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: estrogen, progesterone, and testosterone. A small quantity of testosterone is also produced by the adrenal gland. Proportionally, females have more estrogen and progesterone than males; males have more testosterone.
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.
Progestins/progestagens/gestagens (synonyms) are synthetic progesterone analogues. Progesterone and progestins excite progesteronic receptors, which in cooperation with estrogenic activity, cause the body to further differentiate into female form and function.
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.
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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 genitals opposite those of birth. However, postnatal contrasexual hormone therapy does cause development of secondary sex characteristics as subsequently described in this document.
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. Note, also, that if the androgens are at the bottom end of the scale, then libido and overall energy will likely be lacking as well.)
There are dramatic cyclic and individual variations of estrogen (simple sum of estradiol and 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 or estradiol, you will not be able to accurately judge the results of a blood test.
Unfortunately, serum hormone levels cannot be used as a foolproof device for titrating exogenous hormone dosage, because there is no widely available test for sensitivity to the hormones, which varies considerably between individuals. Levels should be considered a means rather than a goal. After all, M2Fs undergo hormone therapy for transformation of secondary sexual characteristics, and do not have ovaries or a uterus which would impose obvious limitations on hormone levels; non-male-to-female women have entirely different reasons for undergoing hormone replacement therapy which generally requires only a low (endogenous) level.
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 yecount 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. However, this should not be counted on for birth control, because a miniscule sperm count might remain until the testes are surgically removed. Estrogens, progesterone, progestins, 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.
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 generally takes longer if the testes are not removed. These timelines are generalizations based on what many people have reported, but do not necessarily mean that everyone will find development (or reversibility) to be within these limits. 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 ar 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.
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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 migrate away from the waist and toward the hips and buttocks.
-
Body hair growth (not including head, face, or pubic area) generally slows, becomes less dense, and may lighten in color.
-
Blotches (cloasma) appear on the skin of some people during hormone therapy. This is the same effect as the "mask of pregnancy" and probably related to other dermal changes as noted below.
Many people also report the following effects, but they are not verified in any medical literature that the author has read:
-
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. Sometimes, tear glands also become less active, resulting in dryer eyes, which can cause some discomfort for those who wear contact lenses. Dermal gland activity trends can generalized with the formula (A+P)/E where A = androgens, P = progesterone and progestins, and E = estrogens. Synthetic estrogens seem to be especially likely to reduce activity.
-
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.
-
Fingernails become thinner and more brittle.
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Body odors (skin and urine) change. They become less "tangy" or "metallic" and more "sweet" or "musky".
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If exercise is not increased, some muscle tone is lost.
-
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.
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Some middle-aged and older transsexuals who start or resume hormone therapy report improved memory and overall mental faculty.
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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 been occasionally reported that sensitivity to air-born allergens decreases.
Female hormones do not:
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Cause the voice to increase in pitch.
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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:
|
|
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
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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
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B
|
Administer consistently low dosage of estrogens
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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
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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 but extremely important 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 little development after, say, 6 months of hormone therapy, then consider using gross empirical results, e.g., breast growth and fat redistribution, as the primary rather than secondary indicator, provided ones health (especially blood clotting and liver function) 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:
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. Post-ops rarely find any antiandrogen useful except for finasteride. Of transsexuals taking estrogen, those who are older than 25 or so seem to find the anti-androgen much more important than those who are younger.
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2
|
Add progesterone or progestin
|
Progesterone administered with estrogen helps promote breast growth: estrogen stimulates cell mitosis and growth of the ductal system, while lobular development and differentiation seems to be dependent on progesterone (breast fat accretion seems to require both). Progesterone consistently administered with estrogen seems to reduce the risk of fibrosis, cysts, and cancer from administration of estrogen alone. On the other hand, synthetic progesterone (progestins) can partly reverse the lipid (cardiovascular) benefits of estrogen. Moreover, progestins have a slightly androgenic effect in some people, and apparently can even antagonize estrogen absorption. Non-synthetic progesterone (as opposed to a progestin) is very rarely reported to have any adverse effect, and seems to provide a healthier balance for an aggressive estrogen dosage, as well as improving libido and overall energy level.
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3
|
Add another estrogen
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This may cause faster results for some people, but generally not better results in the long run.
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Table 2: Coadministration philosophies
It is possible to vary the hormone dosages on a monthly basis so as to roughly mimic a female menstrual cycle.
Cycling hormones before removal of the testes is not recommended. The gonadotropin axis (feedback mechanism) is already precarious in a pre-op under hormone therapy; small fluctuations in the hormone regimen can translate into large variations in the endogenous androgen level, causing significant physical and emotional discomfort.
Cycling in post-ops is a more interesting topic. Unfortunately, therapy results are even more difficult to evaluate than the usual non-cycling hormone therapy, due to the increase in variables and decrease in objective data.
There is mounting anecdotal evidence, and the theory put forth by at least one reputable endocrinologist, that estrogen receptors can become saturated, temporarily reducing the sensitivity and/or quantity of available receptors. If that is the case, then giving the receptors a rest would improve hormone therapy results. For example, many people have reported a significant surge in breast development when estrogen dosage is sharply increased after months or even years of a very conservative dosage. In some cases, the surge in development continues for quite a few months if the estrogen is cycled. Development often trails off again after 3-6 months, after which, it seems that another, or longer, rest is called for.
Cycling is worth trying for those post-ops who have not achieved significant breast development (sub-A cup). If the estrogen boosts are administered via intramuscular injection or transdermal film, and the patient has no history of adverse reactions to hormones (e.g., blood clotting or prolactin problems), it is generally considered to be a safe experiment.
If one is going to cycle, given the current lack of data to suggest otherwise, one may as well more or less mimic a 28 day female cycle, rather than picking another cycle out of the air. This can be roughly achieved by intramuscular injection of estrogen in oil on day 1, then taking another shot of 1/2 dosage on day 13. Some people will experience menopausal symptoms (hot flashes, night sweats, severe mood swings, etc.) in the days proceeding each shot; if the discomfort is unacceptable, a small, constant dosage of oral or transdermal estrogen can be used to provide a "floor" serum estrogen level. If progesterone is part of the regimen, it can be cycled by intramuscular injection in oil on day 8, or by ramping it orally from days 1-14 with the peak on day 8. Some say that cycling the progesterone is more important than cycling the estrogen; other say that the progesterone must be constant to best avoid breast cancer. Of course, many variations are possible. There is no formula better for a transsexual than "do what works." If enough people report that a different cycle is more appropriate, that will be reflected here in the future.
Estradiol cypionate probably has a longer half-life than estradiol valerate. If ev is not available but ec is, consider eliminating the oral/transdermal floor, as it might not be necessary.
Cycling in this manner usually results in at least some noticable development for 1-3 months, then the rate of improvement generally trails off in an asymptotic curve. In any case, one should revert to a very conservative regimen for 3-6 months (whether it be either low-dosage non-cycling or low-dosage cycling) before trying again. If one does not achieve any result whatsoever from cycling within a few months of starting, it will likely not help to continue the cycling.
Aggressive cycling is meant to facilitate bursts in development, and is not appropriate for pre-ops or lifetime maintenance. However, lifetime post-op cycling can be done safely with more conservative dosages.
For reference--endogenous androgens in genetic women generally peak just before ovulation and again just before menstruation--that is, on roughly days 13 and 27 of the cycle as defined in this document.
Exactly what hormones are available? What Are the Details On Popularity, Dosage, Availability, 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:
Estradiol Valerate
Brand Name Manufacturers
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Delestrogen by B.M. Squibb
Dimenformon Prolongatum?
Progynova by Schering
Progynon-Depot by Schering, Germany
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Generic Manufacturers
|
Goldline
Gynogen by Forest
Major
Schein
Steris
Valergen by Hyrex
|
Pharmacology
|
Ester 17b of estradiol with same effect as endogenous estrogen
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Delivery
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1, 2mg oral tablets.
Sustained release intramuscular injection.
|
Typical dosage
|
Pre-op 15-40mg/2wks or 7-20mg/1wk injection
Pre-op 6-12mg/day oral
Post-op 10-30mg/2-4wks injection
Post-op 2-6mg/day oral
|
Availability
|
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. Estradiol undecylate has a longer chain length than estradiol valerate; its action is therefore prolonged, and smaller dosages are probably appropriate. The author does not have enough information to make any other comments about estradiol undecylate except that it will reportedly go out of production soon due to the side effect of "excessive feminization" for its only labeled usage, prostate cancer.
If you are allergic to any nut oil, be sure to ask your pharmacist about the base, especially for the generic form of this drug. Castor oil is most often employed, which few people are sensitive to, but a few pharmacies employ other oils such as sesame, because it is less viscous and easier to run through their equipment.
|
Estradiol Cypionate
Brand Name Manufacturers
|
Depo-Estradiol by Pharmacia/Upjohn
|
Generic Manufacturers
|
Depogen by Hyrex
Dep-gynogen by Forest
Estro-cyp by Keene
Goldline
Moore
Rugby
Steris
|
Pharmacology
|
Ester with estradiol same effect as endogenous estrogen
|
Delivery
|
Sustained release intramuscular injection, 5mg/ml
|
Typical dosage
|
Pre-op 1.5-4mg/2wks injection
Post-op 1-3mg/2-4wks 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
|
|
Estradiol
Brand Name Manufacturers
|
Almedion by ?
Aquadiol by ?
Climara by Berlex Labs (film)
Dermestril by ? in Italy
Estraderm by Ciba (film)
Estrace by B/M Squibb (oral)
Estrafem by Novo Nordisk in Denmark
Estrovite by ?
Follicyclin by ?
Gynoestryl by ?
Menorest by ?
Oestrogel by ?
Ovociclina by ? in Italy
Ovocyclin by ?
Profoliol B by ? in Switzerland
Vagifem by ?
Vivelle by Ciba (film)
Zumenon by Solvay
|
Generic Manufacturers
|
Apothecon
Geneva
Goldline
Major
Moore
Qualitest
Rugby
Watson
|
Pharmacology
|
17b estradiol with same effect as endogenous estrogen
|
Delivery
|
Oral tablets 0.5, 1, 2mg
Extended release film 0.0375, 0.05, 0.075, 0.1mg/24hrs
Vaginal cream and suppositories.
|
Typical dosage
|
Pre-op oral 4-8mg/day, 2-4 film patches 0.1 changed twice weekly
Post-op oral 1-4mg/day, film 0.05 or 0.1 changed twice weekly - weekly
Need more data about typical cream and suppository dosage and absorption.
|
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 Climara and Vivelle films reportedly lasts longer, and probably deliver more, than the Estraderm brand.
|
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/wk
|
Availability
|
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
Watson
|
Pharmacology
|
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/day
|
Availability
|
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 Solvay
|
Generic 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 2.5-10mg/day
Post-op 0.625-5mg/day
|
Availability
|
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 0.625-3.75mg/day
|
Availability
|
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 killed. This treatment has not been directly witnessed by the author. However, Redwings Horse Sanctuary, World Society for the Protection of Animals, and others have researched this issue, interviewed Wyeth-Ayerst representatives, and directly inspected the farms in question. Furthermore, Wyeth-Ayerst has aggressively blocked every attempt other drug companies have made to obtain FDA approval to sell a synthetic generic equivalent, based on the argument that those generics cannot possibly be equivalent--because they do not contain the same organic impurities.
|
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 reason this document specifies estradiol cypionate as potentially less safe than estradiol valerate is that ec is much stronger and longer-lived, putting the author in mind of the stimulation of liver-based enzyme/clotting factors--and attendant thrombosis risk--when recirculated many times like ethinyl estradiol. Plain (natural) estradiol is also be considered excellent in safety if delivered via a non-oral method.
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.
Progesterone and Progestins
The following progesteronic compounds are popular for treatment of male-to-female transsexuals and are presented in descending order of preference in the humble opinion of the author:
Progesterone
Brand Name Manufacturers
|
Cyclogest by LD Collins in the U.K.
Gestone by ? in the U.K.?
Prometrium by Schering in Canada
Prometrium by Solvay Pharmaceuticals
Utrogestan by Besins-Iscovesco in France
Progesteronum by ? in Poland
|
Generic Manufacturers
|
Compound pharmacies advertising unbranded progesterone on the web include Bajamar Women's Healthcare Pharmacy and Women's International Pharmacy.
|
Pharmacology
|
Suspension of progesterone in oil. This is the same molecule as produced endogenously in females, not a progestin.
|
Delivery
|
Capsules.
Vaginal cream and suppositories.
|
Typical dosage
|
Pre-op 100-400mg/day capsules in conjunction with estrogens.
Post-op 50-400mg/day capsules in conjunction with estrogens.
Need more data about typical cream and suppository dosage and absorption.
|
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
|
Those allergic to peanuts, beware: Prometrium uses a peanut oil medium. Compounding pharmacies supplying non-branded progesterone may also use peanut oil; ask them if you need to know.
Some people call this drug progesterone USP/PharEu/BP (according to the local regulatory commission), to differentiate from progestins. In some countries the drug is simply referred to as progesterone.
The largest fraction progesterone taken orally is destroyed in the digestive tract, which, along with the very short half-life, accounts for the high dosage in comparison to synthetics, and may also account for some of the variability in efficacy.
|
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
Steris
|
Pharmacology
|
Progestogen (progesterone derivative)
|
Delivery
|
125 and 250mg/ml sustained-release intramuscular injection
|
Typical dosage
|
125mg-250/2-4wks 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. Retinal blood clots. Inflamed optic nerves.
- 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
|
|
Dydrogesterone
Brand Name Manufacturers
|
Duphaston by Solvay
|
Generic Manufacturers
|
|
Pharmacology
|
Progestin (progesterone derivative)
|
Delivery
|
5, 10, 20mg tablets
|
Typical dosage
|
Pre-op 5-20mg/day
Post-op 2.5-10mg/day
|
Availability
|
Approved in the U.K. Rejected by U.S. FDA.
|
Indications
|
Endogenous progesterone deficiency. Unopposed estrogen replacement therapy. Premenstrual syndrome. Menstrual abnormalities. Endometriosis. Infertility. Undesired spontaneous abortions.
|
Contraindications
|
None.
|
Adverse reactions
|
Nausea. Breast tenderness. Headache. Bloated feeling. Transient dizziness. Skin reactions.
|
Comments
|
|
Medroxyprogesterone Acetate
Brand Name Manufacturers
|
Amen by Carnrick
Curretab by Solvay
Provera and Depo-Provera by Pharmacia/Upjohn
|
Generic Manufacturers
|
Cycrin by Esi Lederle Generics
Geneva
Goldline
Greenstone
Intl Labs
Major
Martec
Moore
Parmed
PD-RX
Qualitest
RID
Rosemont
Rugby
Schein
URL
Warner Chilcott
|
Pharmacology
|
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. Retinal blood clots. Inflamed optic nerves.
- 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, 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
- Retinal blood clots. Inflamed optic nerves.
- 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
|
|
Dydrogesterone and hydroxyprogesterone caproate are both synthetic analogues of progesterone. This makes them less objectional than other progestins on the market, which seem to be more closely analogued to testosterone.
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 progesterone, 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:
Spironolactone
Brand Name Manufacturers
|
Aldactone by Searle
Spironolacton by ? in Bulgaria
Uractone by ? in Italy
Verospiron by ? in Hungary
|
Generic Manufacturers
|
Caremark
Cheshire
Geneva
Goldline
Heartland
Major
Moore, H.L.
Mutual
Mylan
Parmed
PD-RX
Purepac
Qualitest
Raway
Rugby
UDL
URL
Vanguard
|
Pharmacology
|
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 100-400mg/day
Post-op 50mg/day
|
Availability
|
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 Merck
|
Generic 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 (and speaking of minoxidil: note that a few people have reported that it seemed to have a systemic effect, in that it increased body hair even though it was applied only to the scalp).
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 intersexed genital expression 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 progestin.
|
Delivery
|
10mg, 50mg oral tablets
|
Typical dosage
|
Pre-op 10mg/wk-100mg/day (See comment below)
Post-op not recommended
|
Availability
|
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. Elevated prolactin level. Pituitary size increase. 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.
There are some reports of depression when the dosage is too high for a given individual. There appears to be a causal relationship because the depression evidently disappeared as soon as the dosage was reduced, according to those reports.
|
*Although it is not a general anti-androgen, finasteride coadministered with estrogen, topical minoxidil 5%, and topical Retin-A, is very helpful to halt--and in some cases, partly reverse--male-pattern baldness. Many people report that finasteride 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:
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
|
|
The point of this faq is to be a reference for the popular range of transsexual hormone therapies. Specific recommendations are not easy to make, because individual responses and constraints are so variable. As such, this faq seems too vague for many readers, who produce the remaining most frequent question:
"All of this is quite interesting, but I am a healthy individual, and would really appreciate a specific suggestion. Understanding that adjustments for my situation can be made as I go, what is a good guideline?"
Obligatory reiteration of 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 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.
Subject to the above disclaimer, the context of this entire document (especially the sections on
-
Month 1: Begin twice-monthly injections of 20mg
-
Month 2: Given continued health, add anti-androgens: 100mg/day
-
Month 3: Given continued health, add progesterone or progestin: 200mg/day oral
-
Month 4: If breasts are not yet developing (budding), given continued health, increase estrogen dosage to the following: twice-monthly injections of 40mg estradiol valerate, or 4mg estradiol cypionate. Also, take 1-3mg/day sl-oral estradiol or 2-4mg/day sl-oral estradiol valerate or a single 0.075-0.1mg transdermal estradiol film changed weekly. If these injectables are not available, employ 2 0.1mg transdermal estradiol films changed twice weekly, offset (e.g., change the first film monday morning and thursday evening; change the second film wednesday morning and saturday evening), or 6mg/day sl-oral estradiol, or 9mg/day sl-oral estradiol valerate. Note that injectables or films are much preferable to administration of the entire estrogen therapy orally. Do not increase estrogen at this time if there is currently progress in breast development.
-
Month 5: If androgens are still a problem (continued scalp hair recession, frequent spontaneous erections, etc.), given continued health, increase antiandrogens to the following: 200mg/day spironolactone plus larger fractional tablet (0.1-1mg)/day finasteride. If spironolactone is not available but cyproterone acetate is, employ 25mg/day cyproterone acetate.
-
Month 6: If breasts are not yet developing, given continued health, increase progesterone/progestin dosage to the following: 300-400mg/day oral progesterone, or twice-monthly injections of 125mg hydroxyprogesterone caproate, or 20mg/day sl-oral dydrogesterone.
-
Month 7: If breasts are not yet developing, given continued health, increase estrogen dosage to the following: twice-monthly injections of 60mg estradiol valerate, or 6mg of estradiol cypionate. Also, take 2-4mg/day sl-oral estradiol or 3-6mg/day sl-oral estradiol valerate or a single 0.1mg transdermal estradiol film changed every 4-7 days. If these injectables are not available, employ 3-4 0.1mg transdermal estradiol films each changed twice weekly, offset, or 8mg/day sl-oral estradiol, or 12mg/day sl-oral estradiol valerate (do not attempt to run up the oral doses in the same ramp as other deliveries; if this dose of orals is not doing the job, it is quite unlikely that adding more will help). Do not increase estrogen at this time if there is currently progress in breast development.
-
Month 8: If androgens are still a problem, given continued health, increase antiandrogens to the following: 300-400mg/day spironolactone plus larger fractional tablet (~0.25-2.5mg)/day finasteride. If spironolactone is not available but cyproterone acetate is, employ 50mg/day cyproterone acetate.
-
Given continued health, keep on with this regimen, or adjust as appropriate (titrating downwards, preferrably) for up to 3 years. After that, if one cannot--or does not wish to--obtain orchidectomy or full srs, it is still best to reduce oral estrogen, progestins, and cyproterone acetate after 3 years. Estradiol via injection and film is relatively safe, as is progesterone.
-
Srs minus 1 month: Stop progestins and sl-oral estrogen.
-
At orchidectomy or srs: Stop all estrogens, antiandrogens and progesterone. Beginning 1-2 weeks after, employ a single 0.075mg transdermal estradiol film changed weekly, or 2mg/day sl-oral estradiol, or 3mg/day sl-oral estradiol valerate, or an injection of 15mg estradiol valerate or 1.5mg estradiol cypionate once per 3 weeks. Keep this simple regimen for 3 months to allow time for adjusting to the abrupt reduction of endogenous androgens (unless one was on an effective GnRH agonist course, in which case gonadal androgen production was already shut down).
-
3 months after testes are removed: If menopausal symptoms are noted just before the injection, either increase the frequency of the shots to twice monthly (reducing the dose of each shot, respectively, to 10mg ev or 1mg ec), or add 1mg/day sl-oral estradiol or 2mg/day sl-oral estradiol valerate. If menopausal symptoms are continual, increase the dosage ~50% each month until the symptoms disappear, or at least are tolerable. An alternative, and perhaps safer way to deal with menopausal symptoms and/or low energy, is to add progesterone or a progestin: 100mg/day progesterone or 5mg/day sl-oral dydrogesterone.
-
If one has not attained significant feminization (still using breast growth as the most obvious measuring device, but keeping in mind the modest expectations which are required in this matter), and no progress whatsoever is noted after the testes have been removed for 6 months, try aggressive cycling for 3 months timed as outlined in the
-
If scalp hair continues to recess, try a fractional tablet (0.05-0.5mg)/day finasteride for several months. If it stalls the recession, continue taking it for a year, then stop for a few months to see what happens. If recession resumes, then restart the finasteride and consider yourself a lifetime customer.
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For lifetime maintenance, use the lowest dosages consistent with skeletal and mental health. Lifetime cycling feels right for some people, and is safe as long as it is done with conservative dosages, for example, with timing as described in the philosophy section, and the following peak dosages: 0.075mg-0.1 transdermal estradiol film, or 2-4mg/day sl-oral estradiol, or 3-6mg/day sl-oral estradiol valerate, or 10-20mg injectable estradiol valerate or 1-2mg injectible estradiol cypionate. If progesterone or a progestin is included, peak at 200-400mg/day oral progesterone, or 125mg injectable hydroxyprogesterone caproate, or 10mg/day sl-oral dydrogesterone. Only exceed these peaks on a long-term basis if absolutely necessary. Be especially wary of oral estrogens and progestins. Between peaks, if using orals or films, run the troughs down to as close to zero as you can without causing significant emotional or physical discomfort. The effects at post-op levels are subtle; observe yourself closely to determine what is the most healthy for your individual case.
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If you are post-op more than a couple of years, and find yourself devoid of energy, stamina, motivation, and libido, even when you are on what seems to be the best possible lifetime estrogen/progesterone regimen, consider this: after ruling out purely psychological issues, you might need a subtle boost of testosterone. As perverse as that might sound after spending years fighting the evil T, some post-ops find that residual endogenous androgen production (mainly from the adrenal glands) is just not quite enough to sustain a high level of activity. Some genetic women have the same problem. If this bothers you enough to do something about it, take a tiny daily dose of testosterone. Unfortunately, it can be difficult to find low-dosage preparations, especially to be funded by your national or commercial health plan. 0.25-1.0mg/day of oral fluoxytestosterone or 0.5-2mg/day oral methyltestosterone can do the trick, but tablets are especially difficult to obtain because of laws meant to prevent the abuse of anabolic steroids. Some people cover at least 3/4 of the active surface of a testosterone transdermal film before wearing it (rotating the barrier as needed), or else open the film and apply a small amount of the gel each day. It is also possible to have a compounding pharmacy add 5-10mg of micronized testosterone to a custom estrogen and/or progesterone capsule or pessary. If you prefer to cycle, take into account that endogenous androgens in genetic women generally peak just before ovulation and again just before menstruation--that is, on roughly days 13 and 27 of the cycle described in the