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Researchers Discover Why Grapefruit Juice Interacts With Drugs

Paregoric Kid

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Researchers Discover Why Grapefruit Juice Interacts With Drugs
05.09.06, 12:00 AM ET

TUESDAY, May 9 (HealthDay News) -- Researchers say they've identified the substances in grapefruit juice that can produce unwanted side effects when the juice is taken with certain drugs.

The discovery may make it possible to offer grapefruit juice that is free of these substances, called furanocoumarins, or add them to drugs to boost their effect, the researchers say.

People are routinely told by their doctors to avoid drinking grapefruit juice while taking a variety of medications because of potentially dangerous side effects. For instance, the beverage should be avoided when taking certain blood-pressure or cholesterol-lowering drugs, as well as HIV medications, organ-transplant drugs and sedatives.

The reason: Grapefruit juice can cause these drugs to enter the blood stream more efficiently, thereby increasing the dose and effect -- and the potential for undesirable and even dangerous side effects.

It had been thought that the flavonoids that give grapefruit juice its bitter taste caused the drug interaction, said study lead researcher Dr. Paul Watkins, director of the General Clinical Research Center at the University of North Carolina at Chapel Hill.
"What this study shows is that if you leave all that stuff in and take out a group of substances called furanocoumarins, you get rid of this property of the juice," Watkins said.

The study findings appear in the May issue of the American Journal of Clinical Nutrition.

In their study, Watkins and his colleagues compared orange juice, whole grapefruit juice and grapefruit juice that had the furanocoumarins removed. "We found that once you took the furanocoumarins out, the juice behaved like orange juice," he said. "That's certainly pretty convincing evidence that these are the active ingredients in the juice."
According to Watkins, there are three implications to the finding.

First, since the substances that cause drug interactions have been found, researchers can look at a number of other fruits to see if they contain furanocoumarins and predict whether they will cause the same problem.

Second, manufacturers of grapefruit juice could offer a version of the juice that has the furanocoumarins removed, eliminating the potential for drug interaction, Watkins said. "If there were a market, it would be possible to offer furanocoumarin-free grapefruit juice for people taking certain drugs, just as there is lactose-free milk," he said. "It doesn't affect the taste very much."

Third, furanocoumarins could be added to certain drugs to improve their "bioavailability," or ability to enter the blood stream, Watkins said. "The effect of grapefruit juice is to boost entry of these drugs into the body, and that can be a good thing if you can control it," he said. "It turns out that you don't just get more, you get a more reliable delivery -- there is less variation from one person to another when you do this," he said.

One expert thinks that adding furanocoumarins to medications might be the most important potential development to come out of this study.

"The ability to produce grapefruit juice free of the chemicals that interact with drugs is in some ways trivial, as few people would find avoiding grapefruit juice a true hardship," said Dr. David L. Katz, an associate professor of public health and director of the Prevention Research Center at Yale University School of Medicine.

But, the potential to use these chemicals in grapefruit juice to adjust drug levels is of real interest, Katz said. "As unknowns, chemicals in grapefruit juice interacting with drugs were merely a potential hazard. Now that they have been identified, they may be useful therapeutic agents in their own right," he said.

Link

Link added - Skyline
 
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Source? Pretty cool they've found out what's responsible for the interactions though.
 
pretty surprising that they didn't know what it was in grapfruit juice that caused cytochrome p450 inhibiton when there are already 450 inhibitor drugs on the market

also sorta surprising the article never mentions the p450 pathway
 
^They dont mention shit like that cuz they dont wanna confuse people. most people aint that smart. why the hell woudl they wanna know what the p450 pathway is right? I mean i read this site, know a lil bit when it comes to drugs, and i dont even understand all the talk about that shit when it comes up, so the average stupid reader who is only borderline interested in the story anyways aint gonna care about the specifics, they gotta make it easy for them to understand.
 
are there any rec drugs that this applies to? so our readers at home can be aware of the consequesnces.
 
^^ Benzodiazepines.

I'm curious if these substances could be isolated somehow. Think about it, taking a xanax bar along with extracted furanocoumarins or a grapefruit juice extract in powder form.
 
I've heard DXM mentioned on these forums aswell, no idea how valid that is though. I always just thought it was working as a placebo for some.
 
It always frustrates me when a pop science article is specifically about pharmacology or pharmacokinetics yet they leave out the the most important details.

If drug X is found to do something tell me exactly how it works and why in detail.

From a pharmacokinetic stand point, it's always a bonus if you can receive the same effect with a lower amount of a drug having to be administered.
 
Kritik4lM4ss said:
are there any rec drugs that this applies to? so our readers at home can be aware of the consequesnces.

http://www.bluelight.ru/vb/showpost.php?p=2532264&postcount=13

ToxicFerret said:
I'm curious if these substances could be isolated somehow.
From the article:
Paregoric Kid said:
Second, manufacturers of grapefruit juice could offer a version of the juice that has the furanocoumarins removed, eliminating the potential for drug interaction, Watkins said. "If there were a market, it would be possible to offer furanocoumarin-free grapefruit juice for people taking certain drugs, just as there is lactose-free milk," he said. "It doesn't affect the taste very much."

Third, furanocoumarins could be added to certain drugs to improve their "bioavailability," or ability to enter the blood stream, Watkins said. "The effect of grapefruit juice is to boost entry of these drugs into the body, and that can be a good thing if you can control it," he said. "It turns out that you don't just get more, you get a more reliable delivery -- there is less variation from one person to another when you do this," he said.
 
bowdenta said:
pretty surprising that they didn't know what it was in grapfruit juice that caused cytochrome p450 inhibiton when there are already 450 inhibitor drugs on the market

also sorta surprising the article never mentions the p450 pathway

That's exactly what I was thinking…

Ah, the vagaries of biochemistry…
 
maybe a new furanocoumarins type drug would be more effective than the p450 inhibitor drug(s) already out? I don't know, just a guess.
 
Second, manufacturers of grapefruit juice could offer a version of the juice that has the furanocoumarins removed, eliminating the potential for drug interaction, Watkins said. "If there were a market, it would be possible to offer furanocoumarin-free grapefruit juice for people taking certain drugs, just as there is lactose-free milk," he said. "It doesn't affect the taste very much."
this sounds slightly bad lets hope they dont make it a standard with gen tech and such

Third, furanocoumarins could be added to certain drugs to improve their "bioavailability," or ability to enter the blood stream, Watkins said. "The effect of grapefruit juice is to boost entry of these drugs into the body, and that can be a good thing if you can control it," he said. "It turns out that you don't just get more, you get a more reliable delivery -- there is less variation from one person to another when you do this," he said.

i think maybe i already came across this , in france you have codeine 30 mg "fizzy" tablets that contain grapefruit components (once the tablet dissolves the solution basically tastes like watered down grapefruit juice with apap ,) seems to me its hardly a coincidence but im not sure
 
they already knew it was furanocoumarins i thought :\

still would be cool to get them in a pill form so you don't have to chug shitloads of GFJ =D
 
^
yes , even the mechanism

maybe they unraveled a way to synth this stuff and apply it in medication?
 
i have a magazine from 1,5 years ago that talks about furanocoumarins and how they affect benzos and opiates (science & vie)

frizzantik is not bulshitting his faq is prolly older
 
Yes. I've recently seen articles as far back as 2001 that talked about it. His FAQ is definitely not older than that, a year and a half or something.
 
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