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Estrogen is the most important part of any feminizing regime.

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

Oral estrogens:

estradiol (Estrace®, Estrofem, Progynova), 6 mg daily; OR

conjugated equine estrogen (Premarin®), 5 mg daily; OR

ethinyl estradiol (Estinyl®), Lynoral), 100 mcg (0.1 mg) daily; (ethinyl estradiol is pure synthetic estradiol)

(Diane 35 is also used as it contains a small amount of the anti-androgen, cyproterone)
(Ovral/ Ovran is also used as it contains a small amount of progesterone)


Transdermal estrogen:

estradiol (e.g., Climara®, Estraderm or equiv), two 0.1 mg patches, applied simultaneously;


Injectable (intramuscular) estrogen:

estradiol valerate (Delestrogen®), 20 mg IM every two weeks.

estreva gel, premarin cream and hormodose gel (used in addition to other regimes)

Occasionally half the suggested dosage may be sufficient; sometimes the dosage will need to be increased, rarely even doubled. Beyond a certain point, larger dosages will not increase tissue response, but will only cause more side effects.

Oral estrogens are most commonly used, and are typically very satisfactory. Among the oral preparations, estradiol is preferred. It has low hepatic toxicity. Most clinical laboratories can perform estradiol blood levels; it is more difficult to obtain meaningful measurements of blood levels with conjugated equine estrogen or with ethinyl estradiol. Estradiol is also produced synthetically, without cruelty to animals; this is not the case with conjugated equine estrogen (Premarin®), which is prepared from the urine of pregnant mares.

Estradiol tablets can be taken sublingually (placed under the tongue to dissolve) instead of being swallowed. This may reduce possible liver toxicity, since with sublingual administration, much of the medication is absorbed directly into the blood stream, rather than being metabolized by the liver after first passing through the digestive tract. Less metabolism is also likely to result in higher levels of estradiol itself, and lower levels of its less-active metabolites, estrone and estriol. Micronized estradiol tablets are specifically designed for either oral or sublingual use, and dissolve quickly under the tongue without an unpleasant taste.

Premarin® is the more expensive oral preparation. One of its advantages is its relative potency, which is notably higher than estradiol on a milligram-per-milligram basis. This is because some of the equine estrogens in Premarin, especially equilin, have higher biologic potency than the estrogens normally found in humans. Ethinyl estradiol is a chemically-modified form of natural estradiol; the ethinyl substitution results in a longer duration of action, and greatly increased potency.

Transdermal estrogen causes less clotting tendency than oral estrogen, possibly important to some patients; but transdermal preparations are more expensive, and skin reactions to the adhesives employed are not uncommon. Injectable estrogen also causes less clotting tendency, and is less expensive. Its major drawbacks are the need to employ syringes and perform injections, and the somewhat greater tendency of injectable estrogen to increase serum prolactin levels. If the former is not a problem, and if the latter can be checked regularly, injectable estrogen can be a very good way to go; a good suggestion is Gestadinone injectable estradiol valerate.

If you have access to laboratory testing, a serum estradiol level of about 150 - 200 pg/ml -- about one-third to one-half the normal female mid-cycle peak -- is often considered ideal, at least for the first two years or so of feminizing therapy.  Taking 81 mg of aspirin daily is a good precaution for persons taking oral estrogens, assuming no contraindication to aspirin exists. It is not necessary or desirable to "cycle" estrogen, or any other medication, in an attempt to mimic the normal female menstrual cycle.

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

In persons who have not had an orchiectomy, testosterone levels are also a concern. Although the desired reduction in testosterone can theoretically be accomplished with estrogens alone, the dosage required is usually in excess of what is needed for feminization. Adding an anti-androgen allows lower dosages of estrogen to be used; this is usually highly desirable. Typical dosages of anti-androgens are as follows:

Oral anti-androgens (Male Hormone Inhibitors):

(Without using an anti-androgen, hormones are compromised as to their effectiveness)

spironolactone (Aldactone®), 100 - 300 mg daily in divided doses; OR

cyproterone acetate (Androcur®), 100 - 150 mg daily.

Sometimes 100 mg of spironolactone may be sufficient, but 200 mg is a more typical dose. The Vancouver group uses up to 600 mg daily, apparently without problems. Spironolactone is fairly inexpensive and is usually quite well tolerated. Cyproterone is not available in the US, but is very popular elsewhere. If you have access to laboratory testing, a serum testosterone level of about 5 - 85 ng/dl -- the normal female range -- is usually considered ideal. Within this range, lower numbers are not necessarily better.

Progestogens (progesterone and synthetics) are sometimes added to a hormone regimen. These are optional.

Progestogens are usually given in an attempt to improve breast development. Based on limited anecdotal evidence improved breast development sometimes does occur, but it is usually not very significant. Progestogens can also inhibit testosterone, and are sometimes used for this purpose. Medroxyprogesterone, the most commonly used product, has the disadvantage of counteracting some of the beneficial effects of estrogen on blood lipids; some people also find that it causes mental irritability. Micronized ("natural") progesterone is an alternative, but it is more expensive, and sometimes hard to find without prescription. Progestogens are optional, and usually unnecessary. If you decide to take them, here are some typical dosages:

Oral progestogens:

medroxyprogesterone (Provera®), 5 -10 mg daily; OR

micronized progesterone (Prometrium®, Microgest), 100 mg twice daily; OR

Injectable (intramuscular) progestogen:

medroxyprogesterone (Depo-Provera®), 50 mg every two weeks; OR

progesterone in oil, 50 mg every two weeks.

After orchiectomy (castration) or SRS, dosages can be reduced:

Following orchiectomy or SRS, anti-androgens can be discontinued, and the estrogen dosage can usually be decreased to one-half or one-quarter of the pre-op dosage, i.e.:

Oral estrogens:

estradiol (Estrace®), 1 - 2 mg daily; OR

conjugated equine estrogen (Premarin®), 1.25 - 2.5 mg daily; OR

ethinyl estradiol (Estinyl®), 20 - 50 mcg (0.02 - 0.05 mg) daily.

Cautions with Hormones / HRT
Smoking cigarettes or high alcohol input while using these medicines may increase your risk of stroke, heart attack, blood clots ( deep vein thrombosis, DVT ), high blood pressure, or other diseases of the heart and blood vessels. If you have vomiting or diarrhea for any reason, your medicine may not work as well. Taking certain antibiotics or anticonvulsants while you are using this medicine may decrease the effectiveness of this medicine. For gender changes MtF recommended regimes are listed above.

Possible Side Effects of HRT
Side effects can include nausea, vomiting, breast tenderness, changes of skin and hair texture, increased breast size or weight change. If they continue or are bothersome, check with your doctor. Check with your doctor as soon as possible if you experience persistent or recurren dizziness or fainting, swelling of fingers or ankles, headache, or difficulty wearing contact lenses. Contact your doctor immediately if you experience sharp or crushing chest pain, sudden shortness of breath, sudden severe headache or leg pain, yellow skin or eyes, changes in vision, numbness of an arm or leg, or severe stomach pain. If you notice other effects not listed above, contact your doctor, nurse, or pharmacist.

Use of this medicine will not prevent the spread of sexually transmitted diseases (STDs).

Warning: Never take hormones unless you have consulted a medical specialist or gender identity clinic and are fully aware of the risks and possible side effects. Do not smoke whilst taking hormones as this will increase the risk of (DVT) deep vein thrombosis.