HORMONE
INFORMATION FOR TRANSSEXUALS AND TRANSGENDERED
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SUGGESTED REGIMES FOR M2F GENDER RE-ASSIGNMENT
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:
ethinyl
estradiol (Estinyl®), Lynoral),
100 mcg (0.1 mg) daily; (ethinyl estradiol is pure synthetic
estradiol)
(Diane
35is 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)
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, 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
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:
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
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.
Oral
estrogens:
estreva
gel, 
