The following estrogens are popular for treatment of male-to-female transsexuals:
|
Name |
Safety and Efficacy |
Source |
|
Excellent |
Synthetic (plant-based?) |
|
|
Good |
Synthetic (plant-based?) |
|
|
Good |
Synthetic (plant-based) |
|
|
Fair |
Synthetic |
|
|
Fair |
Synthetic |
|
|
Fair |
Synthetic (plant-based) |
|
|
Fair |
Synthetic (plant-based) |
|
|
Fair |
Live animals or synthetic |
|
|
Table 1: Popular estrogens |
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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.
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:
|
Name |
Safety |
Efficacy |
Source |
|
Excellent |
Highly variable |
Yams or Soy Beans |
|
|
Good |
Variable |
Synthetic |
|
|
Good |
Variable |
Synthetic |
|
|
Fair |
Variable |
Synthetic |
|
|
Fair |
Variable |
Synthetic |
|
|
Table 2: Popular progesteronic compounds |
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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.
* Dydrogesterone detail page is not as complete. It was missing on the source site from which this FAQ was copied. Nonetheless I have done my best to locate information on this drug and provide a data sheet on it in similar format to the others. If I ever locate the missing original page I'll replace mine with it. - GID.info Editor
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.
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 |
Action |
|
Excellent |
Good |
DHT Blocker |
|
|
Excellent |
Good (1) |
Type II 5-AR Inhibitor |
|
|
Excellent |
Excellent (2) |
Type I & II 5-AR Inhibitor |
|
|
Excellent |
Variable |
5-AR Inhibitor (3) |
|
|
Fair |
Excellent |
Testosterone Blocker |
|
|
Fair (4) |
Excellent |
Testosterone Blocker |
|
|
Fair |
Good |
Testosterone Blocker |
|
|
Table 3: Popular anti-androgens |
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Table 6 Note 1: 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 because it blocks Type 2 5-Alpha-Reductase activity.
Table 6 Note 2: Dutasteride also is not a general anti-androgen. Like finasteride it reduces DHT associated with excessive body hair and male-pattern balding. In clinical studies Dutasteride has been found much more effective at inhibiting both Type 1 and Type 2 5-Alpha-Reducatase enzymes.
Table 6 Note 3: It was not clear to me if Micronized Progesterone blocks both Type I and Type II 5-AR or not, but I'm assuming that it does block both or there wouldn't be a progesterone receptor on each of those enzymatic isoforms. As one form exists primarily in skin and the other in organs the method of administration may be the key to determing efficacy. Oral administration will effect systemic Type II 5-AR inhibition, while theoretically transdermal progesterone would target Type I 5-AR inhibition at the skin level. These are only my guesses, I could not find any definitive studies.
Table 6 Note 4: Flutamide can be very liver toxic to some people, especially at high doses and should be used with caution under a doctor's supervision. Reportedly the newly available Flutamide Gel is safer because it does not have to first pass through the liver to enter the bloodstream.
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.
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).
|
Name |
Safety and Efficacy |
|
Excellent |
|
|
Excellent |
|
|
Fair |
|
|
Table 4: Anti-hormones |
|
Top of Form
|
Brand Name Manufacturers |
Delestrogen
by B.M. Squibb |
|
Generic Manufacturers |
Goldline
|
|
Pharmacology |
Ester 17b of estradiol with same effect as endogenous estrogen |
|
Delivery |
1,
2mg oral tablets. |
|
Typical dosage |
Pre-op
15-40mg/2wks or 7-20mg/1wk injection |
|
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. |
Top of Form
|
Brand Name Manufacturers |
Depo-Estradiol by Pharmacia/Upjohn |
|
Generic Manufacturers |
Depogen
by Hyrex |
|
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 |
|
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 1997 pdr generics book shows a 1:10 ratio of cypionate:valerate ovarian failure replacement dosages. This has been roughly confirmed in the limited anecdotal evidence gathered from transsexuals. |
Top of Form
|
Brand Name Manufacturers |
Almedion
by ? |
|
Generic Manufacturers |
Apothecon
|
|
Pharmacology |
17b estradiol with same effect as endogenous estrogen |
|
Delivery |
Oral
tablets 0.5, 1, 2mg |
|
Typical dosage |
Pre-op
oral 4-8mg/day, 2-4 film patches 0.1 changed twice weekly |
|
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. |
Top of Form
|
Brand Name Manufacturers |
Estinyl
by Schering |
|
Generic Manufacturers |
None |
|
Pharmacology |
Synthetic estrogen. Acts on receptors apparently the same as endogenous estrogen but is more potent because the liver cannot break it down as quickly. |
|
Delivery |
Oral
0.02mg, 0.05mg, 0.5mg tablets |
|
Typical dosage |
Pre-op
0.1-0.25mg/day |
|
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 Dizziness. Headache. Mental depression. Migraine. Spasms of limb and facial muscles. Eyes Steepening of corneal curvature. Intolerance to contact lenses. Gastrointestinal Abdominal cramping. Bloating. Cholestatic jaundice. Skin Blotchy skin pigmentation. Blood eruptions from the skin. Easy bruising. Increase of body and facial hair. Loss of scalp hair. Red skin patches from capillary congestion. Other Decreased glucose tolerance. Fluid retention. Increased sensitivity to light. Increased serum calcium level. |
|
Comments |
More thrombosis events seem to be associated with ethinyl estradiol than any other form of estrogen, probably because of its very long half-life (with resulting hepatic recirculation) and popularity in birth-control preparations. If you must take it because it is the only estrogen you can possibly obtain, use the lowest dosage you can. Unfortunately, a safe dosage is individual and almost unpredictable: some women have suffered thrombosis on 0.035mg/day, some transsexuals have survived 1mg/day. The 0.5mg tablets are reportedly no longer manufactured, and remaining stock is rapidly disappearing from the warehouses and pharmacies. In the opinion of the author, it is an excessive daily dose anyway. |