Estrogens

Estrogens are essential to bones, skin, female organs and libido.
An estrogen is any of a group of steroid hormones which promote the development and maintenance of the female body.
Estrogens are produced by both men and women: they are essential to maintenance of bones, skin, female organs, sperm and egg manufacture, pregnancy, and many other processes in both sexes, including nervous system maturation, cognition and libido.

The body makes 3 Estrogens: Estrone (E1), Estradiol (E2) and Estriol (E3).

All three perform essentially the same actions, but there are some important differences.

E2 is the main actor. Of the three, it is dominant.

E2 (Estradiol) is produced primarily in both ovaries and testes by “aromatization” of testosterone. Small amounts are produced in the adrenal glands and peripheral tissues, notably the fat cells. It is responsible for development and care of the female organs, bone building and repair, support of the libido and maturation of the ova (eggs) in the ovaries. it also plays a major role in care and maintenance of the skin.

E1 is one fifth as potent as E2

E1 (Estrone), is produced mainly by the fat cells and therefore tends to be higher in premenopausal, overweight people. It is not only less powerful as an estrogen: its blood level is usually 1/5 that of estradiol, in “cycling” women. But in menopause, when the ovaries shut down, E2 and E3 production approach zero and Estrone becomes the dominant estrogen.
E1 tends to be higher in women with breast cancer: there is no proof that it produces breast cancer; but blood levels of estrone have been thought to be a marker of breast-cancer development, by some practitioners. The idea is that if the estrone level rises suddenly, it gives an early warning of developing cancer of the breast.

E3, like E1, is 1/5 as “strong” as E2 and again, only 1/5th as much is produced, excepting during pregnancy (it is the main estrogen of pregnancy and hardly does anything else).
E3 has a reputation as the “anti-breast-cancer Oestrogen”.

Estrogen therapy

Animal origin and Synthetic estrogens and progestins” were produced and prescribed to women in the second half of the 20^th century, for contraception and hormone replacement. This practice fell into disrepute when a mega-study of American nurses, the “women’s health initiative” was reported in 1995, showing that the synthetic hormones were causing cancer, blood clots, heart attacks and strokes.

The resulting turmoil among patients and doctors was such that hormone replacement therapy has not been recommended by physicians for the past 20+ years. Currently, it is again being recommended, because the risk/benefit is actually not as bad as the “health initiative” results suggested, but the science behind this decision is questionable, because bioidentical human hormones are safer.

Careful study leads to the conclusion that the reason for the terrible side effects of “HRT” lay in the use of synthetic and equine hormones. The irony of this situation is that even after this catastrophic failure by “Big Pharma”, medical doctors have ignored the calls from functional and metabolic medicine practitioners, for the use of bioidentical human hormones, which are relatively risk-free.
The main objection by organised medicine is that they question the quality control exercised in production of the creams by registered pharmacists: they prefer medications prepared by big pharma.

Bioidentical human estrogens and progesterone:

Please visit the following link: BIHRT, as it is called, does not carry any greater risk of blood clots or cancers than that of women’s normal premenopausal hormone production.
Furthermore, precise control of the content of the creams involved is of little importance, because dosages are individualised and easily manipulated. However, modern-day pharmacists use very sophisticated equipment, to ensure that the products they supply to the patient Comply precisely with the prescriptions. — see an example of the equipment, via this link.

A product called “TRIEST”, containing all 3 natural estrogens, was prescribed at one time by BIHRT practitioners, but because of estrone’s association with breast cancer and the fact that it has hardly any estrogenic activity, it was removed from the preparation. “BIEST”, an Oestrogen cream recommended by functional medicine practitioners, contains Estradiol (E2) and Estriol (E3), in an “80%-20% ratio (the normal ratio in a young human female), with no Estrone.

The dose is adjusted so as to control menopausal symptoms without weight gain and bioidentical Progesterone is usually prescribed with it, because progesterone tends to counteract the tendency to weight gain which is the main side effect of treatment with estrogen.

XENO-OESTROGENS, the “UN-natural female hormones”

Many chemicals (XENO-ESTROGENS) and some plant products (PHYTO-ESTROGENS) can mimic the action of estrogens in the body (more on this, later).

Blood Tests for Estrogens

• Most of the time, doctors test for estradiol only: a test for estrone and one for estriol are available, but usually ordered only when necessary:
• Estriol is only of interest during pregnancy.
• Estrone rises in obesity, because it is produced by the fat cells (it also encourages fat cells to grow). It is regarded as unimportant except when breast cancer is suspected. However some practitioners do a yearly check of the estrone level, with analysis of the proportion of “estrone variants”, which may provide an early warning of developing breast cancer.
• Progesterone, the “pregnancy hormone”, while regarded as a female hormone, is not an estrogen.
  Its actions are different and in fact in some ways it is an “anti-estrogen”.
  It has a bearing on estrogen function however because estradiol tends to make women gain weight, while Progesterone counteracts that side effect. It also has a bearing on breast cancer because progesterone tends to prevent it.
• The progesterone/estradiol ratio is calculated (normal is 100-500, and optimal is closer to 500): an P/E ratio of less than 100 indicates “estrogen dominance”and an increased tendency to weight gain.
  Note that Progesterone is reported in nanomoles** per litre, while estradiol is reported in picomoles per litre *….
  one nmol = 1000 pmol, so we multiply the Progesterone “number” by 1,000, then divide the result by the estradiol “number”, to derive the “P/E ratio”.
  
  * The easy definition of a “MOLE” is the molecular weight of a substance, in grams. The mole, or “Mol”, is widely used in chemistry as a convenient way to express amounts of reactants and products of chemical reactions.
  ** A Gram = 1000 Milligrams, a Milligram = 1000 Micrograms, a Microgram = 1000 Nanograms & Nanogram = 1000 Picograms.

FEMALE OESTRADIOL LEVELS:

Age 7	Undetectable : < 29 Pg/ml
Age 10	10-33 Pg/ml
Age 11	15-43 Pg/ml
Age 12	16-77 Pg/ml
Age 14	17-200 Pg/ml

MALE OESTRADIOL LEVELS:

Age 7	Undetectable : < 16 Pg/ml
Age 11	< 22 Pg/ml
Age 13	10-25 Pg/ml
Age 15	10-46 Pg/ml

RHYTHMIC ESTRADIOL SECRETION, IN THE MENSTRUAL CYCLE (graphic from Wikipedia): Note the wide production range.

OESTRADIOL EXCESS (DOMINANCE)

FEMALE:
As said, Estrogens are essential to bones, skin, female organs and libido, but Oestradiol increases female traits, with large breasts and hips and too much “white adipose tissue“, which can be problematic, since “Lipocytes” (fat cells) produce estrone and estrone encourages lipocytes to grow.

The menopausal female has discontinued production of the hormone, so in menopause, estradiol needs to be replaced. But what is “enough”, and how much is too much?
Estrogen excess will occur if the estrogen replacement prescription is too strong, or if the Progesterone prescription is too weak (Progesterone tends to prevent estrogenic weight gain).
MALE:
In the male, estrogens are essential to bones, skin and libido, however, an oversupply can present a problem! We do not prescribe estrogens for men, but DHEA produces testosterone, which the liver “aromatizes” to estradiol. So over-medication with Testosterone or DHEA can result in high levels of estradiol, with breast enlargement, water retention and weight gain.
A man can become estrogen dominant, even without supplementing his DHEA or testosterone: if he is obese, the fat cells will produce estrone, just as they do in women.
estrogen excess in men does the same as it does in women: fat increases on the breasts, hips and thighs.
It is a vicious circle: fat cells produce estrone: the bigger they get, the more they make and the more they make, the bigger they get!

However estrogen does not cause reduction of the libido. In fact, Oestrogen is necessary for the male libido, as well as the female and total oestrogen blockade causes complete loss of libido in both sexes.

OESTRADIOL DEFICIENCY

Low Estradiol (E2) levels in young females is rare, but the cause can usually be identified by means of blood tests. It may be due to failure of the ovaries, or failure of the Pituitary to send stimulating “LH” and “FSH” hormones to them.
If the gonadal-stimulatory hormones, LH and FSH, are high, the fault lies with the ovaries and the cause is usually either genetic (Turner’s syndrome, ovarian failure), or toxic, as in cancer treatment. If LH and FSH are low, the Pituitary is at fault: this can have functional causes, such as starvation, overexercise, severe physical or emotional stress, heavy drug or alcohol use, or organic disease of the hypothalamus or pituitary.
Low estradiol is normal in menopausal women and is common in older men who don’t take DHEA.
Postmenopausal women and older men with low E2 levels are at increased risk of osteoporotic fractures, which can be lethal.

MENOPAUSE

Menopause begins immediately if the ovaries are removed or radiated, or slowly, due to ovarian shutdown.
The “premenopause” starts with irregular menstrual periods and soon (within 6-12 months) a constellation of symptoms begins, with slight variations between people. These symptoms are variable, with some combination of vaginal dryness, hot flashes, cold chills, night sweats, insommnia, mood swings, weight gain, reduced libido, slowed metabolism and occasionally, cognitive loss.
The symptoms usually increase slowly, but can start suddenly and can present with any mixture of low oestradiol, low progesterone and low Allopregnanolone symptoms, sometimes with added low thyroid symptoms as well.

Menopausal symptoms are easily treated with “BIEST”, which contains estriol* and estradiol, in an “80%-20% ratio **).
The dose is adjusted so as to control menopause symptoms without causing weight gain: usually, cream containing between 1.0 and 2.5 mg of estradiol is prescribed.

Progesterone is routinely added to the prescription, either because it is deficient, as a hedge against weight gain or as a treatment for insomnia.

DHEA is prescribed also, because it is naturally deficient by the time of menopause (DHEA production falls by 1 – 2% per annum, from the age of 26, in both sexes).
DHEA may be taken by mouth, but is very effective as a vaginal cream, for treatment of vaginal dryness and urine loss.

* E3 is added because of its anti-cancer effect and E1 is not, because it is pro-cancer.
**80/20 is the usual ratio of E3-to-E2 in humans. Also, in terms of strength, E2 = E3x5.

ANDROPAUSE

Some men suffer identical, though usually less severe, “Andropausal” symptoms, with the same list of discomforts, because their testosterone level is reduced as DHEA production falls due to aging.
Some men also develop low thyroid symptoms, which usually respond well to DHEA.
The tendency to osteoporosis, due to deficient estrogen, is also Eliminated by DHEA supplementation.

DURATION OF SYMPTOMS

In both sexes, estrogen deficiency symptoms usually settle down within 1-2 years without treatment.
However recurrences may occur from time to time and the lack of estrogen causes osteoporosis.

ASSOCIATION WITH OTHER CONDITIONS

Any and all other medical conditions may co-exist with Menopause/Andropause, but the affected individual should be checked carefully for Hypothyroidism (including intracellular hypothyroidism [IH] due to stress), high cholesterol and diabetes, in particular.
Adequate treatment of coexisting true hypothyroidism with T4, or of intracellular hypothyroidism with T3, eliminates hypothyroid symptoms like fatigue, fuzzy thinking and anxiety.
On the one hand, correcting IH will improve wellbeing and render the patient’s situation much more bearable. On the other, it will normalise body temperature, improve cholesterol and glucose management and help to reverse weight gain.

COMPLICATIONS OF ESTROGEN EXCESS:

ESTROGEN DOMINANCE: Progesterone opposes estroen’s tendency to fat production and if the Progesterone level is low relative to the estradiol level, the person is said to be “estrogen dominant”.
This is easily assessed by checking the blood level of each hormone and dividing the Progesterone “number” by that of estradiol: low Progesterone and high estradiol produce the same result.
As previously said in this paper, Progesterone is reported in nanomoles per litre, while estradiol is reported in picomoles per litre (One nmol = 1000 pmol), so we multiply the Progesterone “number” by 1,000 and then divide the result by the estradiol “number”, to derive the ratio. The Normal result is 100-500; optimally, closer to 500.
estrogen dominance can be a problem for younger women, too, either because of high estradiol production or because of Progesterone deficiency.

COMMON PROBLEMS OF ESTROGEN DOMINANCE:
Fat deposition in estrogen-responsive areas: hips, upper thighs, buttocks, lower abdomen and breasts.
Increased PMS, irregular periods, depression, mood swings, headaches, bloating, hot flashes, poor sleep.
Increased liability to cancers of the breast, colon and (in the male) prostate.
High Cholesterol, with increased liability to blood clots in the legs, heart attacks, strokes etc.
Increased liability to diabetes, due to obesity.

TREATMENT OF ESTROGEN DOMINANCE:
Correction of estrogen dominance is easily achieved by prescribing Progesterone or by reducing the strength of any prescribed estrogen preparation, so that the blood Estrogen/Progesterone ratio is between 100 and 500.
Hormone therapy should only be prescribed by a physician who is certified competent to supervise the management of hormonal deficiency.
No hormone restoration therapy, including Progesterone, should be prescribed to a premenopausal womenunless pregnancy and other pre-existing conditions have been excluded by blood, urine or saliva tests, ultrasounds, x-rays or other investigations, as necessary.
In persons who are still “cycling”, it is possible to reduce the amount of estradiol by prescribing an anti-estrogen medication; but this usually results in complete elimination of the libido ***.
For premenopausal women, cyclic administration of progesterone, from the 15^th to 24^th day of the menstrual cycle, is preferred; but taking progesterone every night will eliminate insomnia and may be better for some women.
For the menopausal, it is a better idea to prescribe progesterone on an ongoing, regular basis.

*** You can reduce Oestradiol with medication, but this destroys the libido, in women and in men.
If Progesterone is prescribed, it MUST be BIOIDENTICAL Progesterone, not “Premarin” (pregnant mare’s urine), conjugated equine oestrogens, or any other synthetic “progestin”.
“Progestin” medications are not bioidentical and are dangerous to health: please click this link and read the abstract of the paper: you will see how many conditions used to be treated with poisonous synthetic “progestin” drugs!

PLEASE SEE THE NOTES ON PROGESTERONE, elsewhere in this website.