Opioids Grapefruit juice and 50mg of tramadol worthless?

[ynotrhyme]

I know grapefruit juice increases effects but will it work with the measly 50mg I take every 4 hours ?

Just bought golden grapefruit lol

Why does it have to be white grapefruit?

 

[twotoomany]

I don't know if you want to inhibit enzymes with tramadol. I believe you want to encourage the enzymes to metabolize tramadol into O desmethyltramadol.

 

[ynotrhyme]

Ive been reading around here and the people who seem to know say grapefruit juice inhibits one of the enzymes, therefore potentiating another. Something like that lol, ihave 0 experience in the biology stuff they talkin bout lol, and its extensive the talk about it here. Just was wondering if the amount i take 50mg and then maybe 50-100mg more in about 2-3 hours will benefit also..

 

[twotoomany]

It inhibits the enzyme. The drug is not metabolized, this you stay high longer. With tramadol (and codeine) you WANT the drug metabolized into its stronger metabolite. So enzyme potentiaters aren't going to help.

 

[ynotrhyme]

I was gonna link but highly doubt its allowed. This is off a website im reading:

" Harmlessly Potentiating Tramadol

Tramadol is a fully-synthetic opioid pro-drug with SSNRI activity. Upon ingestion, the digestive cytochrome enzymes - the cytochrome P450 family specifically - metabolize Tramadol into five distinct compounds. O-Desmethyltramadol, one of the five, has a markedly high affinity for the µ-opioid receptor, far more so than Tramadol itself. The same enzymes that convert Tramadol to its 5 metabolites, cytochrome P450, ionize these metabolites for water-soluble excretion. Therefore, the metabolism of Tramadol revolves entirely around the metabolic activity of cytochrome P450 in the liver.

Cimetidine (Tagamet) is a potent inhibitor of the cytochrome P450 enzyme, in addition to acting as a pH neutralizer. Therefore, if one were to ingest cimetidine prior to ingestion of Tramadol, one would likely experience a reduction of effects. However, if one were to wait until ingested Tramadol had time to be converted to its metabolites (30-180 mins), the ionization of the metabolites of Tramadol should be inhibited. This would be expected to enhance and prolong the effects of Tramadol at the µ-opioid receptor considerably. In sum, in order to potentiate the effects of Tramadol with cimetidine, timing and sequence is key.
In addition, subsequent to regular administration of recommended doses of cimetidine, the liver will up-regulate the expression of the enzymes responsible for converting Tramadol to its more potent metabolites. In other words, after ingesting cimetidine for a regular interval of time, one will become more sensitive to the effects of Tramadol. It should be noted, however, that this dynamic would render an individual less sensitive to other non-synthetic and semi-synthetic opiates over time.
A friendly chimp has revealed that this has been a highly effective and reliable method of potentiation. He doesn’t ingest Tramadol without cimetidine anymore. It should be noted that grapefruit juice has indeed been noted to be a cytochrome P450 inhibitor as well, though not quite as potently as cimetidine. This method should produce no anticipated ill-effects, as the magnitude of effects will never exceed the SSNRI activity inherent to the initial dose ingested. So long as one takes care not to initially ingest too-high a dose, this method of potentiation will not enhance SSNRI activity – rather, it should selectively enhance µ-opioid activity because it's the metabolites, not Tramadol, that are being enhanced.

Hope this helps to get the most bang-for-your-milligram in as safe a way as possible ! Since this method of potentiation is so distinct from typical methods for the majority of other opiates, I figured it warranted a thread of its own - I apologize if this was a mistake. I'd be quite interested to know if this works for any other chimps out there. "

 

[twotoomany]

So you have your answer. Wait 60-180 min after dosing to take Tagamet.

 

[ynotrhyme]

So now im reading off livestrong that grapefruit juice inhibits an enzyme which works towards the first pass of metabolism which tramadol goes through in the liver and which reduces the potency of this drug. Therefor if you drink grapefruit juice and wait 30 minutes then that enzyme, which allows the metabolism of the drug in the liver making it weaker, will be inhibited and then taking tramadol will be more potent since the enzyme that reduces its power through the first pass will be inhibited. Making the tramadol stronger. Ima try it out.

 

[twotoomany]

With tramadol, you WANT first pass metabolism. You want it to convert to O desmethyltramadol which is stronger. Did you even read what you posted?

 

[missmeyet?]

Lol

 

[Non Nobis Solum]

No grapefruit juice, no tagment with tramadol.. It uses cytochrome P450 enzymes to metabolize into the useful chemicals such as O-Desmethyltramadol.. Infact I believe Saint Johns Wort to be an inducer of such enzymes, it would certainly have more than a placebo effect. If you want to potentiate Tramadol, take some Saint Johns Wort.

 

[RTrain]

^I was thinking the same thing if you want the parent substance to metabolize quicker to give more of its metabolite. The same thing with buprenorphine and norbuprenorphine, many people believe it works with bupe. But it also will decrease the duration, so keep that in mind. Everything comes with a price. You could just take more, but if you only have 50 mg I guess you have to try to kick up it a notch some way.

 

[Moredopamine]

No grapefruit juice, no tagment with tramadol.. It uses cytochrome P450 enzymes to metabolize into the useful chemicals such as O-Desmethyltramadol.. Infact I believe Saint Johns Wort to be an inducer of such enzymes, it would certainly have more than a placebo effect. If you want to potentiate Tramadol, take some Saint Johns Wort.

That's a bad idea. St John's Wort and tramadol may cause serotonin syndrome. It's not worth the risk to get a little higher off your tramadol.

 

[RTrain]

^oh yeah, don't want that. But what about other p450 inducers? I believe garlic is considered to be one among some other easily accessible substances.

 

[Hannah123]

You are nearly on the money with this one - great-fruit juice, Tagamet, and a host of other compounds and plant extracts inhibit the drug metabolizing drug CYP3A4 - however the more potent O-desmethyl tramadol is the product of CYP2D6 activity. I cant even remember a potent CYP2D6 inhibitor off the top of my head - a rule of thumb is that many opioid drugs are metabolized by CYP2D6. I believe the only way to achieve this end goal is in individuals with high atypical CYP2D6 activity - my girlfriend is one such person - she took a single T3 (co-codamol 30/500) for her period - vomiting, pin-prick pupils - not having a good time and displaying high dose opioid use symptoms. Codeine is a pro-drug and is metabolized by CYP2D6 to morphine.

 

[Non Nobis Solum]

To be honest I won't ever take tramadol ever again, I dosed 30 mg of racemic dl-amphetamine and 400 mg of tramadol, an hour or two later I woke up in an ambulance. Tramadol is a risky drug. Amphetamine and Tramadol decrease the seizure threshold. If one was to take Saint Johns Wort it would be with caution and proper titration until safe satisfactory results.


Stay away from Tramadol.. Immodium and Benzos/Lyrica for detox... Tramadol is a shit pain killer anyways and can often cause stomach pain. It's 1/4 opioid really.

 

[RTrain]

You are nearly on the money with this one - great-fruit juice, Tagamet, and a host of other compounds and plant extracts inhibit the drug metabolizing drug CYP3A4 - however the more potent O-desmethyl tramadol is the product of CYP2D6 activity. I cant even remember a potent CYP2D6 inhibitor off the top of my head - a rule of thumb is that many opioid drugs are metabolized by CYP2D6. I believe the only way to achieve this end goal is in individuals with high atypical CYP2D6 activity - my girlfriend is one such person - she took a single T3 (co-codamol 30/500) for her period - vomiting, pin-prick pupils - not having a good time and displaying high dose opioid use symptoms. Codeine is a pro-drug and is metabolized by CYP2D6 to morphine.

I am on suboxone right now and I read somewhere Bupe is a CYP2D6 inhibitor, not sure if its a potent one. I found this because I take a beta blocker and it is metabolized by CYP2D6, after researching possible interactions. Maybe that is why some people enjoy tramadol and bupe mixed and say its the 1 opioid you can feel on bupe.

 

[Non Nobis Solum]

It's a weak inhibitor RTrain and a strong inducer is Glucocorticoid.

 

[ynotrhyme]

With tramadol, you WANT first pass metabolism. You want it to convert to O desmethyltramadol which is stronger. Did you even read what you posted?

dude, im telling you what i read. no need for a hissy fit.

 

[Toz]

50mg tramadol will do fuck all, combine it with what you want it ain't gonna make a difference anyhow since 50mg is nothing.

edit: maybe you weren't looking to get high, in that case you will get your usual pain relief, grapefruit juice or not. I find all these enzyme potentiators or whatever to be placebo.

 

[ynotrhyme]

You are nearly on the money with this one - great-fruit juice, Tagamet, and a host of other compounds and plant extracts inhibit the drug metabolizing drug CYP3A4 - however the more potent O-desmethyl tramadol is the product of CYP2D6 activity. I cant even remember a potent CYP2D6 inhibitor off the top of my head - a rule of thumb is that many opioid drugs are metabolized by CYP2D6. I believe the only way to achieve this end goal is in individuals with high atypical CYP2D6 activity - my girlfriend is one such person - she took a single T3 (co-codamol 30/500) for her period - vomiting, pin-prick pupils - not having a good time and displaying high dose opioid use symptoms. Codeine is a pro-drug and is metabolized by CYP2D6 to morphine.

Thanks man this was useful. im seeing the mixed opinions on several forums due to cyp3a4 and cyp2d6 and people not knowing whch they are talking about LOL