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Converting a patient from Oral to TopicalHormones



One of the most difficult types of patients to balance on bioidentical

hormones is the patient that has been on conventional hormone

replacement therapies for a number of years. Conventional oral estrogen replacement therapy provides too much estrogen. A dose of 0.625mg of conjugated Equine Estrogen (CEE or Premarin) or 0.5mg of oral estradiol is an excessive estrogen amount for most women. The majority of estradiol taken orally is converted by the first pass effect to estrone; the estrone levels in these patients will be excessively higher than normal, creating an estrogen burden. The problem is worse with CEE or Premarin because they contain 50% estrone and 15-20% equilin and very little estradiol. Converting a patient on conventional hormone replacement to bioidentical therapy too quickly can result in severe symptoms. These patients realize the high dose they have been on is not serving them well and desire to lower the dose. It is only lately that we have come to understand how difficult that transition can be for some women. The best approach is to

taper down the estrogen dose over time before switching to a bi-est (estradiol and estriol) preparation. Switching to bioidentical estrogens before tapering the previous dose will usually result in severe symptoms such as hot flashes.


Why are there problems tapering off high estrogen dosing? Because over

time we see:

  • Increased threshold for estrogen need in the brain

  • Down regulation of number of estrogen receptors

  • Loss in sensitivity of estrogen receptors

  1. Some doctors recommend a liver detox to help the liver detox from the estrogen burden it has been under. At Tahlequah Drug’s Compounding Lab we stock Detoxication Factors by Integrative Therapeutics.

  2. Discontinue any synthetic progestin immediately and initiate natural progesterone. Adding progesterone at the onset may help with estrogen withdrawal symptoms. Plus, it may take several days to a few weeks for progesterone to take full effect. At Tahlequah Drug’s Compounding Lab we sell Progesterone Cream (available without a prescription).

  3. Titrate your current estrogen dose down. In converting patients let the patient determine how quickly she is able to decrease the dose. Patients that have been on excessive estrogen for many years may have permanently desensitized the receptors to some degree. Some practitioners will switch the patient from an oral estrogen to the lowest available dose of an estradiol patch because it provides a more constant estradiol level.


A typical reduction protocol would be to provide half strength and full-strength tablets of the estrogen the patient is already taking. Let’s say the patient in on estradiol 2mg:

Take 2 mg for two days and on the third day take 1mg. Do that for 9 to 12 days. Then take 2mg for one day and 1mg for two days. Do that for 9 to 12 days. Then take 1mg for 9 to 12 days. Then decrease to 1mg for two days out of 3 days. Do that for 9 to 12 days. Finally take 1 mg every other day for 9 to 12 days.


Taken from Jim Paoletti’s book “A Practitioner’s Guide to Physiologic Bioidentical Hormone Balance”. Dr. Pamela Smith says: When converting a patient from oral estrogen to transdermal estrogen expect hot flashes and/or headaches. Cut the oral dose in half before you start the transdermal.

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