Often people turn to us with questions about dihydrotestosterone (DHT) and its derivatives. It seems that people have a misconception about how it works, calling DHT some kind of diabolical androgenic by-product, which does not play any role in the body, believing that as a result of its intake we only “destroy” our prostate and lose hair on our heads.
The real situation, of course, is much more complicated. DHT is one of those conflicting hormones whose work is catastrophically misunderstood. For some people, DHT is not something that needs to be reduced or eliminated in the body. For other people, there is a risk and you need to constantly monitor the level of DHT in the body. By knowing the individual facts about DHT in the body, you can determine what type you belong to and whether there is a risk, specifically, in your case.
Testosterone as a Prohormone
The main androgen that is secreted by the testes is naturally testosterone. However, for the most part of the body, the androgen signal is not carried by testosterone. In these tissues, including: the brain (CNS), skin, genitals, the actual androgen is actually DHT (does not apply to muscles). Testosterone in this case simply acts as a prohormone, which is converted into the active androgen of DHT by the action of the 5alpha reductase enzyme (5-AP). 5-ARs are concentrated in a large volume in almost every androgen-dependent body tissue, with the exception of skeletal muscle. As a result, a very small amount of testosterone in these parts of the body interacts with androgen receptors. Instead, it quickly turns into DHT, which then interacts with receptors.
This transformation has a very important biological function in these tissues. You see, DHT is a stronger androgen than testosterone – it binds about 3-5 times stronger with androgen receptors. If you excluded 5-AR from these tissues and stopped the formation of DHT, then you would see some undesirable changes in physiology. A good example is male pseudohermaphroditism due to congenital 5-AR deficiency. This is a relatively rare disease. With this deviation, men are born with little or no 5-AR enzyme content. They have unformed genitals and are often raised as girls. When puberty occurs in these men, testosterone levels are elevated, although DHT levels remain very low. Their muscles develop normally, as in other adults, however, there is practically no pubic / body hair and they have an underdeveloped prostate and penis. Also, libido and sexual function are often impaired.
Testosterone as an Active Androgen in Muscles
Skeletal muscles are unique tissues in the body, in terms of androgen dependence. In fact, muscle contains little or no 5-AR, and accordingly, almost no DHT is formed. In addition, any DHT that forms, or that is already present in the blood and approaches the muscle, is quickly blocked by the enzyme 3alpha-hydroxysteroid reductase (3a-HSD).
Thus, for muscle tissue, testosterone is the main active androgen. This does not mean that the administration of exogenous DHT does not produce an anabolic effect. It will trigger some anabolic activity in the muscles, although much weaker than that which could be from the same amount of testosterone. This is due to its rapid conversion of 3a-HSD to the weak metabolite 5alpha-androstan-3a, 17b-diol. If this enzyme is somehow blocked, it is likely that DHT will have a very powerful anabolic effect on the muscles.
It is important to understand that although testosterone is an active muscle androgen and DHT has relatively few direct anabolic effects for muscles in men, DHT is still very important for the full effect, due to increased testosterone productivity. Here are some of the features and effects of DHT on the central nervous system: it leads to an increase in neurophysiological activity (endurance), increases resistance to psychological and physical stress, optimizes sexual function and libido.
The Anti-Estrogenic Effects of DHT
One of the important functions of DHT in the body, which is not given due attention, is the antagonism of oestrogen. Some men who took Proscar (a 5-AR inhibitor) were convinced of this in their own skin, figuring out the causes of the appeared gynecomastia. With a decrease in the protection of DHT from oestrogen in the body, men become owners of the so-called “bitch boobs”.
How does DHT protect against oestrogen? There are at least three explanations for how this works. First of all, DH T directly inhibits the activity of oestrogen in tissues. On the one hand, it works by acting as a competitive antagonist with an oestrogen receptor; protection occurs by decreasing oestrogen-induced transcription of RNA at the point of subsequent connection with the oestrogen receptor.
Secondly, DHT and its metabolites, as described above, directly block the formation of oestrogen from androgens by inhibiting the activity of the aromatase enzyme. Studies of the effects of inhibitors on breast tissue have shown that DHT, androsterone, and 5alpha-androstandione are potent inhibitors that affect the formation of estrone from androstenedione. Moreover, it was proved that 5alpha-androstandione is the most powerful inhibitor, and androsterone is the least powerful.
Finally, DHT acts on the hypothalamus and pituitary gland, decreasing the secretion of gonadotropins. By decreasing the secretion of gonadotropins, you decrease the production of raw materials for oestrogen production from testosterone and androstenedione (DHT itself cannot aromatize into oestrogen). This property of DHT is particularly useful when introduced from the outside, but we will talk about this in more detail below.
DHT, Oestrogens and the Prostate
When it comes to sex hormones, it becomes clear that for a wide range of people, the mechanisms of DHT in the functions of the prostate gland are completely unclear. The inaccurate and oversimplified opinion of most people is that DHT is responsible for prostate hypertrophy and contributes to the development of prostate cancer.
The real situation, of course, is much more complicated. You must understand that there are significant differences between the healthy development and the regular growth of the prostate, and prostate growth due to BPH and cancer.
The first period of prostate growth is considered to be the stage associated with age-related changes, confined to puberty and increased secretion of androgens in the testes. This removes the prostate from the state of prepubertal rest, and starts the growth process, which takes place before acquiring the normal size characteristic of a healthy and functional gland of an adult. At the beginning and middle of adulthood, the prostate gland does not change parameters, despite the constantly high levels of androgens in the body. However, if androgens are blocked, then the prostate in a mature man will decrease in size. This can happen by castration, or even 5-AR blockade (recall that DHT is an active androgen in the prostate gland).
As a man grows up, the second stage of growth often begins. This growth is considered benign prostatic hypertrophy (BPH) and occurs at a different hormonal level than regular growth during development. The fact that the presence of high oestrogen and androgen level is found in older men is largely associated with the development of BPH. Experimental studies have shown that androgens with saturated A rings (coupled with DHT) are unable to return the prostate to its original state of hypertrophy. These compounds do not aromatize. On the other hand, aromatization of androgens, such as testosterone or androstenedione, can induce hyperplastic changes in the prostate gland of monkeys, but these effects are the opposite of the addition of an aromatase inhibitor. Thus, oestrogen is obviously a causative factor in BPH. Or, perhaps more precisely, oestrogen in the presence of a certain amount of androgen.
This may not be news for you, but we are sure very few of you know that DHT can actually be used to treat BPH! This occurs by replacing testosterone, resulting in a decrease in the amount of oestrogen in the body.
DHT Can be Used to Treat Benign Prostatic Hypertrophy!
DHT is a strong androgen that will signal the pituitary gland to reduce the production of gonadotropins. A decrease in gonadotropins will cause a decrease in testosterone production, which in turn will cause a decrease in oestrogen levels. As a result, changes occur in the hormonal environment (high DHT, low oestrogen), which apparently leads to a regression of BPH. The clinical application of this theory is discussed in the United States; dihydrotestosterone is patented for use in androgen therapy.
The following two paragraphs taken from patent research illustrate the results:
In 27 subjects who had control of the plasma level of DHT in order to study the effect of the administered dose, an increase in the level from 2.5 to 6 ng per ml was revealed. This indicated a decrease in gonadotropic as well as plasma levels of testosterone, which exceeded at least 1.5 ng per ml (from 0.5 to 1.4, depending on the case); plasma estradiol levels decreased by 50%.
Among this group in the subjects, the prostate volume decreased significantly, which was detected using ultrasound and PSA (prostatic specific antigen). The average prostate volume was between 31.09. + .16.31 g before treatment and from 26.34. + -. 12.72 grams after treatment, for an average reduction of 15.4%, for a treatment having an average duration of 1.8 years with DHT (p = 0.01). So this information goes against the prevailing notion of BPH.
Unfortunately, sometimes people have a natural tendency to classify things as good or bad, black or white, without any grey areas. DHT (like oestrogen) has recently been blacklisted by many, and has often been considered a hormone that has no function in the body other than harm. Now that you have all the necessary facts that you need, you can ultimately see how this point of view is far from the truth.