- 11-06-2009, 01:19 AM
Forgive my ignorance but i was trying to find out a bit about estrogen blockers and was reading about "suicide inhibitors" and how they attach to the aromatase enzyme and permanently disable it.
Does this mean that if you take an estrogen blocker that is a "suicide inhibitor" that your bodies ability to produce estrogen will be permanently downgraded? that doesn't sound very healthy. Or does it just mean that that that individual estrogen enzyme molecule will no longer be acting on you body and will be replaced by a new active molecule in time? If this is the case what is the rate at which your body turns over it's supply of estrogen?
Thanks in advance for any feedback.
- 11-06-2009, 07:46 AM
The way supplement companies word things in advertising is often dramatic and that phrase i agree can set alarm bells ringing. I agree its not healthy to have no estrogen or even a very small amount of estrogen permanently or for a very long time ,There will be obvious signs as a result of this such as joint pain and loss of libido.
As far as i understand it , i may get corrected on this, is that you can only fool the body for so long after which it will produce a further enzyme to help with the correction of too low estrogen .
I personally have used 6 bromo (hyperdrol) but not at the suggested dosage , but at 50 mg ed and on occasion eod.
There are more natural ways of removing estrogen which are documented in the book " the testosterone syndrome" by Dr Shippen.In it he recommends the use of grapeseed extract , reservatrol, and at leat 50 mg of zinc per day.Its important to ensure that the liver is flushing estrogen out of the body and certain foods/supplements will ensure it does just that.On the other hand certain foods slow the process down in the liver of which grapefruit is one and is seen in supplements as naringin and can interfere with the absorbtion of drugs.
If you feel uneasy about taking something like ATD , 6 BROMO, FORMESTANE, then i suggest the more natural route for you .With the 3 listed above you are only able to take for certain periods of time.The use of more natural supplements can be used continually.
Also estrogen should be measured through a blood test to see if it falls within the prameters set by the hospital laboratory before supplementing with a drug .
Anything else is guess work.If youve no reason to introduce an estrogen blocker into your supplement programme why do it?
There is an interesting section in the book William LLewellyns "anabolics 2010" on estrogen aromatization.In it he says that it is an desirable hormone and estrogenic steroids are the best mass builders.It is thought to promote an anabolic state by affecting glucose utilization in muscle;has a role to play in production of gh /igf1 and has other functions.
He finally says that AIs should only be used if there is a clear need for them, so if you are not prone to estrogenic side effects, find something that does aromatise . and the estrogen will help you add mass and provide energy.
Thats my take on it with the help of ANABOLICS 9TH ED 2010.
11-06-2009, 08:52 AM
SERM's (Selective Estrogen Receptor Modulator) : These block certain estrogen receptors, depending on the drug, and dont actually lower estrogen in the blood. Estrogen is left to circulate with nowhere to go. Because of this, SERMS have a posotive effect on cholesterol levels. They have a negative effect on IGF-1, so if bulking, only take them if totally necessary. They are good at blocking gyno, and are commonly used while cycling and in PCT.
AI's (Aromatase Inhibitors) : There are 2 types of AI's. Type I (suicide inhibitor) attaches to the aromatase enzyme and permanently disables it. Type II compete for the enzyme, but dont destroy it. Both are effective at lowering estrogen substantially. Both are commonly used during both cycling and PCT. Used mainly when low estrogen levels are desired, like contest preparation/cutting. Beware that lowering estrogen with strong AI's can have a negative effect on cholesterol levels.
RI's (Reductase Inhibitors) : These drugs stop the conversion of testosterone into DHT wherever 5-alpha reductase enzymes are present. RI's work by blocking the action of the 5-alpha. There are 2 5a's. Type I 5a and Type II 5a. Different RI's block one or both of these 5a's.
SERMS (Selective Estrogen Receptor Modulation)
Nolvadex (Tamoxifen Citrate) : Nolvadex is a SERM. It selectively binds to certain estrogen receptors, effectively blocking the estrogen and stopping unwanted sides such as gyno. It DOES NOT lower estro levels in the blood, it only blocks it from binding to certain receptors. It also helps your blood fat levels. It does not suppress LH, blocks desired estro receptors and helps stop HCG from desensitizing your testicles to natural LH. Nolva should be used during HCG therapy, at 20 mg a day, for the reason i just mentioned. Can be used during cycle if you see signs of gyno. Its mainly used to block the estrogen spike when you come off cycle, and should be used right through to the end until natural test levels are back. One drawback to consider about Nolva is that it may cause progesterone receptors to become more sensitive. This means that while using progestins such as Deca or Tren, you may become more sensetive to progestin related gyno.
Faslodex (Fulvestrant) : Approved for use in 2002 for breast cancer research, this drug is unlike most we have seen. It is classified as an estrogen receptor downregulator. It prevents estrogen from exerting its influence on the estrogen receptor. Similar to Nolvadex, but is not selective. It hits all estrogen receptors. It also does this to progesterone receptors to a lesser degree. It is injectable, at 250mg a month. No information on how it affects blood lipids. It is also very expensive.
Clomid (Clomiphene Citrate) : This drug is also a SERM, almost identicle to Nolva. It is said to be a weaker blocker mg for mg than Nolva. Its common use is in PCT, usually for about a month, used after HCG and all AAS esters have run out of your body. Even though it is weaker than Nolva at blocking, it is believed to be quicker at bringing HPTA back to balance. Both are commonly used during PCT. It binds to different receptors than Nolva. There is a lot of debate on this, but until there is solid proof, it may be prudent to include this in your PCT. Commonly taken at about 100mg a day.
Fareston (Toremifene Citrate) : This is a second generation SERM. Approved for use in 1997. Chemically very similar to Nolva and Clomid, it is less powerful mg for mg. Fareston may have a stronger posotive effect on your cholesterol levels. For those who find this an important issue, this is a drug of choice. Used every day at around 60mg.
Evista (raloxifene) : A newer SERM, Evista is shown to be a blocker in breast tissue, but acts as a receptor agonist in bone tissue (unlike Nolvadex). This action promotes bone density. Taken at about 60mg a day. Evista may prove to be very beneficial, as it also helps cholesterol levels (like Nolvadex). Evista is supposed to have a more powerful gyno blocking effect than Nolvadex.
Cyclofenil : Much like Nolvadex, this is also a SERM. Used at about 600mg a day, it is weaker mg for mg. A good alternative if Nolva is not available, which is usually not the case.
AI (Aromatase Inhibitors)
Teslac (Testolactone) : This is a first generation steroidal aromatase inhibitor. Like a suicide, it permanently attaches to the aromatase enzyme. Taked at a maximum of 250mg a day. It is not as strong as the newer AI's, but some people still like to use it. It can lower estrogen about 50%. Streroidal in structure, it has no anabolic effect.
Aromasin (Exemestane) : This drug is classified as a Type I Suicide AI. It binds to the aromatase enzyme and kills it. It is effective at lowering estrogen up to 85%. Once again, you have to watch out for your cholesterol levels. Used mainly for cutting when low estrogen levels are desired. Aromasin is shown to help bone density. Clinical doses are about 25mg a day, but it has been shown that as little as 2.5mg a day can be as effective.
Lentaron (Formestane) : A Type I Suicide AI. Lentaron is not classified as a drug, and can be sold over the counter as a suppliment. Not as strong as the third generation AIs (arimidex, femera). Can lower estrogen by about 60%. Used as an injectable, it is dosed at about 250mg every 2 weeks. Due to poor bioavailability, daily doses of oral Lentaron are about 250mg.
Arimidex (Anastrozole) : This is a widely used type II AI. It competes with estrogen for the aromatase enzyme. This effectively lowers estrogen up to 80% in the blood. Approved for use in 1995 to fight breast cancer. At doses up to 1mg a day, it has been shown to be very effective at controlling estrogen while on cycle or in PCT. It is usefull for curbing the effects that come with aromatizing AAS's while in cycle, and can be used in PCT. Nolvadex is shown to decrease the effectiveness of Arimidex when used together. In this case a suicide inhibitor may be more well suited, like in PCT. It is also called L-dex, in its liquid form.
Femera (Letrozole) : Letro is a competative Type II AI also. Also farely new compared to other compounds, it is shown to be effective at lowering estrogen by blocking the aromatase enzyme. Doses up to 2.5mg a day are used, but usually as low as .5mg a day can be just as effective. Clinical studies show Femera to lower estrogen by 75-78%. Once again, watch out for you blood lipids (cholesterol) to get out of whack. There may a noted rebound effect of estrogen levels that goes along with Letro use.
11-06-2009, 09:50 AM
11-06-2009, 10:07 AM
11-06-2009, 02:52 PM
your understanding of the big picture is similar to my understanding. I suspect that the suicidal AI binds permenantly to that particular aromatase enzyme. Total estrogen gradually comes back with reintroduction of the enzyme. Theoretically this is a slow process, which is why, again theoretically, a suicidal AI shouldn't require tapering.
What is the context of your question? In other words, why are you asking?
11-06-2009, 02:59 PM
Didn't you just ask this last week?
To answer your question, just no, plain and simple, no!
No, you will not turn off any ability to produce estrogen for the rest of your life.
If I run an AI for a month (suicide inhibitor or modulator, hamburger or bacon), does this mean that I can take steroids for the next 12 years and never run an AI? No, it does not mean that.
---The internet is the father of the electronic lynch-mob---
11-06-2009, 03:04 PM
---The internet is the father of the electronic lynch-mob---
11-06-2009, 06:32 PM
11-06-2009, 06:48 PM
07-02-2011, 04:02 PM
i am hopelessly "androgen resistant". this means if i use ANY androgen, DHEA, aspartic acid,
or even pregnenolone i just get estrogens (estradiol and estrone). i use ZRT saliva test kits
to test these. i heard about suicide substrate aromatase inhibitors and was fascinated, but
rather doubtful. i bought 25 mg ATD. used it for a month and tested testosterone and estradiol.
my testosterone jumped from 50 to 96 on the ZRT scale which is ideal for young men. my
estradiol fell. will this keep up until i die (i'm 65)? i don't know, but i think it will. is it safe?
probably since it is simply an androstenedione analog (trione instead of dione). ATD works
for me and i couldn't be happier. i am going to test 6-oxo later and see if that works, too.
remember this was done with a mere 25 mg of ATD.
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