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Hormone Basics

The two main sexual hormones in women are estrogen and progesterone.  Both are produced in men and women, although in different quantities.  Progesterone is made from pregnenolone, which in turn comes from cholesterol.

Production of progesterone occurs at several places.  In women, it is primarily produced in the ovaries just before ovulation and increase rapidly after ovulation.  It is also produced in the adrenal glands in both sexes and in the testes in males.  Its level is highest during the ovulation period (day 13-15 of the menstrual cycle).  If fertilization does not take place, the secretion of progesterone decreases and menstruation occurs.  If fertilization does occur, progesterone is secreted during pregnancy by the placenta and acts to prevent spontaneous abortion.  About 20-25 mg of progesterone is produced per day during a woman's monthly cycle.  Up to 300-400 mg are produced daily during pregnancy.  During menopause, the total amount of progesterone produced declined to less than 1% of the pre-menopausal level.  This drop is extreme.

Progesterone occupies an important position in the pathway of hormonal synthesis.  In addition to being the precursor to estrogen, it is also the precursor of testosterone and the all-important adrenal cortical hormone cortisol.  Cortisol is essential for stress response, sugar and electrolyte balance, blood pressure and general survival.  In short, progesterone serves to promote survival and development of the embryo and fetus.  It acts as a precursor to many important steroid hormones and helps to regulate a broad range of biological and metabolic effects in the body.  During chronic stress, progesterone production is reduced as the body favors cortisol production to reduce stress.  This is an important point which we will look into later.

Estrogen is produced in the ovaries.  It regulates the menstrual cycle, promotes cell division and is largely responsible for the development of secondary female characteristics during puberty.  In non-pregnant, pre-menopausal women, only 100-200 micrograms of estrogen is secreted daily.  But during pregnancy, much more is secreted.  Estrogen is produced in the ovaries, adrenal and fat tissues.  During menopause, the amount of estrogen in the body declines by about 50 to 60 percent.  Production , however, is augmented in the adrenals and in the fat cells.

Estrogen and progesterone work in synchronization with each other.  They oppose each other in their actions and work as checks and balances to achieve hormonal harmony in both sexes.

Functions of Progesterone

Progesterone acts primarily as an antagonist (opposite to) to estrogen in our body.  For example, estrogen can cause breast cysts while progesterone protects against breast cysts.  Estrogen enhances salt and water retention while progesterone is a natural diuretic.  Estrogen has been associated with breast and endometrial cancer, while progesterone has cancer preventive effect.

Some of the functions of progesterone include:

• It protects the breast, uterus, and ovaries from cancer

• It acts as a natural diuretic

• It produces a calming, anti-anxiety effect

• It contributes to formation of new bone tissue

Most significantly, it is known that high amounts of estrogen can induce a host of metabolic disturbances, and the body's way of counterbalancing estrogen is progesterone.  When this balancing mechanism is dysfunctional, a multitude of health related problems can arise.

Hormone Replacement Therapy (HRT)

Menopause is often a time when the hormonal balance between estrogen and progesterone is off.  Symptoms of such imbalance include hot flashes, vaginal dryness, water retention, weight gain, insomnia, mood swings, short-term memory loss, wrinkly skin and osteoporosis.  The breakthrough in treatment of menopausal symptoms came in 1964, when Dr. Wilson first reported that the lack of estrogen causes menopause.  Pharmaceutical companies introduced a synthetic estrogen hormone called Premarin.  With this drug, symptoms of menopause such as hot flashes were greatly reduced.  There was little doubt then that menopause was solely due to estrogen deficiency.  Few doctors knew then that estrogen deficiency alone did not explain many of the symptoms of menopause.  For example, how does one explain the fact that women who are post-menopausal but cannot be started on HRT can have relief of their menopausal symptoms when using progesterone replacement alone? Clearly there is more to the menopausal picture than deficiency of estrogen alone.

In fact, many women on HRT with estrogen alone are unhappy with fat accumulating at their hips and abdomen, osteoporosis, loss of sex drive and often swollen breasts.  The common perception is that estrogen is the primary regulator of libido, but in reality estrogen replacement often does not restore their previous sex drive.  What is needed is progesterone and in some cases, testosterone is also needed.  While the exact mechanism is not known, it is postulated that estrogen "prime" the brain cells but progesterone "turns on" the sex drive.  This has been studied and clinically observed in laboratory rats whose ovaries are removed.  Supplementing with estrogen alone does not increase sex drive, but supplementing with progesterone together with low dose estrogen does.

During menopause, the absolute level of estrogen decreased by 50 percent to a level below what is needed for pregnancy and enough for other normal body functions through the golden years.  This is the way nature intended it to be.  Menopause is therefore a normal physiological adjustment that does not produce any undesirable symptoms.  It is not a disease.  The current menopausal problem is an abnormality resulting from the relentless insult on the body's hormonal system from industrialized cultures' and deviation from a wholesome and healthy lifestyle.  We shall examine this in more detail.

Dr. John Lee - Pioneer on Natural Progesterone

Dr. John Lee is a world-renowned authority on natural hormonal balance and author of the book Progesterone: The Multiple Roles of A Remarkable Hormone.  He has treated thousands of menopausal women in the 1980s and 1990s with a program that was contrary to popular medical thinking at that time.  Instead of prescribing estrogen alone (the standard of medical practice then), Dr. Lee prescribed natural progesterone alone for treatment of menopausal symptoms.  In addition to relieve the menopausal symptoms, the treatment was able to reverse osteoporosis and prevent cancer.  Studies had confirmed that Dr. Lee's approached by using progesterone alone had vast palliative effects.

The key to Dr. Lee's approach is to understand the balance between estrogen and progesterone.  In the pre-menopausal women, estrogen is always in balance with progesterone.  When these two important hormones are out of balance, hormone related illnesses would emerge.  Symptoms include weight gain, fatigue, auto-immune disorders, fibrocystic diseases, loss of libido, depression, headaches, joint pain and moods swing.  These are just some of the common symptoms experienced during menopause, peri-menopause and pre-menstrual period.

According to Dr. Lee, what is commonly perceived as an absolute estrogen level deficiency during the menopausal years is in effect estrogen dominance caused by extreme low progesterone level.  Since the progesterone's role is to balance estrogen, the extremely low level of progesterone experienced after menopause leads to a relative dominance of estrogen, despite a 50 percent drop.

Dr. Lee treats menopause as an estrogen dominance syndrome.  His treatment is simple - reduce estrogen to progesterone ratio by increasing progesterone.  When the opposing force of progesterone is increased, the toxic effect of estrogen is decreased.  Fortunately for many women who followed Dr. Lee's advice, their menopausal symptoms reduced remarkably.

Why is estrogen and progesterone out of Balance?

Our body normally functions in perfect homeostasis.  With the advent of society and industrial state, in the past 70 years, our body has been subjected to unprecedented insult from environmental estrogen-like hormones.  In less than one hundred years, we have managed to turn our diet from whole fruits and whole food to fast and processed food.  In the past, cattle were raised on grass and natural organic feed and chickens were allowed to run free.  This is in stark contrast to the commercialization of the cattle and poultry farm of today where animals are in cages most of the time.  Worse yet, feeds laced with pesticides and hormones, both of which have estrogen-like activities, are routinely given to animals, which in turn is passed to humans.

Women in non-industrialized cultures, whose diets are whole food based and are untainted with modern processed foods and pesticides, seldom suffer a deficiency in progesterone and the signs of estrogen dominance manifested as menopausal symptoms as described by Dr. Lee.

Some of the reasons for increased environmental estrogen are:

1. Commercially raised cattle and poultry fed with estrogen-like hormones.

2. Commercially grown vegetables that contain pesticide residues whose chemical structure is similar to estrogen.

3. Synthetic estrogens & synthetic progesterones (Progestin, Progesterone Acetate and birth control pills).

4. Exposure to xenoestrogen.  Petrochemical compounds found in general consumer products such as creams, lotions, soaps, shampoos, perfume, hairs spray and room deodorizers.  Such compounds often have chemical structure similar to estrogen and act like estrogen.  They are fat soluble and non-biodegradable.

5. Hormone replacement therapy with estrogen alone without progesterone.  This increases the level of estrogen in the body.

6. Over production of estrogen from ovarian cysts or tumors.

7. Stress, causing adrenal gland exhaustion and reduced progesterone output.  Stress is one of the most frequently overlooked causes of estrogen dominance.

8. Obesity.  Fat has an enzyme that converts adrenal steroids to estrogen.  The higher the fat intake, the higher the conversion to estrogen.

9. Liver disease such as cirrhosis that reduces the breakdown of estrogen.

10. Deficiency of Vitamin B6 and Magnesium, both of which is necessary for neutralization of estrogen in the liver.

11. Increased sugar intake leading to a depletion of magnesium.

12. Intake of process and fast foods that are deficient in magnesium.

13. Increase in coffee intake.  Caffeine intake, from all sources, was linked with higher estrogen levels regardless of age, body mass index (BMI), caloric intake, smoking and alcohol and cholesterol intake.  Studies have shown that women who consumed at least 500 milligrams of caffeine daily, the equivalent of four or five cups of coffee, had nearly 70% more estrogen during the early follicular phase than women who consume no more than 100 mg of caffeine daily, or less than one cup of coffee.

Hormones and Lifestyle

Overeating and under-exercise is the norm in developed countries.  The populations from such countries, especially in the Western hemisphere where a large part of the dietary calorie is derived from fat, have much higher incidents of menopausal symptoms.  Studies have shown that estrogen and progesterone levels fell in women who switched from a typical high fat, refined carbohydrate to a low fat, high-fiber and plant based diet even though they did not adjust their total calorie intake.  Plants contain over 5000 known sterols that have progestogenic effects.  People who eat more wholesome food and exercise more have a far lower incidence of menopausal symptoms because their pre and post menopause level of estrogen does not drop as significantly.

In non-industrialized societies, not subjected to environmental estrogen insults; progesterone deficiency is rare. During menopause, their diet produces sufficient progestogenic substance to keep their sex drive unabated, strong bones and symptom-free passage through menopause.

Therefore, lifestyle is the single most important factor in causing estrogen and progesterone imbalance.

Imbalances of estrogen and progesterone in female:

1. Progesterone deficiency

Symptoms: Premenstrual Syndrome (PMS), insomnia, early miscarriage, painful or lumpy breast, infertility, unexplained weight gain and anxiety.

Discussion: This is the most common hormone imbalance among women of all ages.

Solution: Estrogen free diet, discontinue birth control pill and use natural progesterone cream to increase the progesterone level.


2. Estrogen deficiency

Symptoms: night sweats, mood swings, depression, hot flashes, sagging breast, vaginal dryness, osteoporosis, fibrocystic lumps, night sweats, painful intercourse and memory problem.

Discussion: This hormone imbalance is most common in menopausal women; especially with petite and/or slim women.

Solution: Progesterone is a biochemical precursor to estrogen.  Progesterone cream alone is sufficient to restore estrogen balance and relief of many of the symptoms.  If after 3 months of progesterone cream, proper diet, nutritional supplementation of magnesium and B6 do not relive the symptoms, then low-dose natural estrogen may be considered.  2.5 mg of natural tri-estrogen cream ( 10% estrone, 10% estradiol and 80% estriol) provides the equivalent action of 0.625 conjugated estrogen such as Premarin. Herbs like black cohash have weak estrogenic effect.  Isoflavone extracts and cruciferous vegetables extracts such as DIM may be considered as well.

3. Excessive estrogen:

Symptoms: bloating, rapid weight gain, heavy bleeding, migraine headache, foggy thinking, insomnia, red flush on face and breast tenderness during the first 2 weeks of menstrual cycle.

Discussion: This often comes about from excessive estrogen intake as part of a hormone replacement therapy program.

Solution: Discontinue estrogen replacement therapy that uses estrogen alone.

4. Excessive androgens (male hormones):

Symptoms: Acne, polycystic ovary syndrome (PCOS), excessive hair on face and arm, thinning hair on the head, infertility and mid-cycle pain.

Discussion: Excessive sugar and simple carbohydrates in the diet often cause this. Excessive sugar stimulates androgen receptors on the outside of the ovary.  Androgens also block the release of eggs from the follicle, causing polycystic ovary disease.

Solution: Dietary adjustment to reduce sugar and grains and proper exercise are important.  Natural progesterone cream could be used to maintain hormonal balance and discontinued when symptoms are resolved.  If progesterone levels rise each month during the leuteal phase of the cycle, a normal synchronal pattern of estrogen and progesterone is maintained and excessive androgen seldom occurs.

5. Estrogen dominance:

Symptoms: Combination of absolute progesterone deficiency and excess estrogen, resulting in a relative increase in estrogen in comparison to progesterone.

Common symptoms include:

· Acceleration of the aging process
· Breast tenderness
· Depression
· Fatigue
· Foggy thinking
· Headaches
· Hypoglycemia
· Memory Loss
· Osteoporosis
· PMS
· Pre-menopausal bone loss
· Thyroid dysfunction
· Uterine cancer and fibroids
· Water retention
· Fat gain around abdomen, hips and thighs

Discussion: This is the result of low estrogen but even lower progesterone.  Up to 50% of western women, especially those who are obese between the ages of 40 and 50 suffer from estrogen dominance.

Solution: Reduce stress, sugar and coffee from diet.  Adrenal function is normally compromised in a person with estrogen dominance.  Normalization of the adrenal function should be considered first, as well as relief of stressors. Follow a natural whole food diet, application of stress reduction techniques and natural progesterone cream in physiological doses (20 mg a day).

Estrogen Dominance - Key to the Puzzle

Estrogen dominance commonly occurs during menopause when progesterone production falls to approximately 1% of its pre-menopausal level while the production of estrogen falls to about 50% of its pre-menopausal levels.  The lack of progesterone, to oppose the toxic effect of estrogen dominance, results in a myriad of undesirable symptoms.

In the west, the prevalence of estrogen dominance syndrome approaches 50 percent in women over 35 years old as they enter the transitional phase of aging (age 35 to 45).  Definitive diagnosis can be made through a thorough history and physical examination, together with laboratory tests of estrogen and progesterone levels. Yet few doctors actually do that.  Synthetic estrogen is often passed out on the premise that symptoms presented are due to estrogen deficiency without any consideration for the progesterone part of the equation while in reality, many are suffering from relative estrogen dominance.

What the body needs is natural progesterone as a first line defense and not more estrogen, which it already has a relative oversupply. No wonder, many women given estrogen for these menopausal symptoms do not get well.

The Progesterone Solution

Once the concept of estrogen dominance is understood, the cure is simple - reduce estrogen load and or increase progesterone load.

The best way is first through normalization of adrenal function that is commonly compromised in most people with estrogen dominance. When this fails, one can replace the body with physiological doses of progesterone (approximately 20-30 mg./day) to overcome the estrogen dominance and reestablish hormonal balance. Raising the level of progesterone by supplementation (orally, by injection or topically) often provides dramatic relief from PMS, pre-menopausal and menopausal symptoms.

Taking phytoestrogen rich food, such as soy products, is another alternative way of reducing estrogen as these foods contain weak estrogens that competitively take up the estrogen receptor site, making estrogen less available for use. Foods that have estrogenic activities include: oats, peanuts, cashew nuts, wheat, apples and almonds. Interestingly, ginseng also has a weak estrogenic effect. Phytoestrogen also appear in a host of herbs, including black cohash, alfalfa, pomegranate and licorice.   While widely promoted as the miracle food in recent years by the soy industry, it should be noted that soy products have their own set of problems. Unfermented soy products, such as tofu, contain acid that, in fact, rob the body of many valuable nutrients and should not be taken in large quantity.  Fermented soy products, such as miso, do not have this problem and are the way to go.

Benefits of natural progesterone include:

· Stimulates osteoclast bone building (Osteoporosis Reversal)
· Helps use fat for energy
· Natural Diuretic
· Natural antidepressant
· Restores sex drive (Libido)
· Normalizes zinc and copper levels
· Facilitates thyroid hormone action
· Prevents endometrial and breast cancer
· Protects against fibrocystic breasts
· Normalizes blood sugar levels
· Normalizes blood clotting
· Restores proper oxygen cell levels
· Normalizes Menstrual Cycles

Natural vs. Synthetic Progesterone

The natural form of progesterone is derived from wild yam.  It is very different from the synthetic unnatural form made in a laboratory (the widely prescribed Provera). The synthetic version is a chemical compound called "progestin".  It is a prescription drug commonly used in small amounts to balance the estrogen effect in a hormone replacement program.  Being a drug, progestin is far more powerful than a woman's natural progesterone. It is metabolized in the liver into toxic metabolites which if excessive, can severely interfere with the body's own natural progesterone. This creates other hormone-related health problems and further exacerbating estrogen dominance.

The structural differences between natural and synthetic progesterone is significant with direct bearing on its functionality. Whereas natural progesterone causes a reduction in water and salt retention, synthetic progesterone do the opposite. This is why some women taking synthetic progesterone in their birth control pill or estrogen pill combined with synthetic progesterone during menopause experience bloating and fluid retention.  In fact, studies have shown that administration of synthetic progesterone lowers the blood level of the body's natural progesterone.

Reported side effects of synthetic progesterone include an increased risk of cancer, increased risk of birth defects if taken during the first four months of pregnancy, fluid retention, abnormal menstrual flow, nausea, acne, hirsutism, mental depression, nausea, insomnia, masculinization, and depression.  It is contraindicated in those with thrombophlebitis, liver dysfunction, known or suspected malignancy of breast and genital organs.  One of the metabolites have an anesthetic effect on brain cells.  A woman on high doses of synthetic progesterone is often lethargic and depressed and cannot be cured with anti-depressants such as Prozac.

Natural progesterone is obtained by extracting diosgenin from wild yams and then converting this component into natural progesterone in the laboratory.  Natural progesterone is referred to as natural because it is the identical molecule to that which the human body manufactures. Such yam-derived natural progesterone should not be confused with "yam extracts" that are commonly sold in health food stores.  Our body easily converts natural progesterone into the identical molecule made by the body.  It cannot convert the "yam extracts" into progesterone.  There is no evidence that such "wild yam extract" is converted into progesterone once it enters into the human body and unlike natural progesterone, no conclusive formal studies have ever been conducted that identifies any particular benefits from "wild yam extracts".

Side effects of Natural Progesterone

No known side effects exist when using natural progesterone in physiological amounts (20 - 30 mg a day for women and 6-10 mg a day for men) under normal conditions. It is therefore very safe. But as with most substances, too much can cause problems. Too much progesterone is actually counterproductive, as chronically high dose of progesterone over many months eventually causes progesterone receptors to turn off, reducing its effectiveness and may lead to toxic side effects, Some possible side effects include:

• An anesthetic and intoxicating effect such as slight sleepiness. Excess progesterone down-regulates estrogen receptors, and the brain's response to estrogen is needed for serotonin production. Simply reduce the dose until the sleepiness goes away.
  
• Some women report paradoxical estrogen dominance symptoms for the first week or two after starting progesterone.  It is also common for those who have been deficient in progesterone for years, in the initial application of progesterone, to experience some water retention, headaches, and swollen breasts. These are symptoms of estrogen dominance, but paradoxically exhibited in the initial stages of progesterone application, as the estrogen receptors are being re-sensitized by the progesterone and "waking up". This usually goes away by itself and is not a sign of toxicity.
  
• Edema (water retention).  This is likely to be caused by excess conversion to deoxycortisone, a mineralcorticoid made in the adrenal glands that causes water retention.
  
• Candida. Excess progesterone can inhibit anti-Candida white blood cells, which can lead to bloating and gas. Systemic candidiasis can be treated with a grain-free diet for 2 weeks, followed by 40 mg of progesterone ( using3% progesterone cream) a day applied vaginally and to the breast.  More is applied gradually elsewhere to areas such as the neck, face, brow , and inner aspects of the arms.  If side effects worsen, reduce progesterone dosage.
  
• Excessive progesterone can also lead to the increase in androgen production and ultimately increase in estrogen production within the adrenal hormonal synthesis pathway as the body shunts the excessive progesterone to these other hormones.

Excessive progesterone is normally caused by the excessive built up of progesterone in the body.  This is more commonly seen in those who are self-administering topical progesterone cream in the wrong area.  Progesterone cream should be applied to areas of the body that have good circulation but not high in fat. These areas include the wrist, back of the neck, and under part of the upper arm.  Areas such as the abdomen, buttock and breast are high in fat and will retain progesterone faster than other parts of the body.

Absorption of progesterone from topical application is about 20-30% for the first day.  A residual amount is left behind at the site of application, and this can accumulate in the subcutaneous fat tissue over time.

Routes of Progesterone Delivery

Natural progesterone can be administered orally, topically, sublingual or by injection.  Oral administration is relatively ineffective as it is quickly metabolized in the liver.  Injection is very effective, but can cause irritation to the injection site and it can be quite painful.  To achieve physiological dose (and not the higher pharmacological dose), the best way is sublingual or topical.  Progesterone is easily absorbed by the skin and is 5 to 7 times more effective in reaching the blood stream than oral forms of progesterone.  In other words, 100-200 mg. of oral progesterone is needed to obtain the equivalent benefit of 20-30 mg. of trans-dermal progesterone.  Sublingual progesterone offers the best and most direct delivery route, as it is well absorbed directly into the blood stream.  However, the required alcohol based for sublingual drops may not be tolerated by some.

Salivary level goes up in 3 to 4 hours and is washed off by 8 hours and blood level goes up in a matter of a few weeks, with some women reporting benefits in a few days.

For best stabilization of progesterone absorption and effectiveness, natural prosterone should be taken or applied in divided doses, two to three times a day.

Delivery Systems of Topical Progesterone

To affect maximum absorption and pass the skin barrier, natural progesterone should be carried in an oil/water emulsion that contains the same fatty acid composition as the skin.  Mineral oil will prevent the progesterone from being absorbed into the skin if topical progesterone is used. For oral progesterone, it is micronized.

There is a wide variation in dosage available.  Topical cream should contain at least 400 mg to 600 mg of natural progesterone per ounce.  Each one-half teaspoon application would supply a minimum of 26 mg of progesterone (women usually produce about 20 mg of progesterone daily during normal circumstances). To simplify matters, the better suppliers uses a pump, with one pump delivering about 20 mg of progesterone.  To get the physiologic dose, women would commonly apply one pump full a day (20 mg), while men can apply one-half pump full a day (10 mg).  Common low dose sublingual drops usually contain about 1.2 mg per drop (not droop full).

The consumer should read the label carefully.  Studies have shown that many commonly used topical commercial progesterone formulations contain less than 15 mg of progesterone per ounce.  In fact, some of these creams contain as little as 2 mg of progesterone per ounce.

The way to make sure that progesterone is present and not simply "wild yam extract" is to look for the "U.S.P. progesterone" on the label.  U.S.P. stands for United States Pharmacopoeia, which is the international standard of purity.  It confirms that the progesterone is the identical molecule as is produced by the human body.

Progestacare Pump for Women - 3 oz