Pushing Premarin: Big Pharma, Big Bucks — Part 2


Safety: Big Pharma, Bad Medicine

Premarin foals in feedlot.
Premarin foals in feedlot.

Despite Pfizer’s aggressive marketing strategies, the sad fact is that these drugs derived from horse urine are the same drugs they always were – the drugs that took the lives of thousands of unsuspecting women and continue to exploit and abuse the PMU mares and their foals.

They have the same risks they have always had and the package warnings list even more risks than before as a result of Wyeth’s past indiscretions and failure to sufficiently warn the public of the dangers. Yet they’re deemed safer because of this very reason – make the consumer aware, we aren’t hiding anything – honest.

And, while it’s true that the “recommended” prescribed dosages may be lower along with guidelines that advise reducing the length of time a woman remains on HRT, in effect nothing has changed – they are still recognized as carcinogens by the WHO and other regulatory bodies.

    In women, a recent study has evaluated the potential of HRT to induce DNA damage in peripheral blood leukocytes of postmenopausal women using the comet assay (Ozcagli et al. 2005). Significant increases in DNA damage were observed among women receiving 0.625 mg/day conjugated equine estrogens or conjugated equine estrogens plus medroxyprogesterone acetate as compared to the control group that had never received HRT. Finally, the excessive production of ROS in breast cancer tissue has been linked to metastasis of tumors in women with breast cancer (Malins et al. 1996; Malins et al. 2006; Karihtala and Soini 2007; Benz and Yau 2008). These and other data provide a mechanism of estrogen-linked tumor initiation/promotion by redox cycling of estrogen metabolites generating ROS, which damage DNA.” [1]

ROS stands for “Reactive Oxygen Species”. Various carcinogens, such as CEEs, may partly exert the effect of oxygen derived species (e.g. superoxide radical) by generating reactive oxygen species (ROS) during their metabolism. Oxidative damage to cellular DNA can lead to mutations and may, therefore, play an important role in the initiation and progression of multistage carcinogenesis.

Science says 0.625 mg/day can induce DNA damage and cancer. Today Premarin tablets are still available in dosages of 0.3 mm, 0.45 mg, 0.625 mg, 0.9 mg and 1.25 mg. And physicians continue to prescribe various doses depending on the severity and nature of menopausal symptoms. By comparison Premarin cream contains 0.625 mg per dosage and Duavee 0.45 mg together with 20 mg of bazedoxifene, a drug yet to be approved on its own by the FDA. Is a dosage of 0.45 mg really safer than 0.625 mg? And what about Premarin cream at the same 0.625 mg level?

And let’s not forget about the innocent bystanders, not just the vulnerable women who opt to take these drugs for relief of menopausal symptoms, either of their own volition or on the advice of their doctors.

What many may not be aware of is that creams, lotions and other topical skin products can be absorbed through the skin and into the systemic circulation resulting in unexpected complications.

Since the release of the damaging WHI results demonstrating the risks involved with the Premarin family of drugs, the use of topical hormones such as Premarin cream have escalated. When HRT drugs are applied topically rather than taken orally they avoid the “first-pass” effect through the liver which is generally considered a “safer” route.

    The advantage of this route of administration is that oestrogen is delivered directly to oestrogen-depleted tissues with similar efficacy to oral oestrogen, with the hope of avoiding significant systemic absorption and consequent side-effects. Given some concerns surrounding the safety of systemic HRT, particularly on breast tissue and the coagulation cascade, topical HRT offers a more targeted approach.” [2]

At the same time there are limited studies on the effects of topical estrogens and, in practice, systemic absorption is lower but not negligible and increases with increased doses of estrogen. [3]

And it isn’t simply the women who use Premarin vaginal cream who are at risk – their partners are also exposed to the estrogens in this topical HRT during intercourse which can pose harmful and unwelcome side effects.

According to the North American Menopause Society, vaginal creams such as Premarin should not be used right before sex because the partner may absorb the estrogen hormone through his skin (Journal of Reproductive Medicine, Jan. 2008).

Over time estrogen could have a feminizing effect on a man. [4]

    A few months back I received an email from a reader whose husband was inexplicably gaining weight and growing breasts. She ordered a blood spot hormone test for him, and his results showed low testosterone and high estradiol (estrogen), which certainly explained his symptoms. After a bit of digging, we figured out that she was using a vaginal estradiol cream within a few hours of when she and her husband had intercourse. In fact, she considered it a vaginal lubricant. I suggested she switch to a low dose estrogen patch, and recently heard from her that within a matter of weeks her husband had started losing the weight, and after a couple of months his breasts were back to normal and by the way, so was his sex drive.” [5]

Another word of caution for any and all estrogen-containing topical products.

    Transferring estrogen to children can have serious consequences. For boys, who again are already over-exposed to estrogenic chemicals in the environment, even small amounts of estrogen can block normal development of male characteristics and stimulate weight gain and breast growth. For girls, exposure to excess estrogen can cause early puberty and menstruation, a known risk factor for breast and ovarian cancer later in life.” [6]

And if that’s not enough, even your canine and/or feline family is affected by topical estrogens. An article in the New York Times reports the following:

    Veterinarians around the country are reporting a strange phenomenon: spayed dogs and cats, even some puppies and kittens, are suddenly becoming hormonal.

    In female pets, the symptoms resemble heat: swollen genitals, bloody discharge and behavioral problems. Male animals are showing up with swollen breast tissue and hair loss. Standard treatments and even repeated operations have had no effect.

    Now vets have identified the culprit. The pets were all owned by women who used hormone creams on their hands, arms and legs to counter symptoms of menopause. Animals who licked or cuddled their owners, or rubbed up against their legs, were being inadvertently exposed to doses of hormone drugs.” [7]

Is it really worth it to take any form of estrogen for the relief of menopausal symptoms – Premarin or others?

Other synthetics carry with them the same or similar warnings associated with their use although it has been repeatedly cited in scientific literature that estrogens derived from pregnant mares urine pose a significantly greater risk due to the conspicuous fact that equine estrogens are foreign to humans but, wait for this . . . not horses. What a concept.


First note the disparities between the concentrations of estrone and estradiol and of course the presence of the equine estrogens found exclusively in horses – clearly problematic in relation to the safety profile of these drugs.

And a closer look renders CEE-derived HRT products even more sinister:

    Premarin contains at least 10 estrogens that are the sulfate esters of the ring B saturated estrogens: estrone, 17beta-estradiol, 17alpha-estradiol, and the ring B unsaturated estrogens: equilin, 17beta-dihydroequilin, 17alpha-dihydroequilin, equilenin, 17beta-dihydroequilenin, 17alpha-dihydroequilenin, and delta-8-estrone. Bioassays and estrogen receptor binding studies indicate that all 10 estrogens are biologically active. Moreover, individual components, such as equilin sulfate, delta-8-estrone sulfate, 17beta-dihydroequilin sulfate and estrone sulfate, have potent estrogenic effects. Since all of the estrogens present in Premarin have estrogenic activity, the pharmacological effects of Premarin are a result of the sum of these individual activities.” [8]

The extract of pregnant mare’s urine is nothing less than a dangerous cocktail of alien hormones with demonstrated and lethal side-effects.
The upshot is that, unlike the horse, the female human body does not have the necessary enzymes and co-factors required to metabolize equine estrogens nor does it have the ability to deal with the significantly higher concentrations of Estrone and Estradiol contained in any of the Premarin drugs. Certainly these disproportionate and foreign hormones must create a hormonal imbalance that can have serious antagonistic consequences.

    As two leading reproductive physiologists point out, when women take Premarin, ‘Levels [of equilin] can remain elevated for 13 weeks or more post-treatment due to storage and sloe release from adipose [fat] tissue. In addition, metabolism of equilin to equilenin and 17-hydroxyequilenin may contribute to the estrogen stimulatory effect of [conjugated estrogen] therapy.’ Another metabolite of equilin, 17-dihydroequilin has been found to be eight times more potent than equilin for inducing endometrial growth, a possible precursor to cancer (3). As a result, Premarin produces “estrogenic effects” which are much more potent and longer lasting than those produced by natural human estrogens.” [9]

The bottom line – CEEs still cause cancer and a host of other illnesses. Why on earth are these archaic medications still on the market? Simply put, they shouldn’t be.

    Equilin metabolites appear to have stronger carcinogenic effects than comparable oestradiol metabolites. Oestradiol is now available in pure form, crystalline or as oestradiol valerate, and it seems more sensible to replace the oestradiol deficiency by giving the exact hormone rather than an extract of uncertain composition. Since CEE offers no advantage over physiological oestradiol, it is hard to understand why substitution with a pharmacologically poorly defined oestrogen mixture is still practised. From the point of view of clinical pharmacology, the use of an oestrogen extract should now be considered inappropriate.” [10]

Exactly, there is absolutely no longer any need for these risky equine estrogens.
[1] http://goo.gl/IVnZOd
[2] http://www.patient.co.uk/doctor/hrt-topical
[3] Same as 2.
[4] http://www.webmd.com/menopause/low-dose-vaginal-estrogen-for-dryness-and-atrophy
[5] http://www.virginiahopkinstestkits.com/hormone_transfer.html
[6] Same as 5.
[7] http://well.blogs.nytimes.com/2010/10/25/when-hormone-creams-expose-others-to-risks/?ref=science
[8] http://www.ncbi.nlm.nih.gov/pubmed/9421201
[9] http://www.smart-publications.com/articles/dont-let-your-doctor-give-you-horse-urine-for-menopause
[10] http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2014957/#b4

Read Part 1 » • Read Part 3 »

© The Horse Fund

• Learn more about the horses, the drugs and women at Premstoppers »

ATTENTION! If you see an ad for any Premarin product including Duavee, please contact us and tell us what network, the channel you saw it on, the city and what it was for. Thanks.

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