The U.S. Meals and Drug Administration (FDA) foolishly accredited the harmful Opill (norgestrel), as an over-the-counter (OTC) each day oral contraceptive, in July 2023.1 The contraception tablets — the primary accessible with out a prescription within the U.S. — reached retail pharmacies and on-line shops in March 2024.2 This was a derelict motion by the FDA that violates their mandate to guard the general public well being.
The drug’s maker, Perrigo, is touting Opill as a handy choice for folks with out medical insurance or entry to medical companies. “No prescription, no appointment, no problem. FDA-approved,” its web site states.3 However Opill comprises the hormone norgestrel, which is a sort of progestin.
Norgestrel is efficient in stopping ovulation, thickening cervical mucus to hinder sperm motion and altering the uterine lining to stop implantation of a fertilized egg.4 Nonetheless, progestin, the artificial model of progesterone, is just not really useful because it doesn’t have the well being advantages related to pure progesterone — and carries important well being dangers.
What’s Progestin, the Energetic Ingredient in Opill?
Opill is a progestin-only contraceptive tablet, also known as a “mini-pill.” In contrast to mixture oral contraceptives that include each estrogen and progestin, Opill comprises solely progestin. This single-hormone formulation is usually mentioned to trigger fewer unwanted side effects, but it surely’s removed from a secure choice.
In 1943, chemist Russell Marker began extracting progesterone from wild Mexican yams. Nonetheless, progesterone is poorly absorbed when taken orally, so ladies needed to take inconveniently massive doses.
In 1951, Syntex S.A. (later acquired by Roche) developed norethindrone, the primary artificial progestin (progesterone analogue). A 12 months later, G. D. Searle (now a Pfizer subsidiary), got here up with its personal artificial progestin, referred to as norethynodrel. Each norethindrone and norethynodrel are derivatives of testosterone, the first androgenic hormone.
Syntex and Upjohn Pharmaceutical additionally co-developed medroxyprogesterone acetate, which remains to be extensively used, each in hormone substitute remedy (HRT) and contraceptives, together with Depo Provera. Paradoxically, all these progestins initially acquired FDA approval for gynecological problems brought on by extra estrogen.
Artificial progestins, whereas having among the exercise of progesterone, would not have the identical physiological results because the endogenous progesterone produced by your physique. Progesterone is likely one of the most useful hormones an individual may take whereas the artificial model, progestin, is likely one of the most harmful.
Progestin Will increase Breast Most cancers Threat
In keeping with the FDA, “The commonest unwanted side effects of Opill embrace irregular bleeding, complications, dizziness, nausea, elevated urge for food, stomach ache, cramps or bloating.” Nonetheless, it additionally notes, “Opill shouldn’t be utilized by those that have or have ever had breast most cancers. Customers who’ve another type of most cancers ought to ask a health care provider earlier than use.”5
It is because hormonal contraception, together with progestin-only contraception tablets, might improve breast most cancers danger. A case-control examine and meta-analysis revealed in PLOS Medication, assessed breast most cancers danger related to various kinds of hormonal contraceptives, together with these containing progestagen solely.6
Progestagen is a broad time period that refers to any synthetic or natural substance that has results much like these of progesterone, the pure hormone produced within the physique. It contains artificial compounds like progestin. The examine discovered that present or latest use of hormonal contraceptives was related to an elevated danger of breast most cancers, with researchers stating:7
“Our findings counsel that there’s a relative improve of round 20% to 30% in breast most cancers danger related to present or latest use of both mixed oral or progestagen-only contraceptives …
When our findings for oral contraceptives are mixed with outcomes from earlier research (which included ladies in a wider age vary), they counsel that the 15-year absolute extra danger of breast most cancers related to use of oral contraceptives ranges from 8 per 100,000 customers (a rise in incidence from 0.084% to 0.093%) to be used from age 16 to twenty to about 265 per 100,000 customers (from 2.0% to 2.2%) to be used from age 35 to 39.”
These dangers have been recognized for a while. The Girls’s Well being Initiative, which started in 1991, discovered ladies who used both Premarin, a weak estrogen, alone or together with Provera, the artificial progestin utilized in contraception photographs, had elevated charges of vascular illnesses, cognitive decline, cancers and extra.8
In my interview with Susan Wadia-Ells, Ph.D., creator of “Busting Breast Most cancers: 5 Easy Steps to Hold Breast Most cancers Out of Your Physique,” she additionally described how progestin might provoke breast most cancers:
“In 2010, there was an extremely necessary examine that has gotten buried. The lead researcher was Josef Penninger. On that worldwide examine staff of about 12 folks, one is now the CEO and president of Dana-Farber Most cancers Institute.
The researchers spent 10 years working with mice in preclinical settings, making an attempt to determine why ladies who take progestin-based medicine — be they contraception medicine or menopausal medicine — have anyplace from a 26% to an eightfold elevated danger of growing breast most cancers.
They lastly revealed a examine in 2010 that mainly defined, in some extra element, however not completely, how the progestin pulls out or prompts one thing referred to as RANKL, which is a protein. The RANKL, apparently — although they do not say these phrases — can suffocate the mitochondria in a lady’s breast cell, initiating that first most cancers cell.
The unhappy factor is that no researchers within the discipline of breast most cancers prevention ever cite this examine. They are not conscious of it for some motive. However, it was revealed in October of 2010 in Nature journal,9 which everyone knows is a really important, well-known scientific journal.”
The Well being Advantages of Pure Progesterone
Progestin doesn’t have the numerous useful results of pure progesterone, which is the primary endogenous and most direct and potent glucocorticoid receptor antagonist. As such, it’s additionally a cortisol blocker. Progesterone can also be a GABA agonist and an estrogen blocker.
Estrogens are one of many main elements contributing to rising your most cancers danger — together with the plastic burden contributing their xenoestrogens — as each lower mitochondrial operate. Progesterone is the antidote as a result of it’s not solely anti-estrogen however, as talked about, inhibits cortisol and can enhance mitochondria manufacturing of mobile power by blocking estrogen and cortisol.
Progesterone is the primary feminine hormone, and is a protecting hormone throughout being pregnant, however it is usually necessary in males since it’s a normal brain-regulating and protecting hormone.
Girls who nonetheless menstruate have to be cautious with the timing of their progesterone supplementation, nonetheless. Progesterone is essential for profitable being pregnant, and you’ll severely inhibit your capacity to get pregnant when you take it on the unsuitable time. So, whereas artificial progestin in oral contraceptives like Opill needs to be prevented, correctly administered pure progesterone is sort of useful for well being.
The way to Use Progesterone
Earlier than you think about using progesterone it is very important perceive that it’s not a magic bullet, and that you simply get probably the most profit by implementing a Bioenergetic weight loss program method that means that you can successfully burn glucose as your main gasoline with out backing up electrons in your mitochondria that reduces your power manufacturing. My new guide, “Mobile Well being: The Unified Principle of All Illness for Final Longevity and Pleasure” comes out very quickly and covers this course of in nice element.
After you have dialed in your weight loss program, an efficient technique that may assist counteract estrogen extra is to take transmucosal progesterone (i.e., utilized to your gums, not oral or transdermal), which is a pure estrogen antagonist. Progesterone is certainly one of solely 4 hormones I imagine many adults can profit from. (The opposite three are thyroid hormone T3, DHEA and pregnenolone.)
I don’t suggest transdermal progesterone, as your pores and skin expresses excessive ranges of 5-alpha reductase enzyme, which causes a good portion of the progesterone you are taking to be irreversibly transformed primarily into allopregnanolone and can’t be transformed again into progesterone.
Very best Strategy to Administer Progesterone
Please word that when progesterone is used transmucosally in your gums as I counsel, the FDA believes that in some way converts it right into a drug and prohibits any firm from advising that on its label. That is why firms like Well being Natura promotes their progesterone merchandise as “topical.”
Nonetheless, please perceive that it’s completely authorized for any doctor to suggest an off-label indication for a drug to their affected person. On this case progesterone is a pure hormone and never a drug and may be very secure even in excessive doses. That is not like artificial progesterone referred to as progestins which might be utilized by drug firms, however regularly, and incorrectly, referred.
Dr. Ray Peat has accomplished the seminal work in progesterone and doubtless was the world’s biggest professional on progesterone. He wrote his Ph.D. on estrogen in 1982 and spent most of his skilled profession documenting the necessity to counteract the risks of extra estrogen with low LA diets and transmucosal progesterone supplementation.
He decided that the majority solvents don’t dissolve progesterone effectively and found that vitamin E is one of the best solvent to optimally present progesterone in your tissue. Vitamin E additionally protects you towards injury from LA. You simply have to be very cautious about which vitamin E you employ as most supplemental vitamin E available on the market is worse than nugatory and can trigger you hurt not profit.
It’s crucial to keep away from utilizing any artificial vitamin E (alpha tocopherol acetate — the acetate signifies that it is artificial). Pure vitamin E will probably be labeled “d alpha tocopherol.” That is the pure D isomer, which is what your physique can use. There are additionally different vitamin E isomers, and also you need the whole spectrum of tocopherols and tocotrienols, particularly the beta, gamma, and delta sorts, within the efficient D isomer.
There are additionally different vitamin E isomers, and also you need the whole spectrum of tocopherols and tocotrienols, particularly the beta, gamma, and delta sorts, within the efficient D isomer. For example of a great vitamin E you may take a look at the label on our vitamin E in our retailer. You need to use any model that has the same label.
You should purchase pharmaceutical grade bioidentical progesterone as Progesterone Powder, Bioidentical Micronized Powder, 10 Grams for about $40 on many on-line shops like Amazon. That’s almost a 12 months’s provide, relying on the dose you select.
Nonetheless, you will have to buy some small stainless-steel measuring spoons as you will have a 1/64 tsp which is 25 mg and a 1/32 tsp which is 50 mg. A standard dose is often 25 to 50 mg and is taken half-hour earlier than mattress, because it has an anti-cortisol operate and can improve GABA ranges for a very good evening’s sleep.
Sadly, this vendor regularly runs out of product, and if that’s the case, then you should use Merely Progesterone by Well being Natura. It’s premixed with vitamin E and MCT oil. Once more, whereas Well being Natura states that its product is for “topical use solely,” I like to recommend making use of it transmucosally, by rubbing it in your gums.
In case you are a menstruating lady, you must take the progesterone through the luteal section or the final half of your cycle, which might be decided by beginning 10 days after the primary day of your interval and stopping the progesterone when your interval begins.
In case you are a male or non-menstruating lady you may take the progesterone day-after-day for 4 to 6 months after which cycle off for one week. One of the best time of day to take progesterone is half-hour earlier than mattress because it has an anti-cortisol operate and can improve GABA ranges for a very good evening’s sleep.
That is what I’ve personally doing for over a 12 months with superb outcomes. I’m a doctor so would not have any issues doing this. In case you aren’t a doctor you must seek the advice of one earlier than utilizing this remedy, as transmucosal progesterone remedy requires a health care provider’s prescription.
