Hello Readers ,
So many of my gym buddies recently have been asking me about the
Aromatase Inhibitors (Estrogen Inhibitors) and weather they can be taken as a supplement for bodybuilding or not, so i thought to share my views on this topic.
INTRODUCTION
Now before i get to the drugs and their effect, i would like start with the genreal physiology of estrogen in men, their functions and how important they can be for men.
Estrogen In Males:
In adult male, estrogen is produced in sizable quantities in the testis,as well as the brain,Early studies stated that the primary source of estrogen in the immature male was the sertoli cells, but evidence shows that in adult testis, Leydif cells express P450 aromatase enzyme ( Enzyme located in cytoplasmic droplets of the sperm tail) and actively synthesize estradiol at the rate much greater than that seen in the adult Sertoli cells. Recently a few of the evidence indicates that germ cells also synthesize estrogen, and possible serve as the major source of estrogen in male reproductive tract.
Thus the conversion of androgens to estrogens (under the influence of the enzyme P450 aromatase) remains the primary source of estrogen in the lumen of the reproductive tract of the male.
Here's a simple picture from my notes which will help to understand the synthesize of estrogen in males.
(P.S dont bother the drawing i'm not good in it :D)
Also, as any other steroid the concentration of the estrogen depends on the cholesterol level, and there are 5 major steps that are involved in it's synthesis. These steps are explained below
Few Important Functions of Estrogen in Males:
There is a limited direct evidence that estrogen has a major role in the adult testicular function. In the developing testis,estrogen has significant activity in establishing Sertoli cell function and potentially even in establishing Sertoli-germ adhesion.
Estrogens that are made in male testis have an important role in the efferent ductules, these are the tiny ductules attached to the testis and transport sperm to another duct, the epididymis, where they are stored until ejaculation. These ductules also absorb fluid that accompanies the sperm, an important function that helps pressure in the testis at a proper level.
Also, these estrogen regulate the expression of proteins involved in fluid re-absorption, So any disruption in them may result in dilution of cauda epididymal sperm, disruption of sperm morphology, inhibition of sodium transport and subsequent water re-absorption, increased secretion of CL- and eventually decreased infertility (In short Estrogen plays an important role in the fertility and maintaining morphology of sperm)
Appart from this Estrogen also plays an important role in Bone metabolism ( Bone metabolism involves building and breaking down of bone to maintain bone health as you age. Bone cells called osteoclasts are constantly breaking bone down, while osteoblasts rebuild bone by adding calcium to areas that need strengthening. Osteoblasts release osteoid that contain mineralized matrix to deposit calcium and collagen to harden, building the bone matrix called cortical bone) So, Estrogen inhibits osteoclasts activity in bone and stimulates osteoblasts activity (I.e Helps in prevention from Osteoporosis)
The concentration of estrogen in peripheral blood is typically low in th male, and ranges from 2-180 pg/ml, However a high concentration of estrogen in males is known to be associated with some of the conditions like gynecomastia, Other side effects include loss of muscle tone, a decrease in body hair, shrinking testes, depression, fatigue, lower energy levels, poor memory, low stress tolerance, an increase in fat around the mid-section (belly fat) and erectile dysfunction. Elevated estrogen levels really do cause men to look–and somewhat act–more like women and less like men.
CONTROLLING ESTROGEN LEVEL BY DIET:
- Estrogen levels are known to be controlled by maintaining a proper diet, which includes an increase in
fiber intake, as fiber binds to bile acids to help flush estrogen from the body, hence decreasing it's concentration.
- Adding vegetables like
cauliflower, broccoli, cabbage and Brussels sprouts in your diet, as these vegetables contain
Diindolylmethane (DIM) which eliminates the stored hormones such as estrogen from the body.
- Reducing the amount of
Alcohol intake will also help in maintaining the estrogen levels as alcohol has a direct effect in the liver functioning, and since estrogen is known to metabolize in the liver, alcohol might lead to increase in estrogen level.
Also, Alcoholic drinks specially like beer might increase the level of cholesterol in the body which again may lead to increase in estrogen level (mechanism explained above).
- Next up is
Milk or Dairy products, which might contain estrogen which are excreted by cows, so limiting dairy products can really help in decreasing estrogen levels.
-
Vitamin B6 :
Vitamin B6 is necessary for regulating the hormones in our body,if there is deficiency of vitamin B6 then the liver is unable to metabolize the excess of estrogen, hence leading to an increase in their level.
There are certain food sources which are rich in vitamin B6, such as :
Chickpeas,Bananas,Tuna fish, White and sweet potatoes, Avocados and Sunflower seeds
Or, else if not possible to get vitamin B6 from diet, you can go for Vitamin B complex supplements.
CONTROLLING ESTROGEN LEVEL THROUGH MEDICATION:
Aromatase Inhibitors comes under the group of drugs that are used to treat breast cancer and ovarian cancer in postmenopausal women, also in certain cases of gynecomastia. Recently drugs like Clomid (clomiphene citrate) Cytadren (aminoglutethimide) which comes under this group have become quite popular for bodybuilding. Basically these are two group of anti-estrogen drugs : Aromatase inhibitors ( enzyme inhibitors) and the estrogen receptor blockers.
Aromatase Inhibitors :
The most commonly used aromatase inhibitor in bodybuilding is aminoglutethimide (Cytadren). This drug also inhibits an enzyme (desmolase) necessary for synthesis of cortisol, but fortunately, aromatase can be inhibited with levels of drug that cause only limited inhibition of desmolase.
Contrary to popular belief, it is generally not desirable to inhibit cortisol production. Doing so will likely lead to joint problems, and furthermore once the inhibition ends, the price of above-normal cortisol production must usually be paid.
For an average male, a dose of 250 mg/day (one tablet) appears optimal. The half-life is 8 hours, so the drug is better taken in divided doses. The best plan seems to be to take half a tablet on arising, and quarter tabs six and twelve hours later. This keeps levels generally fairly constant, but allows a small drop in the hours shortly before arising, which is then compensated for by the higher dose on arising. With this scheme, inhibition of cortisol production is generally too low to be noticed, and generally there is no rebound effect on discontinuance. However it is not a bad idea nonetheless to taper off, first omitting the midday quarter tab dose for a few days, then omitting both quarter tab doses, then reducing the initial dose to one quarter tab, and then ending completely. A week is sufficient for the taper.
Some people suffer a degree of lethargy or sedation from aminoglutethimide, even at this low dose, but most do not.
Anastrozole (Arimidex) is a superior aromatase inhibitor which does not have the above side effects. It is, however, very expensive. With moderate doses of testosterone it seems that 1 mg/day is sufficient, and some have claimed half a tab to be sufficient.
Receptor Blockers:
Clomiphene (Clomid) and tamoxifen (Nolvadex) are the most popular drugs of this class. They are more precisely referred to as selective estrogen receptor modulators. This is because their mode of action is not so simple as merely blocking the estrogen receptor. Estrogen receptors require not only hormone but also activation of regions of the receptor called AF-1 and AF-2. AF-1, to be activated, requires phosphorylation, while AF-2 can be activated by any of a number of cofactors, such as IGF-1.
As it happens, clomiphene and tamoxifen are estrogen receptor antagonists (blockers) in cells that depend on activation of the AF-2 region, while in cells which activate AF-1, these compounds are estrogens.
In some cells these drugs activate one of the types of estrogen receptor (ERa) but are antagonists of the other type (ERb).
The result is that these compounds are antiestrogenic in breast tissue, fat tissue, and in the hypothalamus, which is what we want in bodybuilding, but are estrogenic in bone tissue and with respect to favorable effect on blood lipid profile, both of which are, again, desirable. They also appear to have some estrogenic effect on mood, though this may be in only parts of the brain (the matter is not studied.)
Cyclofenil is a similar drug to the above two. Clomiphene will do everything that the other two will do, but for some unknown reason, has been found more effective than tamoxifen both medically and in bodybuilding for increasing LH production.
Raloxifene (Evista) is a new selective estrogen receptor modulator that, for women, has the advantage of being an antiestrogen in the uterus, whereas clomiphene and tamoxifen are estrogens in that tissue. For this reason, the latter two drugs can promote uterine cancer, while raloxifene actually should help prevent it, and is therefore a superior drug for women. It is not known how effective it may be in increasing LH production.
While on high dose androgens it is impossible to maintain LH production in any case, and clomiphene can do no good in that regard. As androgen levels return to normal, however, a dose of 50 mg/day of clomiphene if estrogen levels are reasonable, or 100 mg/day if estrogen levels are high, is usually effective in restoring natural testosterone production.
Because the drug has a long half-life, when one takes 50 mg/day the amount in the system is not only the 50 mg just taken, but also approximately another 250 mg from previous days. Thus, to immediately arrive at the therapeutic level, one would take 300 mg (50 mg six times) on the first day, and then continue with 50 mg/day.
A small percentage of individuals suffer vision problems from use of clomiphene, which is generally reversible upon discontinuance. These persons, of course, should not use the drug after discovering the problem.
Please note that these are prescription drugs, and should be obtained and used only by prescription with medical advice only.
CONCLUSION:
Personally, after going through all the physiologic functions of estrogen in men, i would not recommend to go for drug supplements in order to lower down the estrogen level, as stated above estrogen is not at all a waste product in males, as a matter of fact it can be quite useful as studies have shown, So unless you are suffering from a pathologic condition such as Gynacemastia or any other which requires a medical treatment, you shouldn't go for estrogen inhibitors. Better to control it through diet, in a limit that helps in maintaining a proper balance between the hormone levels.
Stay safe, Stay healthy :)
(P.S The above post is just my general opinion based on the information i collect from different internet resources and books, if there find any mistakes or any changes that should be made, please feel free to
e-mail me on bajajsubhash12@gmail.com or can comment below)
#Medicine #Estrogen #Aromataseinhibitors #Bodybuilding #Diet #Medplus #Supplements #Health #Drugs #aminoglutethimide #tamoxifen #digitalhealth #
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