Estrogens are produced in the ovary throughout the menstrual cycle, but at different concentrations depending on the day of the cycle. They have the effect of increasing the thickness of the endometrium during the first phase of the cycle before ovulation occurs.
The main effects of estrogens on a woman’s body are:
– They determine the accumulation of typically female fat on the hips and around the breasts.
– They are responsible for the appearance of hair during puberty.
– They stimulate the production of vaginal fluid in a way that prevents dryness.
– They help fix calcium in the bones and prevent osteoporosis.
– They have a protective effect on blood vessels so that they reduce the risk of myocardial infarction and stroke.
– They influence the metabolism of fats and cholesterol, protecting the arteries from atheromatous plaques.
But…
Very high levels of estrogen in the blood are related to an increased risk of breast, endometrial, prostate, colon, or ovarian cancers. To prevent these levels from rising, we must take care of our diet and practice regular physical exercise. There are two types of estrogens:
– Endogenous estrogens, which are produced by our own body
– Exogenous estrogens, which come from food and endocrine disruptors that reach our body and have a mimetic effect with estrogens
Therefore, by controlling the endogenous production of estrogens and the intake of exogenous estrogens we will achieve a balance that will protect us against many diseases. To do this we must enhance certain foods, reduce others to a minimum, and undergo hormone replacement therapy.
It has long been held that hormone replacement therapies can be counterproductive. But little has been said regarding the reverse situation, where the inhibition of the action of a certain hormone is deliberately caused. This procedure, which is usually used in the treatment of hormone-dependent malignant tumors (breast cancer, prostate cancer, etc.) is not debatable given the context surrounding the decision to use these substances.
On the other hand, the search for aesthetic perfectionism has led many interested in somehow inhibiting water retention and fat synthesis, to be inclined to use these drugs in order to cut off the biochemical pathways involved.
In other words, estrogens are directly responsible for the metabolic pathways of fat synthesis, inhibiting some enzymes and stimulating others in order to tilt the process towards fat anabolism. In the same way, its ability to cause an increase in the secretion of Aldosterone, a hormone that acts in the nephron (the fundamental unit of the kidney) causing the retention of Na+ (Sodium), determines the reabsorption of water from the lumen of the renal tubules. towards the renal intracellular space first and then towards the general circulation, influencing the increase in the volume of intravascular fluid and its subsequent deposition at the subcutaneous level, which causes a “blurred” appearance, a term widely used by bodybuilders who precisely what they are looking for. It is as “dry” as possible.
Another important reason to use these drugs is their ability to counteract the negative effects that usually appear when female hormone levels increase significantly. Let us remember that the formation of estrogens occurs as a result of a chemical process known as aromatization. This means that if the Testosterone doses used by an athlete are high, the estrogen concentrations will also be high.
High levels of estrogen can cause, among other things, the appearance in the first instance of an increase in the sensitivity of the nipples, followed by pain on palpation and finally the appearance of a lump at the breast level, a process known as Gynecomastia. In some cases, using an estrogen blocker is strongly recommended. If we add to this situation the increase in fat content and significant water retention, which can cause an increase in the risk of developing high blood pressure, we can perfectly understand the reason for the use of estrogen action inhibitors in the population of bodybuilders, both at amateur and professional level.
Within the group of drugs that act on the mechanism of action of estrogens, we can classify them as:
- Peripheral Estrogen Receptor Blockers
- Central Estrogen Receptor Blockers
- Inhibitors of Estrogen synthesis
Although all of these agents seek to act by canceling the action of estrogens, each group does so in a different way.
Among peripheral receptor blockers, Tamoxifen is the drug that represents this group. Its ability to block the binding of estrogen to its receptor is limited in terms of duration and effectiveness (% of the total existing receptors that can be occupied by the drug). This means that even if there is a blockade of 100% of the existing receptors, the duration of the effect is relatively short and this requires continuous administration since estrogen never stops being produced and is waiting to have its opportunity to bind to its specific receptor and act, causing the aforementioned effects.
On the other hand, Clomiphene is the representative drug of estrogenic blockers at a central level. This difference in the location of receptors between peripheral and central is due to the fact that at the central level, the desired effect is to cancel the negative feedback signal that occurs when there are high levels of circulating estrogens, and in this way, it is allowed to continue with high levels of secretion by the Pituitary of the so-called Gonadotrophins (GnRH), namely:
1-Follicle Stimulating Hormone (FSH):
- Stimulates ovulation in women
- Stimulates spermatogenesis in men
2-Luteinizing Hormone (LH):
- Supports the production of Testosterone in men
Finally, within the group of drugs that completely inhibit estrogen synthesis, we can mention Anastrozole as a representative drug. Its inhibiting power on estrogen production makes this drug one of the favorites of the bodybuilding world, but unfortunately, its high cost limits its use.
In summary, the use of estrogen action inhibitors in the world of bodybuilding is a fact. It is necessary to keep in mind that like any drug, its abuse can cause disorders and that if someone decides to use any of these substances, they must be used under strict medical control.
