Aromasin, Arimidex, Letrozole, Oh My!

[Dr Pangloss]

very interesting. it seems the buildup induced by aromatase inhibition results in the accumulation of competitive inhibitors androstendione and testosterone which limits the long-term efficacy in men.

This is a simple problem. if you get maximal suppression of 62% at 12 hours from one dose but it is reduced to 38% after 10 days, you should take more (as long as it's well-tolerated). I think what they're proposing is reasonable. However, it also suggests that simply using higher doses of any of the aromatas inhibitors (including letrozole) in males will result in the maximal suppression numbers approaching those obtained in females with lower doses because the problem is the increase in competitive inhibition. If that is the case, then I'd have to go with high-dose letro for gyno or precontest water reduction and aromasin for everything else.

Dosing aromasin at 12 hrs is a great idea and may be all that is required since it is a suicide inhibitor. That way, constant high levels of aromasin will keep androstenedione and Test from binding aromatase so much.

the arimidex study in men is the one i was thinking of. Paradoxically, 1 mg was no better than 0.5 mg ed. This would tend to argue that competitive inhibition was not the problem. Also, i wish they had not combined the 25mg and 50 mg results.

If these drugs are less effective in men for some idiopathic reason that cannot be overcome with higher doses, then aromasin, arimidex, or perhaps a combination of AIs may be the best way to go to really dry someone out.

[Dr Pangloss]

Heavy, another thing. If these guys are right about Test competing the AI away, then pretty much the entire bodybuilding community has been under dosing on AIs while on cycles of Testosterone.

[heavyiron]

very interesting. it seems the buildup induced by aromatase inhibition results in the accumulation of competitive inhibitors androstendione and testosterone which limits the long-term efficacy in men.

This is a simple problem. if you get maximal suppression of 62% at 12 hours from one dose but it is reduced to 38% after 10 days, you should take more (as long as it's well-tolerated). I think what they're proposing is reasonable. However, it also suggests that simply using higher doses of any of the aromatas inhibitors (including letrozole) in males will result in the maximal suppression numbers approaching those obtained in females with lower doses because the problem is the increase in competitive inhibition. If that is the case, then I'd have to go with high-dose letro for gyno or precontest water reduction and aromasin for everything else.

Dosing aromasin at 12 hrs is a great idea and may be all that is required since it is a suicide inhibitor. That way, constant high levels of aromasin will keep androstenedione and Test from binding aromatase so much.

the arimidex study in men is the one i was thinking of. Paradoxically, 1 mg was no better than 0.5 mg ed. This would tend to argue that competitive inhibition was not the problem. Also, i wish they had not combined the 25mg and 50 mg results.

If these drugs are less effective in men for some idiopathic reason that cannot be overcome with higher doses, then aromasin, arimidex, or perhaps a combination of AIs may be the best way to go to really dry someone out.

I think one of the problems with the study is they tested E2 24 hours after the last dose of Aromasin. So basically the guys took Aromasin for 10 days and they waited 24 hours later (day 11) to test E2, estrone, and estrone sulfate concentrations. Had they administered Aromasin every 12 hours for 10 days and then tested E2 12 hours later (day 10.5) I feel pretty confident we would see greater supression. Now that it has been discovered how short the half life is in men hopefully they will design a trial to better understand E2 supression in the future.

I would be very curious to see the half life of Arimidex in men at this point. This may give us a better strategy for dosing that AI.

You bring up an interesting point. Would the combination of AI's create a greater effect? Since AI's have different supressions of E2, estone and estone sulfate.

This raises another question. Is E2 the main cause of water retention or does estone have an influence as well? I am reminded of the Aromasin study where they looked at various markers. Not just E2.


FIG. 1. Estrogen and androgen plasma levels after 10 d of daily exemestane (25 or 50 mg) in healthy young males (mean ± SD; n = 9–11). To convert to Systeme International units: estradiol, picomoles per liter (x3.671); estrone, picomoles per liter (x3.699); androstenedione, nanomoles per liter (*0.003492); and testosterone, nanomoles per liter (x0.03467).

[heavyiron]

Heavy, another thing. If these guys are right about Test competing the AI away, then pretty much the entire bodybuilding community has been under dosing on AIs while on cycles of Testosterone.

I completely agree.

I have seen labs that absolutely blew me away. Guys with E2 levels WAY over 200pg/ml while running low dose AI's. I personally experimented with 25mg Aromasin every day for 10 weeks on cycle and my strength was outstanding as well as sex drive. I am confidant that crushing E2 is unlikely on a cycle of testosterone. When you look at the data these AI's free up T and control E2. I really think we can get more from our cycles with regular doses of AI's.

[Dr Pangloss]

If the difference in men is idiopathic then using a combination of AIs is probably the best strategy for getting the lowest E2 levels.

Pretty sure estrones also cause water retention. I will confirm in pubmed, but it might be a hard slog, since i'm not sure E2 can be separated from estrone in vivo. Estrone is converted into E2 in the liver.

ok, yes it does cause water retention.

All this time people have been hyper concerned about killing estrogen and it appears with normal doses they're not even getting close.

I'm helping a guy prep for a contest now. I'm going to have him dry-run a combination of letrozole then a combination of aromasin and letrozole (25 mg and 2.5 mg) and see what happens.

[heavyiron]

If the difference in men is idiopathic then using a combination of AIs is probably the best strategy for getting the lowest E2 levels.

Pretty sure estrones also cause water retention. I will confirm in pubmed, but it might be a hard slog, since i'm not sure E2 can be separated from estrone in vivo. Estrone is converted into E2 in the liver.

ok, yes it does cause water retention.

All this time people have been hyper concerned about killing estrogen and it appears with normal doses they're not even getting close.

I'm helping a guy prep for a contest now. I'm going to have him dry-run a combination of letrozole then a combination of aromasin and letrozole (25 mg and 2.5 mg) and see what happens.

I think at the end of the day the best strategy is dropping aromatizing compounds a few weeks before the comp AND continuing to use an AI.

I remember a certain "guru" who used to say he took guys to the stage on a gram of T. Hmmmmm....

[Dr Pangloss]

I think at the end of the day the best strategy is dropping aromatizing compounds a few weeks before the comp AND continuing to use an AI.

I remember a certain "guru" who used to say he took guys to the stage on a gram of T. Hmmmmm....

i remember a certain guru saying 10 mg of aromasin ed was all he needed to cut estrogen and not effect libido. Well, on a gram of test ew 10 mg of aromasin isn't going to cut much estrogen at all...

I have the contest guy dropping all test except test prop (at 300 mg) in "the secret weapon," which is Test prop, masteron prop, and Tren acetate The rest of the drugs are non-estrogenic, non-aromatizable.

even so, tren is reported to have about 20% of the estrogenic activity of E2. Not much, but enough that hitting AIs hard in the last 3 weeks will still leave a little estrogen activity, regardless of how hard you push it.

[ski 1]

Thanks for bring all this information to the masses... Never knew how important using AI in a cycle was... Just got bloods back and my estrogen levels were at 97... Currently using 25mg of aromasin every 12 hours... Dropping water fast!!!! Will check bloods again in two weeks!!!!!!

[Dr Pangloss]

Thanks for bring all this information to the masses... Never knew how important using AI in a cycle was... Just got bloods back and my estrogen levels were at 97... Currently using 25mg of aromasin every 12 hours... Dropping water fast!!!! Will check bloods again in two weeks!!!!!!

that's actually very helpful. Was it 97 before you started aromasin? How much Test and what ester of Test are you taking?

[Kaladryn]

It is interesting to note that reducing E2 has little effect on E1, which is a competitive inhibitor of E2 in most tissues.

[Mike Arnold]

I think at the end of the day the best strategy is dropping aromatizing compounds a few weeks before the comp AND continuing to use an AI.

I remember a certain "guru" who used to say he took guys to the stage on a gram of T. Hmmmmm....

I agree completely. This is the best way to go about...no doubt... and will give superior results.

I have been advocating dropping all aromatizing 2-3 weeks out AND continuing to run 2-3 mg/day of A-dex or 1.5-2mg/day of Letro right up until contest day. It HAS to be done this way for someone to be as hard and dry as possible because there is additonal water retention caused by many AAS that is not estrogen related, as well as making sure all residual estrogen is cleared out. I have been recommeding this for some time for everyone who is prepping for a comp, as you can see in all my cycle recommendations here in this forum.

Anyone who runs a gram of test a week right up until contest day...even if you could completely suppress estrogen....is a fool.

The idea in this thread concerning traditional AI dosing not being sufficent is extremely interesting and something I would most definitely want the answer to.



If we find out that we have been underdosing AI's for precontest prep, this will change the whole ballgame of pre-contest prep.

[Mike Arnold]

i remember a certain guru saying 10 mg of aromasin ed was all he needed to cut estrogen and not effect libido. Well, on a gram of test ew 10 mg of aromasin isn't going to cut much estrogen at all...

(at 300 mg) in "the secret weapon," which is Test prop, masteron prop, and Tren acetate The rest of the drugs are non-estrogenic, non-aromatizable.

even so, tren is reported to have about 20% of the estrogenic activity of E2. Not much, but enough that hitting AIs hard in the last 3 weeks will still leave a little estrogen activity, regardless of how hard you push it.

Sounds good. Yes, tren has been known on occasion to cause slight water retention, but it's effects on the preservation of muscle mass and hardness make it difficult to pass by, as there are few very effective non-methyl available AAS that we can use in high enough doses to enable us to maintain maximum levels of muscle mass and still come in with great condition.

I use to recommend 300 mg/week of test prop right up until the show, but I found that cutting it resulted in even greater crispness than leaving it in. Originally, I feared that cutting it would have deleterious effects on muscle fullness, but I realized this was a non-issue when taking additional measures. This is the standard stack of AAS I usually recommend for a contest BB'r who can tolerate it, for the last 6 weeks (except I cut test at 3 weeks out)


Test prop
Tren ace
Mast prop
Halo
Winstrol
Primo: * only for larger guys who require additional anabolic support, but don't want to use higher doses of androgens, as the combination of Tren, Mast and Halo can already be pretty rough for some guys even in those doses, when combined. Personally, I can't say I blame some of them for not wanting to increase the dose further. Primo can be useful in these circumstances.


Also, the fullness issue can be more than completely reversed by taking other steps not invloving AAS, which can result in an almost scary degree of fullness. A lot of it I adopted from Milos Sarcev. I don't agree with everything Milos does, such as having guys run a moderate amount of Test prop right up until the show, but his multi-faceted loading protocol is capable of delivering crazy good results in muscle fullness.

I know a lot of guys use Test prop right up until the show, but it's just not necessary in my experiences and also causes a very slight blurring of seperation.

From what I've been seeing, the following amounts are enough for almost anyone to hang onto their muscle up until the contest (even guys using 3+ grams of test in the off-season), except in the largest men.


Test prop: 350-400 mg/week.
Tren ace: 350-400 mg/week
Masteron: 350-400 mg/week.
Halotestin: 210-280 mg/week. (halo only last 4 weeks)
Winstrol: 350-400 mg/week.
Primo: 350-400 mg/week. * as stated above...only if needed.


Hey Doc, what is the cycle layout you have your client on? Just curious.

[Dr Pangloss]

I would have cut test down to the first shot in the last week but the guy has TSW. the prop, tren and mast are mixed 1:1:1. Plus, he has no halotestin.

What i did for him was based on what he could get and some preferences. For instance, he hates winny and got injured on it, so no winstrol. Just masteron for hardness.

He's basically ending with 300 300 300 test mast and tren and 5 mg of letro ed for 3 weeks. I may throw in 30 mgs of aromasin the last week, although i would be doing it with no evidence that the combination produces better results. It would just be a precautionary step.

the last week before the show, there is no need to stay on wopping doses, so the last week is just that, 300 300 300.

he's also taking thiazide/aldactone the night before and morning of the show after carb depleting and carbing up. We're going to dry-run that a couple times before the show.

the best strategy is to try and go into the show having done every thing you're going to do for it before. you can't match the situations exactly, but dry-running takes the guess work out of it.

[ski 1]

It was 97 prior to starting aromasin, I started with test p using 1cc every other day, then switched to sus using 500mg per week... I will take bloods in two weeks to see where my estrogen levels are... Also using tren e / 300mg weekly...

[Mike Arnold]

I would have cut test down to the first shot in the last week but the guy has TSW. the prop, tren and mast are mixed 1:1:1. Plus, he has no halotestin.
Sounds good to me. When I put prop in the mix, I also run a 1:1:1 ratio, as well.
What i did for him was based on what he could get and some preferences. For instance, he hates winny and got injured on it, so no winstrol. Just masteron for hardness.
Yeah...injury will tend to do that to you. That is one of the shitty things about Winstrol.
He's basically ending with 300 300 300 test mast and tren and 5 mg of letro ed for 3 weeks. I may throw in 30 mgs of aromasin the last week, although i would be doing it with no evidence that the combination produces better results. It would just be a precautionary step.
I am especially interested regarding higher dosing with AI's and I agree with you taking the "precautionary" measure in regards to the combination and higher dosing in light of what was discussed.

the last week before the show, there is no need to stay on wopping doses, so the last week is just that, 300 300 300.
I also agree. Raising the dose during the last week makes no difference.
.
he's also taking thiazide/aldactone the night before and morning of the show after carb depleting and carbing up. We're going to dry-run that a couple times before the show.
Not enough guys do dry runs when they don't have any experience (or very little) and leave too much on the table come contest time.
the best strategy is to try and go into the show having done every thing you're going to do for it before. you can't match the situations exactly, but dry-running takes the guess work out of it.

Good luck. I'm sure he'll look great.