The U.S. Food and Drug Administration (FDA) foolishly approved the dangerous Opill (norgestrel), as an over-the-counter (OTC) daily oral contraceptive, in July 2023.1 The birth control pills — the first available without a prescription in the U.S. — reached retail pharmacies and online stores in March 2024.2 This was a derelict action by the FDA that violates their mandate to protect the public health.
The drug’s maker, Perrigo, is touting Opill as a convenient option for people without health insurance or access to medical services. “No prescription, no appointment, no hassle. FDA-approved,” its website states.3 But Opill contains the hormone norgestrel, which is a type of progestin.
Norgestrel is effective in preventing ovulation, thickening cervical mucus to hinder sperm movement and altering the uterine lining to prevent implantation of a fertilized egg.4 However, progestin, the synthetic version of progesterone, is not recommended as it does not have the health benefits associated with natural progesterone — and carries significant health risks.
What’s Progestin, the Active Ingredient in Opill?
Opill is a progestin-only contraceptive pill, often referred to as a “mini-pill.” Unlike combination oral contraceptives that contain both estrogen and progestin, Opill contains only progestin. This single-hormone formulation is often said to cause fewer side effects, but it’s far from a safe option.
In 1943, chemist Russell Marker started extracting progesterone from wild Mexican yams. However, progesterone is poorly absorbed when taken orally, so women had to take inconveniently large doses.
In 1951, Syntex S.A. (later acquired by Roche) developed norethindrone, the first synthetic progestin (progesterone analogue). A year later, G. D. Searle (now a Pfizer subsidiary), came up with its own synthetic progestin, called norethynodrel. Both norethindrone and norethynodrel are derivatives of testosterone, the primary androgenic hormone.
Syntex and Upjohn Pharmaceutical also co-developed medroxyprogesterone acetate, which is still widely used, both in hormone replacement therapy (HRT) and contraceptives, including Depo Provera. Ironically, all these progestins initially received FDA approval for gynecological disorders caused by excess estrogen.
Synthetic progestins, while having some of the activity of progesterone, do not have the same physiological effects as the endogenous progesterone produced by your body. Progesterone is one of the most beneficial hormones a person could take while the synthetic version, progestin, is one of the most dangerous.
Progestin Increases Breast Cancer Risk
According to the FDA, “The most common side effects of Opill include irregular bleeding, headaches, dizziness, nausea, increased appetite, abdominal pain, cramps or bloating.” However, it also notes, “Opill should not be used by those who have or have ever had breast cancer. Consumers who have any other form of cancer should ask a doctor before use.”5
This is because hormonal birth control, including progestin-only birth control pills, may increase breast cancer risk. A case-control study and meta-analysis published in PLOS Medicine, assessed breast cancer risk associated with different types of hormonal contraceptives, including those containing progestagen only.6
Progestagen is a broad term that refers to any natural or synthetic substance that has effects similar to those of progesterone, the natural hormone produced in the body. It includes synthetic compounds like progestin. The study found that current or recent use of hormonal contraceptives was associated with an increased risk of breast cancer, with researchers stating:7
“Our findings suggest that there is a relative increase of around 20% to 30% in breast cancer risk associated with current or recent use of either combined oral or progestagen-only contraceptives …
When our findings for oral contraceptives are combined with results from previous studies (which included women in a wider age range), they suggest that the 15-year absolute excess risk of breast cancer associated with use of oral contraceptives ranges from 8 per 100,000 users (an increase in incidence from 0.084% to 0.093%) for use from age 16 to 20 to about 265 per 100,000 users (from 2.0% to 2.2%) for use from age 35 to 39.”
These risks have been known for some time. The Women’s Health Initiative, which began in 1991, found women who used either Premarin, a weak estrogen, alone or in combination with Provera, the synthetic progestin used in birth control shots, had elevated rates of vascular diseases, cognitive decline, cancers and more.8
In my interview with Susan Wadia-Ells, Ph.D., author of “Busting Breast Cancer: Five Simple Steps to Keep Breast Cancer Out of Your Body,” she also described how progestin may initiate breast cancer:
“In 2010, there was an incredibly important study that has gotten buried. The lead researcher was Josef Penninger. On that international study team of about 12 people, one is now the CEO and president of Dana-Farber Cancer Institute.
The researchers spent 10 years working with mice in preclinical settings, trying to figure out why women who take progestin-based drugs — be they birth control drugs or menopausal drugs — have anywhere from a 26% to an eightfold increased risk of developing breast cancer.
They finally published a study in 2010 that basically explained, in some more detail, but not totally, how the progestin pulls out or activates something called RANKL, which is a protein. The RANKL, apparently — though they don’t say these words — can suffocate the mitochondria in a woman’s breast cell, initiating that first cancer cell.
The sad thing is that no researchers in the field of breast cancer prevention ever cite this study. They’re not aware of it for some reason. But, it was published in October of 2010 in Nature magazine,9 which we all know is a very significant, well-known scientific journal.”
The Health Benefits of Natural Progesterone
Progestin doesn’t have the many beneficial effects of natural progesterone, which is the main endogenous and most direct and potent glucocorticoid receptor antagonist. As such, it’s also a cortisol blocker. Progesterone is also a GABA agonist and an estrogen blocker.
Estrogens are one of the primary factors contributing to increasing your cancer risk — along with the plastic burden contributing their xenoestrogens — as both decrease mitochondrial function. Progesterone is the antidote because it is not only anti-estrogen but, as mentioned, inhibits cortisol and will improve mitochondria production of cellular energy by blocking estrogen and cortisol.
Progesterone is the main female hormone, and is a protective hormone during pregnancy, but it is also important in men since it is a general brain-regulating and protective hormone.
Women who still menstruate need to be careful with the timing of their progesterone supplementation, however. Progesterone is crucial for successful pregnancy, and you can severely inhibit your ability to get pregnant if you take it at the wrong time. So, while synthetic progestin in oral contraceptives like Opill should be avoided, properly administered natural progesterone is quite beneficial for health.
How to Use Progesterone
Before you consider using progesterone it is important to understand that it is not a magic bullet, and that you get the most benefit by implementing a Bioenergetic diet approach that allows you to effectively burn glucose as your primary fuel without backing up electrons in your mitochondria that reduces your energy production. My new book, “Cellular Health: The Unified Theory of All Disease for Ultimate Longevity and Joy” comes out very soon and covers this process in great detail.
Once you have dialed in your diet, an effective strategy that can help counteract estrogen excess is to take transmucosal progesterone (i.e., applied to your gums, not oral or transdermal), which is a natural estrogen antagonist. Progesterone is one of only four hormones I believe many adults can benefit from. (The other three are thyroid hormone T3, DHEA and pregnenolone.)
I do not recommend transdermal progesterone, as your skin expresses high levels of 5-alpha reductase enzyme, which causes a significant portion of the progesterone you’re taking to be irreversibly converted primarily into allopregnanolone and cannot be converted back into progesterone.
Ideal Way to Administer Progesterone
Please note that when progesterone is used transmucosally on your gums as I advise, the FDA believes that somehow converts it into a drug and prohibits any company from advising that on its label. This is why companies like Health Natura promotes their progesterone products as “topical.”
However, please understand that it is perfectly legal for any physician to recommend an off-label indication for a drug to their patient. In this case progesterone is a natural hormone and not a drug and is very safe even in high doses. This is unlike synthetic progesterone called progestins that are used by drug companies, but frequently, and incorrectly, referred.
Dr. Ray Peat has done the seminal work in progesterone and probably was the world’s greatest expert on progesterone. He wrote his Ph.D. on estrogen in 1982 and spent most of his professional career documenting the need to counteract the dangers of excess estrogen with low LA diets and transmucosal progesterone supplementation.
He determined that most solvents do not dissolve progesterone well and discovered that vitamin E is the best solvent to optimally provide progesterone in your tissue. Vitamin E also protects you against damage from LA. You just need to be very careful about which vitamin E you use as most supplemental vitamin E on the market is worse than worthless and will cause you harm not benefit.
It is imperative to avoid using any synthetic vitamin E (alpha tocopherol acetate — the acetate indicates that it’s synthetic). Natural vitamin E will be labeled “d alpha tocopherol.” This is the pure D isomer, which is what your body can use. There are also other vitamin E isomers, and you want the complete spectrum of tocopherols and tocotrienols, specifically the beta, gamma, and delta types, in the effective D isomer.
There are also other vitamin E isomers, and you want the complete spectrum of tocopherols and tocotrienols, specifically the beta, gamma, and delta types, in the effective D isomer. As an example of an ideal vitamin E you can look at the label on our vitamin E in our store. You can use any brand that has a similar label.
You can purchase pharmaceutical grade bioidentical progesterone as Progesterone Powder, Bioidentical Micronized Powder, 10 Grams for about $40 on many online stores like Amazon. That is nearly a year’s supply, depending on the dose you choose.
However, you will need to purchase some small stainless steel measuring spoons as you will need a 1/64 tsp which is 25 mg and a 1/32 tsp which is 50 mg. A normal dose is typically 25 to 50 mg and is taken 30 minutes before bed, as it has an anti-cortisol function and will increase GABA levels for a good night’s sleep.
Unfortunately, this vendor frequently runs out of product, and if that’s the case, then you can use Simply Progesterone by Health Natura. It’s premixed with vitamin E and MCT oil. Again, while Health Natura states that its product is for “topical use only,” I recommend applying it transmucosally, by rubbing it on your gums.
If you are a menstruating woman, you should take the progesterone during the luteal phase or the last half of your cycle, which can be determined by starting 10 days after the first day of your period and stopping the progesterone when your period starts.
If you are a male or non-menstruating woman you can take the progesterone every day for four to six months and then cycle off for one week. The best time of day to take progesterone is 30 minutes before bed as it has an anti-cortisol function and will increase GABA levels for a good night’s sleep.
This is what I have personally doing for over a year with very good results. I am a physician so do not have any problems doing this. If you aren’t a physician you should consult one before using this therapy, as transmucosal progesterone therapy requires a doctor’s prescription.