Estrogen dominance - How to supplement PROGESTERONE

 *** FIRST*** -  Please read: Estrogen dominance treatment 1-2-3

Use PROGESTERONE supplementation cautiously

PROGESTERONE "therapy" to counter estrogen dominance has 3 steps.   FIRST, use other tactics to NATURALLY reduce estrogen levels in the body and boost PROGESTERONE via diet and lifestyle changes before considering supplementation (Step 3):

Estrogen dominance treatment 1-2-3

Used in the long-term, it is important to use a delivery route that avoids hormonal build-up in the fat cells - this problem is now recognized as a consequence of long-term transdermal application. Delivery routes are discussed on this post.

An annual urine test (most accurate) or saliva test (next best alternative) to monitor PROGESTERONE levels is advisable.   The saliva value should be below 300 (some have reported numbers over 10,000, which may take up to two years to return to normal, since PROGESTERONE is stored in the fat and releases very slowly). If PROGESTERONE level is not below 300, one should not resume PROGESTERONE until it is.

To understand why blood tests for hormones are useless:

Testing hormone levels

PROGESTERONE supplementation may INITIALLY have an estrogenic effect.   PROGESTERONE reactivates "sleepy" estrogen receptors. In premenopausal women, a deficiency of PROGESTERONE causes a "turning-down" of estrogen receptor sensitivity, and when women begin using PROGESTERONE , those Estrogen receptors are reactivated. This causes them to become overly sensitive, with ensuing estrogen dominance effects - e.g. water retention, headaches and swollen breasts. There can also be a temporary buildup of the endometrium, causing spotting and irregular bleeding. Most of these symptoms should disappear within a couple of cycles.

Use only bioidentical PROGESTERONE cream or gel

Any PROGESTERONE supplementation therapy should use BIOIDENTICAL PROGESTERONE.   i.e. the identical molecule that your body produces.

• i.e. DO NOT use synthetic PROGESTERONE (i.e. Progestins ).   This is DIFFERENT to the bioidentical molecule.
• The label should say U.S.P. PROGESTERONE .  USP (United States Pharmacopeia) means the formulated PROGESTERONE is of pharmaceutical grade and provides assurance that the product is bioidentical to that which is secreted from the female ovaries.

Natural, bioidentical PROGESTERONE is NOT DIRECTLY found in any plant.     It is synthesized from fat saponins such as diosgenin from Mexican wild yam or soy. After extraction from a plant source it is chemically modified/compounded in a laboratory -since the body can not metabolize diosgenin (derived from plant dioscin) into PROGESTERONE . Until 1970, wild yam was the main base source for production of PROGESTERONE in the contraceptive pill, and as a precursor for corticosteroids, such as CORTISONE. Today, natural and bio-identical PROGESTERONE is mostly produced from soybeans.

• "Natural" does not necessarily mean "bioidentical".    Bioidentical term refers to the shape of the molecule rather than the source of the hormone being identical. Some formulations may have been derived from plant-based sources, but are not even close to the shape of the natural molecule. E,g, Numerous plant-based HRT and purely yam-based creams that have not been chemically-modified.
• Soybean-source PROGESTERONE should use a NON-GMO soy

Cream/Gel should contain 1.5-3% USP natural PROGESTERONE by volume - this is equivalent to 450-900 mg /oz. of cream. When used transdermally, PROGESTERONE is absorbed into the fat and is released from the fat into the blood stream in direct proportion to the concentration of the cream. A higher dose cream will not release the hormone into the blood stream smoothly over a 12 hour period, and since PROGESTERONE only has a half life of five minutes once it is in the blood, this will significantly limit its effectiveness.

Highlights From My Time With Dr. John Lee by Dr. Mercola

The de facto standard cream concentration is 500mg of PROGESTERONE in 30g of cream (1.6%)

~¼ tsp. contains ~20mg

PROGESTERONE cream / gel / suppositories should NOT contain parabens as preservatives.     They should also be free of any other harmful substances.    E.g. liquid paraffin, parabens, phenoxyethanol, sodium lauryl sulphate, propylene glycol, fragrances, artificial colours and PEG emulsifying waxes (can contain the carcinogen dioxane).

Dr. Lee and Virginia Hopkins did not and do not endorse any particular brand, but they provide the following list of some good choices

http://www.virginiahopkinstestkits.com/PROGESTERONE list.html

-   This author has found these good brands:

•  Pro-gest.      Been around for a while and has been used in clinical tests.

•  NOW Natural PROGESTERONE.     Easily found online; 1 -3oz (85g) container USP PROGESTERONE (1.54%) from wild yam.

•  Renewed Balance

•  Serenity

•  Life pro Progestacare

•   Natpro.     Contains the maximum allowed dosage of USP PROGESTERONE from soy (3.33%), which means you use a smaller amount, which takes less time to rub in, and also absorbs quicker than lower percentage creams

 

Which PROGESTERONE delivery route to choose?

PROGESTERONE supplementation should try to emulate the body's natural production

• PROGESTERONE is produced naturally by the ovaries and adrenals - for transport into the blood stream and delivery to hormone-sensitive cells in the body. PROGESTERONE has an extremely short half-life in the blood of 5-20 min.  Can KJ. ABC of endocrinology. I. Hormones in general. Lancet 1970; 1:763-765.
• PROGESTERONE is produced by the ovarian corpus luteum during the luteal phase (following ovulation) of the menstrual cycle.   Ovarian connections located in the pelvic area are:
  • The fallopian tubes directly connect the ovaries to the uterus;
  • The ovaries empty into a pelvic plexus of veins having direct access to the blood stream - Substances absorbed through the vaginal membranes also enter this same pelvic plexus of veins.
• All delivery methods should use bioidentical PROGESTERONE  -  i.e. the same molecule that your body produces. The label should say U.S.P. PROGESTERONE

Vaginal or rectal route using hormonal gel or cream is the most efficient

RECOMENDED delivery method.  Via absorption through the mucous membranes.

• The vaginal route is best for women
• The scrotal route (possibly with permeation enhancement, such as combining with DMSO) or rectal routes are best for men.

Topical PROGESTERONE is well absorbed by the skin

However, long-term Topical PROGESTERONE use can build-up in fatty tissues causing high PROGESTERONE levels.

Oral  PROGESTERONE supplementation route is unsatisfactory

NOT a good route for any steroid hormones - since only 10% of the PROGESTERONE reaches the bloodstream and metabolism by the GI tract and liver produces several undesireable metabolites.

• 80-90% of oral PROGESTERONE is destroyed in GI tract and liver (so-called "first pass"liver metabolism).   Even when micronized and in oil, or with fatty foods (it does not dissolve in water). PROGESTERONE does not have any natural reason to be in the GI tract, which is not an efficient transport route for any steroid hormone. Swallowed hormones encounter absorbing foods, but PROGESTERONE is not affected by stomach acid. "Survivors"must later be broken down by the liver, and since only 10-20% reaches target cells a dose 5 times higher than utilized is needed.

Simon JA, Robinson DE, Andrews MC, Hildebrand JR 3rd, Rocci MLJr, Blake RE, Hodgen GD. The absorption of oral micronized PROGESTERONE : the effect of food, dose proportionality, and comparison with intramuscular PROGESTERONE . Fertil Steril 1993;60:26- 33.[PubMed]

• When processing PROGESTERONE , the liver creates >30 different metabolites.   These can have several undesirable side-effects. Notably 5a-reduced metabolites are known to cause neuropsychological side effects. Arafat et al addressed the sedative and hypnotic effects that may be mediated through these metabolites. The bioidentical PROGESTERONE Prometrium® can have several unpleasant side-effects.

KhalilNahoul, LouisDehennin, MichelJondet, MarcRoger. Profiles of plasma estrogens, PROGESTERONE and their metabolites after oral or vaginal administration of ESTRADIOL or PROGESTERONE . Volume 16, Issue 3 , Pages 185-202, May 1993  Maturitas

Arafat ES, Hargrove JT, Maxson WS, Desiderio DM, Wentz AC, Andersen RN.Sedative and hypnotic effects of oral administration of micronized PROGESTERONE may be mediated through its metabolites. Am J Obstet Gynecol. 1988 Nov;159(5):1203-9. PubMed

Sublingual / buccal drops

Drops of PROGESTERONE in an oil-based suspension are placed under the tongue.    Enter the blood stream directly and will not build up in your tissues like dermally applied cream. This method is preferred by Dr. Raymond Peat because it is efficiently absorbed through mucosa in the mouth. Sublingual PROGESTERONE , being fat-soluble is more effective when dissolved in vitamin E. He purports that it will stimulate the ovaries to produce PROGESTERONE (if the ovaries are still functioning) and will energize the adrenals and thyroid. Since each drop is about one milligram, you can determine an accurate dose. However, IT IS VERY BITTER!

Sublingual PROGESTERONE for hot flashes, migraines and cramping (at 15 minute intervals until symptoms resolve) has been suggested.

Intramuscular (I.M.) injections

Most common administration in clinics

• Guarantees adequate and verifiable plasma levels of active component.  Effective in infertility.
• PROGESTERONE half-life significantly longer than when injected into arm.   Due to higher concentration of adipose cells, which store then release PROGESTERONE when plasma levels decrease;
• Injections cause pain at injection site. 
• They are also inconvenient and invasive, but do get the hormone directly into the blood stream.
• Tolerated by those women highly motivated to reduce threat of abortion, prevent pre-term labor and for assisted reproduction (especially those with PCOS who are resistant to clomiphene citrate, which is used to stimulate hormones promoting ovulation); for those not willing to undergo the pain, this is not an effective method for long-term treatments.

How much PROGESTERONE to use, when to use it,  and for how long?

How long to supplement?

A minimum 2-3 months supplementation - needed to raise and maintain your PROGESTERONE level for maximum improvement of symptoms due to estrogen dominance. For menopause and osteoporosis treatment, use PROGESTERONE cream indefinitely.

How much USP bioidentical PROGESTERONE should you use and when?

Proper dosage and compliance are essential

The right dose is the dose that works, but . . . -  when it comes to balancing hormones, more is not better. The amount required depends on the specific application and should be tailored to the individual's needs and response. To avoid hormonal imbalance one should not use higher than the recommended dosage; A dosage chart is given as a guideline (most dosages recommended by Dr. John R. Lee, MD for transdermal application):

PROGESTERONE Dosage Chart

FDA-approved ORAL Dose.   In Oct 1999, the FDA approved a 200 mg daily dose of Prometrium, an oral PROGESTERONE , for use in preventing uterine cancer in women taking estrogen- i.e. this dose has been acknowledged as sufficient to oppose estrogen. Bear in mind that a 200 mg dose of oral PROGESTERONE actually delivers about 20 mg of PROGESTERONE (also be aware that with oral administration, 180 mg is excreted by the liver or transformed into other substances, which can cause problems).

The cream, gel or suppositories are best used twice a day - to better simulate the body's natural production. With slow-release bio-adhesive gel, once/day may be sufficient (follow package instructions)

Pre-menopausal women

Pre-menopausal women must take at least 3-7 days off each month without applying any PROGESTERONE cream/gel/suppository - since the body's natural production of PROGESTERONE is cyclical, supplementation should ideally mimic the body's naturally changing concentrations to affect a proper physiological response. i.e. the body should recognize some times when the PROGESTERONE llevel is low.

• Non-ovulating - PROGESTERONE supplementation should re-create what your body would produce if you were ovulating - both in the timing and amount used. The usual dose is 15-24 mg/day for 14 days before expected menses, stopping the day or so before menses.To figure the PROGESTERONE start date, count back 14 days from when your next period is due (i.e. Day 1 of next cycle), then beginning on that date, supplement PROGESTERONE for 14 days. The abrupt lowering of the PROGESTERONE level is the primary trigger for starting your period, at which time any PMS and painful periods will be dramatically reduced.
• Ovulating - wait until the day after ovulation (i.e. the luteal phase) to begin supplementation, which will then augment the body's own PROGESTERONE production from the corpus luteum. Supplementation should continue through the last 14 days of the cycle. After which, stopping the supplementation should initiate menses. Using PROGESTERONE earlier than ovulation would prevent ovulation resulting in no corpus luteum and therefore no PROGESTERONE production, which would be working against the body's own mechanisms. To accurately determine ovulation, you should purchase a fertility monitor.

Family Planning Tools

Menopausal women - may only need ~15 mg PROGESTERONE, but taken for the first 25 days of the month, then take 5 or 6 days off without applying any PROGESTERONE cream/gel/suppositories - so that one's body will not develop resistance or tolerance to the PROGESTERONE , and so become ineffective. Restart on the first of the month.

Men - may need 5-10 mg/day to keep in range of their normal, low, but constant amounts of PROGESTERONE production and counter estrogenic presence. Take 5 or 6 days off each month without using any PROGESTERONE cream/suppositories so that one's body will not develop resistance or tolerance to the PROGESTERONE .

Ensure sufficiency of magnesium and B-vitamins

It is essential to ensure sufficient B-vitamins and Magnesium whilst supplementing PROGESTERONE.    Magnesium & B vitamins aid liver's estrogen clearance

B-vitamins.  You need ~5-8 mg of B6 along with all the other B-complex vitamins).

Magnesium - The Missing MIneral.    Supplement with 400-600 mg oral Magnesium and also use transdermal magnesium for a few months to quickly increase magnesium levels in your body.

 

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