The U.S. Meals and Drug Administration (FDA) foolishly authorised the damaging Opill (norgestrel), as an over-the-counter (OTC) every day oral contraceptive, in July 2023.1 The contraception tablets — the primary obtainable 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 individuals with out medical insurance or entry to medical providers. “No prescription, no appointment, no trouble. FDA-approved,” its web site states.3 However Opill comprises 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 Nevertheless, progestin, the artificial model of progesterone, shouldn’t be beneficial because it doesn’t have the well being advantages related to pure progesterone — and carries vital well being dangers.
What’s Progestin, the Lively 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 effects, but it surely’s removed from a secure choice.
In 1943, chemist Russell Marker began extracting progesterone from wild Mexican yams. Nevertheless, progesterone is poorly absorbed when taken orally, so ladies 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 broadly used, each in hormone alternative remedy (HRT) and contraceptives, together with Depo Provera. Sarcastically, all these progestins initially acquired FDA approval for gynecological problems attributable to extra estrogen.
Artificial progestins, whereas having a few of 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 helpful hormones an individual may take whereas the artificial model, progestin, is likely one of the most harmful.
Progestin Will increase Breast Most cancers Danger
In response to the FDA, “The commonest unwanted effects of Opill embrace irregular bleeding, complications, dizziness, nausea, elevated urge for food, belly ache, cramps or bloating.” Nevertheless, 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 health care provider earlier than use.”5
It is because hormonal contraception, together with progestin-only contraception tablets, could enhance breast most cancers threat. A case-control examine and meta-analysis printed in PLOS Drugs, assessed breast most cancers threat related to several types 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 current use of hormonal contraceptives was related to an elevated threat of breast most cancers, with researchers stating:7
“Our findings recommend that there’s a relative enhance of round 20% to 30% in breast most cancers threat related to present or current 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 recommend 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 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 Preserve 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 crew of about 12 individuals, one is now the CEO and president of Dana-Farber Most cancers Institute.
The researchers spent 10 years working with mice in preclinical settings, attempting to determine why ladies who take progestin-based medicine — be they contraception medicine or menopausal medicine — have wherever from a 26% to an eightfold elevated threat of creating breast most cancers.
They lastly printed a examine in 2010 that principally 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 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 don’t seem to be conscious of it for some motive. However, it was printed in October of 2010 in Nature journal,9 which everyone knows is a really vital, well-known scientific journal.”
The Well being Advantages of Pure Progesterone
Progestin doesn’t have the various 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 main elements contributing to rising your most cancers threat — 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 vitality by blocking estrogen and cortisol.
Progesterone is the principle feminine hormone, and is a protecting hormone throughout being pregnant, however it is usually 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 means to get pregnant in the event you take it on the mistaken 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.
The way to Use Progesterone
Earlier than you think about using progesterone you will need to perceive that it’s not a magic bullet, and that you simply get essentially the most profit by implementing a Bioenergetic weight loss plan method that lets you successfully burn glucose as your main gas with out backing up electrons in your mitochondria that reduces your vitality manufacturing. My new guide, “Mobile Well being: The Unified Concept of All Illness for Final Longevity and Pleasure” comes out very quickly and covers this course of in nice element.
After getting 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 every of 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 take to be irreversibly transformed primarily into allopregnanolone and can’t be transformed again into progesterone.
Splendid Approach to Administer Progesterone
Please be aware that when progesterone is used transmucosally in your gums as I counsel, the FDA believes that by some means converts it right into a drug and prohibits any firm from advising that on its label. This is the reason corporations like Well being Natura promotes their progesterone merchandise as “topical.”
Nevertheless, 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 could be very secure even in excessive doses. That is in contrast to artificial progesterone known as progestins which might be utilized by drug corporations, however ceaselessly, and incorrectly, referred.
Dr. Ray Peat has carried out the seminal work in progesterone and doubtless was the world’s best 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 the majority solvents don’t dissolve progesterone properly and found that vitamin E is the most effective 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 utilize 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 might 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 varieties, 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 varieties, within the efficient D isomer. For example of a really perfect vitamin E you may have a look at the label on our vitamin E in our retailer. You need to 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 almost a yr’s provide, relying on the dose you select.
Nevertheless, you will want to buy some small chrome 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 standard dose is usually 25 to 50 mg and is taken half-hour earlier than mattress, because it has an anti-cortisol operate and can enhance GABA ranges for an excellent night time’s sleep.
Sadly, this vendor ceaselessly 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.
If you’re a menstruating lady, it’s best to take the progesterone in the course of 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.
If you’re a male or non-menstruating lady you may take the progesterone on daily basis 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 operate and can enhance GABA ranges for an excellent night time’s sleep.
That is what I’ve personally doing for over a yr with superb outcomes. I’m a doctor so would not have any issues doing this. For those who aren’t a doctor it’s best to seek the advice of one earlier than utilizing this remedy, as transmucosal progesterone remedy requires a health care provider’s prescription.