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Orals and Grapefruit

ihatethesesns

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Since there are a lot of guru's here I wanted to see what your opinions on the effects of drinking grapefruit juice when taking orals. I didn't do a lot of searching after I ran across this article, so if anyone has any links to similar studies I would like to read them.

© The American Physiological Society - Press Room - New Research Examines The Metabolic, Cardiovascular Effects Of Caffeine Consumed In Conjunction With Naringin, The Property That Makes Grapefruit Unique


New Research Examines The Metabolic, Cardiovascular Effects Of Caffeine Consumed In Conjunction With Naringin, The Property That Makes Grapefruit Unique
April 9, 2003 (San Diego, CA) -- If you are one of the millions of overweight Americans then your breakfast may be comprised of black coffee (five calories), dry toast (70 calories), and a grapefruit (60 calories for one-half). Many believe that grapefruit influences caffeine???s effect on the body.

A flavonoid (plant pigment) compound found in grapefruit, naringin gives grapefruit its characteristic bitter flavor. Grapefruit processors attempt to select fruits with low naringin content, and often blend juices obtained from different grapefruit varieties to obtain the desired degree of bitterness. Naringin is believed to enhance our perception of taste by stimulating the taste buds; that???s why some people consume a small amount of grapefruit juice before a meal.

But there are downsides to the healthy fruit.

Previous research has found that naringin interferes with enzymatic activity in the intestines thus slowing the breakdown of certain drugs and resulting in higher blood levels of the drug. A number of drugs that are known to be affected by the naringin in grapefruit include calcium channel blockers, estrogen, sedatives, medications for high blood pressure, allergies, AIDS, and cholesterol-lowering drugs. Consuming grapefruit or grapefruit juice may also extend caffeine levels and effects of caffeine.

While the effect of naringin on the metabolism of a drug can increase the drug's effectiveness, it can also result in dosages that are inadvertently too high. Therefore, many physicians do not recommend that patients take any drugs with grapefruit juice unless the interaction with the drug is known. In addition, the effects of drinking grapefruit juice is cumulative, which means that if you drank a glass of grapefruit juice daily with your medication for a week, the drug interaction would be stronger at the end of the week than at the beginning.

Flavonoids from grapefruit juice have been reported to affect hepatic metabolism by influencing Cytochrome P450 enzyme system, or CYP3A4. Many medications are metabolized in the liver by the cytochrome P450 enzyme complex or CYP3A4, including calcium channel blockers, HMG-CoA reductase inhibitors, anxiolytics, and some neuropsychiatrics. Adverse reactions have been reported by this drug-food interaction.

The majority of caffeine (approximately 86 percent) is metabolized by a similar enzyme group, CYP1A2. Other enzymes (CYP2E1 and CYP3A4) play a minor role in caffeine metabolism. However, naringin, the bitter constituent of grapefruit juice, has been documented to inhibit CYP34A activity in human liver as well as CYP1A2.

A New Study

New research has examined the metabolic and cardiovascular effects of caffeine consumed in conjunction with naringin. The authors of ???Caffeine and Naringin (Grapefruit) Does Not Affect Resting Energy Expenditure??? are Tasha L.P. Ballard and Matthew Vukovich, Ph.D., FACSM, of South Dakota State University, Brookings, SD. They will present their findings at the American Physiology Society (APS) conference, Experimental Biology 2003, being held April 11-15, at the San Diego Convention Center, San Diego, CA.

Dr. Vukovich hypothesized that a caffeine/naringin combined dosage would increase the half-life of caffeine and further alter metabolic markers and hemodynamic variables. The parameters of interest included oxygen consumption, respiratory exchange ratio, resting energy expenditure, heart rate and blood pressure.

Methodology

Caffeine-naïve subjects were studied before and after the ingestion of caffeine (C, 200mg) with and without naringin (100mg or 200mg). Data was collected for 8 hours every half-hour. Parameters measured included resting metabolic rate, heart rate, blood pressure, blood levels of caffeine.

Results

The consumption of caffeine significantly increased resting metabolic rate or calories burned at rest. However, the addition of naringin did not further enhance energy expenditure. Furthermore, blood levels of caffeine were not influenced by the co-consumption of naringin.

Conclusions

Their findings suggest that naringin, when taken in conjunction with caffeine, does not significantly alter caffeine metabolism. This is evidenced by the lack of significance among the trials with all of the predetermined variables. These results differ with reported results, which found significant increases in caffeine half-life in vivo. The reasons for the differences between the two studies may be due to a number of different factors, including methodology and subject population.

-end-
 
This thread pops up every couple months or so...I have posted research in the past. I'll try to dig it up again, but if you do a search on the forum...you'll probably find it.
 
Here it is from the Archives...

Posted by: GMO

A glass of grapefruit juice makes dianabol more effective

Achieve the same results by taking less dianabol? With grapefruit juice it???s possible. At least, you can read this into a review article published by Israeli pharmacologists in the European Journal of Clinical Nutrition.


The Israelis??? article is about the relationship between grapefruit and medicines. Scientists came across this at the end of the 1980s when doing experiments with strong-tasting substances. To make the comparison with the placebo group as true-to-life as possible, the researchers added a grapefruit taste to the preparations. Suddenly the levels of medicines being tested were much higher than you???d expect.

Later on it became clear that grapefruit inhibits the enzyme CYP3A4. This enzyme is responsible for breaking down substances in a process that scientists call 6beta-hydroxylation. Medicines that are sensitive to this form of breakdown disappear quickly out of the body.

And still later scientists discovered that grapefruit only inhibits CYP3A4 in the small intestine. The enzyme is also found in the liver, but grapefruit does not affect it there. Less CYP3A4 in the small intestine therefore means that a large group of substances is more easily absorbed by the body.

Since then another protein has been found that is inhibited by grapefruit: P-glycoprotein or P-gp. P-gp is also found in the small intestine and also decreases the absorption of pharmacological substances.

The figure below shows what the effect can be. The graph shows the concentration of the medicine lovastatine broken down by CYP3A4 after drinking large amounts of water ??? or large amounts of grapefruit juice.



You reach maximum effect, the researchers say, after drinking a 250 ml glass of grapefruit juice. Four hours after intake, 47 percent of the enzyme has been deactivated. Twelve hours after drinking the juice, the effect was still pretty optimal. Twenty four hours afterwards, a third of the effect still remains.

For the researchers, one of the conclusions of their study is that users of CYP3A4-sensitive medicines are better off avoiding grapefruit juice and the whole fruit.

Dianabol

Halotestin

Turinabol

The dosages for these medicines are not based on improved uptake, and if this happens the users may experience more negative side-effects.

In the future, the Israelis add, once the grapefruit-effect is better understood, it may be possible to add the active ingredients to medicines so that dosages, and manufacturers' production costs, can be lowered.

The relevance of this publication for chemical athletes is that certain oral anabolic steroids are also broken down by CYP3A4. In the mid nineties doping hunter Wilhelm Schaenzer published a study on beta-hydroxylation of testosterone, boldenon, methyltestosterone, halotestin, dianabol and turinabol, which had been administered orally to the test subjects.

Schaenzer examined the metabolites in the urine of his human test subjects. He discovered that the 6beta-hydroxylation of boldenone, testosterone and methyltestosterone was negligible, but was important for the breakdown of turinabol, dianabol and halotestin. Between 17 and 46 percent of these hormones leave the body in the 6beta-hydroxylated form.

Source:
Eur J Clin Nutr. 2004 Jan; 58(1): 1-9.
Steroids. 1995 Apr; 60(4): 353-66


Posted by: GMO

...and this is drug interactions for grapefruit juice:

GRAPEFRUIT JUICE DRUG INTERACTIONS
This food-drug interaction was actually discovered by accident. A study that was intending to test the interaction of alcohol and a blood pressure medication, used a mixture of alcohol with grapefruit juice to disguise the taste of alcohol for the study. Ironically, alcohol had no effect on the tested medication, but the grapefruit juice seemed to enhance the absorption of the drug. (4)

The researchers then confirmed the finding by comparing drug levels when taken with either grapefruit juice or water and found five-fold higher blood levels of the drug when it was taken with juice. Orange juice did not show this effect.

Grapefruit juice inhibits a special enzyme (CYP3A4) in the intestines that is responsible for the natural breakdown and absorption of many medications. When the action of this enzyme is blocked, the blood levels of these medications increase, which can lead potentially toxic side effects from the medications.

Research has suggested that flavonoids and/or furanocoumarin present in Grapefruit are the substances that act to block the enzyme in the intestines that normally metabolizes many drugs.

Some medications that interact with grapefruit juice: (5)

Statins (Cholesterol Lowering Drugs)
Antihistamines: Terfenadine
Calcium Channel Blockers (Blood Pressure Drugs):
Anti-convulsant: Tegretol (Carbamazepine)
Anxiolytics: Valium (Diazepam)
Anti-depressant: Sertraline Clomipramine
Cortico-steroids: Methylprednisolone
Oestrogens: Ethinyl estradiol
Anabolic Steroids: dianabol
Impotence Drug: Viagra

Although some drugs are given with others to enhance their effects, grapefruit juice should not be used for this purpose because its impact can be unpredictable and potentially dangerous.

The above list is by no means exhaustive. Please consult with your doctor or pharmacist regarding possible interactions between grapefruit juice and medications you may currently be taking if you consume grapefruit/ juice regularly..
 
I believe that 100% white grapefruit juice works best. I read this somewhere.
 
A capping company actually offered to add it to your ingredient list when making custom caps.
 
I see that white grapefruit juice is mentioned, would any type of grapefruit juice work in this case? I've also read else where that if you take your orals with 8 oz of grapefruit juice at your first dose, you are good for the rest of the day, even when there is a second dose. Anybody else hear of this or have heard differently? Thanks guys...
 
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