The U.S. Food and Drug Administration (FDA) foolishly approved the dangerous Ophir (norgestrel) as an over-the-counter (OTC) oral contraceptive in July 2023.One The first over-the-counter birth control pill in the United States hit retail pharmacies and online stores in March 2024.2 This is an unjustified action that violates FDA's duty to protect public health.
The drug's manufacturer, Perigo, promotes Ophil as a convenient option for people who don't have health insurance or access to medical care. “No prescriptions, no appointments, no hassle. FDA approved,” the website says.three However, Ophir contains the hormone norgestrel, a type of progestin.
Norgestrel works by preventing ovulation, thickening cervical mucus to impede sperm movement, and changing the uterine lining to prevent implantation of a fertilized egg.4 However, progestins, synthetic versions of progesterone, are not recommended because they lack the health benefits associated with natural progesterone and pose serious health risks.
What is progestin, the active ingredient in Ophir?
Opill is a progestin-only birth control pill, often called a “minipill.” Unlike combined oral contraceptives, which contain both estrogen and progestin, Opill contains only progestin. This single-hormone formulation is often said to have fewer side effects, but it is far from a safe choice.
In 1943, chemist Russell Marker began extracting progesterone from wild Mexican yam. However, progesterone was poorly absorbed when taken orally, so women had to take uncomfortably high doses.
In 1951, Syntex SA (later acquired by Roche) developed the first synthetic progestin (a progesterone analogue), norethindrone. A year later, GD Searle (now a Pfizer subsidiary) developed its own synthetic progestin, norethindrone. Norethindrone and norethindrone are both derivatives of the major androgen hormone, testosterone.
Syntex and Upjohn Pharmaceuticals also co-developed medroxyprogesterone acetate, which is still widely used in both hormone replacement therapy (HRT) and birth control pills (including Depo-Provera). Ironically, all of these progestins were originally FDA approved for gynecological conditions caused by excess estrogen.
Synthetic progestins have some of the activity of progesterone, but they do not have the same physiological effects as the endogenous progesterone produced by the body. Progesterone is one of the most beneficial hormones a person can take, and the synthetic version, progestin, is one of the most dangerous.
Progestins increase breast cancer risk
According to the FDA, “The most common side effects of Opill are irregular bleeding, headache, dizziness, nausea, increased appetite, abdominal pain, cramps, or bloating.” However, it also notes that “Opill should not be used by people who have or have had breast cancer. Consumers with other forms of cancer should consult their physician before use.”5
This is because hormonal contraceptives, including progestin-only contraceptives, may increase the risk of breast cancer. A case-control study and meta-analysis published in PLOS Medicine evaluated the risk of breast cancer associated with different types of hormonal contraceptives, including progestin-only contraceptives.6
Progestagen is a broad term for natural or synthetic substances that have effects similar to progesterone, a natural hormone produced by the body. This includes synthetic compounds such as progestins. The study found that current or recent use of hormonal contraceptives was associated with an increased risk of breast cancer, and the researchers said:7
“Our study found that current or recent use of combined oral contraceptives or progestagen-only contraceptives was associated with a relative increased risk of breast cancer of approximately 20% to 30%.
“When we combine our findings on oral contraceptives with those from previous studies (including a wider age range of women), we find that the 15-year absolute excess risk of breast cancer associated with oral contraceptive use ranges from 8 per 100,000 women aged 16 to 20 years (an incidence rate increasing from 0.084 to 0.093%) to about 265 per 100,000 women aged 35 to 39 years (an incidence rate increasing from 2.0 to 2.2%).”
These risks have been known for some time. The Women's Health Initiative, which began in 1991, found that women who used Premarin, a weak estrogen, alone or with Provera, a synthetic progestin used in birth control injections, had higher rates of vascular disease, cognitive decline, and cancer.8
In an interview with Dr. Susan Wadia-Els, author of “Breast Cancer Fight: 5 Simple Steps to Kick Breast Cancer Out of Your Body,” she also explains how progestins can cause breast cancer.
“In 2010, a hugely important study was buried. The lead investigator was Josef Penninger, one of about a dozen international researchers who is now the CEO and president of the Dana-Farber Cancer Institute.
The researchers spent a decade studying mice in a preclinical setting to try to figure out why women who take progestin-based drugs, whether they're birth control pills or menopause medications, have anywhere from a 26 percent to an eight-fold increased risk of developing breast cancer.
They finally published a study in 2010 that basically detailed, but didn't fully explain, how progestins pull down or activate a protein called RANKL. RANKL apparently – they didn't use that word – can start the first cancer cells by choking the mitochondria in women's breast cells.
The sad thing is that no one in the breast cancer prevention field has cited this study. They don't know about it for some reason. But the study was published in Nature magazine in October 2010.9 As we all know, it is a very important and well-known scientific journal.”
Health Benefits of Natural Progesterone
Progestins lack many of the beneficial effects of natural progesterone, the major endogenous and most direct and potent glucocorticoid receptor antagonist. Therefore, it is also a cortisol blocker. Progesterone is also a GABA agonist and an estrogen blocker.
Estrogen is one of the main factors that increases the risk of cancer, and plastic burden contributes to xenoestrogens, both of which reduce mitochondrial function. Progesterone is not only an antidote to estrogen, but also, as mentioned earlier, suppresses cortisol and improves cellular energy production in mitochondria by blocking estrogen and cortisol.
Progesterone is the primary female hormone and is a protective hormone during pregnancy, but it is also important for men because it is a general hormone that regulates and protects the brain.
However, women who are still menstruating should be careful about when to take progesterone supplements. Progesterone is essential for a successful pregnancy, and taking it at the wrong time can seriously impair your ability to conceive. Therefore, synthetic progestins found in oral contraceptives such as Ophir should be avoided, but natural progesterone, when administered appropriately, is very beneficial to your health.
How to Use Progesterone
Before considering progesterone use, it is important to understand that it is not a panacea, and you will benefit most from implementing a bioenergetic diet approach that effectively burns glucose as your primary fuel without backing up electrons in your mitochondria. My new book, Cellular Health: The Unifying Theory of All Disease for Ultimate Longevity and Joy, will be out soon and will cover this process in detail.
After adjusting your diet, an effective strategy to help offset excess estrogen is to take mucosal progesterone (i.e., the one you put on your gums, not orally or transdermally). This is a natural estrogen antagonist. Progesterone is one of four hormones that many adults believe can benefit from it. (The other three are thyroid hormone T3, DHEA, and pregnenolone.)
I do not recommend transdermal progesterone. Since the skin contains large amounts of 5-alpha reductase, a significant portion of the progesterone you take will be irreversibly converted to allopregnanolone, which cannot be converted back to progesterone.
The ideal way to administer progesterone
If you use progesterone topically on your gums as I advise, the FDA believes it somehow converts to a drug and prohibits any company from recommending it on their labels. This is why companies like Health Natura promote their progesterone products as “topical.”
However, please understand that it is perfectly legal for any doctor to recommend a drug off-label to their patient. In this case, progesterone is a natural hormone, not a drug, and is very safe even in high doses. This is different from the synthetic progesterone called progestin, which is used by pharmaceutical companies but is often and incorrectly referred to.
Dr. Ray Pitt pioneered progesterone research and is probably the world’s leading expert on progesterone. He wrote his PhD on estrogen in 1982 and has spent most of his professional career documenting the need to address the dangers of excess estrogen with a low LA diet and mucosal progesterone supplementation.
He found that most solvents do not dissolve progesterone well, and that vitamin E is the best solvent for optimal delivery of progesterone to the tissues. Vitamin E also protects against damage caused by LA. Most supplemental vitamin E on the market is worse than useless, and will do more harm than good, so you have to be very careful about which vitamin E you use.
It is important to avoid using synthetic vitamin E (alpha tocopherol acetate – the acetate indicates that it is synthetic). Natural vitamin E is labeled “d alpha tocopherol.” This is the pure D isomer that the body can use. There are other vitamin E isomers, and for an effective D isomer, you need the full spectrum of tocopherols and tocotrienols, especially the beta, gamma, and delta types.
There are other vitamin E isomers, and you want the full spectrum of tocopherols and tocotrienols, especially the beta, gamma, and delta types, in the effective D isomer. For an example of the ideal vitamin E, look at the label of vitamin E sold in stores. Any brand with a similar label will do.
You can buy 10 Grams of Pharmaceutical Grade Bioidentical Progesterone Powder, Bioidentical Micronized Powder from many online stores like Amazon for about $40. This will last you almost a year, depending on the dosage you choose.
However, you will need to buy a small stainless steel measuring spoon as you will need 1/64 tsp (25 mg) and 1/32 tsp (50 mg). The usual dosage is usually 25-50 mg and is taken 30 minutes before bedtime. It has anti-cortisol properties and increases GABA levels to help you sleep better.
Unfortunately, this seller is often out of stock, and in that case, you can use Simply Progesterone from Health Natura. It is pre-mixed with vitamin E and MCT oil. Health Natura says that the product is for “topical use only,” but I recommend applying it transmucosally by rubbing it into the gums.
Menstruating women should take progesterone during the luteal phase or second half of their cycle. This can be determined by starting it 10 days after the first day of menstruation and stopping it once menstruation begins.
If you are a man or a woman who does not menstruate, you can take progesterone daily for 4 to 6 months and then stop your cycle for a week. The best time to take progesterone is 30 minutes before bedtime. It has anti-cortisol properties and increases GABA levels to help you sleep better.
This is the method I have personally used for over a year with very good results. I am a doctor so I have no problem doing this. If you are not a doctor, you should consult with your doctor before using this treatment. Transmucosal progesterone therapy requires a doctor's prescription.
