Hormones for feminization
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Abstract

This document contains a list of frequently asked questions and their answers regarding hormone therapy (secondary sexual reassignment) for male-to-female transsexuals. More generally, this document contains information about gonadal hormones and anti-hormones, so it can be a helpful reference for the treatment of androgen and estrogen-sensitive conditions–for example, certain cancers of the reproductive organs and breasts.

Please send additions, corrections, and suggestions to the Staff.

Disclaimer

The answers in this document are collected from a variety of sources: medical literature, pharmaceutical company advertizement, verbal advice of medical doctors, second-hand anecdotes, and personal experience. Despite the authoritative tone of this document, it is presented for educational interest only, not direct advice. It contains opinions, sweeping generalizations, and at least one mistake. The author is not a medical doctor, and makes no claim or warranty as to the suitability of the information in this document for application to any particular individual. YOU, the reader, take sole responsibility for interpretation and application of this information. Form your own opinions by doing your own research. May your favorite deity permanently curse you if you seriously consider sueing the author for misinforming you.

The endocrine feedback system is intricate, delicate, and poorly understood. Even the experts do not entirely agree on how to best meddle with it. Hormone therapy is fraught with risk as well as promise. Be sure you have fully considered the implications before you start. Work with a medical doctor who is qualified to interpret your signs, symptoms, blood tests, and development in the context of your personal medical history. Do not take hormones that you did not obtain directly from a licensed pharmaceutical distributor; the quality of drugs obtained through other channels is not only suspect, but possibly dangerous–especially those in injectable form.

Notes

  • The words “female” and “male” refer to the original physical form, not to gender identification.
  • This document does not address hormone therapy of the individual with an endocrine system disorder.
  • Prices are listed in wholesale U.S. dollars. The retail markup varies widely. A very limited survey by the author returned answers from pharmacists of as little as 8% plus a fixed $7.25 fee all the way to 100%, with the average markup being about 40% and the median being about 60%. The retail markup percentage is usually higher for brand names than generics.
  • Pre-op hormone dosages are determined mainly from verbal advice of medical doctors, second-hand anecdotes, and personal experience.
  • Post-op hormone dosages are determined mainly from the Physician’s Desk Reference (PDR) according to the recommendation of hormone replacement of normal gonadal hormone production.
  • Drugs are ranked by three criteria:
  1. Safety and efficacy: excellent, good, fair, unknown, or poor. This is based on normal indications (i.e., when the primary indication is female hormone replacement, it is suitable for transsexual hormone therapy), delivery method (sustained-release injectibles and transdermal films are easier on the liver than oral tablets), literature, medical doctor advice, anecdotes, and other factors noted in the individual hormone comment field. Safety and efficacy are generally closely linked, so the ranking is combined for all drugs except anti-androgens.
  2. Source: unknown, animal by-products, or live animals
  3. Wholesale price per day of treatment at nominal pre-op dosage using the most economical delivery method. This is no guarantee that the most economical delivery is available at any given time from the pharmaceutical suppliers.
  • Of the injectable hormones and anti-hormones available, only those that are sustained-release (requiring injection less frequently than once per week) are listed.
  • The adverse effects listed in this document are gleaned primarily from drug information sheets and the PDR. They are translated from medibabble into English where possible. While this information should not be taken lightly, it should be viewed with slight suspicion, since it is first and foremost advertizement and legal copy from pharmaceutical companies. To attempt to reduce their exposure to lawsuits, they list not only the effects reasonably shown to be caused by the drug during clinical trial(s), but also every other adverse effect that the patients experienced while taking the drug–or any other drug of the same class–whether or not the effect was proven statistically relevant by controlled study for the drug in question. In particular, the reader should not be unduly worried about the mention of increase of body hair and loss of scalp hair from estrogens, nor about increase of body hair and deepening of voice from androgen receptor antagonists and GnRH agonists. Finally, adverse effects are only listed here if they make sense in their application to transsexuals, i.e., adverse effects on uniquely female organs are not listed for drugs intended for male-to-female transsexuals, and vice-versa. One should really read the PDR for the drugs of interest in order to provide context for the adverse effects listed in this document.

Questions Answered in This Document

What are hormones, and how do they work?
What are normal endogenous androgen and estrogen levels?
What effect does female hormone therapy have on a male, and how soon?
What are the popular treatment philosophies?
How are hormones delivered?
How can the intended effects of hormone therapy be maximized and the dangers minimized?
How can one obtain hormones?
Are birth-control pills a good source of estrogen?
How can lactation be induced?
How can a male be neutered without causing feminization?
Exactly what hormones are available? What are the details on popularity, dosage, availability, price, contraindications, adverse effects, etc.?
Where is there more information about hormones?

What are hormones, and how do they work?

Hormones are long-range chemical messengers of the body, manufactured and controlled by the endocrine system. Hence the title of endocrinologist for hormone doctors.

The hypothalamus produces gonadotropin-releasing hormone (GnRH). This signals the anterior pituitary gland to synthesize and release luteinizing hormone (LH). To a lesser degree, GnRH also triggers the synthesis and release of follicle stimulating hormone (FSH). Subsequently, LH and FSH signal the gonads (ovaries in females, testes in males) to synthesize and release hormones that cause differentiation of the body tissue into female or male form: estrogens, progesterones, and testosterones. A small quantity of testosterones are also produced by the adrenal gland. Proportionally, females have more estrogens and progesterones than males; males have more testosterones.

Estrogens include natural and synthetic estradiols, estrones and estriols. They excite estrogenic receptors, causing the body to differentiate into female form and function. Natural and synthetic estrogens are hereafter referred to simply as estrogens.

Progestogens (or progestins) are synthetic progesterone analogues. Progesterones and progestogens excite progesteronic receptors, which in cooperation with estrogenic activity, cause the body to further differentiate into female form and function. Natural and synthetic progesterones are hereafter referred to simply as progesterones.

Various testosterones are collectively known as androgens. They excite androgenic receptors, causing the body to differentiate into male form and function. Natural and synthetic testosterones are hereafter referred to simply as androgens.

Anti-hormones can be useful in transsexual hormone therapy because they block hormone action or production. The basic mechanisms are:

  • Androgen receptor antagonist: blocks the action of androgens at certain receptor sites.
  • Androgen conversion inhibitor: blocks the conversion of one type of androgen to another.
  • GnRH agonist: Briefly overstimulates then effectively suppresses pituitary LH and FSH production.

Aggressive exogenous hormone therapy indirectly reduces endogenous (natural) gonadal hormone production by fooling the pituitary into thinking that there are plenty of hormones already in the body; consequently, the pituitary reduces the LH and FSH signals that stimulate the gonads.

Postnatally administered hormones do not cause development of are opposite those born with. However, postnatal contrasexual hormone therapy does cause development of secondary sex characteristics as described below.

What are normal endogenous androgen and estrogen levels?

The normal endogenous androgen range in a male is 300-1100 nanograms per deciliter. Estrogen is generally below 50 picograms per milliliter.

The normal endogenous androgen range in a female is 10-100 nanograms per deciliter. (within this range lower numbers are not necessarily considered better; remember, free-circulating androgens cannot bind to receptors very well, and therefore cannot cause much harm, if an androgen blocker is being used).

There are dramatic cyclic and individual variations of estrogen (estradiol + estrone) in females, with 100-400 picograms per milliliter being the most usual, with 25-700 being possible depending on the individual. 400 is considered a nominal “mid-peak” (ovulation) level. 200-250 is considered a reasonable target for exogenous estrogen treatment. Note that only natural estrogens can be meaningfully measured, so it you take any estrogen besides estradiol valerate, estradiol cypionate, or estradiol, you will not be able to accurately judge the results of a blood test.

What effect does female hormone therapy have on a male, and how soon?

The longer after puberty hormone therapy is started, the less effective it is–but not a linear scale, e.g., results are considerably more dramatic in an 18 year old than a 28 year old, but results are not on the average dramatically different between a 38 year old and a 48 year old.

The following effects have been observed in varying degrees–anywhere from little to moderate–with extended treatment. With effective and continuous dosages, most of the changes that a particular body is genetically prone to start within 2 to 4 months, start becoming irreversible within 6 to 12 months, start leveling off somewhat within 2 years, and be mostly done within 5 years. The leveling may take longer if the testes are not removed. High levels of estrogen will cause faster development up to a point, but not better results in the long term than moderate levels of estrogen.

  • Fertility decreases. Sperm count drops rapidly. Sometimes it returns to almost normal if hormonal treatment is discontinued within the first couple of months, but permanent sterility can occur in as little as six months. This should not be counted on for birth control, because a miniscule sperm count might remain until the testes are surgically removed. Estrogens, progesterones, and gonadal androgen production inhibitors are the chemicals responsible for lowering fertility. It appears to the author that the other types of anti-androgens do not necessarily effect fertility–but one would be wise to take frequent fertility tests if one chooses to employ only the other types of anti-androgens with the intent of maintaining fertility.
  • Male sex drive decreases. Directly stimulated erections can become infrequent and difficult to maintain. Spontaneous erections usually stop. Semen secretion decreases, usually resulting in less intense ejeculatory orgasms (however, the ability to achieve a satisfying orgasm–even with little or no semen–is determined more by psychological factors and frequent practice than anything else). The testes and prostate atrophy. The penile skin also shrinks if erections are not regularly encouraged.
  • Breast size increases. Typical growth is to one to two cup sizes below closely related females (mother, sisters). The growth is not always symmetrical–neither is it for females. Sometimes the areoles and nipples swell, but generally not significantly, unless the body is less than a decade past puberty.
  • Fat is redistributed. The face becomes more typically female in shape. Fat tends to move away from the waist and toward the hips and buttocks.
  • Body hair growth (not including head, face, or pubic area) slows, becomes less dense, and may lighten in color.

Many people also report the following effects, but they are not verified in any medical literature that the author has read:

  • If exercise is not increased, some muscle tone is lost.
  • Outer skin layer becomes thinner, lending a finer translucent appearance and increased susceptibility to scratching and bruising. Tactile sensation becomes more intense.
  • Oil and sweat glands become less active, resulting in dryer skin, scalp, and hair.
  • Scalp hair becomes thicker, and male pattern baldness generally stops advancing. In some cases, a fine fuzz may grow back along the line of where scalp hair was recently lost–but only from the living follicles, not dead ones.
  • Metabolism decreases. Given a caloric intake and exercise regimen consistent with pre-hormonal treatment, one tends to gain weight, lose energy, need more sleep, and become cold more easily. Sometimes the ability to concentrate is also initially diminished, but the tiredness and distraction generally pass once the body and brain become used to operating with less androgens to maintain intensity.
  • Fingernails become thinner and more brittle.
  • Body odors (skin and urine) change. They become less “tangy” or “metallic” and more “sweet” or “musky”.
  • Internal emotions are amplified, becoming more apparent, distinguishable, and influential. Some people report reduced anxiety and increased sense of well-being. This could be a placebo effect. Changing the hormone therapy (adjusting dosages up or down in the regimen) sometimes causes a week or two of depression and otherwise unexplainable emotional angst.
  • “Female” sex drive and enjoyment increase. This observation is obviously completely subjective since males have no way to directly compare the experience. Non-ejeculatory orgasms become more likely for those with the predisposition to have them, if for no other reason than the fact that ejeculatory orgasms are difficult or impossible to achieve, and the need for sexual release forces a rewiring of perceptions and responses.

Female hormones do not:

  • Cause the voice to increase in pitch.
  • Dramatically reduce facial hair growth in most people. There are some exceptions with people who have the proper genetic predisposition and/or are less than a decade past puberty.
  • Change the shape or size of bone structure. However, they may change the bone density slightly.

What are the popular treatment philosophies?

The following estrogen dosage philosophies are popular for treatment of male-to-female transsexuals, and are presented in descending order of preference in the humble opinion of the author.

 

Dosage Reasoning
1 A Adjust estrogen to achieve a serum estrogen level in the normal range of a female; more or less ignore the serum androgen level The body cannot make good use of more estrogen than a female would naturally generate Androgens do not directly compete with estrogens for estrogen receptor sites A higher level of exogenous estrogen might cause adverse effects
B Administer consistently low dosage of estrogens
2 A Adjust estrogen to achieve a serum androgen level in the normal range of a female; more or less ignore the serum estrogen level The body might be able to make good use of more estrogen than a female would naturally generate Androgens might compete with estrogen for estrogen receptor sites High levels of exogenous estrogen over a limited period, i.e., less than 3 years, do not usually cause adverse effects in a person with a very healthy liver.
B Administer consistently high dosage of estrogens
Table 1: Estrogen dosage philosophies

Clearly, philosophy 1 and 2 reasonings flatly contradict each other. There are good endocrinologists in each camp, which demonstrates that we still really do not know exactly how hormones work. However, there is more compelling evidence for the reasoning of philosophy 1. In some people philosophy 1 might have a not have quite as steep of a ramp of results as philosophy 2–but, with patience, the results seem to be just as good. The A philosophies adjust to the body’s assimilation of the estrogens, whereas the B philosophies assume “one size fits all.” Gross empirical results, i.e., breast development, should be used as a secondary rather than primary indicator. Finally, note that the endogenous level of estrogen in women (F2M) seems to be a less important factor for development than the endogenous level of androgens in men (M2F).

The following estrogen coadministration philosophies are popular for treatment of male-to-female transsexuals, and are presented in descending order of preference in the humble opinion of the author.

 

1 Add anti-androgen The remaining endogenous androgens (including those from the adrenal gland) can be more safely and effectively fought with an anti-androgen than by mega-dosing with estrogen. Spironolactone and finasteride are recommended.
2 Add progesterone Progesterone administered with estrogen can, in some people, promote extra breast growth by increasing the volume of the lactation and ducting tissue. Some studies of birth control pills in females seem to show that progesterones administered with estrogens reduce the risk of cancer from administration of estrogens alone. Some endocrinologists mimic a female cycle by decreasing or eliminating estrogen for one week of the month and/or adding or increasing progesterone for the same week. The author is not aware of compelling evidence that this is either beneficial or harmful, although a recent study in females seemed to show that cycling progesterones may decrease the beneficial effect of estrogen on cardiovascular health. The primary effect of cycling is the invocation of extreme mood swings similar to PMS in females.
3 Add another estrogen This may cause faster results for some people, but generally not better results in the long run.
Table 2: Coadministration philosophies

How are hormones delivered?

Advantages Disadvantages
Oral Convenience Increased stress on the liver since it has to process the hormones twice instead of just once
Injection Less liver stress than oral delivery Less steady hormone level. Pain and slight infection risk from hypodermic needle usage.
Transdermal film Less liver stress than oral delivery. Hormone level more steady than injections.. Inconvenience and skin irritation.Multiple simultaneous patches required for pre-op dosage. Expensive.
Cream Less liver stress than oral delivery. Low transfer rate into the body–too low to be effective unless it is very frequently rubbed on very large skin surfaces. Application to just the breast area does not limit the distribution to that area; the little estrogen absorbed is distributed throughout the body and in insufficient quantity to make the breasts grow significantly (the only obvious effect is moister and healthier skin).
Table 3: Delivery methods

Note that the absorbtion of oral preparations varies greatly among individuals. With some the absorbtion is poor; in that case, injection or transdermal film is indicatedSustained-release intramuscular injectable hormones are suspended in oil. This is the usual procedure for administration:

  1. If you are very sensitive to pain, obtain 2 new needles for each administration: 1 to fill the syringe (18-22 guage), and another for the injection (22 guage). That way the injection needle will be entirely sharp. Be careful not to drag the injection needle across anything, even skin, before the injection, because that will dull it.
  2. If you are fairly tolerant of pain, or cannot afford 2 needles for each injection, then use the same new needle (22 guage) to fill the syringe as to make the injection. Do not under any circumstances reuse needles between injection periods, or between different people.
  3. Warm the vial (ampule) between your hands for a moment to help the oil flow more freely.
  4. Cleanse the top of the vial and the area for injection with a swipe of povidone-iodine (10%), or if you cannot obtain that, use rubbing alcohol (95-99%) or hydrogen peroxide (3-5%).
  5. The best intramuscular injection sites are the upper outer quadrant of the buttock, or upper outer thigh. Either is fine, as long as you are hitting at least two inches of fat and muscle, not bone or an artery.
  6. Securely mount the drawing needle on the syringe, then if you are using a rubber-corked vial, pull back the plunger about 1/4-1/3 cc farther than the intended injection amount (e.g., if you intend to inject 1 cc, then draw back 1 1/4 – 1 1/3 cc of air).
  7. With the vial right-side-up, insert the needle in the top, such that the needle end is in the bottle air, but not the oil. Inject all of the air from the syringe into the vial.
  8. Be sure the needle end is in oil (not air, and not bumping against the glass), then slowly but firmly draw back the plunger until you have a bit more than the injection amount. You will probably see some small air bubbles; that is normal. Inject the extra solution, along with the top bubble, back into the vial. If you have a rubber-corked vial, this is easiest if the vial is upside-down.
  9. Withdraw the needle (still needle up), then set the vial down. If you are using a second needle for the injection, swap needles now. Make sure the injection needle is securely fastened (usually a twist-on).
  10. With the injection needle pointed up, tap the syringe and very slowly squeeze out the final bubbles. You might lose a bit of the solution, but it is important to be patient amount removing all of the significant bubbles (however, you need not worry about the suspended bubbles which are so tiny as to be nearly invisible).
  11. If you need to change position to make the injection, put the protective cover on over the needle so you can set it down. Some people find it easiest to stand; others prefer to lay on their stomach if the buttock is target. If possible, have someone you trust make the actual injection; it is much easier that way.
  12. Uncover the needle, grasp the outside of the syringe firmly (finger off the plunger), place the needle against your skin, perpendicular, then bravely push straight in (no bending at all) to a depth of roughly 2 1/2 – 3 1/2 cm , (1 – 1 1/3 inches). There should not be much pain past the initial prick. Once the needle is in, try not to shift your weight around or flinch such that the muscles there would move.
  13. Still holding the outside of the syringe, pull back the plunger to be sure you did not hit a significant blood vessel. If you see no blood in the syringe, then very slowly but firmly depress the plunger. If you do see blood, then withdraw the needle, apply pressure to the site for a minute, then [optionally install a new needle and] try again a few centimeters away, or on the opposite side of your body.
  14. Remove the needle from your body, replace the protective cover, and dispose of that part into a sharps container, or at least a container of strong composition that cannot be punctured by the used needles.
  15. It is normal for there to be slight oozing of blood and/or oil from the injection site (and a small bruise later), given the large needle guage. If it oozes for more than a few seconds, apply pressure for a minute. If you are the extraordinarily tidy type, you can also place a dot bandaid over it, but it is not really necessary.

How can the intended effects of hormone therapy be maximized and the dangers minimized?

  • Before starting hormone therapy, take a full physical exam, and have blood drawn to check liver function (enzymes) and clotting factors. If you can possibly afford it, also take tests for thyroid, kidney, electrolyte, lipid (cholesterol), prolactin, sugar, estrogen, and androgen levels. It is also interesting to monitor the skeletal health via the calcium and phosphorus levels, especially if you are more than 40 years old (better yet, with a bone densitometer).
  • If you take oral estrogen or synthetic progesterone (progestin), repeat the liver and clotting tests a few months after each significant increase of dosage. At the very minimum, recheck them 6 months and 12 months after starting. Even after achieving a stable long-term (> 2yr) oral regimen, it is not a bad idea to recheck the liver and clotting again every couple of years. If you are only on injectible or transdermal hormones, a single recheck 9-12 months after starting should be sufficient, if you are otherwise healthy.
  • If you take spironolactone, have an electrolyte test about a month after each significant increase of dosage, especially if you have any known problems with potassium levels.
  • Discharge from the nipples may be a sign of a dangerously elevated prolactin level due to intolerance of the estrogen dosage. Immediately take a serum prolactin test. Note that there may be a dramatic spike in the prolactin level, causing significant lactation for up to a week, if a high estrogen dosage is suddenly stopped; this is similar to the process in a female who has just bore her child.
  • Be constantly aware of your body so that adjustments can be made if any new problems develop during therapy.
  • Have regular medical checkups (minimally every year; more often if you have any significant health problem); pay close attention to vital signs.
  • Eat well, and take a good multi-vitamin/mineral supplement to help be sure the body has everything it needs for new development. It might be worth paying special attention to the B vitamens: it has been reported by some that 1-2mg/day folic acid seems to help increase estrogen assimilation, and that, more generally, the entire B-complex (hello vegemite) has helped many feel better overall during pre-op level estrogen therapy (just do not go overboard with mega doses of supplements). Also, milk thistle has been promoted as a liver tonic, which seems reasonable because it contains silymarin. Silymarin has been shown to protect the liver from free radical damage by directly acting as an antioxidant, as well as by increasing the liver’s content of glutathione and superoxide dismutase, which help the liver detoxify a wide range of hormones, drugs, and chemicals. Perhaps most interesting is silymarin’s reputed ability to stimulate protein synthesis and the production of new liver cells, suggesting that it may be useful not only in preventing acute liver toxicity, but also in promoting recovery from chronic liver damage.
  • Do not start taking the maximum planned dosage of all hormones at once. Start with a low dosage of one, and carefully watch for negative vital signs and symptoms. If there are no problems after 2 months, increase the dosage to the planned level. Wait another 2 months before adding the next hormone or anti-hormone. Do not change the regimen radically or more often than once per 2 months. Give the body time to adjust.
  • Use the lowest hormone dosage that affords the desired changes. Not everyone needs the same dosage, because of differences in body weight and genetically-disposed sensitivity to the hormones. Hormone dosage can usually be reduced to a nominal maintenance level after the testes are surgically removed. It is not recommended to take pre-operative dosages of hormones for more than about 3 years.
  • Keep your hormone levels as even as you can. If possible, divide oral drugs into twice-daily portions. For injections, if you can stand the hassle and extra cost of syringes, divide your dose for taking every 1-2 weeks rather than letting it go 3-4 weeks.
  • Try the daily dosage of a hormone before moving to a sustained-release version, e.g., make sure you do not have adverse allergic or psychological reactions to Provera tablets before you use Depo-Provera (the sustained release intramuscular injection).
  • Estrogens delivered orally strain the liver more than other delivery methods. However, it is not highly dangerous unless the liver is already weakened by alcohol, drug use, or infection. It is a good idea to reduce alcohol and other drug intake.
  • Susceptibility to hardening of the arteries decreases somewhat, but susceptibility to blood clots, phlebitis (inflammation of lower extremity and pelvic veins), varicose veins, elevated high blood pressure increases somewhat. Stop smoking, reduce stress, and increase aerobic exercise. Investigate severe leg pain by x-ray or ultrasound to determine if it is caused by a blood clot before massaging it. Leg and foot cramping not caused by a blood clot might be reduced with potassium and vitamin E supplements (but one should not take potassium concurrently with spironolactone). Stop or drastically reduce estrogen dosage at least one month before having major surgery that would keep you in bed for more than 1 full day without any walking (to reduce the risk of thrombosis). If you take a significant oral estrogen dosage, consider adding about 80mg/day aspirin to reduce the risk of blood clots; take it with food and liquid to reduce the risk of stomach ulcer–or, better yet, use the enteric safety-coated variety.
  • Since spironolactone is a diuretic, anyone taking it should drink plenty of water, especially before and after exercise, and may need to reduce dietary intake of potassium–especially if the kidneys are already stressed.
  • Breast cancer risk seem to be low in comparison to females receiving estrogen replacement therapy. Certain studies in females seem to show that the cancer risk is lowered by consistently administering progesterone with the estrogen.
  • Perform monthly breast self-exams, anyway; take mammograms every 2 years before age 40, every year thereafter. Prostate cancer risk is significantly reduced in comparison to males not receiving estrogen therapy. Have the prostate examined once a year if possible, anyway.

Results

A hormone therapy regimen that works well for one person may not for another. If development is not well under way in, say, 6 months, some experimentation may be in order; try different hormone types and/or combinations. However, if you change a regimen sooner than 6 months after a previous change, it will be difficult to tell which regimen was working best. Be patient. The obvious exception is if you have a strong adverse effect that you or your physician deem dangerous; in that case you obviously must stop taking the hormone (or anti-hormone) in question. It is unusual for the therapy to not work; the most common cause is the choice or oral preparations since the absorbtion varies among individuals.

Hormone dosage can usually be reduced to a nominal maintenance level after the testes are surgically removed.

How can one obtain hormones?

In the U.S., most reputable therapists and medical doctors who regularly work with transsexuals follow the Harry Benjamin Standards of Care, a plan that specifies that one must undergo a minimum of 3 months of psychotherapy to obtain a letter of recommendation to an endocrinologist. One can choose to work with doctors who do not follow the Benjamin Standards, but, in any case, it is a very good idea to meditate and cogitate on the implications for at least 3 months before starting hormone therapy. Some transsexuals find the Benjamin Standards too restrictive–even insulting; others find it worth the trouble to go through the hoop in order to be referred to an endocrinologist who is particularly knowledgeable in the treatment of transsexuals. Choose carefully.

If a sympathetic endocrinologist is not available, try local gynecologists; they are sometimes more understanding, and are used to prescribing estrogens and progesterones.

One should only take hormones that were obtained directly from a licensed pharmaceutical distributor; the quality of drugs obtained through other channels is not only suspect, but likely dangerous–especially those in injectable form.

It is possible to have a health insurance company to cover hormones just like any other prescription drugs, especially if the doctor prescribes them for a “hormone imbalance” or “hormone replacement” rather than “transsexual hormone therapy.” When a health insurance company subcontracts out prescription drug coverage to another company, benefits for hormones are not generally questioned since there is little communication between the two companies.

Some people in the U.S. have reportedly taken advantage of the U.S. FDA Personal Use Import Policy to purchase hormones directly from international sources.

Additional Information at The Houseof Sissify.Com:

Are birth-control pills a good source of estrogen?

No. Although early birth-control pills contained significant quantities of estrogen, modern ones do not. A typical birth-control pill now contains a tiny dosage of progesterone, with or without a tiny dosage of estrogen–less than one-tenth the strength required for an effective course of treatment for a transsexual. If one is absolutely determined to use a particular birth-control pill, then one should carefully study the PDR to understand the dosages of the component hormones of the pill in question, compared to the typical dosages of the same hormones in this FAQ.

How can lactation be induced?

This section is provided for curiosity only; the author has no medical references–only anecdotes from other transsexuals and mothers, popular media, and some experience with bovines–to substantiate the answer.

  • One must maintain a high level of estrogen for quite a while–probably a minimum of 6 months–then suddenly drop it. That is apparently enough in some males to kick the pituitary into releasing enough prolactin (milk-producing hormone) to make it possible to start some lactation.
  • Along with estrogen, progesterone plays a significant role in the development of lactating tissue (glands and ducts), so maintaining a moderate to high level of progesterone for probably at least 6 months previous would also help.
  • Finally, assuming the lactating tissue is developed and the milk comes in, one would need to frequently stimulate the milk “let-down” secretion reflex with oxytocin, by either artificially administrating it, or naturally generating it with practice with similar enviromental stimuli that nursing females use (relaxing, hearing or thinking of the baby being hungry, direct sucking stimulation of the nipples and immediately surrounding tissue, orgasm, etc.).
  • Not a lot of milk is produced unless suckling (or expressing) is frequent and consistent, say every 2-3 hours. Less stimulation than that, say, once every 5-8 hours, will result in dramatically less milk production. Less than that will result in complete cessation of milk production within 1-3 weeks after it starts.

In summary, one has to be committed to the notion of actively and consistently nursing and/or expressing; it is quite a project, and will not work for everyone.

If the milk is to be used for feeding a baby (not particularly recommended or encouraged), one should consult one’s physician and the PDR for warnings about usage of hormones and other drugs while nursing.

For more information, see the La Leche League International site or ring them at 800.LALECHE. They specialize in issues of breast-feeding.

How can a male be neutered without causing feminization?

One can cause the gonads to dramatically reduce androgen production by shutting down the output of LH and FSH from the pituitary gland. This can be done one of two ways:

  • Introducing consistently large quantities of any estrogen or progesterone. Progesterone does not have a feminizing effect, so one could usemedroxyprogesterone acetate. This has been demonstrated to work on males with severe behavioral disorders exacerbated by androgens (read: serial rapists), who were given the choice of taking periodic shots or remaining in prison. The sustained-release injectable preparation is easier on the liver than orally delivered tablets, but one should first try the tablets for a month or two to be sure there is not an allergic reaction. Be aware that there are annoying and dangerous adverse effects with progesterones, ranging from severe mood swings to blood clotting disorders.
  • Alternatively, one can use a GnRH agonist. This is a more elegant solution, and has fewer adverse affects than progesterones. However, it is more expensive, and it might be very difficult to persuade a doctor to prescribe one.

Note that neither of these methods can be used for reliable birth control; some small amount of sperm may still be produced, even if the androgen levels are forced to be very low. This can be easily checked with a periodic sperm count check.

Stopping the administration of progesterone or GnRH agonist will usually result in the gonads resuming androgen (and sperm) production within a few months. The degree to which production is restored depends on how long the progesterone or GnRH agonist was used; the opinion of the author is that treatment of more than a few months will result in some degree of atrophy of the gonads; more than six months may result in permanent sterility. There has been little research on the reversibility of this treatment.

Exactly what hormones are available? What are the details on popularity, dosage, availability, price, contraindications, adverse effects, etc.?

Estrogens

The following estrogens are popular for treatment of male-to-female transsexuals, and are presented in descending order of preference in the humble opinion of the author:

 

Name Safety and Efficacy Source Price
Estradiol Valerate Excellent ? $0.054/day
Estradiol Cypionate Excellent ? $0.023/day
Estradiol Excellent ? $0.65/day
Ethinyl Estradiol Good Synthetic $0.54/day
>Quinestrol Good ? ?
Estropipate Good ? ?
Conjugated Estrogens Good Live animals $1.50/day
Esterified Estrogens Good Live animals $1.20/day
Chlorotrianisene Fair Synthetic ?
Diethylstilbestrol Poor Synthetic ?
Table 4: Popular estrogens

Other prescription estrogens are available; however, they are mixed with other drugs and are therefore not as suitable for treatment of transsexuals.

The following natural sources of phytoestrogens (estrogen-like compounds) have been identified, but the author is not aware of an effective course of treatment using them. They work by weakly binding to estrogen receptors. In males, this may result in a mild feminizing effect (in females, it may give the opposite result, that is, a mild androgenic effect, since the phytoestrogens are competing with endogenous true estrogens for the estrogen receptors). Since phytoestrogens are not nearly as efficacious as true estrogens, huge and potentially toxic amounts of these items would have to be consumed. They are presented in alphabetical order:

Preparations advertized to contain “raw ovaries” from any animal have not been proven to be effective.

Progesterones

The following progesterone is popular for treatment of male-to-female transsexuals:

  • Medroxyprogesterone Acetate

The following progesterone has been suggested for treatment of male-to-female transsexuals, but the author does not have information about how suitable, effective, or safe it is for transsexuals:

  • Norethindrone Acetate

The following natural sources of phytoprogesterones (progesterone-like compounds) have been identified, but the author is not aware of an effective course of treatment using them. Since phytoprogesterones are not nearly as efficacious as true progesterones, huge and potentially toxic amounts of these items would have to be consumed. They are presented in alphabetical order:

Note that the Women’s International Pharmacy at 800.279.5708 manufactures by-prescription-only “natural” progesterone pills from an unspecified source. This pharmacy and their progesterone products have received rather a lot of attention on women’s health support USENET groups such as alt.support.menopause.

Anti-androgens

The following anti-androgens are popular for treatment of pre-operative male-to-female transsexuals. They are presented in descending order of preference in the humble opinion of the author:

 

 

Name Safety Efficacy Price
Cyproterone Acetate Good Excellent ?
Spironolactone Excellent Good $0.95/day
Flutamide Fair Good $7.20/day
Finasteride Excellent Poor* $1.89/day
Table 5: Popular anti-androgens

 

 

*While not a good general anti-androgen, finasteride has shown promise as a legitimate scalp hair regrowth treatment.

Prescription adrenal androgen production inhibitors are available but not listed because adrenal androgen production is insignificant (i.e., about the same as in females) in comparison to gonadal adrenal production. Adrenal androgens are best ignored, or if absolutely necessary, countered with a mild androgen receptor antagonist.

Other prescription anti-androgens are available but not listed because their primary indication is not as an anti-androgen, and/or because the adverse effects are dangerous when weighed against the possible benefit.

The following natural sources of phytoantiandrogens (anti-androgen-like compounds) have been identified, but the author is not aware of an effective course of treatment using them. Since phytoantiandrogens are not nearly as efficacious as true antiandrogens, huge and potentially toxic amounts of these items would have to be consumed. They are presented in alphabetical order:

Other Anti-Hormones (GnRH Agonists)

These pharmaceuticals can be used to dramatically reduce gonadal hormone production in both males and females. They are used mainly by pediatricians to reduce precocious puberty, so it may be difficult to persuade a doctor to prescribe them for an adult. Also, they are very expensive. None the less, this type of chemical castration is worth investigating for those cases when the pre-operative male-to-female cannot take the hormones of choice because of other health problems (e.g., hormone dependent tumors or blood clotting disorders), and cannot yet have the surgery performed (note that such a problem is quite rare). They are presented in descending order of preference in the humble opinion of the author:

 

Name Safety and Efficacy Price
Goserelin Acetate Excellent $11.49/day
Nafarelin Acetate Excellent $25.87/day
Leuprolide Acetate Fair $11.60/day
Table 6: Anti-hormones

 

 

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