something, so we'll see how that goes.

23:10... Swim was nodding off a bit, though he has stopped now. Cognition is still not functioning at optimal levels. Should be time to try and go to sleep soon.

1:00... Swim is very level headed now. Not much in the way of noticeable effects, though swim can't say he noticed an obvious come-down period of any related effects. Rather, he is in the process of a nice smooth, gradual decline. Time is passing by very slowly. Swim could go to sleep if he wanted, but he is going to listen to a little soothing music first so he can appreciate it in his current state before he tires enough to really want to sleep.

10:00... Swim ended up sleeping in a bit more than he wanted. He woked up feeling groggy and a little dehydrated. Tiny bit of a headache.

10:30... Swim ate breakfast and drank some coffee. He is bright and energized again. No euphoria really, but it feels as though there are some lingering Tramadol effects. He is good to go about his day.




Swim tried the Tramadol + grapefruit juice potentiator combo the next day as well, though without all the cannabis consumption. He would definitely agree that the effects stretch out and last longer when Tramadol is consumed with grapefruit juice, though its harder for him to directly evaluate any changes in potency or other effects. I do believe he was much more energized than normal though, especially when he added cannabis to the mix. It was a very nice high, and I think if swim takes tramadol and grapefruit juice again he will also smoke cannabis, as it took the edge off the more irritable effects and produced some interesting synergy as well.

The alcohol mixed nicely as well, but left swim a bit hungover the next day, and probably contributed a good deal to his dehydration as well. Swim only drank two shots, and he was propelled upwards quite a bit. Before swim has mixed Tramadol and alcohol (stupidly at that time) to a greater extent but didn't get the very euphoric effect he got with the two shots on the grapefruit potentiated Tramadol. I don't think swim would venture to try alcohol with Tramadol again, especially if it were potentiated by grapefruit juice, as the potential for pleasure isn't worth the annoying side effects and dangers involved.

[Paracelsus]

SWIP is usually not just a little incredulous when experimenting with new substances/combinations, but very skeptic. That’s what I meant by saying SWIP is immune to placebo. He usually even overlooks effects like slight tiredness or slight mood lift, even if they might have been caused by the substance.

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Anyways, update on the situation. Grapefruit juice does NOT inhibit CYP2D6, but CYP3A. Many probably know this, but much more don’t. I have posted more about this here.

So since CYP2D6 remains unaffected, the metabolism of tramadol to the active O-desmethyltramadol remains the same. But less of the inactive N-desmethyltramadol and N,N-didesmethyltramadol are formed, because the responsible enzyme (CYP3A) is inhibited by grapefruit. This might explain the potentiating effect that grapefruit juice has on tramadol.

[monkeygone2heaven]

thanks for the info guys, time to hit the supermarket for some grapefruit juice.

oh just realised have some grapefruits at home!

[Secure.H]

Swim tried the Juice with 50mg didn't notice any difference. Tried again a few hours later: nothing.

Tram is worth mixing experimentally with GABA and Acetiminophen though according to some.

[someone111]

swim takes around 1200mg of tramadol at once.... should he try grapefruit juice and see if he can lower his dose....

[trammy]

what about tramadol and zantac??

[delphinen]

Tramadol does not work with grapefruit guys, sorry.

[Paracelsus]

Really? I could testify that it does. You don't need to be sorry, as it probably didn't work for your subject. Everyone's different. Theoretically it should work, and quite some anecdotal reports strongly suggest it does.

[delphinen]

im a super metabolizer (have multiple copies of CYP2D6) and after 2 years of Tramadol tries.. grapefruit didnt help

[Paracelsus]

The ultrarapid CYP2D6 would theoretically lower the efficacy of CYP3A inhibition in this case. Was your CYP2D6 genotype tested for (that's the only way to find out if you have multiple alleles)?

[delphinen]

SWIM gets a second plateau of DXM with only 300mg
SWIM gets extreme pleasure with Tramadol when it reaches O-Desmethyl

both drugs are metabolized by CYP2D6, do you have another explanation?

[Donniedrko]

Placebo = (Endogenous Morphine) a.k.a Endorphins = Thinking things are happening, and might very well be happening, but not due to the grapefruit juice. You body's natural endorphins are most likely responsible for this effect.

[Paracelsus]

Grapefruit juice is well-known to increase max. concentration and half-life of many CP3A substrates, including some opioids. This is not documented with tramadol, but it is theoretically logical. Look it up if you think that grapefruit juice potentiation is placebo.

[Herbal Healer 019]

y dont u guys just try tagamet {cimetadine (sp?)}, a cyp2d6 inhibiter??