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Grapefruit Juice and Orals
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Freejay
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Grapefruit Juice and Orals - 03-15-2005, 10:33 PM

Hey Bro's here's a question for you. Do any of you know if grapefruit juice should be avoided while taking orals? I know some perscription drugs (Lipitor for example) are not to be used with grapefruit juice as it can caus too much of the drug to get into the liver. Just wondering if any oral gear is the same.


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tee
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03-16-2005, 07:55 AM

Punchier Narkotika--Med Grapefruktjuice
Et glass grapefrukt-juice hjelper ikke bare p-piller gå ned, det gjør det også mer potent. Nå, en studie i dagens Journal of Clinical Investigation har åpenbart hvorfor: Et stoff i juice kjemper en narkotika-nedverdigende enzym i tarmen. Innsikten kan være et første skritt mot å øke effektiviteten av noen p-stoffer.
Om 3 år siden, forskere bemerket at grapefrukt juice hjelper kroppen absorbere mange typer rusmidler, inkludert beroligende, hormoner, og proteasehemmere. En gruppe av leger fra University of Michigan og London Health Sciences Centre, i London, Ontario, satt ut for å undersøke. De er fokusert på et enzym i leveren og tarmen, kalt CYP3A4, som vanligvis bryter ned giftstoffer fra bortskjemt mat. "Det er [også] den mest profilerte av stoffet-nedbrytende enzymer," sier Paul Watkins, medlem av Michigan-teamet. Faktisk, det bidrar til nedbrytning av om lag halvparten av alle kjente humane legemidler.
Watkins og hans kolleger ga felodipin, en calcium kanal blokker brukes til å kontrollere høyt blodtrykk, 10 friske menn, både med og uten grapefrukt juice. Den grapefruktjuice økt blod konsentrasjoner av felodipin mer enn firling. Teamet har også målt konsentrasjoner av CYP3A4 nivåer i tarmen og funnet ut at de falt med 62%. Noe i grapefruktjuice ser ut til å være å blokkere virkningen av CYP3A4. Men konsentrasjonen av CYP3A4 i leveren var uendret--noe som tyder på at juice ikke påvirker den hastigheten som stoffet metaboliseres når den kommer inn i blodbanen.
Hvis den aktive ingrediensen av grapefruktjuice kan bli identifisert og isolert, rusmidler kan gjøres mer effektiv-og mindre kostbart per nyttig dose. Å legge grapefrukt er CYP3A4 blocker til en pille kan også sikre et sett dosering, en fordel, fordi folk vil naturligvis variere 10-fold i hvor mye av et stoff som de absorberer. "Det vil gjøre en stor forskjell i måten folk tar narkotika," spår Raymond Woosley, en pharmacologist ved Georgetown University Medical Center


Ikke spør meg hvor du skal få ting....Jeg prøver fortsatt å finne som en del ut!


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Freejay
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03-16-2005, 09:11 AM

I think the danger might also be that the 17-alpha and methalated substance might be more toxic to the liver. I'll do some more investigating as well.


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03-16-2005, 11:18 AM

Here's some research for you:

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 whole article.

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. Within 4 hours of ingestion, a reduction in the effective CYP3A4 concentration occurs, with effects lasting up to 24 hours. 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. An effect is seen with the whole fruit as well as its juice, so caution should be exercised with both. 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. A recent study, however, that tested the known interference of grapefruit juice with cyclosporine showed no similar effect with Seville oranges.

There is some interest in the potential therapeutic benefit of adding grapefruit juice to a drug regimen to increase oral bioavailability. 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, 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. 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
   
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03-16-2005, 04:30 PM

Thanks Oracle. I don't take any oral rec drugs, so that isn't an issue.


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ORACLE
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03-16-2005, 06:49 PM

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Opprinnelig Skrevet av Freejay
Thanks Oracle. I don't take any oral rec drugs, so that isn't an issue.
Yeah that's good....but the first paragraph should help you out as far as gear goes.
   
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