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Feminization Regimen

A gender reassignment program for male to female transsexuals normally includes reducing androgen effects with spironolactone (cyproterone has been used in European countries) and stimulating feminization of secondary sex characteristics with estrogen.

There can be risks attached to hormone therapy in both men and women and therefore it is definitely inadvisable to take any form of hormone product unless it is medically prescribed.

The use of progesterone to augment breast development is controversial in physicians treating MTF transsexuals. When deciding on a hormone regimen, prescribers should remember that it is estrogen that causes the serious side effects, so the lowest effective dose should be used.

The manufacturers of oestrogen and progesterone products specify them for medical use in females and do not acknowledge their use for transsexuals, so there is little clinical data available regarding this usage.


Estrogen dosing regimens for gender transition vary widely. Estrogen should be prescribed at the lowest possible effective doses to avoid the serious complications of high-dose estrogen therapy.

Current recommendations for estrogen dosing range from starting doses of 0.625 to 2.5 mg of conjugated estrogen.

Estrogen is the most important part of any feminizing regimen.

Some typically-used estrogen dosages for pre-operative transsexual women who have not had an orchiectomy (castration) are as follows:

Oral Estrogens

Conjugated estrogens such as Premarin® 5 mg daily.
Estradiol such as Progynova (Oestradiol Valerate) or Estrofem 4 mg daily.

Injectable Estrogen

Progynon Depot is an alternative form of Oestradiol Valerate and comes in an injectable form.

Transdermal Estrogen

Estradiol 0.1 mg patch, changed twice weekly. Transdermal patches uniformly contain estradiol as the active medication, produced in 0.05mg (50 mcg), 0.075mg (75 mcg) and 0.1 mg (100 mcg) concentrations, and are branded under a variety of names such as Estradot / Vivelle, Climara and Estraderm.

Transdermal estrogen causes less clotting tendency than oral estrogen, possibly important to some patients; but this is a very expensive product.

Estrogen Gels

If you do not wish to use estradiol patches, an option is estradiol gel applied daily to the skin. The gel is usually alcohol based and is absorbed through the skin. The medication imparted into the skin usually takes about 12 hours for absorption into the blood stream, which produces a similar continuous action like the patch. Gels have the advantage as the wearer is not burdened with wearing a patch and the potential irritation from the adhesive that holds the patch in place.

Gels roughly corresponds to the daily doses found in the 50 mcg and 100 mcg patches.

Sandrena is an Estradiol Gel which comes in 1 gram sachets.

Estrodose Gel is the same as Estrogel. It is a clear, odorless, hydro-alcoholic gel that provides for delivery of estradiol for estrogen replacement in a non-patch transdermal form.

Other Forms of Estrogen

InhousePharmacy.biz is able to provide three other forms of Estrogen these are Premarin Cream which is a conjugated Estrogen Cream and Ovestin which is a low dose Estriol Cream.

Aerodiol - Aerodiol nasal spray containing estradiol hemihydrate 150µg per spray has been launched by Servier Laboratories The product is licensed for replacement therapy for oestrogen deficiency symptoms in postmenopausal women.

Serious health risks of estrogen therapy include stroke, pulmonary embolism, myocardial infarction, and breast cancer.

Combination estrogen and progesterone

InhousePharmacy.biz is able to supply Kliogest and Kliovance / Activelle, a combination of oestradiol and norethisterone and is used to produce female hormones estrogen and progesterone.


Besides providing estrogen, a hormone regimen should also reduce testosterone to normal female levels. This usually requires adding an anti-androgen.

Spironolactone acts as an antiandrogen of testosterone to dihydrotestosterone. Spironolactone in doses of 200–400 mg per day allows the practitioner to decrease exogenous estrogen doses tophysiologic or “hormone replacement” levels while still obtaining desired effects of breast development, feminization of skin, and female fat distribution.

Spironolactone can usually be discontinued after sex reassignment surgery.

Androcur (Cyproterone acetate) is a powerful antiandrogen and progestagen used in Europe for transgendered patients. Its use is limited by interference with corticosteroid production, high cost, and side effect profile.

Cyproterone is a generic form of Androcur. It performs is exactly same way as Androcur but at a cheaper cost.

Finasteride is an antiandrogen that opposes the formation of DHT, but not of testosterone itself. Finasteride is present in Proscar in a 5mg dosage and in Propecia in a 1mg doasge.

Dutasteride is also an antiandrogen that opposes the formation of DHT, but not of testosterone itself.

There are several other antiandrogens which are used for other indications but have no reported data in the transgendered patient. Flutamide and Bicalutamide are nonsteroidal antiandrogens normally used in the management of Management of Prostate Cancer.


Progesterone is the third and optional component of the MTF regimen.

Medroxyprogesterone is available as Provera and Depo-Provera. Medroxyprogesterone is a weak antiandrogen, and testosterone suppression may be accomplished with lower doses of estrogen. Medroxyprogesterone is less androgenic than norethindrone and orgestrel.

Micronized Progesterone is advantageous because it has a more favorable side effect profile (anxiety and irritability) than medroxyprogesterone. It is also less androgenic when higher progesterone doses are needed, but is more costly. Micronized progesterone is available as Prometrium or in a generic form as Microgest.

Duphaston (Dydrogesterone) may be used as an alternative to medroxyprogesterone acetate. It is not metabolised into testosterone within the body, and is therefore free of the virilising effects which some patients experience ftom other progesterones. A typical pre-op (or early post-op) dose would be 20mg in two doses, reducing to a single dose of 10mg daily post-op.

Crinone is another medication available and contains the female hormone progesterone.

Cyproterone plus Estrogen
While Androcur is available in 50 mg tablets, sometimes Diane-35 is used when small doses are desired. Diane-35 is a contraceptive with anti-acne properties (due to the cyproterone contained), and is comprised of 2 mg of cyproterone acetate and 0.035 mg ethinyl estradiol. Diane-35 generics are available.

InhousePharmacy.biz can supply Diane 35 which is comprised of 2 mg of cyproterone acetate and 0.035 mg ethinyl estradiol.

A generic form of Diane 35 is also available, this is manufactured by Cipla and is known as Ginette 35.

Climen is also a combination of an Estrogen with Cyproterone. Climen is normally used in Hormone Replacement Therapy Calendar-pack containing 11 tablets of 2 mg estradiol-17-valerate each, plus 10 tablets of 2 mg estradiol-17-valerate and 1 mg cyproterone acetate each. Brandnames in other countries - Climene, Climen/Clisin.

Facial Hair Reduction

Eflora / Vaniqa Cream is used for the reduction of unwanted facial hair. Eflora / Vaniqa Cream does not remove hair, it slows the regrowth.

Transdermal Testosterone

Instrina Transdermal Patches provides a measured daily dose of testosterone via a discreetly placed patch on your body.


Anastrozole is a non-steroidal aromatase inhibitor that decreases the amount of estrogen the body makes.

Arimidex contains the active ingredient anastrozole to decrease the body's production of estrogen.

InhousePharmacy.biz are unable to provide advice on treatment regimes. However the following sites may be of some assistance.

Transsexual Women's Resources
TransGenderCare - An educational offering of the Tampa Gender Identity Program. Has useful features on hormones and medical care.


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