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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.
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Serving the transgendered community Dial 773.288.4491 or telnet palace.ppp.ripco.net |
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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 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.
- 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.
- 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 the following criteria:
- 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.
- Source: unknown, animal by-products, or live animals
- 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.
- What are hormones, and how do they work?
- What are normal endogenous androgen and estrogen levels?
- What effect does contrasexual hormone therapy have, 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?
- Exactly what hormones are available? What are the details on popularity, dosage, availability, contraindications, adverse effects, etc.?
- Where is there more information about hormones?
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.
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.
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 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.
- It has even been occasionally reported that sensitivity to air-born allergens decreases.
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.
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 Adjust estrogen for gross empirical results while paying extra attention to health See discussion below. 3 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 3 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 3--but, with patience, the results are often just as good. The A philosophies adjust to the body's assimilation of the estrogens, whereas the B philosophies assume "one size fits all."
Philosophy 2 occupies an awkward space in between, where we acknowledge that in some cases neither endogenous nor exogenous hormone levels are great indicators, because the levels in "typical" post-pubescent non-transsexual bodies do not always relate well to the plethora of absorption and response factors in a given post-pubescent transsexual body, especially when anti-hormones are added to the mix. If there is unusually low development after, say, two years of hormone therapy, it might be that the gross empirical results, e.g., breast growth and fat redistribution, should be used as a primary rather than secondary indicator, provided ones health (especially of the liver) is not compromised. Finally, note that the endogenous level of estrogen in females (F2M) seems to be a less important factor for development than the endogenous level of androgens in males (M2F) anyway.
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
Advantages Disadvantages Oral Convenience. Possibly more beneficial for blood cholesterol levels than injections. Increased stress on the liver since it has to process the hormones twice instead of just once Injection Less liver stress than oral delivery. Inexpensive. 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 absorption of oral preparations varies greatly among individuals. With some the absorption is poor; in that case, injection or transdermal film is indicated.
Sustained-release intramuscular injectable hormones are suspended in oil. This is the usual procedure for administration:
- 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.
- 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.
- Warm the vial (ampule) between your hands for a moment to help the oil flow more freely.
- 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%).
- 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.
- 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).
- 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.
- 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.
- 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).
- 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).
- 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.
- 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.
- 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.
- 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.
- 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.
Congratulations!
- 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 the regimen very often, it will be difficult to tell which one 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 of 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.
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 should 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. Please note that Confluence Publications does not have any further information about these potential sources.
Details On Popularity, Dosage, Availability, Contraindications, AdverseNo. 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 pre-op 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.
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 Estradiol Valerate Excellent Synthetic (plant-based?) Estradiol Cypionate Excellent Synthetic (plant-based?) Estradiol Excellent Synthetic (plant-based) Ethinyl Estradiol Good Synthetic Quinestrol Good ? Estropipate Good Synthetic (plant-based) Esterified Estrogens Good Synthetic (plant-based) Conjugated Estrogens Good Live animals Table 4: Popular estrogens Estradiol Valerate
Brand Name Manufacturers Delestrogen by B.M. Squibb
Progynova by Schering
Progynon-Depot by Schering, GermanyGeneric Manufacturers Goldline
Gynogen by Forest
Major
Schein
Steris
Valergen by HyrexPharmacology Same as endogenous estrogen Delivery 1, 2mg oral tablets.
Sustained release intramuscular injection.Typical dosage Pre-op 20-60mg/3wks injection or 15-40mg/2wks or 7-20mg/1wk injection
Pre-op 8mg/day oral
Post-op 10-30mg/2-3wks injectionAvailability Injection approved by U.S. FDA. Oral tablets may be approved but do not seem to be available in U.S. Indications Estrogen replacement therapy in females Contraindications Active blood clotting disorders. Estrogen-dependent tumors. History of blood clotting disorders associated with estrogen use. History of sensitivity to estradiol or any part of the preparation. Known or suspected breast cancer except in appropriately selected patients. Adverse reactions
- CNS
- Convulsions. Dizziness. Headache. Migraine. Mental depression. Spasms of limb and facial muscles.
- Eyes
- Intolerance to contact lenses. Steepening of corneal curvature.
- Gastrointestinal
- Abdominal cramps. Bloating. Cholestatic jaundice. Nausea. Vomiting.
- Skin
- Blotchy skin pigmentation. Localized skin irritation. Loss of scalp hair. Increase of body hair. Red skin patches from capillary congestion.
- Other
- Blood clotting disorders. Elevated blood pressure. Fluid retention. Glucose intolerance. Increased serum calcium level. Increased sensitivity to light. Liver tumors.
Comments Note that "Progynon-Depot" by Schering, Germany is estradiol valerate, but "Progynon-Depot 100" by the very same company is an entirely different substance, estradiol undecylate (which apparently is not an effective feminizing hormone).
Estradiol Cypionate
Brand Name Manufacturers Depo-Estradiol by Pharmacia/Upjohn Generic Manufacturers Depgen by Hyrex
Dep-gynogen by Forest
Estrocyp by Keene
Goldline
Moore
Rugby
Schein
SterisPharmacology Same as endogenous estrogen Delivery Sustained release intramuscular injection, 5mg/ml Typical dosage Pre-op 2-4mg/3wks injection or 1.5-3mg/2wks injection??
Post-op 1-2mg/2-3wks injection??Availability Approved by U.S. FDA Indications Estrogen replacement therapy in females Contraindications Active blood clotting disorders. Estrogen-dependent tumors. History of blood clotting disorders associated with estrogen use. History of sensitivity to estradiol or any part of the preparation. Known or suspected breast cancer except in appropriately selected patients. Adverse reactions
- CNS
- Convulsions. Dizziness. Headache. Migraine. Mental depression. Spasms of limb and facial muscles.
- Eyes
- Intolerance to contact lenses. Steepening of corneal curvature.
- Gastrointestinal
- Abdominal cramps. Bloating. Cholestatic jaundice. Nausea. Vomiting.
- Skin
- Blotchy skin pigmentation. Localized skin irritation. Loss of scalp hair. Increase of body hair. Red skin patches from capillary congestion.
- Other
- Blood clotting disorders. Elevated blood pressure. Fluid retention. Glucose intolerance. Increased serum calcium level. Increased sensitivity to light. Liver tumors.
Comments The reason there are question marks for the pre-op dosage is:
- The author extrapolated from the 1:10 ratio of cypionate:valerate ovarian failure replacement dosages recommended in the 1997 pdr generics listings, in turn, roughly adjusted against the popular anecdotal valerate pre-op dosage, and;
- The author has found no cypionate anecdotes either to support or change this guess.
Estradiol
Brand Name Manufacturers Climara by Berlex Labs (film)
Estraderm and Vivelle by Ciba (film)
Estrace by B/M Squibb (oral)Generic Manufacturers Apothecon
Geneva
Goldline
Major
Moore
Qualitest
Rugby
WatsonPharmacology Same as endogenous estrogen Delivery Oral tablets 0.5, 1, 2mg
Extended release film 0.0375, 0.05, 0.075, 0.1mg/24hrsTypical dosage Pre-op oral 4-12mg/day, 1 or 2 film patches 0.1 changed twice weekly
Post-op oral 2-6mg/day, film 0.05 or 0.1 changed twice weeklyAvailability Approved by U.S. FDA Indications Estrogen replacement therapy in females Contraindications Active blood clotting disorders. Estrogen-dependent tumors. History of blood clotting disorders associated with estrogen use. History of sensitivity to estradiol or any part of the preparation. Known or suspected breast cancer except in appropriately selected patients. Adverse reactions
- CNS
- Convulsions. Dizziness. Headache. Migraine. Mental depression. Spasms of limb and facial muscles.
- Eyes
- Intolerance to contact lenses. Steepening of corneal curvature.
- Gastrointestinal
- Abdominal cramps. Bloating. Cholestatic jaundice. Nausea. Vomiting.
- Skin
- Blotchy skin pigmentation. Localized skin irritation. Loss of scalp hair. Increase of body hair. Red skin patches from capillary congestion.
- Other
- Blood clotting disorders. Elevated blood pressure. Fluid retention. Glucose intolerance. Increased serum calcium level. Increased sensitivity to light. Liver tumors.
Quinestrol
Brand Name Manufacturers Estrovis by Parke-Davis Generic Manufacturers None Pharmacology 3-cyclopentylether of ethinyl estradiol. Acts on receptors apparently the same as endogenous estrogen. Delivery Oral 0.1mg tablets Typical dosage Pre-op ?
Post-op 0.1-0.2mg/wkAvailability Approved by U.S. FDA Average Wholesale Price $141.70/100 Indications Estrogen replacement therapy in females Contraindications Active blood clotting disorders. History of blood clotting disorder in association with estrogen therapy. Known or suspected breast cancer. Known or suspected estrogen-dependent tumors. Adverse reactions
- CNS
- Dizziness. Headache. Mental depression. Migraine. Spasms of limb and facial muscles.
- Eyes
- Intolerance to contact lenses. Steepening of corneal curvature.
- Gastrointestinal
- Abdominal cramps. Bloating. Cholestatic jaundice. Nausea. Vomiting.
- Skin
- Blood eruptions from skin. Blotchy skin pigmentation. Increase of body and facial hair. Loss of scalp hair. Red skin patches from capillary congestion.
- Other
- Blood clotting disorders. Breast and liver tumors. Elevated blood pressure. Fluid retention. Gall bladder disease. Increased calcium level in blood. Increased sensitivity to light. Reduced carbohydrate and glucose tolerance.
Comments Estropipate
Brand Name Manufacturers Ogen by Pharmacia/Upjohn Generic Manufacturers Caremark
Duramed
Goldline
Ortho-est by Ortho Pharm
Qualitest
Rugby
Schein
URL
Warner Chilcott
WatsonPharmacology Sulfate of estrone, stabilized with piperazine. Apparently acts on receptors the same as endogenous estrogen. Delivery Oral 0.75, 1.5, 3mg tablets Typical dosage Pre-op ?
Post-op Oral 1.5-9mg/dayAvailability Approved by U.S. FDA Indications Estrogen replacement therapy in females Contraindications Active blood clotting disorders. Known or suspected breast cancer, unless that is the target. Known or suspected estrogen dependent tumors. Adverse reactions
- CNS
- Dizziness. Headache. Mental depression. Migraine. Spasms of limb and facial muscles.
- Eyes
- Intolerance to contact lenses. Steepening of corneal curvature.
- Gastrointestinal
- Abdominal cramps. Bloating. Cholestatic jaundice. Nausea. Vomiting.
- Skin
- Blood eruptions from skin. Blotchy skin pigmentation. Increase of body and facial hair. Loss of scalp hair. Red skin patches from capillary congestion.
- Other
- Blood clotting disorders. Breast tumors. Elevated blood pressure. Fluid retention. Gall bladder disease. Increased calcium level in blood. Increased sensitivity to light. Reduced carbohydrate tolerance.
Comments Since estropipate is a quot;natural estrogenic substance prepared from purified crystalline estrone", the source is likely to be pregnant mares, the same as for conjugated and esterified estrogens. Refuting or confirming evidence would be appreciated. Esterified Estrogens
Brand Name Manufacturers Menest by SK Beecham Pharm
Estratab by SolvayGeneric Manufacturers Cheshire Pharmacology Esterified estrogens are a mixture of the sodium salts of the sulfate esters of the estrogenic substances, principally estrone. They seem to act on estrogenic receptors the same as endogenous estrogen. Delivery Oral 0.3, 0.625, 1.25, 2.5mg tablets Typical dosage Pre-op 2.5-7.5mg/day
Post-op 1.25mg/dayAvailability Approved by U.S. FDA Indications Estrogen replacement therapy in females. Inoperable progressing breast or prostate cancer. Contraindications Active blood clotting disorders. Estrogen-dependent tumors. History of blood clotting disorders associated with estrogen use. History of sensitivity to estradiol or any part of the preparation. Known or suspected breast cancer except in appropriately selected patients. Adverse reactions
- CNS
- Dizziness. Headache. Mental depression. Migraine. Spasms of limb and facial muscles.
- Eyes
- Intolerance to contact lenses. Steepening of corneal curvature.
- Gastrointestinal
- Abdominal cramps. Bloating. Cholestatic jaundice. Nausea. Vomiting.
- Skin
- Blood eruptions from skin. Blotchy skin pigmentation. Increase of body and facial hair. Loss of scalp hair. Red skin patches from capillary congestion.
- Other
- Blood clotting disorders. Breast and liver tumors. Elevated blood pressure. Fluid retention. Gall bladder disease. Increased sensitivity to light. Increased serum calcium level. Reduced glucose tolerance.
Comments Conjugated Estrogens
Brand Name Manufacturers Premarin by Wyeth-Ayerst Generic Manufacturers None Pharmacology Sodium salts of estrogen sulfates. Apparently acts on receptors the same as endogenous estrogen. Delivery 0.3mg, 0.625, 0.9, 1.25, 2.5mg tablets Typical dosage Pre-op Oral 1.25-7.5mg/day
Post-op Oral 0.625-5mg/dayAvailability Approved by U.S. FDA Indications Estrogen replacement therapy in females. Treatment of selected breast and prostate cancers. Contraindications Active blood clotting disorders. Known or suspected breast cancer, unless that is the intended target. Known or suspected estrogen dependent tumors. Adverse reactions
- CNS
- Dizziness. Headache. Mental depression. Migraine. Spasms of limb and facial muscles.
- Eyes
- Intolerance of contact lenses. Steepening of corneal curvature.
- Gastrointestinal
- Abdominal cramps. Bloating. Cholestatic jaundice. Nausea. Vomiting.
- Skin
- Blood eruptions from skin. Blotchy skin pigmentation. Increase of facial and body hair. Loss of scalp hair. Red skin patches from capillary congestion.
- Other
- Blood clotting disorders. Breast tumors. Elevated blood pressure. Fluid retention. Gall bladder disease. Increased calcium level in blood. Increased sensitivity to light. Reduced carbohydrate tolerance.
Comments Conjugated estrogens are derived from pregnant mare urine under cruel conditions including continual confinement, continual standing with no option to lay down or turn around, restriction of drinking water, inadequate veterinary oversight, killing of the newborn or young foals, then immediate reimpregnation. The pregnancies are repeated until the mare becomes infertile or sick, at which time she is slaughtered. This treatment has not been directly witnessed by the author. However, Redwings Horse Sanctuary, World Society for the Protection of Animals, People for the Ethical Treatment of Animals, and others have researched this issue, interviewed Wyeth-Ayerst representatives, and directly inspected the farms in question. Other prescription estrogens are available; however, they are mixed with other drugs, or are intended only for treatment of inoperable cancer, 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: Black Cohosh (Cimicifuga racemosa), Blue Cohosh, Borrage, Butterfly Weed, Caraway, Chaste Tree or Vitex (Verbenaceae species), Dates, Dill, Dong Quai (Angelica sinensis), False Unicorn root, Fennel seed, Fenugreek, Ginseng, Goats Rue, Gotu Kola, Licorice root, Linseed or Flaxseed, Milk thistle, Motherwort, Pennyroyal (Hedeoma pulegioides), Pleurisy root, Pomegranates, Red Clover Sprouts, Red Raspberry leaf, Southernwood, Soya Flour, Tansy.
Preparations advertized to contain "raw ovaries" from any animal have not been proven to be effective.
Progesterones
The following progesterones 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 Efficacy Source Progesterone Excellent Highly variable Wild yams Hydroxyprogesterone Caproate Excellent Highly variable Synthetic Medroxyprogesterone Acetate Fair Highly variable Synthetic Norethindrone Acetate Fair Highly variable Synthetic Table 5: Popular progesterones Progesterone
Brand Name Manufacturers Utrogestan by Besins-Iscovesco in France
Prometrium by Schering in Canada
Prometrium by Solvay PharmaceuticalsGeneric Manufacturers Compound pharmacies advertising unbranded natural progesterone on the web include Bajamar Women's Healthcare Pharmacy and Women's International Pharmacy.
Pharmacology Suspension of micronized natural progesterone in oil. Reputedly the same molecule as produced endogenously in females. Delivery Custom-packed capsules from a compounding pharmacy.
Vaginal cream.Typical dosage Pre-op 100-400mg/day capsules in conjunction with estrogens.
Post-op 50-400mg/day capsules in conjunction with estrogens.
Unclear how well cream is absorbed.Availability Approved by U.S. FDA Indications Menopausal discomfort Contraindications Active or past blood clotting disorders. Liver dysfunction or disease. Adverse reactions Generally mild and transient. Comments This drug is often suspended in a base of peanut oil, so those with nut allergies should beware.
Natural progesterone has received rather a lot of attention on women's health support USENET groups such as alt.support.menopause.
Some people call this drug progesterone USP, to differentiate from progestins. USP is an abbreviation for United States Pharmacopeia, a legally recognized compendium of standards for drugs, published by The United States Pharmacopeial Convention, Inc., and revised periodically. It includes assays and tests for the determination of strength, quality, and purity. In other countries the drug is simply referred to as progesterone.
Hydroxyprogesterone Caproate
Brand Name Manufacturers Caposten by ?
Capton by ?
Caprosteron by ?
Hormofort by ?
Delalutin by ?
Depolut by ?
Estralutin by ?
Neolutin by ?
Primolut-Depot by ?
Progesteron-retard by ?
Prolutin-Depot by ?
Syngynon by ?Generic Manufacturers Hylutin by Hyrex
Moore, H.L.
Rugby
Schein
SterisPharmacology Progestogen (progesterone derivative) Delivery 250mg/ml sustained-release intramuscular injection Typical dosage 125mg-250/2wks intramuscular injection Availability Approved by U.S. FDA Indications Unusual menstrual bleeding Endometriosis Contraindications Active or past blood clotting disorders. Cerebral clotting or haemorrhage. Adverse reactions
- CNS
- Headache. Insomnia. Loss of coordination. Mental depression. Sleepiness. Slurred speech. Weakness, numbness, or pain in extremeties.
- Eyes
- Change of vision.
- Gastrointestinal
- Cholestatic jaundice. Nausea.
- Skin
- Skin discoloration, rash, itching, and other allergic reactions.
- Other
- Blood clotting disorders. Chest pain. Decreased glucose tolerance. Fever. Fluid retention. Shortness of breath.
Comments Medroxyprogesterone Acetate
Brand Name Manufacturers Amen by Carnrick
Curretab by Solvay
Provera and Depo-Provera by Pharmacia/UpjohnGeneric Manufacturers Cycrin by Esi Lederle Generics
Geneva
Goldline
Greenstone
Intl Labs
Major
Martec
Moore
Parmed
PD-RX
Qualitest
RID
Rosemont
Rugby
Schein
URL
Warner ChilcottPharmacology Progestin (progesterone derivative) Delivery 2.5, 5, 10mg tablets
400mg/ml sustained-release intramuscular injection (brand-name only)Typical dosage Pre-op 2.5-10mg/day tablets in conjunction with estrogens
Pre-op 50mg/2weeks injectible in conjunction with estrogens
Pre-op ? for neutering without estrogens
Post-op ?Availability Approved by U.S. FDA Indications Endometrial and kidney cancer. Unusual menstrual bleeding. Contraindications Active or past blood clotting disorders. Known or suspected breast or gonadal tumors. Known sensitivity to medroxyprogesterone acetate. Liver dysfunction or disease. Adverse reactions
- CNS
- Headache. Insomnia. Loss of coordination. Mental depression. Sleepiness. Slurred speech. Weakness, numbness, or pain in extremeties.
- Eyes
- Change of vision.
- Gastrointestinal
- Cholestatic jaundice. Nausea.
- Skin
- Skin discoloration, rash, itching, and other allergic reactions.
- Other
- Blood clotting disorders. Chest pain. Decreased glucose tolerance. Fever. Fluid retention. Shortness of breath.
Comments There are many anecdotal reports of inexplicable or exacerbated depression while taking this drug. In that case, natural progesterone is indicated.
Upjohn claims that the bioavailability of Provera is higher than generic formulations.
The article "Gender Dysphoria Update" by Blaine R. Beemer (originally published in Journal of Psychosocial Nursing and Mental Health Services, 1996: 34(4), 12-19) reports that clients at Vancouver (BC) "routine receive the progestin medroxyprogesterone acetate (Provera)" and asserts that apart "from its effect as an antiandrogen, medroxyprogesterone has been shown to promote bone formation, and may counter the bone loss that might occur with the bllockade of male hormones," citing as a reference: Prior, JC, Vigna, YM, Barr, SI, Rexworthy, C, & Lentle, BC (1994), "Cyclic medroxyprogesterone treatment increases bone density: A controlled trial in active women with menstrual cycle disturbances. American Journal of Medicine, 96, 521-530. A question to consider: does the medroxyprogesterone administration have to be cyclic to have the bone density effect?
Norethindrone Acetate
Brand Name Manufacturers None Generic Manufacturers Aygestin by Esi Lederle Generics Pharmacology Progestin Delivery Oral 5mg tablets Typical dosage Pre-op 2.5-15mg/day
Post-op ?Availability Approved by U.S. FDA Indications Endometriosis. Unusual menstrual bleeding. Contraindications Blood clotting disorders. Known or suspected breast or gonadal cancer. Known sensitivity to norethindrone acetate. Liver dysfunction or disease. Adverse reactions
- CNS
- Insomnia. Mental depression. Sleepiness.
- Eyes
- foo.
- Gastrointestinal
- Cholestatic jaundice. Nausea.
- Skin
- Acne. Increase of body and facial hair. Loss of scalp hair.
- Other
- Blood clotting disorders. Fever. Fluid retention. Mild to severe allergic reactions.
Comments 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 unrefined items would have to be consumed. They are presented in alphabetical order: Suma, Vitex, Wild or Mexican Yam.
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 Spironolactone Excellent Good Finasteride Excellent * Cyproterone Acetate Fair Excellent Table 6: Popular anti-androgens Spironolactone
Brand Name Manufacturers Aldactone by Searle Generic Manufacturers
Caremark
Cheshire
Geneva
Goldline
Heartland
Major
Moore, H.L.
Mutual
Mylan
Parmed
PD-RX
Purepac
Qualitest
Raway
Rugby
UDL
URL
VanguardPharmacology Mostly inhibits production of testosterone at the stage of 17-hydroxylation, and competes with DHT (dihydrotestosterone) for bonding at peripheral receptors. It is also said to intensify catabolism of androgens, and activate conversion of testosterone into estrogens. Delivery 25, 50, 100mg oral tablets Typical dosage Pre-op 100-300mg/day
Post-op 50mg/dayAvailability Approved by U.S. FDA Indications Congestive heart failure. Elevated blood pressure. Fluid retention. Hyperaldasteronism. Inadequate pottasium retention. Liver cirrhosis. Contraindications Elevated potassium levels. Inadequate urine production. Kidney disfunction. Adverse reactions
- CNS
- Confusion. Dizziness. Drowsiness. Headache. Lethargy. Loss of precise motor control.
- Gastrointestinal
- Cramping. Diarrhea. Dry mouth. Gastric ulceration and other stomach inflammation. Vomiting.
- Skin
- Acne. Itchy, fluid-filled patches of skin. Increase of body and facial hair. Red skin patches from capillary congestion.
- Other
- Deepening of the voice. Drug fever. Pottasium retention. Severe decrease of blood granulocytes. Sodium loss.
Comments One person reported suicidal depression as an adverse effect. The brand-name formulation tastes awful; the generic formulation is much less offensive. Finasteride
Brand Name Manufacturers Proscar by Merck
Propecia by MerckGeneric Manufacturers None Pharmacology Androgen conversion inhibitor. Inhibits the production of dihydrotestosterone (DHT) from testosterone by inhibiting the binding of 5a-reductase, which is the enzyme responsible for converting testosterone to DHT. DHT is the active androgen found in the skin and prostate gland, and is associated with the development of male pattern baldness, excess body hair, and benign prostatic hypertrophy. Not suitable as a general anti-androgen since it only affects DHT production. However, it seems to be more helpful in counteracting male-pattern baldness and excess body hair than general anti-androgens. Delivery 5mg oral tablets (Proscar)
1mg oral tablets (Propecia)Typical dosage Pre-op 0.05-1mg/day
Post-op 0.05-1mg/day
(See comments below)Availability Approved by U.S. FDA Indications Benign prostate enlargement Contraindications Hypersensitivity to any component of the product. Adverse reactions Generally mild and transient Comments Anecdotal evidence strongly suggests that pill fragments (say, 4-12 from each pill) taken daily are just as effective as taking the entire pill. There might issues with oxidation, so avoid handling the unused fragments, and keep them in a small, air-tight container. Pre-ops who take finasteride should consider coadministration of a more general anti-androgen such as spironolactone (since finasteride only blocks conversion of testosterone to DHT, the body sometimes boosts the testosterone level in response.)
On the subject of scalp hair regrowth: In addition to finasteride therapy, it is customary to apply minoxidil 5% (topical) daily to the balding scalp area in order to achieve maximum results. Some people also add tretionin (retinois acid) creme 0.05%, but it is not yet clear whether that always helps.
Do not let a female who is pregnant, or might be pregnant, anywhere near finasteride fragments or powder. It is a strong teratogen, known to cause genital deformity in the male fetus.
Based on rabbit and rat studies, there may be a slight effect on male fertility that would reverse within 6 weeks of discontinuing.
Cyproterone Acetate
Brand Name Manufacturers Androcur by Schering AG, Farma (Germany)
Cyproteron by NM Pharma (England)Generic Manufacturers ? Pharmacology Androgen receptor antagonist. Weak gonadal androgen production inhibitor. Weak progesterone. Delivery 10mg, 50mg oral tablets Typical dosage Pre-op 10mg/wk-100mg/day (See comment below)
Post-op not recommendedAvailability Not approved by U.S. FDA Indications Acne and/or overactive oil glands. Androgen dependent loss of scalp hair. Hirsutism. Inoperable prostate tumors. Contraindications Lactation. Dubin-Johnson syndrome. Liver disease or tumor. Previous or existing blood clotting disorder. Rotor syndrome. Severe chronic-depression. Severe diabetes with vascular changes. Sickle-cell anaemia. Wasting diseases (with the exception of prostate tumor). Adverse reactions
- CNS
- Headache. Lessened ability to concentrate. Mental depression. Tiredness.
- Gastrointestinal
- Nausea.
- Other
- Blood clotting disorders. Carbohydrate metabolism changes. Liver dysfunction or tumors. Shortness of breath.
Comments The extreme range of dosage comes from input that some people find 10mg/wk sufficient to induce total impotence, and yet others take as much as 200mg/day with no obvious short-term adverse effects. Given this range, it would seem prudent to start on the low side and work your way up only if necessary. More than 100mg/day is generally considered excessive. *Although it is not a general anti-androgen, finasteride coadministered with minoxidil 5% (topical) and estrogen is very helpful to halt--and in some cases, partly reverse--male-pattern baldness. Many people report that it also helps to reduce excess body hair.
Cyproterone acetate is a very strong anti-androgen but also causes strong adverse effects in some people.
Nilutamide and flutamide have been suggested, but are not entirely suitable for transsexuals, especially as monotherapy: because of the way they interfere with normal negative feed-back action of androgens, they stimulate gonadotropin production and subsequently androgen production.
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 finasteride.
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: Saw Palmetto.
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 might 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 Goserelin Acetate Excellent Nafarelin Acetate Excellent Leuprolide Acetate Fair Table 7: Anti-hormones Goserelin Acetate
Brand Name Manufacturers Zoladex by Zeneca Generic Manufacturers None Pharmacology GnRH agonist. After an initial stimulating phase, the pituitary is desensitized to GnRH, which causes it to stop producing LH, which in turn dramatically decreases gonadal production of hormones within a month. Delivery Sustained release subcutaneous injection 3.6, 10.8mg Typical dosage Pre-op 3.6mg/month
(3.6mg implant is for 1 month; 10.8 mg implant is for 3 months)Availability Approved by U.S. FDA Indications Androgen-sensitive prostate cancer Contraindications Known hypersensitivity to GnRH, GnRH analogues, or any of the components of the product Adverse reactions
- CNS
- Dizziness. Insomnia. Lethargy.
- Gastrointestinal
- Anorexia. Nausea.
- Skin
- Sweating.
- Other
- Congestive heart failure. Fluid retention. Hot flashes. Increased calcium level in blood. Mild to severe allergic reactions. Obstructive pulmonary disease. Ureteral and spinal compression.
Comments Nafarelin Acetate
Brand Name Manufacturers Synarel by Searle Generic Manufacturers None Pharmacology GnRH agonist. After an initial stimulating phase, The pituitary is desensitized to GnRH, which causes it to stop producing LH, which in turn dramatically decreases gonadal production of hormones within one month. Delivery Nasal spray Typical dosage Pre-op 1600mcg/day (2 sprays into each nostril twice a day) Availability Approved by U.S. FDA Indications Central precocious puberty. Endometriosis. Contraindications Hypersensitivity to GnRH, GnRH agonists analogs or any component of the product Adverse reactions
- CNS
- Headache. Insomnia. Mental depression.
- Skin
- Acne. Body odor. Increase of body and facial hair. Itchiness. Itchy, fluid-filled patches of skin. Oily skin. Rash. Vaginal dryness.
- Other
- Chest pain. Fluid retention. Hot flashes. Muscle pain. Nasal irritation. Ovarian cysts. Shortness of breath. Vaginal bleeding.
Comments Leuprolide Acetate
Brand Name Manufacturers Lupron by Tap Generic Manufacturers None company Pharmacology GnRH agonist. After an initial stimulating phase, the pituitary is desensitized to GnRH, which causes it to stop producing LH, which in turn dramatically decreases gonadal production of hormones within one month. Delivery 5, 7.5, 11.25, 15, 22.5mg sustained-release intramuscular injection Typical dosage Pre-op 3.75-7.5mg/month Availability Approved by U.S. FDA Indications Advanced prostate cancer. Endometriosis. Contraindications Hypersensitivity to GnRH or GnRH analogs. Adverse reactions
- CNS
- Anxiety. Delusions. Dizziness. Headache. Hearing disorders. Insomnia. Memory disorder. Nerve disorders. Personality disorder.
- Eyes
- Eye disorders.
- Gastrointestinal
- Anorexia. Constipation. Coughing up blood. Dry mouth. Nausea. Thirst. Vomiting.
- Skin
- Change of facial and body hair. Skin rash.
- Other
- Ankylosing spondylosis. Blood in the urine. Bone and muscle pain. Change in heart electrical activity. Congestive heart failure. Decrease of bone density. Decreased tolerance of protein. Decreased red blood cell count. Decreased white blood cell count. Difficulty urinating. Elevated blood pressure. Elevated LDH. Elevated phosphorus. Escape of blood into the tissues from ruptured blood vessels. Fluid retention. Hair loss. Hot flashes. Increased heart beat rate. Increased uric acid. Increased urination frequency or urgency. Lactation. Liver disorder. Loss of strength. Low blood pressure. Lymphadenopathy. Mild to extreme allergic reaction. Palpitations. Pelvic fibrosis. Penile swelling. Prostate pain. Pulmonary disorders. Respiratory disorders. Temporary increase of hormone production. Temporary suspension of respiration and circulation.
Comments
----- endMedline Articles
These are the articles in Medline containing the words "transsexual" and "hormone" and less than 10 years old, as of 1998 May, courtesy of the U.S. National Institute of Health.
35 citations found
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Basic Endocrinology
- Dr. Susan Love's Hormone Book: Making Informed Choices about Menopause by Susan Love M.D.
- Dr. Susan Love, one of the most important amd reputable doctors addressing women's issues today, helps readers sort through the confusing media reports, complex and contradictory scientific evidence, and medical bias regarding hormone therapy, discussing what is known and not known about it as well as alternatives.
- Endocrinology by Mac Hadley
- Hadley provides an comprehensive coverage of endocrinology, centralizing on the critical roles of chemical messengers and hormones--whether they are of endocrine or neural origin--in the control of physiological processes. This up-t o-date Fourth Edition depicts, through demonstration, the entire human endocrine system in examples designed specifically for premedical and related professional courses. Hadley examines several recently discovered hormones--including their origin , biosynthesis, chemistry, secretion, circulation and metabolism, physiological roles, control of secretion, mechanisms of action and pathophysiology.
- Estrogen by Lila Nachtigall, Joan Rattner Heilman
- Highlighting new, groundbreaking discoveries in hormone replacement therapy's benefits, the nation's foremost authority offers a complete examination of this popular treatment used to counter the negative effects of menopause.
- The Estrogen Alternative: Natural Hormone Therapy With Botanical Progesterone by John Lee, Judi Gerstun, Raquel Martin
- Sylvia Crawley, M.D. reviews The Estrogen Alternative saying "As women become more and more involved in decisions about hormone therapy, this book "serves a vital need. It is very timely and addresses this increasinly complex problem. The dilemma is due, in great part, to the many inconclusive and contradictory studies pubished by traditional medical institutions. It examaines the benefits of natural progesterone supplementation for women of all ages, with the author's shared experiences making THE ESTROGEN ALTERNATIVE even more appealing. She offers educational support for women who wish to participate actively in decisions about their own care. She also presents a challenge to the physicians who, it is hoped, will become more receptive to patients wishing to consider a more natural approach." Joseph A. Randall, M.D. states that this book "has been instrumental in changing the health care I provide to women. Where once I focused on synthetic HRT with estrogen, thinking the benefits outweighed the risks, I now strongly support the use of natural HRT. For example, the book documents the fact that estrogen replacement merely delays but does not prevent osteoporosis. Natural progesterone, with its virtual absnce of side effects, makes sense; and using it in my practice (OB/GYN and fertility) has greatly improved my patient's quality of life."
- Estrogen and Breast Cancer: A Warning to Women by Carol Ann Rinzler
- A statistics-laden, fact-filled chronicle linking the increasing use of estrogen with the growing incidence of breast cancer, plus some solid ideas about remedying the situation. Medical writer Rinzler (Cosmetics, 1977, etc.) adeptly wends her way through a host of scientific studies, translating them into lay language and sorting out their implications. Her take- home message: The estrogen in oral contraceptives, used by millions of young women, and in hormone-replacement therapy, used by millions of older women, promotes the growth of existing tumors and may initiate cancers in susceptible women. Rinzler's story essentially begins with legal approval of the Pill in 1960, but there's also a brief look at how female medical problems were treated in earlier days, including some fascinating medical lore- -e.g., that in 1934, the Merck Manual, a standard reference book of current medical opinion, listed cannabis as a treatment for the symptoms of menopause. Rinzler generally lets the facts speak for themselves, offering no shrill diatribe against pharmaceutical companies or physicians, no easy indictment of the medical establishment. The picture she creates is more complex, since powerful medications such as estrogen are never risk-free, and the benefits always must be weighed against the dangers. Overall, Rinzler's criticisms are validated and her recommendations restrained: Women must be told the truth about estrogen, and those at risk for cancer must be identified; the rules for prescribing estrogen must be tightened; safer alternatives must be found. If the author meets her aim, women won't abandon the Pill or hormone-replacement therapy, but will ask critical questions of their physicians and make informed decisions about the risks they're willing to take. Straight talk--informative and accessible--about a health issue of concern to millions.
- The Hormone of Desire: The Truth About Sexuality, Menopause, and Testosterone by Susan Rako
- "Conditions of testosterone deficiency do exist, need attention, and can be treated," Rako maintains as she draws on her practical experience as a psychiatrist as well as her thorough knowledge of relevant medical literature to discuss the usefulness of small doses of testosterone in helping women through menopause and stimulating positive sexual and psychological feelings. Women produce some testosterone just as men produce some estrogen. Yet many physicians, especially male gynecologists and endocrinologists, believe that giving testosterone to women is unnatural and potentially dangerous. Rako points out, however, that women do not display a simple dose-response curve for such treatment. This means that physicians not only have to overcome feelings of unnaturalness if they wish to aid some of their female patients but also must take the time and effort to match dosage to each individual's need.
- Natural Woman, Natural Menopause : Complete Program for Healthy Menopause by Marcus Laux, Christine Conrad
- Accessible as well as authoritative, Natural Woman, Natural Menopause features the stories of other women who, like Christine Conrad, found that they didn't have to accept less than a completely safe alternative. More important, in Natural Woman, Natural Menopause Marcus Laux and Christine Conrad offer readers their complete plan for long-lasting health and renewed vitality. Following their "Natural Woman Plan," which features the right combination of plant-derived hormones, nutritional supplements, a plant-rich diet, and an exercise program to eliminate and even reverse the effects of bone loss, women will find that not only will they be more energetic and radiant than they thought possible but they will be adding years of good health to their lives.
Advanced Endocrinology
Technical references are generally expensive and special-order. If you are interested, you can search for all books on endocrinology. Of General Interest to Transsexuals
- Body Alchemy : Photographs by Loren Cameron
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- Body Alchemy: Transsexual Portraits is photographer Loren Cameron's intensely personal photo documentary of female-to-male transsexuals (FTMs). A transsexual himself, Loren Cameron brings a sensitive, sophisticated insider's eye to his subject matter. Using documentary style, a series of before-and-after photographs of FTMs in Cameron's transsexual community, his own striking self-portraits, and intimate autobiographical text, he invites the viewer to experience this transformational rite of passage. Body Alchemy includes intimate, narrative photographs of Loren and his partner, Kayt, a lesbian-identified woman whose relationship to Cameron affords her much to say about the fluidity of gender and queer identity. Finally, Body Alchemy includes photographs of genital reconstructions, accompanied by text from three anonymous FTMs who discuss how they feel about their surgeries. Andy Warhol, Robert Mapplethorpe, Dianne Arbus among many others have all trained their lenses on the transgendered figure. Never have the transgendered seriously photographed their own. Not until Loren Cameron, that is.
- Conundrum by Jan Morris
- Ftm : Female-To-Male Transsexuals in Society by Holly Devor
- Holly Devor spent many years compiling indepth interviews and researching the lives of transsexual and transgendered people, many of whom became her friends. She traces the everyday and significant events that coalesce in transsexual identity, culminating in gender and sex transformation. After an introduction which grounds the discussion in historical and theoretical contexts, the author takes a life course approach to understanding female-to-male transsexualism. Using her subjects' own words as illustrations, Devor looks at how childhood, adolescent, and adult experiences with family members, peers, and lovers work to shape and clarify female-to-male transsexuals' images of themselves as people who should be men.
- Gender Outlaw: On Men, Women, and the Rest of Us by Kate Bornstein
- Kate Bornstein has been through some changes--a former heterosexual male, one-time Scientologist and IBM salesperson, now a lesbian woman writer and actress. In this work, she covers everything readers want to know about gender (but are too confused to ask) and takes a witty, incisive look at the radical new politics of sexuality and gender. Also includes Bornstein's play, Hidden: A Gender
- In Search of Eve: Transsexual Rites of Passage by Anne Bolin
- In Search of Eve is an absorbing account of the sociocultural aspects of gender transition. . . . [Bolin] has produced a carefully crafted, clearly written monograph which scholars of both sexuality and gender can profitably read. I would recommend it also for upper-level students in such courses. The book contains many fascinating insights and new findings.
- Sex Changes : The Politics of Transgenderism by Pat Califia
- Pat Califia needs no introduction for lesbian and gay readers. Her writings on sexuality, pornography, censorship, S/M, and other controversial topics have earned her the reputation of a fearless defender of the rights of sexual minorities -- and a fearless intellectual adversary. Sex Changes: The Politics of Transgenderism is Califia's honest, meticulously researched analysis of the contemporary history of transsexuality. Based on in-depth interviews with gender transgressors who "opened their lives, minds, hearts, and bedrooms to the gaze of strangers," Sex Changes demonstrates Pat Califia's hallmark candor and insight. Writing about both male-to-female and female-to-male transsexuals, Califia examines the lives of early transgender pioneers like Christine Jorgenson, Jan Morris, Renee Richards and Mark Rees; partners of transgendered people like Minnie Bruce Pratt; and contemporary transgender activists like Leslie Feinberg and Kate Bornstein. Includes bibliography, resources, index. Pat Califia is well-known as a sharp critic of repressive American attitudes toward gender, sexuality and pornography. She is the author of many books, including Public Sex: The Culture of Radical Sex. Califia lives in San Francisco, where she works as a therapist, primarily serving the gay/lesbian and transgendered communities.
- Read My Lips : Sexual Subversion and the End of Gender by Riki Anne Wilchins
- Over the course of the past decade transgender politics have become the cutting edge of sexual liberation. While the sexual and political freedom of homosexuals has yet to be fully secured, questions of who is sleeping with whom pale in the face of the battle by transgender activists to dismantle the idea of what it means to be a man or a woman. Riki Anne Wilchins's Read My Lips is a passionate, witty, and extraordinarily intelligent look at how society not only creates men and women--ignoring the fluidity of maleness and femaleness in most people--but also explains how those categories generate crisis for most individuals. It is impossible to read Wilchins's ideas and not be provoked in fundamental and mysterious ways.
- Transgender Care : Recommended Guidelines, Practical Inforrmation, and Personal Accounts by Gianna Israel, Donald Tarver
- By empowering clients to be well-informed medical consumers and by delivering care providers from the straitjacket of inadequate diagnostic standards and stereotypes, this book sets out to transform the nature of transgender care. In an accessible style, Gianna Israel and Donald Tarver discuss the key mental health issues, with much attention to the vexed relationship between professionals and clients. They propose a new professional role, that of "Gender Specialist." The book contains a wealth of practical information and accounts of people's experiences about coming out to one's employer or to one's friends or spouse. Several essays spell out the legal rights of transgender people with regard to insurance, work, marriage, and the use of rest rooms. The second part of the book consists of thirteen essays on a range of controversial topics.
- Transsexuals: Candid Answers to Private Questions by Ramsey Gerald, Phd
- This is a great resource book for anyone trying to decide if they are really male-to-female or not. For those getting ready to step out of the closet this book will likely answer many of the questions your going to be asked by family and friends. It is also loaded with facts and figures, a detailed description of what to expect when going to a Gender Identity committee for the first time, and a complete listing of the Standards of Care by the Harry Benjamin International Gender Dysphoria Association, Inc.
- True Selves : Understanding Transsexualism for Families, Friends, Coworkers, and Helping Professionals by Mildred Brown, Chloe Rounsley
- What is it like to grow up in the wrong body? Are transsexuals considered homosexuals? Filled with real-life stories, actual letters, and touching poems, True Selves paints a heartfelt portrait of the risk-taking, confusion, and--ultimately--the courage that transsexuals face as they struggle to reveal their true being to themselves and to others.
Other Web Sites
- Bajamar Women's Healthcare Pharmacy
- http://www.thorcomp.com/bajamar/
- Gonadotrope Cytochemistry by Gwen Childs, PhD
- http://cellbio.utmb.edu/childs/gon1.htm
- Hormones and Heart Disease by Rebecca Anne Allison, MD
- http://www.primenet.com/~beckster/hormheart.html
- Hormone Treatment in Transsexuals by Henk Asscheman, MD and Louis J.G. Gooren, MD
- http://www.geocities.com/WestHollywood/Village/5046/hrt.htm
- Medline Search by the National Institute of Health
- http://www.ncbi.nlm.nih.gov/Entrez/medline.html
- Menopausal Hormone Replacement Therapy and Cancer Risk by the National Cancer Institute
- http://imsdd.meb.uni-bonn.de/cancernet/600310.html
- RXMed
- http://www.rxmed.com
- [Scalp Hair] Regrowth Reference by John Ertel
- http://www.regrowth.com/reference/
- Standards of Care by the Harry Benjamin International Gender Dysphoria Association
- http://www.symposion.com/ijt/ijtc0405.htm
- Transsexual Women's Resources: Hormone Therapy by Anne Lawrence, MD
- http://www.mindspring.com/~alawrence/hormoneindex.html
- U.S. FDA Personal Use Import Policy by the Cognitive Enhancement Research Institute
- http://www.ceri.com/import.htm
- United States Pharmacopeia
- http://www.usp.org
- Women's International Pharmacy
- http://www.wipws.com
