Thread: Grapefruit and greater absorption of AAS/PH

Originally Posted by TJTJ

Wasnt sure which section to open this thread in. If a Mod feels it should be moved to a more appropriate section, go for it.

Now to my question, who has included eating/drinking grapefruit to help increase absorption of their products? I have read around and found that one glass can last up to 24 hours in the body.

How much did you take? Did you see any increases? What is you impression of grapefruit on your cycles?

Grapefruit juice is supposed to keep levels of dianabol higher in your blood stream. There was a study done on this that I posted some months ago. I'll see if I can dig it up for you. It was only effective on dianabol, t-bol and halotestin though, not all oral aas or PH's.

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

...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..

Thanks man, I was looking for a post I believe was from you but couldnt find it.