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INFORMATION FOR TRANSSEXUALS
SUGGESTED HORMONE REGIMES FOR M2F GENDER RE-ASSIGNMENT

FOR 10 YEARS NPD HAS BEEN A LEADING SUPPLIER OF TRANSGENDER HORMONES
ON THIS PAGE ARE THE MOST POPULAR MEDICATIONS USED IN GENDER REASSIGNMENT
.... AND YOU CAN BUY THEM RIGHT NOW WITHOUT PRESCRIPTION

Warning: Never take hormones unless you have consulted a medical specialist or gender reassignment clinic and are fully aware of the possible risks and side effects. Do not smoke whilst taking hormones. Serious risks can include venous thromboembolism (VTE), i.e. deep venous thrombosis (DVT deep vein thrombosis), pulmonary embolism and cardiac problems.

For the full range of hormone related products that we have available (including birth control pills and HRT drugs) and also including those drugs which are mentioned on this page please visit our hormone section. You should note that these medications listed are the real thing and are NOT phyto or herbally based estrogens as supplied on some transgender related websites under the banner of sex change drugs.

For more detailed information on each drug please click on any of the medication names below to go to the specific medication page. If a drug is not listed use our site search on our medications index page. For complete comprehensive information on transsexualism, transgender resources, links and gender re-assignment see www.crissywild.com the leading transgender library online.

The following information should be used as a general guide

Estrogen is the most important part of any feminizing regime ..

A gender reassignment program for male to female transsexuals normally includes the prescription of feminising hormones, oestrogen and progesterone which develop female secondary sexual characteristics. In addition this may be accompanied before surgery by anti-androgen treatment to reduce the effect of the patients own male sex hormones. 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.

Estrogens are powerful steroid hormones, chemicals which affect the form and function of the body and its organs. In M2F transsexuals the effects of these hormones will become obvious after three months and usually irreversable after six to nine months.

There are three basic human estrogens: estradiol, estrone, and estrial. Estradiol is the most active form and estrial is the least active. In women, large amounts of estrogen are produced by the ovaries, and in men a small amount is present due to chemical conversion of testosterone.

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, Zumenon 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 and favoured by many gender reassignment clinics)
OTHER OPTIONS ..
(Diane-35® is also used as it contains a small amount of the anti-androgen, cyproterone and inhibits facial hair growth)
(Ovral/ Ovran is also used as it contains a small amount of progesterone)

OR

Transdermal estrogen:

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

OR

Injectable (intramuscular) estrogen:

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

estreva gel 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:

Note: For pre-operative transsexuals taking estrogen alone will not be properly effective without anti androgens as the natural male body hormones will counter the effects of the estrogen..

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.


Combination Medications:

Diane-35® (cyproterone acetate/ ethinyl estradiol)


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 (venous thromboembolism (VTE), i.e. deep venous thrombosis or pulmonary embolism), 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, bleeding between menstrual periods, 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 recurrent abnormal vaginal bleeding, a missed menstrual period, 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.

Estrogens are powerful steroid hormones, chemicals which affect the form and function of the body and its organs. In M2F transsexuals the effects of these hormones will become obvious after three months and usually irreversable after six to nine months.

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

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