Oral and Grapefruit Juice

[Growingpains]

Orals and Grapefruit Juice
I found this on another site. Check it out. Hopefully all you people with thread A.D.D. will be able to read the whole thing

Here's some info that many of you may know or have seen posted elsewhere. Basically, if you drink 250ml of grapefruit juice with your oral medications, it will increase their absorbtion, blood serum concentrations, etc...There was a study done specifically with some 17A drugs, but I decided not to copy it here. The article I did copy (below) is alot more reader-friendly and less technical.
If you are too lazy to read the article, here's the summary:
Drink 250ml of grapefruit juice (thats 8.4 ounces) with your oral steroids , and you just need to drink it once per day, even if you take your orals spread out throughout the day.
I've seen studies where absorbtion of some drugs was increased by up to 500%!
Also...before you ask about the effects of grapefruit juice on oral rec drugs the answer is YES, this applies to ALL ORAL MEDICATIONS/DRUGS.


Grapefruit juice interacts with a number of medications. This unusual discovery was made serendipitously in 1989 during an experiment designed to test the effect of ethanol on a calcium-channel blocker.1 The observed response was later determined to be due to the grapefruit juice delivery vehicle rather than the alcohol. In the past decade, the list of drug interactions with grapefruit juice has expanded to include several classes of medication, precipitating a recent advisory from Health Canada.2

The interaction: As little as 250 mL of grapefruit juice can change the metabolism of some drugs.3 This drug–food interaction occurs because of a common pathway involving a specific isoform of cytochrome P450 — CYP3A4 — present in both the liver and the intestinal wall. Studies suggest that grapefruit juice exerts its effect primarily at the level of the intestine.4

After ingestion, a substrate contained in the grapefruit binds to the intestinal isoenzyme, impairing first-pass metabolism directly and causing a sustained decrease in CYP3A4 protein expression.5 Within 4 hours of ingestion, a reduction in the effective CYP3A4 concentration occurs, with effects lasting up to 24 hours.6 The net result is inhibition of drug metabolism in the intestine and increased oral bioavailability. Because of the prolonged response, separating the intake of the drug and the juice does not prevent interference.

Individuals express CYP3A4 in different proportions, those with the highest intestinal concentration being most susceptible to grapefruit juice–drug interactions.5 An effect is seen with the whole fruit as well as its juice, so caution should be exercised with both.7 The precise chemical compound in grapefruit that causes the interaction has not been identified. There is no similar reaction with orange juice, although there is some suspicion that "sour oranges" such as the Seville variety, may have some effect.8 A recent study, however, that tested the known interference of grapefruit juice with cyclosporine showed no similar effect with Seville oranges.9

There is some interest in the potential therapeutic benefit of adding grapefruit juice to a drug regimen to increase oral bioavailability.3 The limitation is the individual variation in patient response. However, if the chemical that causes grapefruit's CYP3A4 inhibition is elucidated, there may be an opportunity to modulate that pathway in a controlled fashion.

What to do: Much of the data obtained on grapefruit juice–drug interactions involved measuring serum drug concentrations in small numbers of healthy volunteers. Because of the limited data and only occasional case reports,10 it is difficult to quantify the clinical significance for individual patients. One may assume that the interaction occurs primarily with oral medicines, and only with those that share the CYP3A4 metabolism pathway, with the consequence being increased oral bioavailability, higher serum drug concentrations and associated adverse effects.

Physicians should review medication lists often, with the goal of warning patients about adverse interactions. A list of medicines with which patients should not consume grapefruit is provided in Table 1.3,11,12 In the case of several medications that share the CYP3A4 metabolism pathway, but for which a clinical effect has not been elucidated or is theoretical, patients should be advised to consume grapefruit cautiously and be monitored for toxicity.

[JohnnyB]

Damn, I have seen that one in years, it never panned out

JohnnyB

[guest589745]

More info backing up this fact.

http://repositories.cdlib.org/cgi/vi...nutritionbytes

[powerliftmike]

this has been known for quite some time. most pharmacies warn patients from taking medicine with grapefruite b/c drug concentrations can become dangerously high. my dad takes cholestrol meds and doc told him not to drink/eat grapefruits.

[guest589745]

this has been known for quite some time. most pharmacies warn patients from taking medicine with grapefruite b/c drug concentrations can become dangerously high. my dad takes cholestrol meds and doc told him not to drink/eat grapefruits.

Me and another member stumbled upon this in our attempt to figure out how to increase the effects of intravenously/orally administered aas.


Still need to figure out how to increase injectables besides increasing the dose and frequency of administration.

[Property of Steroid.com]

Orals and Grapefruit Juice
I found this on another site. Check it out. Hopefully all you people with thread A.D.D. will be able to read the whole thing

Here's some info that many of you may know or have seen posted elsewhere. Basically, if you drink 250ml of grapefruit juice with your oral medications, it will increase their absorbtion, blood serum concentrations, etc...There was a study done specifically with some 17A drugs, but I decided not to copy it here. The article I did copy (below) is alot more reader-friendly and less technical.
If you are too lazy to read the article, here's the summary:
Drink 250ml of grapefruit juice (thats 8.4 ounces) with your oral steroids, and you just need to drink it once per day, even if you take your orals spread out throughout the day.
I've seen studies where absorbtion of some drugs was increased by up to 500%!
Also...before you ask about the effects of grapefruit juice on oral rec drugs the answer is YES, this applies to ALL ORAL MEDICATIONS/DRUGS.

If anyone's interested, I wrote this part about 4 years ago (in early 2002)...the part that follows is a C/P from the article I found the information in. I'm surprised that it survived this long on the boards....or that anyone was repeating what I was saying 4 years ago....

[guest589745]

And I meant INTRAMUSCULARLY, not intravenously.

[Warrior21]

Alot of people are saying it dosen't pan out, yet we are finding tons of studies to support it.

Skull beleive it or not injects are metabolized in the liver too. The difference is that orals go through the liver twice, while injects only once.

I think that grapefruit juice only inhibits CYP3A4 in the intestines though. But I read the drug flows through the intestines first, then the liver.

Will be back on in one or two hours guys.

[STEROIDZZ]

So is it wise to drink that amount of grapefruit juice while using dbol .. cause i drink grapefrut juice everyday ???