Oral steroids and grapefruit juice???

[Presa]

Can you explain "chemically" how taking grapefruit juice with some prescription medication, and possibly oral AAS causes an increase in potency?

I know that many drug scripts say not to take with grapefruit juice, and I know many bro scientist say its a way to increase oral effectiveness of AAS...

 

[FL3X MAGNUM]

http://en.m.wikipedia.org/wiki/Grapefruit_drug_interactions

 

[Presa]

^^^^^nailed it^^^^^

 

[mike0589]

I see mainly MAOI inhibitors and OTC narcotics, not AAS.

Possible other in-vivo data?

 

[FL3X MAGNUM]

Grapefruit juice inhibits the CYP3A4. CYP3A4 is partially responsible for the timely metabolism of prohormones. That's about as far as I can get into that without talking out of my ass.
Bump for PA.

I'm sure he's answered this question before btw

 

[Quadzilla99]

What supplement contains grapefruit juice and steroids?

 

[mike0589]

From what I've gathered, CYP3A4 is an enzyme mainly involved in glucocorticoids and some pharmacological agents.

Apparently, it metabolizes some steroids and carcinogens.

I would love to hear from Coop, PA, or other seasoned vets about this.

 

[Beejis60]

They are effective but the effect is highly variable from person to person. Many steroids interact with CYP3A4; for the most part, they are converted to weaker metabolites. 6b-hydroxylation seems to be the most abundant steroid-CYP3A4 interaction. 3-keto-4-ene structure is a moiety that mostly undergoes 6b-hydroxylation. DHT derivatives like 1T and M1T which don't contain the 4-ene double bond might be less susceptible to inactivation via 6b-hydroxylation. This does not mean they are not deactivated by hydroxylating other positions though. Hydroxylation at other positions have also been observed. CYP 3A4 also hydroxylates cholesterol into oxysterols.

Bergamottin, dihydroxybergamottin, and paradisin (found in grapefruit juice) seem to be the main CYP3A4 inhibitors.

Naringenin might be a CYP19 (aromatase) inhibitor. Quercetin seems to be an aromatase activator probably by increasing intracellular cAMP concentrations. Both are found in grapefruit juice. Their dual interaction makes it difficult to determine what kind of effect grapefruit juice would have on aromatizing steroids. However, if you manage to increase the bioavailability of a steroid via CYP3A4 inhibition, that would mean more of the steroid is free to bind to aromatase, indirectly increasing estrogen levels. Naringen also seems to be a 17b-HSD inhibitor which would not be good for 17-ketone prohormones which depend on 17b-HSD reduction to produce the active 17-hydroxyl steroid.

There is also some evidence to suggest that morin, galangen, kaempferol, quercetin, and naringenin are esterase inhibitors. Meaning taking grapefruit juice with esterified steroids might prevent or slow down the hydrolyses of the ester.

 

[Patrick Arnold]

Can you explain "chemically" how taking grapefruit juice with some prescription medication, and possibly oral AAS causes an increase in potency?

I know that many drug scripts say not to take with grapefruit juice, and I know many bro scientist say its a way to increase oral effectiveness of AAS...

It might increase blood levels of some orals yes. How much cant really be estimated

 

[Patrick Arnold]

Grapefruit juice inhibits the CYP3A4. CYP3A4 is partially responsible for the timely metabolism of prohormones. That's about as far as I can get into that without talking out of my ass.
Bump for PA.

I'm sure he's answered this question before btw

the methylated orals are often metabolized by hydroxylation reactions which would fall under that class of enzymes

 

[Patrick Arnold]

They are effective but the effect is highly variable from person to person. Many steroids interact with CYP3A4; for the most part, they are converted to weaker metabolites. 6b-hydroxylation seems to be the most abundant steroid-CYP3A4 interaction. 3-keto-4-ene structure is a moiety that mostly undergoes 6b-hydroxylation. DHT derivatives like 1T and M1T which don't contain the 4-ene double bond might be less susceptible to inactivation via 6b-hydroxylation. This does not mean they are not deactivated by hydroxylating other positions though. Hydroxylation at other positions have also been observed. CYP 3A4 also hydroxylates cholesterol into oxysterols. .

16 hydroxylation is often observed with methylated androgens

 

[mike0589]

Off topic, but is there anything that can be taken to enhance absorption, nor hinder absorption?

I've seen a few members mention taking oral AAS's with EPA and DHA.

 

[murk01]

u guys are blowing my mind!!
so i should be popping my sd with grapefruit juice and fish oils?

 

[Patrick Arnold]

Off topic, but is there anything that can be taken to enhance absorption, nor hinder absorption?

I've seen a few members mention taking oral AAS's with EPA and DHA.

oral steroids generally have good bioavailability. I wouldnt rack your brain over this.

 

[Beejis60]

u guys are blowing my mind!!
so i should be popping my sd with grapefruit juice and fish oils?

Not necessarily. Fish oils are a waste. While I eat plenty of g-fruits, the only thing close to g-fruit juice to me is my IPAs I drink... Dat Double Trouble is dank as fuk

 

[Patrick Arnold]

Not necessarily. Fish oils are a waste.

for steroid bioavailability perhaps but fish oil is cardioprotective and great anti-inflammatory

 

[jbree]

What about just taking orals on an empty stomach? any issues with that?

 

[Patrick Arnold]

What about just taking orals on an empty stomach? any issues with that?

perhaps not but i take most pills with food to be safe

 

[jbree]

perhaps not but i take most pills with food to be safe

Thanks!

 

[tinytony]

perhaps not but i take most pills with food to be safe

Care to explain your reasoning? I've just always read the nature of a PH, or oral steroid causes it to be rendered useless by fats. If this is not based in fact I'm happy to change. I've just always taken them on empty stomach and had great gains.

 

[jbryand101b]

Care to explain your reasoning? I've just always read the nature of a PH, or oral steroid causes it to be rendered useless by fats. If this is not based in fact I'm happy to change. I've just always taken them on empty stomach and had great gains.

Steroids are fat soluble. So you would want to take say ment (not menadione) an active steroid with no 17a protection with foods containing fats in hopes of increasing absorption. Washed down with freshly squeezed grapefruit juice of course.

 

[Madevilz]

I heard only white grapefruit juice is effective?

 

[Patrick Arnold]

Care to explain your reasoning? I've just always read the nature of a PH, or oral steroid causes it to be rendered useless by fats. If this is not based in fact I'm happy to change. I've just always taken them on empty stomach and had great gains.

why would fat render a steroid useless? That makes no sense

 

[jbryand101b]

why would fat render a steroid useless? That makes no sense

that's because you are smarter than the average bear!

 

[tinytony]

that's because you are smarter than the average bear!

You have a talent for belittling people man.

 

[bigbb123]

You have a talent for belittling people man.

No nuthugging, but i dont think anyone on this forum is qualified to "belittle" Patrick Arnold LOL

 

[tinytony]

No nuthugging, but i dont think anyone on this forum is qualified to "belittle" Patrick Arnold LOL

Haha not what I meant either.. Every thread I ever post in jbry pops in and let's go with enough comments to show how smart he is and how stupid I am. And not just me. Can't even ask a question or discuss with anyone else. Veeeeeeery tired of it. there are a lot of theories on this topic. Fats with methyl, fats with non methyl, fats with 17 aa steroids or 17 a. So many mixes here. Supposedly 17 aa are fat soluble and then someone else says no. Lota PHs used to recommend on empty stomach. Some aren't anymore. I've always taken on empty except for one cycle and have gotten awesome results. That's why I wanted to see what Patrick A has to say. Hes a chemist I trust and well known. Which ones could possibly be helped by fat and will non methyl PH like Trenavar be the same? I've tried to get my hands on as much info ads possible but too many people disagree

 

[jbryand101b]

You have a talent for belittling people man.

That's because I love you guys so much, like I love my left nut!

 

[tinytony]

That's because I love you guys so much, like I love my left nut!

Lol I can feel the love

 

[jbryand101b]

Lol I can feel the love

:smoker:

 

[Patrick Arnold]

Haha not what I meant either.. Every thread I ever post in jbry pops in and let's go with enough comments to show how smart he is and how stupid I am. And not just me. Can't even ask a question or discuss with anyone else. Veeeeeeery tired of it. there are a lot of theories on this topic. Fats with methyl, fats with non methyl, fats with 17 aa steroids or 17 a. So many mixes here. Supposedly 17 aa are fat soluble and then someone else says no. Lota PHs used to recommend on empty stomach. Some aren't anymore. I've always taken on empty except for one cycle and have gotten awesome results. That's why I wanted to see what Patrick A has to say. Hes a chemist I trust and well known. Which ones could possibly be helped by fat and will non methyl PH like Trenavar be the same? I've tried to get my hands on as much info ads possible but too many people disagree

if u want me to elaborate i would say that the prohormones you take in large dosages might benefit by some fat because there is a lot to solubilize and absorb.

Another factor is whether the steroid is properly formulated. Is the steroid milled down to a fine enough particle size so it can absorb well without needing dietary fat to help it dissolve/disperse?

I think taking with food with some fat is a good idea to be safe. However if you have some digestive problem like diarrhea with fat malabsorption then the possibility exists that you can poop some out

 

[tinytony]

if u want me to elaborate i would say that the prohormones you take in large dosages might benefit by some fat because there is a lot to solubilize and absorb.

Another factor is whether the steroid is properly formulated. Is the steroid milled down to a fine enough particle size so it can absorb well without needing dietary fat to help it dissolve/disperse?

I think taking with food with some fat is a good idea to be safe. However if you have some digestive problem like diarrhea with fat malabsorption then the possibility exists that you can poop some out

Yeah that makes sense to me. I'll tinker with fat consumption at the same time and see how it feels!

 

[Beejis60]

Another factor is whether the steroid is properly formulated. Is the steroid milled down to a fine enough particle size so it can absorb well without needing dietary fat to help it dissolve/disperse?

This. I always take steroids with high fats; probably 10-15g in the meal.

And whoever that guy is about fats blocking steroids, I got bulk phera LONG ago and it would only dissolve well in oil, like cooking oil. And at a very high dose, I can say that it worked incredibly well... like, my body couldn't keep up with the strength gains well.

fyi, it wasn't JUST phera though.

 

[tinytony]

This. I always take steroids with high fats; probably 10-15g in the meal.

And whoever that guy is about fats blocking steroids, I got bulk phera LONG ago and it would only dissolve well in oil, like cooking oil. And at a very high dose, I can say that it worked incredibly well... like, my body couldn't keep up with the strength gains well.

fyi, it wasn't JUST phera though.

Man ill gladly stand down and change my dosing if this makes it more effective. I'm all about it but I felt like hearing all sides first. But this makes sense.

 

[Patrick Arnold]

This. I always take steroids with high fats; probably 10-15g in the meal. And whoever that guy is about fats blocking steroids, I got bulk phera LONG ago and it would only dissolve well in oil, like cooking oil. And at a very high dose, I can say that it worked incredibly well... like, my body couldn't keep up with the strength gains well.fyi, it wasn't JUST phera though.

before phera was a supplement i made it and provided it to atheltes as an undetectable steroid. many used it very succesfully (at least one big baller owes his career to it) and never got caught. I imagine that by this point the statute of limitations is up so i dont have to be afraid to say thisi provided the stuff dissolved in corn oil and thats how they took it

 

[tinytony]

before phera was a supplement i made it and provided it to atheltes as an undetectable steroid. many used it very succesfully (at least one big baller owes his career to it) and never got caught. I imagine that by this point the statute of limitations is up so i dont have to be afraid to say thisi provided the stuff dissolved in corn oil and thats how they took it

Nice! So would you say it'd be better absorption to take them dissolved like that or eat with fats and hope for the best? That is an interesting idea ..

 

[Patrick Arnold]

Nice! So would you say it'd be better absorption to take them dissolved like that or eat with fats and hope for the best? That is an interesting idea ..

hope for the best

i dissolved in oil because it allowed it to be dosed accurately. i didnt have enough material to encapsulate

 

[tinytony]

hope for the best

i dissolved in oil because it allowed it to be dosed accurately. i didnt have enough material to encapsulate

I hear you. So you would say treat nonmethyls the same? I guess they would be the same only no methyl for keeping liver from degrading it. Isn't there a relation between testosterone and fats/cholesterol? Meaning testosterone is formed from this or something.. that would say that steroids or testosterone derivatives are fat-friendly..

 

[Patrick Arnold]

I hear you. So you would say treat nonmethyls the same? I guess they would be the same only no methyl for keeping liver from degrading it. Isn't there a relation between testosterone and fats/cholesterol? Meaning testosterone is formed from this or something.. that would say that steroids or testosterone derivatives are fat-friendly..

androgens can affect lipid and cholesterol biosynthesis in the liver

 

[tinytony]

Bringing up this thread again. Should I treat M1T as all fat soluble steroids with its protection? Its small doses also. I'm afraid it'll slip thru

 

[tinytony]

i used to buy m1t powder before the ban and dissolve it in oil to dose it accurately. it worked very well. i tried dissolving sd powder in oil and 20mg in oil was better than 30mg in capsules. of course this is anecdotal because i cant be sure there was actually 10mg in each cap as the label claimed and i dosed the oil 5mg 4 times a day and the caps 10mg 3 times a day.
as far as non methyls, exemestane is a steroidal compound, 6-methylenandrosta-1,4-diene-3,17-dione, and the prescribing info states-

Absorption: Following oral administration of radiolabeled exemestane, at least 42% of radioactivity was absorbed from the gastrointestinal tract. Exemestane plasma levels increased by approximately 40% after a high-fat breakfast.

http://www.drugs.com/pro/aromasin.html

I'm going to try it with coconut oil. MCTs are good energy and they are fats and so could be better delivery system in one way than taking them with just a fatty meal