Taking HRT orally.

The majority of women take their HRT in pill form by mouth (oral HRT). While very convenient, this results in changes in the metabolism of estrogen that can be harmful. The reason for this is called the "first pass effect." When any substance is ingested orally, it is absorbed by the small intestines and then the whole dose hits the liver immediately. This does not mimic what occurs naturally when the ovaries are releasing estrogen into the circulation gradually all day and then it gradually hits the liver.

When a large amount of estrogen hits the liver at once, the processing of the estrogen changes the metabolism of the liver and results in a number of deleterious effects:

1. There is an increase in clotting factors, hence the warnings on the box that women who smoke and older women may have an increase in blood clots in the veins of the legs that can then cause a potentially fatal pulmonary embolism.

2. There is an increase in the carrier molecule of the sex hormones called 'sex hormone binding globulin (SHBG),' which can result in too tight binding of testosterone, human growth hormone and thyroid hormones thus producing a completely new series of symptoms -for example SHBG has a tremendous high affinity for free testosterone thus you will see signs of testosterone deficiency-decreased libido, vaginal dryness, thinner bones, and sagging skin. This side effect is commonly used to treat acne in females by placing them on birth control pills, which greatly increase sex hormone binding globulin produced by the liver. The increased SHBG binds with free testosterone decreasing the amount bio-available testosterone thus improving acne. A very round about way through hormonal manipulation to treat acne I would say.

3. The metabolism of fats and protein is changed which results in the loss of lean muscle and increase in fat. These often counter balance each other to cause no change in weight, but an undesirable body composition.

4. When a woman drinks the equivalent of even just one glass of wine or other alcohol a day and takes estrogen orally, her level of estrogen can increase 300% above when she is not drinking. This can cause levels of estrogen that are higher than are ever experienced in a normal menstrual cycle. This may be one of the causes of an increased risk of breast cancer with oral HRT. In contrast, transdermal estrogen results in only a 30% increase in estrogen level with alcohol consumption.

5. An increase in the incidence of gallstones which can lead to the need for gall bladder removal. 6. An increase in triglycerides, a form of cholesterol that is a known risk factor for increased heart disease.

Transdermal (topical patches and creams)

None of these "side effects" occur with transdermal ERT because the daily dose is released gradually into the general circulation as occurs when the ovaries are functioning naturally. So why aren't all women taking their ERT transdermally? We believe that there are three major reasons why they are not:

1. Historically: transdermal therapy has not been available nearly as long as oral therapy, and once a pill-a-day therapy takes hold, it is hard to change the preferences of both physicians and women. To date almost all research which comes from the deep-pocketed pharmaceutical industry has been done on oral once a day pills

2. Oral ERT raises HDL (the good cholesterol) higher than transdermal ERT. This argument is often the sole reason put forth by gynecologists and internists when asked why they persist in prescribing oral ERT in the face of the six reasons against it listed above. The reasoning here is flawed in most cases. While it is true that HDL is raised considerably more with oral therapy, the majority of women have an HDL in a very good range even off ERT so raising them from 60 to 80 mg/dl does not confer enough benefit to outweigh the above negatives. Moreover, it has been shown that only about 30 to 40 percent of the heart disease reduction benefit of ERT comes from the changes in the cholesterol profile, which further mitigates the marginal benefit of raising HDL in a woman with a good baseline level. This is not to say that in some cases, e.g., when a woman's HDL is less than 30, oral therapy on balance is preferable, but certainly not in the majority of cases.

3. Convenience: most women don't want to wear a patch. Many develop an allergy or contact dermatitis to the adhesive tape. This problem is solved with transdermal creams and gels that exhibit excellent absorption and provide steady estrogen levels. The only problem is that at least in the United States, the pharmaceutical companies have not wanted to market these forms of ERT. This is understandable given that Premarin is the most prescribed medication in the country.

4. Contraindications: Only transdermal estrogen therapy is indicated in certain medical conditions that precludes oral estrogens, this includes hypertriglyceridemia, non-response to oral estrogens, oral estrogen-induced hypertension, and high-risk cholelithiasis patients

Sublingual

Lastly I will mention another type of delivery systems, which most individuals are not familiar with Sublingual drops or troches. This method works by placing either a few drops or a small easily absorbable pill under the tongue where it will be absorbed in seconds. The advantage of this delivery is that it too bypasses the first-pass effect on the liver similar to the transdermals . What differs between the use of transdermals versus sublingual is the pharmokinetics (how rapidly and in what concentration and how long a drug will appear at its target organ). Sublinguals take effect much more rapidly within minutes effects can be felt. In contrast transdermals are slowly absorbed and remain in the blood stream longer. It is the difference between these two that can be use to help patients with differing symptoms. For example in a patient whom has occasional migraine headaches associated with a drop in estrogen levels prior to her menses I would use sublingual estrogen drops. Just a few drops under the tongue and headache symptoms resolve in five or so minutes. Another example would be a patient whom is perimenopausal and only gets hot flash every once in a while but is otherwise fine. Taking just a few sublingual drops every now and then might be all that she needs.

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