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M
musclebones
Guest
grape fruit juice, before/after meals, etc ?
anything ?
anything ?
Anavar - anything you can take it with to increase absorption ?
C
Citruscide
Guest
In all honesty... I think that it will absorb just as well without any sort of juice...
I usually take my orals WITH food, however... it helps it get into the blood stream better. Since it is an ORAL, it will be broken down at the same rate your food is... depending on what you have (Papervar, it doesn't matter)... The use of Juice wouldn't help advance it into your bloodstream any faster... at least not me... I drink as glass and I'm peeing it out 5 minutes later
C-ditty
I usually take my orals WITH food, however... it helps it get into the blood stream better. Since it is an ORAL, it will be broken down at the same rate your food is... depending on what you have (Papervar, it doesn't matter)... The use of Juice wouldn't help advance it into your bloodstream any faster... at least not me... I drink as glass and I'm peeing it out 5 minutes later
C-ditty
6-8 0z grapefruit juice 20 minutes prior to administration.It will neutralize phase I liver enzymes,which destruct a certain portion of the orals.
F
Frackal
Guest
do da joof
HUCKLEBERRY FINNaplex said:
Thats interesting to know. I have never heard of that before. The only thing I have heard of is some people using T3 to help out with certain AAS they were taking. I will definately have to try the grapefruit trick. Does that work with other orals as well?
Yes,pretty much all oral meds succumb to some phase I destruction in the liver.Neutralizing it bipasses or at least lessens the impact and allows more of the drug to reach its targeted cells.
jacobswell
New member
is the amount extra measurable and worth it. i mean to say if its like 0.1 mg then prob not but maybe if its like 10-20% and especially with var being so damn expensive then its prob worth adding the grape juice
M
musclebones
Guest
jacobswell said:
bump for that
drveejay11
New member
Zagreus
New member
HUCKLEBERRY FINNaplex said:
Any idea what chemical found in grapefruite juice neutralizes the phase 1 enzymes and can it be supplimented? I am on a TKD program and want to use cleaner carbs than grapefruite juice for my one a day carb up. Also will be breaking my var dossage up throughout the day and don't want the extra carbs. Thus, I would like to see if there are any non carb soloutions? Anyone?
Thanks,
Zag-
Zagreus said:
Naringenin,amongst some other less understood mechanisms...
Drug interactions with grapefruit juice. Extent, probable mechanism and clinical relevance.
Fuhr U.
Institute for Pharmacology, Universitat zu Koln, Germany. [email protected]
Concomitant intake with grapefruit juice increases the concentrations of many drugs in humans. The effect seems to be mediated mainly by suppression of the cytochrome P450 enzyme CYP3A4 in the small intestine wall. This results in a diminished first pass metabolism with higher bioavailability and increased maximal plasma concentrations of substrates of this enzyme. The effect was most pronounced in drugs with a high first pass degradation and in many cases has the clear potential to reach clinical relevance, as shown by an occasional change in drug effects or tolerability. For felodipine, nitrendipine, nisoldipine and saquinavir, the interaction was most marked with median increases of area under the curve (AUC) and/or the maximum (peak) plasma drug concentration after single-dose administration (Cmax) values exceeding 70% of respective control periods. Less pronounced, but possibly relevant, concentration increases were found for nifedipine, nimodipine, verapamil, cyclosporin, midazolam, triazolam and terfenadine. This list is not complete because many drugs have not been studied yet. The components of grapefruit juice which are the most probable causes of the interactions are psoralen derivatives, but the flavonoid naringenin may also contribute. Concomitant grapefruit juice intake does not generally decrease the variability of drug pharmacokinetic parameters. Therefore, it is recommended that patients refrain from drinking grapefruit juice when they are taking a drug that is extensively metabolised, unless a lack of interaction has already been demonstrated for the drug. It is also recommended that drugs possibly interacting with grapefruit juice should be appropriately labelled. A place for grapefruit juice as a drug-sparing agent in treatment involving expensive medicine cannot be derived from the information currently available on grapefruit juice interactions.
Fuhr U.
Institute for Pharmacology, Universitat zu Koln, Germany. [email protected]
Concomitant intake with grapefruit juice increases the concentrations of many drugs in humans. The effect seems to be mediated mainly by suppression of the cytochrome P450 enzyme CYP3A4 in the small intestine wall. This results in a diminished first pass metabolism with higher bioavailability and increased maximal plasma concentrations of substrates of this enzyme. The effect was most pronounced in drugs with a high first pass degradation and in many cases has the clear potential to reach clinical relevance, as shown by an occasional change in drug effects or tolerability. For felodipine, nitrendipine, nisoldipine and saquinavir, the interaction was most marked with median increases of area under the curve (AUC) and/or the maximum (peak) plasma drug concentration after single-dose administration (Cmax) values exceeding 70% of respective control periods. Less pronounced, but possibly relevant, concentration increases were found for nifedipine, nimodipine, verapamil, cyclosporin, midazolam, triazolam and terfenadine. This list is not complete because many drugs have not been studied yet. The components of grapefruit juice which are the most probable causes of the interactions are psoralen derivatives, but the flavonoid naringenin may also contribute. Concomitant grapefruit juice intake does not generally decrease the variability of drug pharmacokinetic parameters. Therefore, it is recommended that patients refrain from drinking grapefruit juice when they are taking a drug that is extensively metabolised, unless a lack of interaction has already been demonstrated for the drug. It is also recommended that drugs possibly interacting with grapefruit juice should be appropriately labelled. A place for grapefruit juice as a drug-sparing agent in treatment involving expensive medicine cannot be derived from the information currently available on grapefruit juice interactions.
geoboy
New member
geoboy said:
Never mind, answered my own question (see below). Appears the Seed Extract not effective for this purpose.
". . . It is compatible with other natural remedies and prescription drugs.
There are no reports of any drug interactions or contraindications of any kind. There is a danger in drinking fresh grapefruit juice or eating grapefruits when taking certain medications (consult a doctor). Grapefruit seed extract contains 0.1% or less of the compounds that increase absorption of certain medications. Consult your Physician to be sure. . . ."
In our case, we are seeking the "dangerous side effect"
http://www.pureliquidgold.com/benefits.htm
Zagreus
New member
Thanks for your post Huck, you go above and beyond!
A sentence from your post:
"A place for grapefruit juice as a drug-sparing agent in treatment involving expensive medicine cannot be derived from the information currently available on grapefruit juice interactions."
If I am reading this sentence properly and understanding you, what is said is that it is not fully understood how grapefruite juice neutralize phase I liver enzymes.
Thus, supplimenting with Naringenin as a grapefruite juice alternative to neutralize phase I liver enzymes may not be as effective?
I also did a search on Naringenin and found it packaged with fat burning suppliments. ECA Knock offs mainly. Though I could not find it as a main suppliment source.
If I did not understand properly that Naringenin is in fact a worth while suppliment to use in conjuction with Anavar as a Phase I liver enzymes neutrilizer, any ideas of a non-carb source / suppliment with sufficent concentration?
Thanks Again!
Zag
A sentence from your post:
"A place for grapefruit juice as a drug-sparing agent in treatment involving expensive medicine cannot be derived from the information currently available on grapefruit juice interactions."
If I am reading this sentence properly and understanding you, what is said is that it is not fully understood how grapefruite juice neutralize phase I liver enzymes.
Thus, supplimenting with Naringenin as a grapefruite juice alternative to neutralize phase I liver enzymes may not be as effective?
I also did a search on Naringenin and found it packaged with fat burning suppliments. ECA Knock offs mainly. Though I could not find it as a main suppliment source.
If I did not understand properly that Naringenin is in fact a worth while suppliment to use in conjuction with Anavar as a Phase I liver enzymes neutrilizer, any ideas of a non-carb source / suppliment with sufficent concentration?
Thanks Again!
Zag
Zagreus-Unfortunately,naringinen is only a PIECE of the puzzle which makes grapefruit so effective at neutralizing enzymatic destruction of oral meds.There are probably several co-factors which are working synergistically together to achieve the overall effect.Your best bet is using a non-sweetened grapefruit juice,or squeezing your own from a fresh grapefruit.
geoboy
New member
Followup-> the lnk above is just a distributor-geoboy said:
here is the manufacturers site (you can order here):
http://www.getyourgrapefruit.com/
here is the press release on the product- says its made from the inside, the skin, everything.
http://www.prnewswire.com/Tbutton/Beta/grapefruitoffer.html
Now karma me
, and Huck, whats your opinion on this product's specs.
Last edited:
hhajdo
New member
Grapefruit juice inhibits intestinal, not liver CYP3A4.
Even if the drug is CYP3A4 substrate, it's metabolism might not be affected by GFJ.
No one can tell you if it'll work with orals or not.
from "Grapefruit Juice and Drug Interactions"
Jessica R. Oesterheld, M.D.
...Gfj is a competitive and mechanism-based inhibitor, (similar in potency to TAO) of intestinal CYP 3A4 and CYP 3A5 but not of liver CYPs (Schmeidlin-Ren 1997). Inhibition occurs almost immediately if the gfj dose is high enough (e.g., a single glass of reconstituted frozen concentrate inhibits CYP3A4 within the first 4 hours. Schmiedlin-Ren 1997). Drug inhibition can last up to 3 days after gfj intake ceases (Tankanaga 2000a, Tankanga 2000 b).
Different preparations of gfj vary as CYP3A inhibitors. Reconstituted frozen concentrate is generally used in clinical studies, and it is a more potent CYP3A4 inhibitor than fresh gfj because gfj rind (which contains an oil that itself is a potent CYP3A inhibitor) is added to frozen concentrate during processing (Schmiedlin-Ben 1997). White gfj is a more potent inhibitor than pink gfj (Fukuda 2000).
To be significantly effected by gfj, not only must a CYP3A substrate have low bioavailability, but it must have a significant portion metabolized by intestinal CYP3A and/or be a substrate and/or inhibitor of PCP. Conversely, if a known substrate of CYP 3A can be shown be have no significant interaction with gfj, it can be assumed that it is mostly metabolized by hepatic CYPs (e.g., alprazolam Yasui 2000, quinine, Ho 1999). The ability to analyze the relative contributions of liver CYP 3A metabolism, intestinal CYP 3A metabolism and PGP effects to a CYP3A drug-drug interaction is now available by adding gfj as a "knock-out" drug and small bowel biopsy PGP studies to standard bioavailability studies. (Hall 1999).
Even if the drug is CYP3A4 substrate, it's metabolism might not be affected by GFJ.
No one can tell you if it'll work with orals or not.
from "Grapefruit Juice and Drug Interactions"
Jessica R. Oesterheld, M.D.
...Gfj is a competitive and mechanism-based inhibitor, (similar in potency to TAO) of intestinal CYP 3A4 and CYP 3A5 but not of liver CYPs (Schmeidlin-Ren 1997). Inhibition occurs almost immediately if the gfj dose is high enough (e.g., a single glass of reconstituted frozen concentrate inhibits CYP3A4 within the first 4 hours. Schmiedlin-Ren 1997). Drug inhibition can last up to 3 days after gfj intake ceases (Tankanaga 2000a, Tankanga 2000 b).
Different preparations of gfj vary as CYP3A inhibitors. Reconstituted frozen concentrate is generally used in clinical studies, and it is a more potent CYP3A4 inhibitor than fresh gfj because gfj rind (which contains an oil that itself is a potent CYP3A inhibitor) is added to frozen concentrate during processing (Schmiedlin-Ben 1997). White gfj is a more potent inhibitor than pink gfj (Fukuda 2000).
To be significantly effected by gfj, not only must a CYP3A substrate have low bioavailability, but it must have a significant portion metabolized by intestinal CYP3A and/or be a substrate and/or inhibitor of PCP. Conversely, if a known substrate of CYP 3A can be shown be have no significant interaction with gfj, it can be assumed that it is mostly metabolized by hepatic CYPs (e.g., alprazolam Yasui 2000, quinine, Ho 1999). The ability to analyze the relative contributions of liver CYP 3A metabolism, intestinal CYP 3A metabolism and PGP effects to a CYP3A drug-drug interaction is now available by adding gfj as a "knock-out" drug and small bowel biopsy PGP studies to standard bioavailability studies. (Hall 1999).
Outside of these studies,it definitely works in the real world.Just ask any of the vets/mods who have experimented with it(AF has a few threads up on it).I will be running it with my next upcoming var cycle.I will chug down 4-6 oz 10-15 minutes prior to the var.
hhajdo
New member
geoboy said:
Geoboy, not all oral drugs are CYP3A4 substrates.
Liver breakdown has nothing to do with it, since GFJ inhibits intestinal, not liver CYP3A4.
Even some drugs which are CYP3A4 substrates are not affected by GFJ.
I would still recommend you to try it, and if you do, post results here.
Potential Drug Interactions With Grapefruit list can be found here:
http://www.fhma.com/grapefruit.htm
hhajdo
New member
Milk Thistle inhibts CYP3A4 in Human Hepatocyte Cultures
:
http://dmd.aspetjournals.org/cgi/content/full/28/11/1270
:
http://dmd.aspetjournals.org/cgi/content/full/28/11/1270
