GRAPEFRUIT JUICE AND SUPPS
- Thread starter thebigt
- Start date
The Solution
Legend
Where did you hear that?
Are you referring to the claims that taking juice with creatine will aid its effects? When in reality it will not. Grape Fruit Juice would just add additional carbohydrates to whatever you are taking. There is nothing magical about utilizing it with supplements
Everyone thinks that grapefruit juice and other citrus fruit causes the meds/supps to break down faster, increase absorption, etc. In fact it's the opposite. They actually affect the enzyme that breaks down meds/supps for example The enzyme CYP3A4 is also the enzyme that breaks down testosterone naturally in the body.
next thing you know kids will be mixing stuff with coca cola and saying its the next best thing haha
Are you referring to the claims that taking juice with creatine will aid its effects? When in reality it will not. Grape Fruit Juice would just add additional carbohydrates to whatever you are taking. There is nothing magical about utilizing it with supplements
Everyone thinks that grapefruit juice and other citrus fruit causes the meds/supps to break down faster, increase absorption, etc. In fact it's the opposite. They actually affect the enzyme that breaks down meds/supps for example The enzyme CYP3A4 is also the enzyme that breaks down testosterone naturally in the body.
next thing you know kids will be mixing stuff with coca cola and saying its the next best thing haha
doogans
Active member
It has something to do with the inhibition of CYP3A4. I know a lot of prescription drugs shouldn't be taken with grapefruit juice
The Solution
Legend
I stated that ^^^
"Everyone thinks that grapefruit juice and other citrus fruit causes the meds/supps to break down faster, increase absorption, etc. In fact it's the opposite. They actually affect the enzyme that breaks down meds/supps for example The enzyme CYP3A4 is also the enzyme that breaks down testosterone naturally in the body."
doogans
Active member
Oops! Apparently I skipped over that entire paragraph lol.
thebigt
Legend
lol...obviously you have never taken viagra with grapefruit juice!!! years ago it was common to take ph's with it...
rtmilburn
Well-known member
Juices make certain medication degrade faster. This is due to the ascorbic acid decreasing the ph of urine for example all amphetamine are decreased blood concentration by 85%. Although if the medication isn't affected by ph then grapefruit juice (not all other juices just grape fruit juice) can increase the amount of the medication that is absorbed. This is because of CYP3A4 enzyme breaks down a lot of our supplements and medications and grapefruit juice or extract brakes down that enzyme. This allows more of the medications to reach the blood stream.
thebigt
Legend
exactly...creatine for example should never be taken with citrus juice....but if i remember right eric potratz the founder of primoridial performance included grapefruit extract in his andro series ph's ....eric is a clever guy, imo!!!
Danes
Well-known member
I do agree with The Soultion , grapejuice CAN have opposite effect of some medicines:
Grapefruit juice reduces the absorption of fexofenadine
says Huang, decreasing the effectiveness of the drug. Fexofenadine (brand name Allegra) is available in both prescription and non-prescription forms to relieve symptoms of seasonal allergies. Fexofenadine may also be less effective if taken with orange or apple juice, so the drug label states “do not take with fruit juices.
Why this opposite effect?
It involves the transportation of drugs within the body rather than their metabolism, explains Huang. Proteins in the body known as drug transporters help move a drug into cells for absorption.
Substances in grapefruit juice block the action of a specific group of transporters. As a result, less of the drug is absorbed and it may be ineffective, Huang says.
But....
It seems like its not all about inhibiting CYP3A4 enzyme
"Since then another protein has been found that is inhibited by grapefruit: P-glycoprotein or P-gp. P-gp is also found in the small intestine and also decreases the absorption of pharmacological substances.
ergo-log.com/grapefruit.html
ncbi.nlm.nih.gov/pubmed/14679360
And this would be great read:
ncbi.nlm.nih.gov/pmc/articles/PMC1873672/
Sorry, could not post whole link due to low postnumber
Grapefruit juice reduces the absorption of fexofenadine
says Huang, decreasing the effectiveness of the drug. Fexofenadine (brand name Allegra) is available in both prescription and non-prescription forms to relieve symptoms of seasonal allergies. Fexofenadine may also be less effective if taken with orange or apple juice, so the drug label states “do not take with fruit juices.
Why this opposite effect?
It involves the transportation of drugs within the body rather than their metabolism, explains Huang. Proteins in the body known as drug transporters help move a drug into cells for absorption.
Substances in grapefruit juice block the action of a specific group of transporters. As a result, less of the drug is absorbed and it may be ineffective, Huang says.
But....
It seems like its not all about inhibiting CYP3A4 enzyme
"Since then another protein has been found that is inhibited by grapefruit: P-glycoprotein or P-gp. P-gp is also found in the small intestine and also decreases the absorption of pharmacological substances.
ergo-log.com/grapefruit.html
ncbi.nlm.nih.gov/pubmed/14679360
And this would be great read:
ncbi.nlm.nih.gov/pmc/articles/PMC1873672/
Sorry, could not post whole link due to low postnumber
Danes
Well-known member
You saw what I posted earlier about viagra and piperine?? That will DEFF boost bioavailability lol
Piperine and Viagra
The drug sildenafil (Viagra®) is metabolized mainly by the enzyme CYP3A4, which is found in many tissues, including the small intestine and the liver. Consequently, when one takes a dose of this drug, some of the dose is destroyed before it reaches the bloodstream, and more of it is destroyed in the liver before it reaches the rest of the body. About 40% of the sildenafil successfully reaches the general circulation. Once there, half of it gets metabolized every 4 hours during passes through the liver and other tissues. Thus, out of a 100 mg dose, about 20 mg remains in circulation after 4 hours.
Piperine, as indicated above, is an inhibitor of the CYP3A4 enzyme. If a dose of piperine is taken shortly before a dose of sildenafil, the sildenafil will not have to ‘run the gauntlet’ of CYP3A4 metabolism on its way to the bloodstream. This will boost the efficiency of a dose of sildenafil – potentially by as much as a factor of 2.5. This means that a 100 mg dose taken with piperine could be equivalent to a 250 mg dose taken without it – a dose likely to produce unpleasant side effects at the very least. Piperine will also prolong the action of sildenafil, probably by about two hours, which is how long the inhibition of CYP3A4 lasts in the liver.
thebigt
Legend
grapefruit juice will do the same thing-i know this not because some guy did a study but because i have actually experienced this effect!!!
i remember a number of supps including grapefruit extract to improve absorption.
JudoJosh
Pro Virili Parte
Context
It depends on what it is interacting with. Grapefruit juice can in fact increase the oral bioavailability of a number of compounds - Invalid Link Removed
thebigt
Legend
exactly...solutions blanket statement that grapefruit juice decreases effects of all drugs is absurd!!!
i am looking for ingredients in supps that grapefruit juice might potentiate....
Godstrength
Board Sponsor
Thoughts about grapefruit juice and kratom? I have heard that it increases effects and duration....
The Solution
Legend
Not everyone on here is using those "Enhanced" Supplements. So for some or many it may not apply, but it is good to know this can apply to compounds or PH's or anything along those lines for those who do "Use"
T-Bone
Banned
Yes I believe they did. Also the AndroSeries by Primordial Performance.
JudoJosh
Pro Virili Parte
this thread needs @right hook. He is far more knowledgeable in pharmakinetics than I am
But if I were to take a swing at it, sime of the flavonoids in grapefruit juice block a few different cytochrome enzymes in your intestinal wall. These enzymes are involved in the metabolism of a few different compounds. Their role in drug metabolisim is one of regulation. By inhibiting these enzymes, you can increase the blood level of some drugs, which in turn puts you at risk of experiencing adverse side effects. This is why it is generally recommended you avoid grapefruit juice with drugs that are effected by it. As for over the counter supplements, off hand I don't know of any that would benefit from this although some may, as I said I'm not a big pharma guy. Maybe my PES brethren Synapsin will chime in
But if I were to take a swing at it, sime of the flavonoids in grapefruit juice block a few different cytochrome enzymes in your intestinal wall. These enzymes are involved in the metabolism of a few different compounds. Their role in drug metabolisim is one of regulation. By inhibiting these enzymes, you can increase the blood level of some drugs, which in turn puts you at risk of experiencing adverse side effects. This is why it is generally recommended you avoid grapefruit juice with drugs that are effected by it. As for over the counter supplements, off hand I don't know of any that would benefit from this although some may, as I said I'm not a big pharma guy. Maybe my PES brethren Synapsin will chime in
thebigt
Legend
i welcome all informed thoughts/opinions!!!
The_Old_Guy
Well-known member
No idea on "regular" supps, but for stuff that you *would* want hanging around a long time, the compounds in GFJ inhibit the CYP enzymes (3A4 & 450) - as has been said 10 times now. 6,7,DHB, which is/was included in Finiflex, Hardrock, etc "supps" is thought to be one of the compunds - though the research thinks there is a lot more to GFJ than the 6,7,DHB. AMS uses Berberine, Rhizoma Coptidis and Cobalt. The Israelis did a recent study on GFJ, and used 250ml. At 8oz of GFJ per "supplement" dose - it appears cheaper to buy purpose made CYP Inhibitors... GFJ is expensive as heck where I live! 
mr.cooper69
Legend
For MOST ingredients, grapefruit juice will increase bioavailability and half-life of the compound. It not only inhibits PgP, but it inhibits the CYP system both intestinally (increased absorption of parent compound) and hepatically (decreased metabolism of parent compound).
Notable exceptions are:
Prodrugs, which need the CYP system to convert to active form. Grapefruit juice would decrease the effects of these.
Appreciable effects are only really seen with white grapefruit juice
Notable exceptions are:
Prodrugs, which need the CYP system to convert to active form. Grapefruit juice would decrease the effects of these.
Appreciable effects are only really seen with white grapefruit juice
thebigt
Legend
i read somewhere that it won't increase effects of stimulants like caffeine, do you agree?
what are your thoughts on ingredients like tongkat/fadogia/arimistane?
btw-thank you for the informed post!!!
GreenMachineX
Well-known member
Wait, so could DHB/bergamottin degrade epiandro then because it is a prodrug, correct? There's a product that has both in it and that would be silly if it works against itself.
What effect would these enzyme inhibitors have on SARMs like LGD-4033 and ostarine?
Grambo
Board Sponsor
Inhibitors of CYP3A4 will definitely increase efficacy and duration of caffeine. Trying to do this with juice is not specific enough with too much variability.
This drug is a crazy inhibitor of CYP enzymes. It's drug interactions are widespread anyone taking any other medications should be extremely careful.
It will only degrade it if it needs those enzymes (CYP/PGP) to be metabolized into their parent drug.
To understand if the inhibitors will cause any changes in drug metabolism just look up their pharmacokinetics and see what enzymes it is metabolized by, then you'll be able to know if inhibiting the enzyme will cause any effects.
Grambo
Board Sponsor
Technically yes, it would increase the plasma concentration for a longer period of time due to metabolism of the compound (specifically talking about caffeine here) being inhibited. Like I said the amount of inhibitor in the juice will vary so if you were really trying to inhibit the CYP enzymes using cimetidine is more specific and not as variable.
thebigt
Legend
thank you!!!
thebigt
Legend
well....drinking a coke with aspirin does seem to speed it's effects, lol--haha!!!!
Synapsin
Well-known member
It really depends on the drug, how it works, etc.
DonnieM
Active member
Yes, of course. I've read it has something to do with what therapeutic index the drug have, the wider index, more/higher risk of being affected by the CYP3A4 enzyme?
But in theory, when would one take bergamottin (for example in OL Ar1macare) if taking meds? At least 6-8 hrs apart?
Nyrin
Member
That's going to depend on the medications involved and is a question best reserved for your prescribing physician. Too much liability involved with anyone tied to any company to make a recommendation.
Not all drugs are metabolized exclusively (or at all) through CYP3A4; some don't use it all, others have multiple metabolic pathways involved. The impact of CYP3A4 inhibition is going to be specific to each individual substance.
CYP3A4 inhibition, particularly through something like unstandardized grapefruit juice, is also highly variable; that's where the therapeutic window (ratio of TD/LD50 to ED50) comes in. The variability means that it's particularly scary/dangerous for narrow therapeutic windows, as effective doses can quickly and unpredictably become toxic ones if the difference between an effective and toxic dose is small.
As for the timing, "Duration of effect of grapefruit juice on the pharmacokinetics of the CYP3A4 substrate simvastatin" suggests that CYP3A4 inhibition lasts for several days; 3 days later, there was still a 1.5-fold increase in concentration of simvastatin and it wasn't until they tested at 7 days out that no differences were seen.
If you're taking any particularly therapeutically-narrow drugs with primary metabolism via CYP3A4, your physician will most likely advise you to completely avoid CYP3A4 inhibitors like grapefruit, as cumulative dosing over a period of several days will progressively increase inhibition.
But again, talk to your doctor -- depending on the meds involved, a little suppression of CYP3A4 may not be of enough concern for this to be a huge issue.