Getting The Most From Your Orals

  1. Getting The Most From Your Orals

    (Perverts, I swear) From Hooker

    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.
    Here's the article:

    James Maskalyk
    Editorial Fellow, CMAJ

    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.

  2. I remember reding this on labels of many prescription medications......especially with Zocor a cholesteol lowering drug which I didn't end up taking. It said to absolutely not drink GF juice when taking the med because it interupts the effects of the medication in some way.

    Interesting read.....YJ you must have alot of time on your hands or really like the research.....with all these studies you pull up. LOL! keep'em coming....learn something new every day.

  3. Aww man... I thought I was going to get the most from another kind of orals... oh well

  4. Great read! Everyone should stock up on Grapefruit juice......

  5. This is a time when carbs are DAMN GOOD!
    For answers to board issues, read the Suggestion and News forum at the bottom of the main page.

  6. Originally posted by pogue
    Aww man... I thought I was going to get the most from another kind of orals... oh well

    funny, for some reason I thought the same

  7. I took my winny with grapefruit juice 2 cycles ago. Really didnt see a huge difference, but something like this is so subjective, it is hard to tell

  8. well , just eat the grape juice post workout then , lets make use of the insulin spike and as well as make use of the orals better a doc over here told me this actually , i looked all over for info on this , glad yj posted this .

  9. Can i use grapefruit juice on a regular basis for two/three weeks while on methyl-1-test and then stop afterwards without affecting my everyday usage of zocor ya think? i figure two weeks of super-effective zocor wouldnt really hurt me, or even more cautius would be for those 2-3 weeks to half my zocor dosage or just stop altogether.

  10. grapefruit juce increases uptake of all meds one is taking at the time.....If you read the zocor instructions, it mentions to stay away from gfj. I recently read up on this, just search for 'grapefruit juice and zocor' on the'll get tons of hits. I actually did it for a couple of wwks and didn't notice a diff....I was and still using m4ohn.


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