problem fighting gyno with aromatase inhibitors

[CCS]

http://endo.endojournals.org/cgi/conten ... 108/4/1597

Kinetic evidence is presented for a time-dependent decrease in human placental aromatase activity by enzyme-generated intermediates derived from two widely used steroids previously described as competitive inhibitors of estrogen biosynthesis. Thus, 4-androstene-3,6,17-trione binds to the enzyme with an apparent Ki of 0.43 microM and has a pseudo- first order overall rate constant for decrease in activity of 4.03x10(- 3)sec-1, while 1,4,6-androstatriene-3,17-dione has an apparent Ki of 0.18 microM and a pseudo-first order overall rate constant for decrease in activity of 1.10x10(-3)sec-1. These findings imply that the potent inhibition of estrogen biosynthesis caused by these steroids results primarily from a decrease in enzyme activity caused by enzyme-generated intermediates from the parent steroids.

1,4,6-androstatriene-3,17-dione is the active ingredient in AIFM

This means that even if you apply it to your breats, it first must be converted to something else before it inhibits aromatase. Not sure where that conversion takes place, but it may mean that you can't just locally inhibit aromatase. AIFM may lower estrogen everywhere in your body equally.


But for $3, it is very cheap:
http://www.bulknutrition.com/p2189_1_4_ ... st400.html

 

[CCS]

Next I want to find out if the active ingredients of any of these work locally:
----------------------------------------
Rx:

Nolvadex, Istubal, and Valodex: Prescription.
Active ingredient Tamoxifen. some say it blocks the estrogen receptor.

Aromasin: Rx
Active ingredient: exemestane

Clomid: Rx used to make women pregnant. Not an ArI
Clomiphene

Arimidex: 1mg per day reduces estrogen production 50%. Rx

Femara: Rx
Active ingredient: Letrozole

Raloxifene: experimental. big molecule.
------------------------------------------------------------------------------
OTC
formestane -- not approved by FDA. -- 4-hydroxyandrostenedione -- very powerful. Rx in other countries.
http://www.bulknutrition.com/?products_id=4973
It can reduce oestrogen by 65%. It only inhibits converstion of androstinedione to oestrogen. It is not very effective at treating breat cancer.

3,17-keto-etiochol-triene: fast acting, very strong but where to buy it. I can get it in a mix for $30. But very little is in there.

6, 17-keto-etiocholeve-3-ol tetrahydropyranol: slow acting OTC. probably no local effect.

1,4,6-androstatriene-3,17-dione -- AIFM
http://www.bulknutrition.com/?products_id=2189
cheap, but no local effect.

Viratase (5-alpha-androstanedione) -- OTC: very strong ArB. But it does not do a permenant lock. Just competitive with other stuff. It works locally, and is not converted to anything else.

6-oxo-androstenedione --- http://www.fitfuel.com/ergopharm-6oxobr ... ZAodjhoPoQ
another local, permenant lock.
http://ergopharm.net/images/6oxo_incledon.pdf
Active ingredient:
3,6,17-androstenetrione: OTC, but may get converted to estrogen itself
It works locally.
60 500mg pills are $45
----------------------------------------------------------------------------------
Herbals:

Rebound Reloaded: Herbal OTC, supported by blood tests to reduce estrogen 50% and raise testosterone 75%.

Grape seed extract actually inhibits aromatase, strongly, but at 1 gram per day. i think more would absorbed if taken with fat.
http://www.cbcrp.org/RESEARCH/PageGrant ... ant_id=281

chrysin -- natural herbal. boosts testosterone 30%. small molecule, isoflavone

indole-3-carbinol -- another herbal that weakly reduces estradiol. Available at vitacost.

calcium d-glucarate -- another herbal ArB in some foods. It is why people who eat certain foods have lower cancer rates.

trihydroxystilbene -- another name for resversatrol, also found in grapes. grape juice can reduce estrogen levels.

 

[CCS]

for maximum absorption, either make a topical, or eat the stuff with fat and a little grapefruit juice. To get enough buy eating it, a lot of people take 500mg, 3+ times per day. I'm sure they took it with 10 grams of fat, they could cut that dose in 1/3. Topicals get much better absorption. The nipples and the dick have very thin skin, though there are other places too.

Anyway, I'm going to put some homemade AIFM on my testicles every 4 days to get it absorbed well. Need my brother to mail me some oleic acid as a penetration enhancer. Then I'll put 6-oxo on my dick and on my nipples. That will save me a lot of money over taking it orally, and be a lot easier on my liver.

My goal is to lower total estrogen 30%, local (nipples and dick) estrogen 60%, and boost total serum testosterone 60%. That should put me on the high side of normal so I recover a bit faster from workouts. Then I need to start using a topical androgen receptor blocker. Currently using spironolactone shampoo, though I don't trust it. So I'll probably start using my Eucapil again.

I'm currently putting Andractim gel on my penis and niples, and I think it is real because it makes my penis hard more often. It never gets as small as it used to. Always has some blood pressure in there.

 

[stampede]

Anyway, I'm going to put some homemade AIFM on my testicles every 4 days to get it absorbed well. Need my brother to mail me some oleic acid as a penetration enhancer. Then I'll put 6-oxo on my dick and on my nipples. That will save me a lot of money over taking it orally, and be a lot easier on my liver.

:shock: :lol:

That is all!

 

[Pondle]

CCS are you getting gyno problems? I know you were using Dutas for a while, and I seem to remember a post where you said you'd noticed your chest getting distinctly larger.

 

[purecontrol]

for maximum absorption, either make a topical, or eat the stuff with fat and a little grapefruit juice. To get enough buy eating it, a lot of people take 500mg, 3+ times per day. I'm sure they took it with 10 grams of fat, they could cut that dose in 1/3. Topicals get much better absorption. The nipples and the dick have very thin skin, though there are other places too.

Anyway, I'm going to put some homemade AIFM on my testicles every 4 days to get it absorbed well. Need my brother to mail me some oleic acid as a penetration enhancer. Then I'll put 6-oxo on my dick and on my nipples. That will save me a lot of money over taking it orally, and be a lot easier on my liver.

My goal is to lower total estrogen 30%, local (nipples and dick) estrogen 60%, and boost total serum testosterone 60%. That should put me on the high side of normal so I recover a bit faster from workouts. Then I need to start using a topical androgen receptor blocker. Currently using spironolactone shampoo, though I don't trust it. So I'll probably start using my Eucapil again.

I'm currently putting Andractim gel on my penis and niples, and I think it is real because it makes my penis hard more often. It never gets as small as it used to. Always has some blood pressure in there.

Have you considered getting a saliva test for various estrogen, test, and then DHT? Very very accurate.

I am about to start dutasteride, Arimidex, and Eucapil

I would also like to use topical Caffine but can't find it anywere and also like to try topical GTE since reading some of your posts.

 

[stampede]

Arimidex is amazing stuff. I took a tiny fraction of a pill and even that was too strong. Lost loads of fat off my chest/sides, face went really oily etc.

It's expensive but it really works.

 

[purecontrol]

Arimidex is amazing stuff. I took a tiny fraction of a pill and even that was too strong. Lost loads of fat off my chest/sides, face went really oily etc.

It's expensive but it really works.

This is a very very interesting coment, as those are areas that are most prone to effects of estrogen. Why did you discontinue and how much were you using?

 

[stampede]

Arimidex is amazing stuff. I took a tiny fraction of a pill and even that was too strong. Lost loads of fat off my chest/sides, face went really oily etc.

It's expensive but it really works.

This is a very very interesting coment, as those are areas that are most prone to effects of estrogen. Why did you discontinue and how much were you using?

I'm not discontinuing using it as such, but I think that 0.1mg a WEEK might be sufficient. I don't want to use more than that because I honestly feel dangerous while on it :lol: no lie, I feel like ten men.

 

[supercop]

Hi, CCS and everyone.

Will Calcium D-Glucarate work in alleviating the excess visceral belly fat?

I wanted to know if you guys have tried or if it does work in theory. What is ArB, CCS?

I lost my insurance and could not afford Arimidex at the moment so I was hoping if you guys could tell me if getting Glucarate is worth it or not. I tried DIM once and it actually gave me horrible migraines and made me lose even more hair (it is an NF-kappa B inhibitor which made me lose hair. It also blocks the PI3K/Akt pathway so I'm not sure if this is good for hair growth)

I've read more than one review on iHerb saying that Glucarate works and they've lost fat on their bellies so I'm assuming it affects the estrogen receptors.

I'm so depressed tonight but I am hanging on. Thank you.

 

[Ende]

What's the problem exactly? You're already using the most potent drug available when it comes to reversing gynecomastia; andractim. Large amounts of zinc or a tiny amount of arimidex every week, will keep your estrogen under control. I believe zinc is more appropriate for maintenance, as arimidex is very potent, and causes trouble with joints, brain function and sexual function when you drive the estrogen level too low.

Edit: I just saw the date on the post...

 

[supercop]

Hey enden, can high estrogen levels actually cause hair loss? Because my hair loss is diffused and now turning in to male pattern baldness - all of which happened when I was taking acne medication. I never took finasteride or Propecia.

I say this because I experience hair loss ALL OVER my body not just the scalp. It's diffuse which is slowly turning to male pattern baldness.

 

[Ende]

Hi,

Not that I'm aware of, no. Changes in hormone levels may cause hairloss, but it's androgens which are responsible for miniaturization. Are you talking about accutane? I've heard people have been suffering from hair loss after using that drug. Do you have signs of elevated estrogen level, like reduced libido and softer erections? (it's symptoms of too low estrogen level too - just so you know) I think too low estrogen level can cause hair loss (it's listed as a side effect in the arimidex leaflet), but if that's the case, you'll have cracking joints. Loss of body hair is a sign of reduced testosterone level.

 

[CCS]

It is good you are testing your hormone levels before just changing them. Life extension.org has test that are two hormones for $50.

Fat actually secretes estrogen, making it hard to get rid of it. But you need to get your hormone levels into the optimal or normal range. Do not make them outside of normal ranges or your chances of cancer and other problems go up.

As for calcium glucarate, the glucarate is a spectator ion, and of little importance, I believe. I'd have to google it to be sure. The active ingredient most likely is the calcium. There are a few studies by the dairy industry showing that taking calcium helps you lose weight. My advice is to just say in the normal range.

As for the aromatase inhibitors, you estrogen levels might not be as resiliant as your DHT levels with finasteride. I would be careful before using prescription aromatase inhibitors that could affect your levels a bit longer term than you want.

If you want to get rid of the fat, you need to exercise, and eat high fiber food with plenty of carbs from grain or fruit. Drop soda. Do moderate, sustainable dieting. And get 8 hours of sleep, and drink plenty of water. Avoid sugary drinks, including fruit juice unless you eat fiber with it. But if your estrogen levels are really high, you will have an easier time losing weight if you bring them back into normal ranges. If you use prescription drugs, ask some doctors, such as the life extension.org ones, what the risks are and how to minimize them. They may help you by email after you forward your test results to you.

 

[mpbsux20]

^^That will be highly informative for many.

 

[Ende]

I would be careful before using prescription aromatase inhibitors that could affect your levels a bit longer term than you want.

True. I recommend arimidex if your estrogen level is severly elevated, large amounts of zinc if it's still in range, or slightly elevated. Stay away from suicide inhibitors like aromasin.