The U.S. Meals and Drug Administration (FDA) foolishly accredited the harmful Opill (norgestrel), as an over-the-counter (OTC) every day oral contraceptive, in July 2023.1 The contraception drugs — the primary obtainable and not using 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 possibility 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 incorporates the hormone norgestrel, which is a kind 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, just isn’t really helpful 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 capsule, sometimes called a “mini-pill.” Not like mixture oral contraceptives that include each estrogen and progestin, Opill incorporates solely progestin. This single-hormone formulation is commonly stated to trigger fewer unwanted effects, but it surely’s removed from a secure possibility.
In 1943, chemist Russell Marker began extracting progesterone from wild Mexican yams. Nonetheless, progesterone is poorly absorbed when taken orally, so girls needed to take inconveniently giant doses.
In 1951, Syntex S.A. (later acquired by Roche) developed norethindrone, the primary artificial progestin (progesterone analogue). A yr later, G. D. Searle (now a Pfizer subsidiary), got here up with its personal artificial progestin, known as norethynodrel. Each norethindrone and norethynodrel are derivatives of testosterone, the first androgenic hormone.
Syntex and Upjohn Pharmaceutical additionally co-developed medroxyprogesterone acetate, which continues to be extensively used, each in hormone alternative remedy (HRT) and contraceptives, together with Depo Provera. Mockingly, all these progestins initially obtained FDA approval for gynecological issues brought on by extra estrogen.
Artificial progestins, whereas having a number of the exercise of progesterone, do not need the identical physiological results because the endogenous progesterone produced by your physique. Progesterone is likely one of the most helpful hormones an individual might take whereas the artificial model, progestin, is likely one of the most harmful.
Progestin Will increase Breast Most cancers Threat
Based on the FDA, “The most typical unwanted effects of Opill embody irregular bleeding, complications, dizziness, nausea, elevated urge for food, belly 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 every other type of most cancers ought to ask a physician earlier than use.”5
It’s because hormonal contraception, together with progestin-only contraception drugs, could enhance breast most cancers threat. A case-control examine and meta-analysis printed in PLOS Medication, assessed breast most cancers threat related to various kinds of hormonal contraceptives, together with these containing progestagen solely.6
Progestagen is a broad time period that refers to any man-made or natural substance that has results much like these of progesterone, the pure hormone produced within the physique. It consists of artificial compounds like progestin. The examine discovered that present or latest use of hormonal contraceptives was related to an elevated threat of breast most cancers, with researchers stating:7
“Our findings counsel that there’s a relative enhance of round 20% to 30% in breast most cancers threat 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 girls in a wider age vary), they counsel that the 15-year absolute extra threat 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 identified for a while. The Girls’s Well being Initiative, which started in 1991, discovered girls who used both Premarin, a weak estrogen, alone or together with Provera, the artificial progestin utilized in contraception pictures, had elevated charges of vascular ailments, cognitive decline, cancers and extra.8
In my interview with Susan Wadia-Ells, Ph.D., writer of “Busting Breast Most cancers: 5 Easy Steps to Maintain Breast Most cancers Out of Your Physique,” she additionally described how progestin could provoke breast most cancers:
“In 2010, there was an extremely essential 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 girls who take progestin-based medicine — be they contraception medicine or menopausal medicine — have wherever from a 26% to an eightfold elevated threat of growing breast most cancers.
They lastly printed a examine in 2010 that mainly defined, in some extra element, however not completely, how the progestin pulls out or prompts one thing known as RANKL, which is a protein. The RANKL, apparently — although they do not say these phrases — can suffocate the mitochondria in a girl’s breast cell, initiating that first most cancers cell.
The unhappy factor is that no researchers within the subject of breast most cancers prevention ever cite this examine. They don’t seem to be conscious of it for some cause. However, it was printed 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 helpful results of pure progesterone, which is the principle endogenous and most direct and potent glucocorticoid receptor antagonist. As such, it’s additionally a cortisol blocker. Progesterone can be a GABA agonist and an estrogen blocker.
Estrogens are one of many major components contributing to growing your most cancers threat — together with the plastic burden contributing their xenoestrogens — as each lower mitochondrial perform. 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 vitality by blocking estrogen and cortisol.
Progesterone is the principle feminine hormone, and is a protecting hormone throughout being pregnant, however additionally it is essential 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, nevertheless. Progesterone is essential for profitable being pregnant, and you may severely inhibit your potential to get pregnant for those who take it on the fallacious time. So, whereas artificial progestin in oral contraceptives like Opill ought to be averted, correctly administered pure progesterone is kind of helpful for well being.
How you can Use Progesterone
Earlier than you think about using progesterone it is very important perceive that it’s not a magic bullet, and that you just get essentially the most profit by implementing a Bioenergetic weight loss plan method that lets you successfully burn glucose as your major gas with out backing up electrons in your mitochondria that reduces your vitality manufacturing. My new guide, “Mobile Well being: The Unified Idea 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 plan, 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 one in all solely 4 hormones I imagine many adults can profit from. (The opposite three are thyroid hormone T3, DHEA and pregnenolone.)
I don’t advocate 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 observe that when progesterone is used transmucosally in your gums as I counsel, the FDA believes that one way or the other converts it right into a drug and prohibits any firm from advising that on its label. Because of this firms like Well being Natura promotes their progesterone merchandise as “topical.”
Nonetheless, please perceive that it’s completely authorized for any doctor to advocate 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 known as progestins which are utilized by drug firms, however regularly, and incorrectly, referred.
Dr. Ray Peat has finished the seminal work in progesterone and possibly 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 hazards of extra estrogen with low LA diets and transmucosal progesterone supplementation.
He decided that almost all solvents don’t dissolve progesterone properly and found that vitamin E is the very best solvent to optimally present progesterone in your tissue. Vitamin E additionally protects you in opposition to harm 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 entire 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 entire spectrum of tocopherols and tocotrienols, particularly the beta, gamma, and delta sorts, within the efficient D isomer. For instance of an excellent vitamin E you possibly can have a look at the label on our vitamin E in our retailer. You should use any model that has an analogous label.
You should buy pharmaceutical grade bioidentical progesterone as Progesterone Powder, Bioidentical Micronized Powder, 10 Grams for about $40 on many on-line shops like Amazon. That’s practically a yr’s provide, relying on the dose you select.
Nonetheless, you will want to buy some small stainless-steel measuring spoons as you will want a 1/64 tsp which is 25 mg and a 1/32 tsp which is 50 mg. A traditional dose is usually 25 to 50 mg and is taken half-hour earlier than mattress, because it has an anti-cortisol perform and can enhance GABA ranges for a superb evening’s sleep.
Sadly, this vendor regularly runs out of product, and if that’s the case, then you should utilize 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 girl, it’s best to take the progesterone throughout the luteal section or the final half of your cycle, which will 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 girl you possibly can take the progesterone day by day for 4 to 6 months after which cycle off for one week. The most effective time of day to take progesterone is half-hour earlier than mattress because it has an anti-cortisol perform and can enhance GABA ranges for a superb evening’s sleep.
That is what I’ve personally doing for over a yr with excellent outcomes. I’m a doctor so do not need any issues doing this. In the event you aren’t a doctor it’s best to seek the advice of one earlier than utilizing this remedy, as transmucosal progesterone remedy requires a physician’s prescription.
