What is the difference between natural progesterone in capsules to be taken orally and the transdermal cream?

Approximately 90% of all hormone replacement therapy prescribed in the United States is an oral medication. There are, however, alternative routes available that bypass the stomach and possible related side effects.

Hormones taken orally in pill form enter the bloodstream from the small intestine, and go directly to the liver. Because the liver is not accustomed to receiving large amounts of hormones, it begins to break them down, leaving only a small percentage of the ingested hormone available to cells.

This is called first pass loss (or first-pass metabolism) through the liver.

By comparison, transdermally delivered hormones such as progesterone are up to 80% more bioavailable than equivalent doses administered orally. This has been proven by salivary hormone testing. In other words, oral delivery systems provide only a fraction of biological activity in comparison to the same dosage of steroid hormones administered from a transdermal delivery system (TDS).

In practical terms, an oral dose of 100 mg progesterone might be equivalent to 20 mg progesterone cream delivered transdermally.

Don’t confuse oral (swallowing a pill) with lozenges (sometimes called by the French name of troches) dissolved between the teeth and the cheek that, like cream, will bypass the liver.

The effective transdermal application of steroidal hormones like progesterone, testosterone or estrogen is possible because these prerequisites are all met:

• These steroidal hormones are small, fat-soluble molecules that are easily absorbed across the skin where they can be stored in the fat tissues.
• The hormones can reach a saturation level that is sufficiently high so that the fatty tissue diffuses them into the capillaries for uptake by the general blood circulation and transports them to the target tissues.
• During the transdermal delivery process, the skin does not inactivate these steroid hormones, nor does it produce harmful metabolites from them.

From a purely economic viewpoint, you don’t need to use as much progesterone when you use the transdermal form. It could be said, oral delivery is less cost effective.

Natural hormones in forms that are absorbed directly into the blood circulation before they get to the liver include hormone creams, lozenges and patches, however creams give more flexibility because they can be tailor-made to suit the individual, and can be compounded to include any variety of natural hormones such as the three different types of natural estrogen (estradiol, estrone and estriol), natural progesterone, testosterone and DHEA.

The hormonal lozenges are placed between the upper gum and the cheek, and left to slowly dissolve into the small blood vessels under the surface of the mucous membrane of the cheek. They must not be chewed, sucked or swallowed, otherwise they will end up in the intestines and pass straight through the liver. The doses used in the lozenges are generally higher than those used in the creams. And, like creams, lozenges can be tailor-made to suit the individual, using any possible combination, and amounts of natural hormones such as estradiol, progesterone, testosterone and DHEA.

Let’s pause a moment to consider the liver. A variety of medications can cause organ damage, and anyone who has a history of liver disease should check carefully with their doctor before starting new medications. Steroid-based medications can result in hepatitis-like side effects, as can oral contraceptives, antibiotics, analgesics, and any medication designed to alter liver function.

Many women with a fatty / dysfunctional liver often cannot cope with potent doses of oral hormone replacement therapy as it overloads the workload of the liver. And this can actually aggravate weight problems and obesity. These ladies usually do quite well with natural progesterone transdermal cream.

We know that bioidential hormones such as progesterone, estrogen and testosterone cannot be patented. However, pharmaceutical companies tip-toe around this barrier by patenting their unique delivery system. Many women are probably already familiar with estradiol patch therapy developed around transdermal delivery. Vivelle-Dot transdermal estradiol patch, for example, use the patented DOT Matrix? technology. ?DOT? stands for ?Delivery Optimized Thermodynamics. We also have Ortho Evra, a combination birth control patch containing bioidentical estradiol & artificial progestin, also based on TDS and targeting the Contraception market.

The Trimegestone patch, still in research & development stage, contains a combination of estradiol and potent progestin which, according to the company, “promises a product with a safety margin exceeding currently available products.” The 1995 PEPI trials clearly demonstrated that natural progesterone actually works better than synthetic progestin in terms of protecting the heart, and that natural progesterone can protect against uterine cancer as well as synthetic progestin. Yet drug companies continue to convince us otherwise!

Transdermal patches containing bioidentical progesterone cannot be used in the treatment of infertility as the volume of progesterone that needs to be delivered renders this method prohibitive. However, drug companies have developed a patented bioadhesive 4% and 8% vaginal gel containing micronized progesterone in an emulsion system, which is contained in single use, one piece polyethylene vaginal applicators.

There are many premium progesterone creams containing micronized progesterone USP on the market today priced at between US$20~$25 which can deliver up to approximately 10% (100mg) progesterone per application and last up to 3 months per jar.

Interesting indeed that the makers of Crinone? state in the their Patient Leaflet that there have been no reports of overdosage. That’s precisely what we’ve been singing from the roof tops for years … bioidentical progesterone supplementation delivered transdermally has a significant safety margin and carries none of the side effects or health risks of synthetic progestins.

We’ll leave the final word on this subject to Dr Martha Howard: “oral pharmaceuticals can be harmful to the liver and gall bladder. Oral administration is outmoded. Plant-derived creams fit better in the body’s receptors. I prefer transdermal delivery systems - it’s safer and more natural.”