Increasing DBOL potency with grapefruit juice?

[michael tyson]

does anyone know how much grapefruit juice actually increases the potency? I have read that there is a 30% and 50% increase. Pretty significant difference between 30 and 50 so is it a guess and check results type of thing? anyone have experience with this?

[james21]

just get some tagamet, or 100% white grapefruit juice, and take and drink it about 5-10 minutes before taking the dbol

[michael tyson]

just get some tagamet, or 100% white grapefruit juice, and take and drink it about 5-10 minutes before taking the dbol

my question is how much does it increase the effects? I am going to plan my dosages accordingly and possibly run my dbol longer than 4 weeks if I can.

[Merc.]

I was recently asked about this .. this is a copy and paste of my reply .. Also I dont know if the exact rate of increased absorption can be truly estimated .. ( it will vary from person to person)..


There is evidence that a chemical in grapefruit juice inhibit a cytochrome enzyme known as CYP3A4 .. CYP3A4 is a very important enzyme to degrade things from this system ...

Only certain drugs ( ones that use the CYP3A4 pathway) are effected by grapefruit juice ..

You see MANY steroidal compounds do go by route of CYP3A4 .. which means that you should likely adjust your dose( if using grapefruit juice).. Or you could see GREATLY increased effects .. Keep in mind though as potency is increased. So is the potential of side effects ..

Grapefruit juice is a CYP3A4 inhibitor.... things that require this enzyme for first pass processing dont get processed the same way ..

[michael tyson]

well my plan is to take dbol 40mg ED weeks 1-4....

If I can, I would like to take dbol 30mg w/grapefruit juice ED weeks 1-5

basically I will take the dbol an extra week if grapefruit will allow me to obtain similar results

[james21]

well it lowers the enzyme that destroys the chemical to a certain extent. Just like merc said. Cimetidine is the chemical that does the job. It will also extend the half-life of the drug.

[james21]

Sure you can do that, just take something for liver support as well.

[michael tyson]

Sure you can do that, just take something for liver support as well.

tyler's detox factors in hand

[AnabolicBoy1981]

I personally dont like the idea. If you want more d-bol just take more d-bol. its not dirt cheap but its not terribly expensive. Thing is, you dont know how much its iihibiting the enzyme ona given day. We dont know if the effect increases or decreases over time. Taking more d-bol would be more predictable. You could have uneven fluctuating levels, and uneven fluctuating estrogen levels.

[james21]

why would it fluctuate ? if anything it would keep it more stable

[urbanbody]

I personally dont like the idea. If you want more d-bol just take more d-bol. its not dirt cheap but its not terribly expensive. Thing is, you dont know how much its iihibiting the enzyme ona given day. We dont know if the effect increases or decreases over time. Taking more d-bol would be more predictable. You could have uneven fluctuating levels, and uneven fluctuating estrogen levels.

I agree dbol is cheap enough to just take more to be certain. But this is all new to me never knew that grapefruit could help with dbol.

[michael tyson]

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. 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:
-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

[Merc.]

If you wanted some soild info on this subject here is a pretty good read by James Maskalyk...




Orals and Grapefruit Juice

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.



Merc.

[SuperLift]

I dont see how some juice could make the effects greater.. not saying its untrue, I just dont see how that is possible.

[james21]

because it contains a chemical that lowers a certain enzyme... it happens that grapefruit juice contains it. like i said tagamet contains 200mg's of the chemical, same thing. And its used for heart burn.

[michael tyson]

I dont see how some juice could make the effects greater.. not saying its untrue, I just dont see how that is possible.

if you want to see how it is possible, read the posts discussing it in this thread.

[.EA.]

So does this mean if I drink half a liter of grapefruit juice before the booze I can get gassed faster?



Sweet...






On another note, it says on almost every type of bipolar medication to avoid ingesting Grapefruit juice with the drug, so there has to be truth to it.

[BREW-MAN]

what about it helping out with protein intake ,will i get more out of each meal if i drink a glass of gfj with every meal?

[lovbyts]

That's funny, I am on week 2 1/2 of dbol in my cycle and have not felt much but this week I have been drinking grapefruit juice also which usually I only drink water and I have had crazy pumps like never before especially in my legs.

[Swifto]

I was recently asked about this .. this is a copy and paste of my reply .. Also I dont know if the exact rate of increased absorption can be truly estimated .. ( it will vary from person to person)..


There is evidence that a chemical in grapefruit juice inhibit a cytochrome enzyme known as CYP3A4 .. CYP3A4 is a very important enzyme to degrade things from this system ...

Only certain drugs ( ones that use the CYP3A4 pathway) are effected by grapefruit juice ..

You see MANY steroidal compounds do go by route of CYP3A4 .. which means that you should likely adjust your dose( if using grapefruit juice).. Or you could see GREATLY increased effects .. Keep in mind though as potency is increased. So is the potential of side effects ..

Grapefruit juice is a CYP3A4 inhibitor.... things that require this enzyme for first pass processing dont get processed the same way ..

Really?

Because I havent been able to find anything at all supporting that statement.

Patrick Arnold stated it may increase oral bioavailability, but also states it will increase hepatoxicity.

If oral steroids are metabolized by CYP34A it may help...

You got any data on it Merc...

[james21]

Same with anxiety meds, pain meds etc. Running some kind of liver support like he says he has in hand, well then.... plus i think the hepatotoxicity is over rated with many orals(note i didnt say all). I had a really wonderful chart somewhere i will look for that had the diff enzymes and what suppresses and raises each one. By the way smoking elevates cyp34a enzyme. I believe coffee does too... Ill try to find the chart

[Merc.]

Really?

Because I havent been able to find anything at all supporting that statement.

Patrick Arnold stated it may increase oral bioavailability, but also states it will increase hepatoxicity.

If oral steroids are metabolized by CYP34A it may help...

You got any data on it Merc...

Sup Swifty ...

Why of course ( I have some studies ) ... I didnt read where Patrick Arnold said that ( not saying I dont believe ya my friend ... I just didnt get any info about grapefruit juice and orals from him) ..

So anyways here is a study ...


Metabolism of anabolic steroids in humans: synthesis of 6 beta-hydroxy metabolites of 4-chloro-1,2-dehydro-17 alpha-methyltestosterone, fluoxymesterone, and metandienone.

Schänzer W, Horning S, Donike M.
Institut für Biochemie, Deutschen Sporthochschule Köln, Germany.

Hydroxylation at position 6 beta testosterone I (17 beta-hydroxyandrost-4-en-3-one) and the anabolic steroids 17 alpha-methyltestosterone II (17 beta-hydroxy-17 alpha-methylandrost-4-en-3-one), metandienone III (17 beta-hydroxy-17 alpha-methylandrosta-1,4-dien-3-one), 4-chloro-1,2-dehydro-17 alpha-methyltestosterone IV (4-chloro-17 beta-hydroxy-17 alpha-methylandrosta-1,4-dien-3-one), and fluoxymesterone V (9-fluoro-11 beta, 17 beta-dihydroxy-17 alpha-methylandrost-4-en-3-one) was achieved via light-induced autooxidation of the corresponding trimethysilyl 3,5-dienol ethers dissolved in isopropanol or ethanol. The reaction further yielded the 6 alpha-hydroxy isomer in low amounts. The 6 beta-hydroxy isomer of I-V and the 6 alpha-hydroxy isomers of I, III, and IV were isolated and characterized by 1H and 13C NMR, high-performance liquid chromatography, gas chromatography, and mass spectrometry. Human excretion studies with single administered doses of boldenone (17 beta-hydroxyandrosta-1,4-dien-3-one), 4-chloro-1,2-dehydro-17 alpha-methyltestosterone, fluoxymesterone, metandienone, 17 alpha-methyltestosterone, and [16,16,17-2H3] testosterone showed that 6 beta-hydroxylation is the major metabolic pathway in the metabolism of 4-chloro-1,2-dehydro-17 alpha-methyltestosterone, fluoxymesterone, and metandienone, whereas for boldenone, 17 alpha-methyltestosterone, and testosterone, 6 beta-hydroxylation is negligible.

PMID: 8539789 [PubMed - indexed for MEDLINE]



So in the above study he saying that the 6beta-hydroxylation of boldenone , testosterone and methyltestosterone was minimal .. but was important for the breakdown of dianabol and halotestin ...



Heres another study that basically states the same thing as the one above


Metabolism of anabolic steroids by recombinant human cytochrome P450 enzymes. Gas chromatographic-mass spectrometric determination of metabolites.

Rendic S, Nolteernsting E, Schänzer W.
Faculty of Pharmacy and Biochemistry, University of Zagreb, Croatia.

Metabolism of steroid hormones with anabolic properties was studied in vitro using human recombinant CYP3A4, CYP2C9 and 2B6 enzymes. The enzyme formats used for CYP3A4 and CYP2C9 were insect cell microsomes expressing human CYP enzymes and purified recombinant human CYP enzymes in a reconstituted system. CYP3A4 enzyme formats incubated with anabolic steroids, testosterone, 17alpha-methyltestosterone, metandienone, boldenone and 4-chloro-1,2-dehydro-17alpha-methyltestosterone, produced 6beta-hydroxyl metabolites identified as trimethylsilyl (TMS)-ethers by a gas chromatography-mass spectrometry (GC-MS) method. When the same formats of CYP2C9 were incubated with the anabolic steroids, no 6beta-hydroxyl metabolites were formed. Human lymphoblast cell microsomes expressing human CYP2B6 incubated with the steroids investigated produced traces of 6beta-hydroxyl metabolites with testosterone and 17alpha-methyltestosterone only. We suggest that the electronic effects of the 3-keto-4-ene structural moiety contribute to the selectivity within the active site of CYP3A4 enzyme resulting in selective 6beta-hydroxylation.PMID: 10630892 [PubMed - indexed for MEDLINE


This study also

Cytochrome P450 3A4-catalyzed testosterone 6beta-hydroxylation stereochemistry, kinetic deuterium isotope effects, and rate-limiting steps.

Krauser JA, Guengerich FP.
Department of Biochemistry and Center in Molecular Toxicology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-0146, USA.

Testosterone 6beta-hydroxylation is a prototypic reaction of cytochrome P450 (P450) 3A4, the major human P450. Biomimetic reactions produced a variety of testosterone oxidation products with 6beta-hydroxylation being only a minor reaction, indicating that P450 3A4 has considerable control over the course of steroid hydroxylation because 6beta-hydroxylation is not dominant in a thermodynamically controlled oxidation of the substrate. Several isotopically labeled testosterone substrates were prepared and used to probe the catalytic mechanism of P450 3A4: (i) 2,2,4,6,6-(2)H(5); (ii) 6,6-(2)H(2); (iii) 6alpha-(2)H; (iv) 6beta-(2)H; and (v) 6beta-(3)H testosterone. Only the 6beta-hydrogen was removed by P450 3A4 and not the 6alpha, indicating that P450 3A4 abstracts hydrogen and rebounds oxygen only at the beta face. Analysis of the rates of hydroxylation of 6beta-(1)H-, 6beta-(2)H-, and 6beta-(3)H-labeled testosterone and application of the Northrop method yielded an apparent intrinsic kinetic deuterium isotope effect ((D)k) of 15. The deuterium isotope effects on k(cat) and k(cat)/K(m) in non-competitive reactions were only 2-3. Some "switching" to other hydroxylations occurred because of 6beta-(2)H substitution. The high (D)k value is consistent with an initial hydrogen atom abstraction reaction. Attenuation of the high (D)k in the non-competitive experiments implies that C-H bond breaking is not a dominant rate-limiting step. Considerable attenuation of a high (D)k value was also seen with a slower P450 3A4 reaction, the O-dealkylation of 7-benzyloxyquinoline. Thus P450 3A4 is an enzyme with regioselective flexibility but also considerable regioselectivity and stereoselectivity in product formation, not necessarily dominated by the ease of C-H bond breaking.

PMID: 15772082 [PubMed - indexed for MEDLINE]





Merc.

[Swifto]

Thanks Merc. I got PA's thoughts on GJ and steroids from BB.com.

Its strange, 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.

For Dbol , Halo, grapefruit juice maybe used as an addition, but I wouldnt be using less Dbol to make up for the increase in bioavailability.

[Critical Mass]

This is good news.

[SuperLift]

hmm interesting.. maybe ill try it next time.

[Merc.]

Thanks Merc. I got PA's thoughts on GJ and steroids from BB.com.

Its strange, 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.

For Dbol, Halo, grapefruit juice maybe used as an addition, but I wouldnt be using less Dbol to make up for the increase in bioavailability.

Yep the human body is so dam complex ( it really is insane ).. some compounds take diffrent pathways ( ones you wouldnt really expect them too )..

Take Test Undecanoate ( Andriol ) for instance .. It is able to by-pass the liver and go through the lymphatic system ...


Merc.

[G-Force]

sweet
so a 250ml glass with every dianabol dose? so taking 3 tabs a day would mean three glasses
or better to drink it allthrough the day?

dunno about anyone else but i am stocking up on grapefruit juice

[Merc.]

sweet
so a 250ml glass with every dianabol dose? so taking 3 tabs a day would mean three glasses
or better to drink it allthrough the day?

dunno about anyone else but i am stocking up on grapefruit juice

If one was to wanna possible try it ...

From the studies and articles I have read it would prob be best to
Drink 250ml of grapefruit juice total ( like a little over 8 ounces ) with your oral .. You would only need to drink it once per day... even if you take your orals throughout the day.


Merc.

[Ashop]

just get some tagamet, or 100% white grapefruit juice, and take and drink it about 5-10 minutes before taking the dbol

Ive heard the TAGEMET mentioned in some other circles as well,,,same purpose.

[Merc.]

Ive heard the TAGEMET mentioned in some other circles as well,,,same purpose.

Yea some people hate the taste of grapefruit juice ....





Merc.

[james21]

Hey its all the same chemical, doing what we want. I like grapefruit juice, but for convenience i pop some tagamet.

[Merc.]

Hey its all the same chemical, doing what we want. I like grapefruit juice, but for convenience i pop some tagamet.

Yea for convenience tagamet would suffice ..





Merc.

[Merc.]

Anyone that posted here tried it yet ?? just curios ??



Merc.

[Kibble]

I will try the grapefruit juice... but I may add a teaspoon of sugar. Thanks for bumping this thread because I had no idea about this. I am going to just eat a grapefruit in the morning before I start the dbol

[big_k]

Would the Grapejuice work with Anavar ?

And secondly since I will be doing Low Carb on Cut, I can't be pounding grapefruit juice, where can I get tagamet, is it legal?

Edit: Found tagamet

[Merc.]

I will try the grapefruit juice... but I may add a teaspoon of sugar. Thanks for bumping this thread because I had no idea about this. I am going to just eat a grapefruit in the morning before I start the dbol

[Berserker88]

I personally dont like the idea. If you want more d-bol just take more d-bol. its not dirt cheap but its not terribly expensive. Thing is, you dont know how much its iihibiting the enzyme ona given day. We dont know if the effect increases or decreases over time. Taking more d-bol would be more predictable. You could have uneven fluctuating levels, and uneven fluctuating estrogen levels.

Isnt dirt cheap in aus.