Index:
1. Functions of DHT
1.1. Formation of the body and puberty
1.2. Adulthood
a. Maintenance of prostate health
b. Libido and hormonal balance
2. Problems that Finasteride can cause to the hormonal balance of men
3. The importance of a high level of testosterone for general health
4. Secondary hypogonadism
5. Does Saw palmetto also inhibit DHT?
Finasteride inhibits the conversion of testosterone into DHT (dihydrotestosterone). This causes a decrease of 70% in the level of DHT in those taking finasteride.
1. Functions of DHT (dihydrotestosterone) in a man's body:
1.1. Development of the body and puberty:
Result: High Libido
Mature men (normal)
Testosterone - median in range
DHT - elevated
Estrogen (estradiol) - Higher than a young man
Prolactin - median in range
Result: average libido
Old men (normal situation)
Testosterone: medium-low
DHT - medium
Estrogen (estradiol) - medium
Prolactin -high
Result: Low Libido
Young men taking Finasteride - the first month
Testosterone - Elevated, anything between 15-20%
DHT - Very low (reduced by 70 %)
Estrogen (estradiol)?
Prolactin?
Result:?
Young men taking Finasteride - after a few months
DHT very low (reduced by 70%)
Estrogen (estradiol) - elevated (excess testosterone is converted into estrogen only, instead of E2 and DHT. Possibility of feminization of the body)
Prolactin: elevated (increasing the level of estrogen causes increased prolactin)
Impact on libido: Lower libido due to high levels of Prolactin, Estradiol and low level of DHT.
1. Functions of DHT
1.1. Formation of the body and puberty
1.2. Adulthood
a. Maintenance of prostate health
b. Libido and hormonal balance
2. Problems that Finasteride can cause to the hormonal balance of men
3. The importance of a high level of testosterone for general health
4. Secondary hypogonadism
5. Does Saw palmetto also inhibit DHT?
Finasteride inhibits the conversion of testosterone into DHT (dihydrotestosterone). This causes a decrease of 70% in the level of DHT in those taking finasteride.
1. Functions of DHT (dihydrotestosterone) in a man's body:
1.1. Development of the body and puberty:
- Formation of the male sex
organs in the fetus. Boys who are born without the ability to convert testosterone into DHT are born with ambiguous genitalia, malformed penises. Pseudohermaphrodites.
- Development of male characteristics at puberty. DHT is responsible for the emergence of body hair (including beard), penis growth, development of the libido and sexual function and prostate. In pseudohemaphrodites these functions do not develop fully at puberty, despite having a normal level of testosterone. They only develop male musculature, with little body hair and their sexual organ is between a micro penis and an overdeveloped clitoris. However, they never develop baldness.
1.2. Adult stage :
a) Maintaining the health of the prostate .
The prostate is where it is found the greatest concentration of DHT in the male body. In a simple analogy, DHT has to the prostate the same importance that oil and gasoline would have to an engine. It lubricates the prostate, maintains the size, stimulates and keeps the prostate functioning. And how important is the prostate? Well, without a prostate the penis does not work ... Men who undergo total prostatectomy (complete removal of the prostate), have impotence, decreased penis size, change in penile corpus cavernosum tissue (the tissue becomes cartilage, impairing the ability of erection), Peyronie's disease (scar in penile tissue, causes deformation and pain), among other problems. In a ripple effect, we can say that DHT is essential to maintain the structure and health of the penis. In the most severeous cases of men affected by finasteride (it has been called Post Finasteride Syndrome) they have exactly these problems ... change in penile tissue and Peyronie's disease (and impotence), which means that the inhibition of 5 alpha reductase in these men was so strong that their prostates were seriously affected (again, these patients are the most serious cases of SPF, not most cases). What's worse is that finasteride causes shrinkage of the prostate and this occurs by apoptosis (cell death), which means that depending on how this happens in the body (time of use, drug sensitivity, propensity, age, among other factors) the prostate can suffer serious consequences because of the use of Finasteride.
b) Libido and hormonal balance :
DHT is a hormone 5 times more erogenous and more potent than testosterone. The truth is that medicine is still crawling on the task of explaining the male libido and exactly how sexual hormones work together. What is known is there is a very subtle balance between testosterone, free testosterone, DHT, estrogen and prolactin (this one released in the brain). Furthermore, each of these hormones have by-products, each is transformed by enzymes into other hormones. It is like a large, interconnected network and one influences the other ... DHT also is subsequently transformed by the same 5 alpha reductase in 3 adiol G - 3 Alpha Androstenadiol Glucuronide (women with high levels of 3 Adiol G have excess hair and reproduction difficulties ... it is a masculinizing hormone. Unfortunately it is common to find an extremely low level of 3 Adiol G in men with persistent effects of finasteride.
2. Problems that Finasteride can cause to the hormonal balance of men
To understand how Finasteride can affect the hormonal balance of a man, one must understand a bit how it works. Depending on the age, this balance occurs differently. In a very simplified explanation, this is glimpse of how it works: Men in andropause ("menopausal" in men) have a high level of DHT and estrogen and mean level of testosterone, as well as a higher level of prolactin. Young men have a "low" level of DHT and estrogen, high testosterone and low levels of prolactin. After ejaculation, at any age, prolactin level in the brain rapidly rises, causing lack of sexual interest at that time. The younger you are, the faster the prolactin level will fall back, and soon you will feel sexual interest again. Older men have a higher prolactin level and therefore are less interested in sex. This gradual increase in prolactin level, occurs naturally as the years go by. This is why older men have higher levels of prolactin then young men. The body, to maintain balance and sex drive, increases the level of DHT everytime the estrogen level increases. They are interconnected. The excess testosterone is converted into DHT and estradiol at similar levels. So, to make it clear: In men, DHT has the effect of enhancing libido and estrogen inhibits libido (because the last is linked to prolactin in the brain).
To maintain the balance of a man's body, DHT and estrogen are interconnected. When the level of one is low, the level of the other must be also low. When the level of one increases, the level of the other also increases. Never, in his natural state, a man has a high level of estrogen and a low DHT level, because estrogen is a highly feminizing hormone and DHT a highly masculinizing hormone. Only when a man takes Finasteride, he creates this imbalance in his body.
Below is a rough sketch to facilitate understanding. Note that the level of DHT in young men, seems low compared to a mature man, but the balance between DHT and a low level of Estradiol gives him a higher libido. Remember, estrogen neutralizes libido in men:
Young Men (normal situation)
Testosterone - high level
DHT low - normal
Estrogen (estradiol) low level - normal
Prolactin low - normal - Development of male characteristics at puberty. DHT is responsible for the emergence of body hair (including beard), penis growth, development of the libido and sexual function and prostate. In pseudohemaphrodites these functions do not develop fully at puberty, despite having a normal level of testosterone. They only develop male musculature, with little body hair and their sexual organ is between a micro penis and an overdeveloped clitoris. However, they never develop baldness.
1.2. Adult stage :
a) Maintaining the health of the prostate .
The prostate is where it is found the greatest concentration of DHT in the male body. In a simple analogy, DHT has to the prostate the same importance that oil and gasoline would have to an engine. It lubricates the prostate, maintains the size, stimulates and keeps the prostate functioning. And how important is the prostate? Well, without a prostate the penis does not work ... Men who undergo total prostatectomy (complete removal of the prostate), have impotence, decreased penis size, change in penile corpus cavernosum tissue (the tissue becomes cartilage, impairing the ability of erection), Peyronie's disease (scar in penile tissue, causes deformation and pain), among other problems. In a ripple effect, we can say that DHT is essential to maintain the structure and health of the penis. In the most severeous cases of men affected by finasteride (it has been called Post Finasteride Syndrome) they have exactly these problems ... change in penile tissue and Peyronie's disease (and impotence), which means that the inhibition of 5 alpha reductase in these men was so strong that their prostates were seriously affected (again, these patients are the most serious cases of SPF, not most cases). What's worse is that finasteride causes shrinkage of the prostate and this occurs by apoptosis (cell death), which means that depending on how this happens in the body (time of use, drug sensitivity, propensity, age, among other factors) the prostate can suffer serious consequences because of the use of Finasteride.
b) Libido and hormonal balance :
DHT is a hormone 5 times more erogenous and more potent than testosterone. The truth is that medicine is still crawling on the task of explaining the male libido and exactly how sexual hormones work together. What is known is there is a very subtle balance between testosterone, free testosterone, DHT, estrogen and prolactin (this one released in the brain). Furthermore, each of these hormones have by-products, each is transformed by enzymes into other hormones. It is like a large, interconnected network and one influences the other ... DHT also is subsequently transformed by the same 5 alpha reductase in 3 adiol G - 3 Alpha Androstenadiol Glucuronide (women with high levels of 3 Adiol G have excess hair and reproduction difficulties ... it is a masculinizing hormone. Unfortunately it is common to find an extremely low level of 3 Adiol G in men with persistent effects of finasteride.
2. Problems that Finasteride can cause to the hormonal balance of men
To understand how Finasteride can affect the hormonal balance of a man, one must understand a bit how it works. Depending on the age, this balance occurs differently. In a very simplified explanation, this is glimpse of how it works: Men in andropause ("menopausal" in men) have a high level of DHT and estrogen and mean level of testosterone, as well as a higher level of prolactin. Young men have a "low" level of DHT and estrogen, high testosterone and low levels of prolactin. After ejaculation, at any age, prolactin level in the brain rapidly rises, causing lack of sexual interest at that time. The younger you are, the faster the prolactin level will fall back, and soon you will feel sexual interest again. Older men have a higher prolactin level and therefore are less interested in sex. This gradual increase in prolactin level, occurs naturally as the years go by. This is why older men have higher levels of prolactin then young men. The body, to maintain balance and sex drive, increases the level of DHT everytime the estrogen level increases. They are interconnected. The excess testosterone is converted into DHT and estradiol at similar levels. So, to make it clear: In men, DHT has the effect of enhancing libido and estrogen inhibits libido (because the last is linked to prolactin in the brain).
To maintain the balance of a man's body, DHT and estrogen are interconnected. When the level of one is low, the level of the other must be also low. When the level of one increases, the level of the other also increases. Never, in his natural state, a man has a high level of estrogen and a low DHT level, because estrogen is a highly feminizing hormone and DHT a highly masculinizing hormone. Only when a man takes Finasteride, he creates this imbalance in his body.
Below is a rough sketch to facilitate understanding. Note that the level of DHT in young men, seems low compared to a mature man, but the balance between DHT and a low level of Estradiol gives him a higher libido. Remember, estrogen neutralizes libido in men:
Young Men (normal situation)
Testosterone - high level
DHT low - normal
Estrogen (estradiol) low level - normal
Result: High Libido
Mature men (normal)
Testosterone - median in range
DHT - elevated
Estrogen (estradiol) - Higher than a young man
Prolactin - median in range
Result: average libido
Old men (normal situation)
Testosterone: medium-low
DHT - medium
Estrogen (estradiol) - medium
Prolactin -high
Result: Low Libido
Young men taking Finasteride - the first month
Testosterone - Elevated, anything between 15-20%
DHT - Very low (reduced by 70 %)
Estrogen (estradiol)?
Prolactin?
Result:?
Young men taking Finasteride - after a few months
DHT very low (reduced by 70%)
Estrogen (estradiol) - elevated (excess testosterone is converted into estrogen only, instead of E2 and DHT. Possibility of feminization of the body)
Prolactin: elevated (increasing the level of estrogen causes increased prolactin)
Impact on libido: Lower libido due to high levels of Prolactin, Estradiol and low level of DHT.
The last two schemes are the only
unbalanced ones. In
the long run it is unsustainable for the man's body. This is because, as I said before,
DHT and Estrogen are connected. DHT is the male body's natural protection against the
increase of estrogen (estradiol). With finasteride, men artificially induce low levels of DHT,
then the excess testosterone is converted into Estrogen only, instead of DHT and Estrogen.
The body will
try to find the balance every day, while you keep that state artificially.
The problem is the body can find a balance in a way that is not good for the patient ...
And that may
cause some of the persistent effects in some men.
Risk 1: Risk of developing
secondary hypogonadism
The body can interpret this
increase in estrogen as an overproduction of testosterone (yes, you read that
right). The
pituitary "reads" estrogen and testosterone as a single hormone, the pituitary
is the same in men and women, just suffered the action of different hormones during development. So if your body understands it is producing excess
testosterone, the pituitary will signal to gradually decrease the testicles natural production of testosterone,
which also causes a decrease in testicular size (irreversible in most cases).
This is called
secondary hypogonadism. So there are men who took finasteride and now show a low level of testosterone. The same thing can happen with someone who takes
anabolic steroids. Result: low testosterone levels, infertility, impotence,
lack of energy, depression, etc., etc.. Many doctors will roll the chair
if you say that Finasteride can cause secondary hypogonadism in some men, but
there are proven cases and published studies. The problem is that Merck hid the
risk (or did not know it, it may never have appeared in the short-term studies). A few years ago, doctors
around the world began calling for a thorough examination of sex hormones
before
the patient started treatment with finasteride. Thus, it is possible to prove that
the fall in testosterone production was caused by the medicine.
When secondary hypogonadism happens, the body can no longer return to the previous level of testosterone production alone in most cases. What you can do is try to reconnect the hypothalamic-testicles through drugs like Clomid and Nolvadex, which stimulate the production of FSH in the pituitary (more information in the "secondary hypogonadism", below).
When secondary hypogonadism happens, the body can no longer return to the previous level of testosterone production alone in most cases. What you can do is try to reconnect the hypothalamic-testicles through drugs like Clomid and Nolvadex, which stimulate the production of FSH in the pituitary (more information in the "secondary hypogonadism", below).
Risk 2: Raise the level of estrogen (E2) and affect the relationship E2 x DHT:
On this situation, the level of testosterone is not
affected, but estrogen stabilizes at a high level. Consequences: Possibility of
feminization of the body, gynecomastia or pseudo-gynecomastia, increased fat
accumulation in the hips, reduced libido etc., etc.. If your body can balance the
level of DHT with the Estrogen when you stop Finasteride, these effects will be
mitigated. A
possible treatment for this problem is the use of drugs such as Arimidex.
It inhibits
the conversion of testosterone into estrogen. But it is a very meticulous process, to balance precisely this way.
If you overdo
the dose and duration of treatment, estrogen level may plunge (and this may worsen erection). So it may only be suitable for someone who is showing a very
high level of estrogen and low DHT, and already has a reasonable time he stopped
taking finasteride.
Risk 3 :
No known cause. Many men have normal
levels of Testosterone, Estrogen and DHT after stopping Finasteride and still
have lingering effects of the drug. Probably this group's problems are related to the consequences of 5 alpha reductase inhibition, as it has other
functions in the body.
3. The importance of a high testosterone level for overall health
Testosterone is the locomotive of
the male body. It runs several processes in the body, since the hormones interact in cycles
(feedback loop). Having a higher testosterone level, a man will feel more
energy, better health, better fertility, increased sex drive, a faster metabolism,
improved memory, more muscle tone, stronger bones, better
mood, increased sense of satisfaction and peace. It is therefore extremely serious that finasteride decreases testosterone production in some men. Normal levels of testosterone
range between 300 and 1000 ng/dl. However, this is a general range,
doctors use this range for men from 13 to 80 years old. Obviously, the testosterone level
in an adolescent is closest to the upper limit and in older men it will be closer to the
lower limit. A normal level of testosterone for a young man is in the
upper third of the scale. Then, on the range presented here, a normal level for a
man from 20 to 30 years would be 700 to 1000 ng/dl. For an elderly person, the
expected level would be approximately between 300 and 560 ng/dl. Men who have testosterone levels below the lower limit are considered to present hypogonadism. There are other ranges
and the analysis must be done according to the range and the age of the patient.
A normal testosterone level for a 60-year-old man would be approximately around 450-560 ng/dl, according to this
scale. Unfortunately Finasteride is bringing testosterone
production to these levels in men 20 to 30 years old. But they still have a whole life
ahead and already present hormone levels as 60 year old men. And in some young men, this decrease in
production was more severe, and they have testosterone levels below 300 ng/dl (more about
hypogonadism below).
From the age of 30, a man loses
1% of his testosterone production per year until the end of life. It's a very slow progress,
and men only realize this situation when this process is close to 60 years old or later and he has already lost 30% of his testosterone level. It is a very different situation if you loose 30% in one
year ... as it has happened to some users of Finasteride.
4. Secondary
hypogonadism
Hypogonadism is a medical term
that describes the decreased functional activity of the gonads (testes in men).
Hypogonadism,
as a result of defects in the hypothalamus or pituitary is called secondary
hypogonadism. In secondary hypogonadism men show a decreased secretion of
hormones (LH stimulates the testes to produce testosterone) and FSH (which
stimulates the testes to produce sperm). Men who suffer from hypogonadism have testosterone levels
below the lower limit of the scale . In a range of 300 to 1000 ng / dL, it would be any level
below 300. Problems that men can develop over the years, if they suffer
from hypogonadism and do not seek treatment:
Low or complete lack of libido
Infertility
Depression
Anxiety
Irritability
Fatigue
Poor sleep
Cognitive problems such as difficulty concentrating and
memory loss
Reduction in quality of life
Dry skin and weak nails
Decreased hair in the pubic area, underarms and legs
Decreased sense of smell
Bone loss (osteoporosis)
Increase in abdominal fat
Intolerance to glucose and diabetes
High Cholesterol
Muscle atrophy and loss
Decreased growth of facial hair and body hair.
Decrease in the size of the testicles, penis and prostate
Erectile Dysfunction
Frequent desire to urinate.
Gynecomastia and feminization of the body in general.
Does Saw palmetto also inhibit DHT?
Some men begin treatment with the
supplement known as saw palmetto, in an attempt to escape from the side effects of
finasteride. Unfortunately, saw palmetto is also an inhibitor of 5 alpha
reductase. It reduces DHT levels and may cause the same side effects
than finasteride. There are men enrolled in Propecia Help who never used finasteride, but were treated with saw palmetto and present the same Post-Finasteride Syndrome symptoms. Unfortunately, the way it affects men also is similar to
finasteride. Some do not have any side effects,
others develop temporary effects that go away when they stop the drug and a third group has permanent and irreversible effects that do not resolve even years after
stopping treatment with saw palmetto.
Sources:
- 5-Alpha-Reductase Deficiency | WebMD
- Traish AM, Hassani J, Guay AT, Zitzmann M, Hansen ML (March 2011). "Adverse side effects of 5α-reductase inhibitors therapy: persistent diminished libido and erectile dysfunction and depression in a subset of patients". The Journal of Sexual Medicine 8 (3): 872–84.doi:10.1111/j.1743-6109.2010.02157.x.PMID 21176115.
- Irwig, Michael S. (2012). "Depressive Symptoms and Suicidal Thoughts Among Former Users of Finasteride With Persistent Sexual Side Effects". The Journal of Clinical Psychiatry 73 (09): 1220-1223.doi:10.4088/JCP.12m07887. ISSN 0160-6689.PMID 22939118.
- Irwig MS and Kolukula S "Persistent Sexual Side Effects of Finasteride for Male Pattern Hair Loss" J Sex Med 2011;8:1747–1753.http://onlinelibrary.wiley.com/doi/10.1111/j.1743-6109.2011.02255.x/abstract
- Finn DA, Beadles-Bohling AS, Beckley EH, et al.(2006). "A new look at the 5alpha-reductase inhibitor finasteride". CNS Drug Reviews 12 (1): 53–76.doi:10.1111/j.1527-3458.2006.00053.x.PMID 16834758.
- Gina Kolata (June 15, 2008). "New Take on a Prostate Drug, and a New Debate". NY Times. Retrieved 2008-06-15.
- Altomare G, Capella GL (October 2002). "Depression circumstantially related to the administration of finasteride for androgenetic alopecia". The Journal of Dermatology 29(10): 665–9. PMID 12433001.
- Rossi, A.; Cantisani, C.; SCARNò, M.; Trucchia, A.; Fortuna, M. C.; Calvieri, S. (2011). "Finasteride, 1 mg daily administration on male androgenetic alopecia in different age groups: 10-year follow-up". Dermatologic Therapy 24(4): 455-461. doi:10.1111/j.1529-8019.2011.01441.x.ISSN 13960296. PMID 21910805.
- Römer B, Gass P (December 2010). "Finasteride-induced depression: new insights into possible pathomechanisms". Journal of Cosmetic Dermatology 9 (4): 331–2. doi:10.1111/j.1473-2165.2010.00533.x.PMID 21122055.
- Rahimi-Ardabili B, Pourandarjani R, Habibollahi P, Mualeki A (2006). "Finasteride induced depression: a prospective study". BMC Clinical Pharmacology 6: 7.doi:10.1186/1472-6904-6-7. PMC 1622749.PMID 17026771.
- Rossi S (Ed.) (2004). Australian Medicines Handbook 2004. Adelaide: Australian Medicines Handbook. ISBN 0-9578521-4-2.
- Morrow, David J. (March 19, 1999). "New Profits in Old Bottles; Companies Find Bonus in Drugs That Cure Several Ills". The New York Times. Retrieved June 6, 2010.
- Drugs.com | Propecia Side Effects
- 5α-reductase inhibitors (5-ARIs): Label Change - Increased Risk of Prostate Cancer | U.S. Department of Health & Human Services ^ Walsh, PC (2010 Apr 1). "Chemoprevention of prostate cancer.". The New England Journal of Medicine 362 (13): 1237–8. doi:10.1056/NEJMe1001045. PMID 20357287.
- Package Leaflet Information for the User, Swedish package insert for Propecia 1mg.
- MHRA PUBLIC ASSESSMENT REPORT | The risk of male breast cancer with finasteride
- PROPECIA® (finasteride) | Merck & Co., Inc.
- <http://www.fda.gov/Drugs/DrugSafety/InformationbyDrugClass/ucm299754.htm?utm_source=fdaSearch&utm_medium=website&utm_term=finasteride&utm_content=2>
- <http://www.accessdata.fda.gov/drugsatfda_docs/appletter/2011/020180s039ltr.pdf>
- <http://www.businessweek.com/ap/2012-04/D9U3HR3G0.htm>
- Gunn BG, Brown AR, Lambert JJ, Belelli D (2011)."Neurosteroids and GABA(A) Receptor Interactions: A Focus on Stress". Frontiers in Neuroscience 5: 131.doi:10.3389/fnins.2011.00131. PMC 3230140.PMID 22164129.
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