A HOW TO for: SERMs, Aromatize inhibitors, Gyno and PCT *A must read
SERMs and Aromatize inhibitors
Well today I would like to talk about something EVERYONE should know about before ever considering any sort of steroid use .
Now I feel steroids can be used fairly safely but there are some basics you need to know or you may end up with lifelong issues or a costly one.
Now that was not meant to seem as bad as it may sound, I am talking about Gynaecomastia mainly and why it is so important to understand. I also want to talk about the compounds that can help you avoid it, help it and possibly cure it.
Sadly once gyno has developed extensively and has been there for some time, there might not be any other option but to get your breast glands cut out if you wished to get rid of the gyno. There has been some help with high dosed Aromatase inhibitor (AI) use like Letro, but that is very unhealthy to the body as some estrogen is needed for functions.
Sounds like a bad idea not to know what an Aromatase inhibitor (AI) or SERM is now huh?
Thats why I want to talk about Selective estrogen receptor modulators (SERMs) and Aromatase inhibitors (AIs) today.
They are VERY easy tools to use that everyone should have on hand to keep any Gyno issues at bay. They also aid you in Post Cycle Therapy (PCT) possibly leading to a faster, fuller recovery after a steroid cycle .
If you are new to this all then here is a small definition of what Gyno is:
Gyno is the abnormal development of large mammary glands in men, resulting in breast enlargement.
Yah thats right you might just grow a pair of tits if you dont know what you're doing!
It really bothers me when I see so many posts like; how do I take away my gyno or is this gyno? or even I have gyno and I am taking an Aromatase inhibitor (AI) with my Tren and Test, so why is there gyno? (The last one was due to not knowing there is more than one type of gyno that is handled differently then with just estrogen related gyno)
These are things that should have been well researched before even considering the use of any sort of steroid.
There is more than one type of gyno, so make note of it!
Most of the Gyno issues you hear about are related to estrogen and seems to be the most common, thats where some might get into trouble when using other compounds that dont Aromatase but are progesterone/progestin based like Deca or Trenbolone .
Progestin seems to have a role in gyno development also and would warrant the use of not just an Aromatase inhibitor (AI) but also something to lower your progestin/prolactin levels like a prolactin antagonizer called Pramipexole while using compounds where things other than estrogen might be involved.
Prog-Gyno can even lead to leaky nipples! Yes like milk type thing!
I know trust me***8230; I was once young and new to all this myself.
Now I never had full blown gyno but I did get the wet nipples on a deca cycle early on in my Studies!
I found using an Aromatase inhibitor (AI) helped keep this away without a prolactin antagonizer, but that wont work for everyone, so gain HAVE IT ON HAND JUST IN CASE!
There seems to be a lower chance prog-Gyno issues when keeping estrogen levels low during cycles of say for e.g.; Deca and teste or tren and test, but I would not solely rely on an Aromatase inhibitor (AI) and would ALWAYS recommend having a prolactin antagonize like Prami (Pramipexole) on hand when using compounds like NPP, Deca or Trenbolone even if you do not plan to use it.
So what Aromatase inhibitor (AI), SERM or Prolactin antagonizer should I take?
Well there are a few out there, along with some debate on which is better or what combo is better, but the basics are basics and any pick will do.
So what is a SERM?
SERM stands for "Selective estrogen receptor modulators".
SERMs are a class of compounds that have an effect on the estrogen receptor. SERMs effects on tissue vary, giving it the possibility to selectively inhibit or stimulate estrogen-like actions in various tissues. It also stimulates an increase of follicle-stimulating hormone and luteinizing hormone from the pituitary gland.
What we care about its blocking of estrogen at the breast glands and the follicle-stimulating hormone and luteinizing hormone from the pituitary gland which is why we use it in Post Cycle Therapy (PCT).
At the end of a steroid cycle your own bodys natural hormonal production will most likely (if not every time) be suppressed/shut down and although stopping all steroids and waiting would eventually lead to recovery (if that was what was going to happen in your case). But the thing is it may take much longer to recover and that means a much greater chance of lost gains and emotional mood swings amongst other things.
That is why a SERM is highly recommended, SO much so that some even think if you DONT do a PCT that you wont recover!
Now although that is not true, it is true you SHOULD ALWAYS have a good PCT ready and on hand EVERY time you start a steroid cycle.
Doing so would aid the body in stimulation of the endocrine system and get things going in the direction you want quickly! (recovery).
What is an AI?
An Aromatase inhibitor (AI) stands for Aromatase inhibitor. (AI's) are a class of drugs originally developed for and used in the treatment of breast cancer and ovarian cancer. AIs also have the off-label use to treat or prevent Gynaecomastia in men. Aromatase is the enzyme which synthesizes estrogen in your body, sometimes even right from testosterone . AIs are usually taken to block the production of estrogen.
An Aromatase inhibitor (AI) should be on hand EVERY time a steroid cycle is started EVEN if you dont think you will need it and dont plan to use it, HAVE IT ON HAND!
Another good thing about keeping estrogen in check is Blood pressure, you might have some bloating and higher blood pressure if your estrogen levels are too high or unstable (fluctuations usually from miss-use of an Aromatase inhibitor (AI) and steroid or it would just be high all around in most cases).
That means using an Aromatase inhibitor (AI) will not only keep Gyno away but it may also lower your BP and help keep bloat/edema away!
Awesome stuff I think!
Cant I just use a SERM like Clomid for gyno and PCT?
NO! Well I mean you could, but it is not optimal and I strongly recommend against it.
This is why:
SERMS like Clomid, Tamox and others, only BLOCKS estrogen at some receptors like the breast glands. But it WILL NOT lower estrogen in your body!
If you have Gyno setting in and started up Clomid or Nolva sure you would block the gyno but your estrogen levels would still be building up and in my opinion that is NOT a good thing.
If you were not very smart, didnt think ahead and didnt have an Aromatase inhibitor (AI) on hand and only SERMs, then yes you could start a low dose while you wait for the Aromatase inhibitor (AI) to come, BUT USE THE Aromatase inhibitor (AI) for gyno control long term!
I ALWAYS tell people to use an Aromatase inhibitor (AI) for gyno/estrogen control; its just the most effective and healthy way to go about it.
Save the SERM for PCT use and IF NEEDED the onset of gyno while waiting for the Aromatase inhibitor (AI) to take full effect (if that ended up being the case).
Other than that I feel a SERM should not be used for gyno control and only as part of a PCT.
Some of the older guys may have used a SERMs for gyno control, but we know better now and its time to move with the times.
I am going to list the most used and well known of these compounds with a small description on each, then I will move into how you may want to implement its use and some standard ways of doing so that are generally accepted.
Increases production of gonadotropins by inhibiting negative feedback on the hypothalamus. It is also used in female infertility. Clomiphene has estrogenic and anti-estrogenic effects in the body. It also appears to stimulate the release of gonadotropins, follicle-stimulating hormone (FSH), and leuteinizing hormone (LH). Dosing of 30-100mg daily seems the norm for PCT use.
Tamoxifen Citrate (Nolvadex )-
Tamoxifen is usually used as an endocrine (anti-estrogen) therapy for hormone receptor-positive breast cancer in women. It is an antagonist of the estrogen receptor in the breast, while in other tissues it acts as an agonist sort of like how Clomid does. Half-life is about 6 days, so ed to eod dosing is best for PCT use. 20-50mg daily seems the norm for this.
Toremifene Citrate (Torem/Fareston)-
Torem Is SERM similar to Tamoxifen (Nolva). Torem is also used to treat breast cancer and also does this by exerting estrogen antagonistic effects in certain tissues like breast tissue (anti-estrogen). It can act as an antagonist in the hypothalamus and pituitary, which could also increase testosterone production (why I recommend it as a PCT). Torem also seems to have a better ability to increase testosterone levels over Tamox because its andro to estro ratio is much greater than Tamox/Nolva. Half life is about 5 days. Dosing daily to eod is recommended for PCT use. Dosing of Torem for PCT at 20-100mg ed seems to be the norm.
Raloxifene is a second generation Selective Estrogen Receptor Modulator (SERM). Raloxifene is similar in its action to that of tamoxifene but with much less of an increase in testosterone levels when compared to Tamox or Torem. The half-life is only about 27hrs so daily dosing is optimal for use in PCT. Dosing of 30-100mg ed seems to be the norm for PCT use.
Prolactin Antagonizer (PA):
Prami has actions similar to Cabergoline (another type of PA) but with a significantly more positive impact on libido and mood. Pramipexole acts as a dopamine agonist and one of dopamine's main function as a hormone is to inhibit the release of prolactin. Pramipexole plays an important role in the inhibition of prolactin secretion which is important to some using some types of steroids where prolactin build up may be an issue. Prami is also used for treating early-stage Parkinson's disease (PD) and restless legs syndrome (RLS). Pramipexole has a half-life between 8-10 hours. Normal dosing is 0.25-0.5mg ED (pre-bedtime dosing is recommended as it make some feel a bit sleepy)
Letro lowers estrogen production in the body by blocking the aromatase enzyme, the enzyme responsible for estrogen synthesization. Letro has a very high rate of estrogen suppression in the area of 90%+, so care should be given to dosing as over suppression could lead to side effects associated with low estrogen levels, like achy joints, low energy levels etc. This can be an issue with all AIs but Letro is very good at its job and that leads to helping prevent bloating and gyno which may be associated with the use of AAS. Letro has a fairly long active life so dosing of every other day, to even 1-2 times a week is optimal at doses of 0.25mg - 1.3mg.
Anastrozole (aka LiquiDex/Dex)-
Dex lowers estrogen production in the body by blocking the aromatase enzyme, the enzyme responsible for estrogen synthesization. Dosing of 0.5 mg to 1 mg a day should reduce serum estradiol about 50% in men, which leads to helping prevent bloating and gyno which may be associated with the use of AAS. Active life is fairly short so daily to eod dosing is optimal.
Exemestane (Stane/Aromasin )-
Exemestane lowers estrogen production in the body by blocking the aromatase enzyme, the enzyme responsible for estrogen synthesization. Exemestane has about an 85% rate of estrogen suppression and does this by selectively inhibiting aromatase activity in a time-dependent and irreversible way. That helps prevent bloating and gyno which may be associated with the use of steroids. Stane has a fairly short active life so daily to every other day dosing is optimal.
As you can see there is quite the selection of compounds and this I not all of them.
I think these are the most often used, safe and effective for our topic today.
How would I use this in a steroid cycle?
Do I take it as soon as I stop them?
Do I wait a few weeks?
Well I will give you a few examples of how you would properly incorporate these compounds into your cycle, but something you need to understand is the compounds you are using.
Steroids have differing release and clearance times!
Some might leave your system in hours, like with more orals if you were to stop them today you could start PCT tomorrow (I do not recommend oral only cycles BTW, this is just an example).
But if you were taking for example teste or testcyp, well if you stopped today you would wait 1-2 weeks before starting your PCT because their release times and active life are much longer then the orals.
But some injectables are also very short in active life like NPP or trenAce, with then you would wait 2-4 days and start pct. It is very important to understand EVERY compound you put in your body to be able to use them safely and effectively.
I will list a few examples of AAS cycles with an Aromatase inhibitor (AI) and PCT/SERM implemented:
Wk1-12 500mg teste ew
Wk1-14 0.6mg e3d (2X a week) Letro
Wk14-18 PCT Clomid 50mg ed
Wk1-14 500mg TestE ew
Wk1-12 300mg Deca ew
Wk4-15 0.25mg Prami ed (pre-bedtime)
Wk1-16 12.5mg ed Stane
Wk16-20 50mg Clomid and/or 20mg Nolvadex or 40mg Torem ed
Wk1-10 50mg TrenAce eod
Wk1-12 100mg TestProp eod
Wk1-10 0.25mg Prami ed (pre bed)
Wk1-13 12.5mg Stane ed
Wk12/13-17 50mg Clomid ed
Wk1-14 400mg TestE ew
Wk1-14 400mg MastE ew
Wk1-16 12.5mg Stane ed
Wk16-20 30-50mg Clomid ed or 20-30mg Nolvadex ed
You can see there are varying ways of doing things, and some may debate on what is best (in my op what I put is best lol) but the basics are there and should be followed regardless of your opinion.
I hope this helps someone out with their Gyno, Aromatase inhibitor (AI) or PCT questions!
1) Riggs BL, Hartmann LC (2003). "Selective estrogen-receptor modulators -- mechanisms of action and application to clinical practice". N Engl J Med 618***8211;29. Selective estrogen-receptor modulators -- mecha... [N Engl J Med. 2003] - PubMed - NCBI
2) Endocr J. 2010;57(6):517-21. Epub 2010 Apr 6. Clomiphene citrate elicits estrogen agonistic/antagonistic effects differentially via estrogen receptors alpha and beta. Kurosawa T, Hiroi H, Momoeda M, Inoue S, Taketani Y. Clomiphene citrate elicits estrogen agonistic/antag... [Endocr J. 2010] - PubMed - NCBI
3) Br J Pharmacol. 2006 January; 147(S1): S269***8211;S276.Published online 2006 January 9 Tamoxifen (ICI46,474) as a targeted therapy to treat and prevent breast cancer Tamoxifen (ICI46,474) as a targeted therapy to treat and prevent breast cancer
4) Pramipexole (Sifrol and Sifrol ER) for Parkinson***8217;s diseaseMedicine Update August 2010: Date published: December 2009 Updated: August 2010 Pramipexole (Sifrol and Sifrol ER) for Parkinson
5) Effects of Aromatase Inhibition in Elderly Men with Low or Borderline-Low Serum Testosterone Levels. Benjamin Z. Leder, Jacqueline L. Rohrer, Stephen D. Rubin, Jose Gallo and Christopher Longcope Effects of Aromatase Inhibition in Elderly Men with Low or Borderline-Low Serum Testosterone Levels
6) Effects of Suppression of Estrogen Action by the P450 Aromatase Inhibitor Letrozole on Bone Mineral Density and Bone Turnover in Pubertal Boys Sanna Wickman, Eero Kajantie and Leo Dunkel Hospital for Children and Adolescents, University of Helsinki, Helsinki, FIN-00029 HUS, Finland Effects of Suppression of Estrogen Action by the P450 Aromatase Inhibitor Letrozole on Bone Mineral Density and Bone Turnover in Pubertal Boys
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