Exactly what hormones are available? What Are the Details On Popularity, Dosage, Availability, Contraindications, Adverse Effects, Etc.?

Hormone dosages are determined mainly from verbal advice of medical doctors, second-hand anecdotes, and personal experience. Post-op hormone dosages are also influenced by the Physician's Desk Reference (PDR) according to the recommendation of hormone replacement of normal gonadal hormone production. Of the injectable hormones and anti-hormones available, only those that are sustained-release (requiring injection less frequently than once per week) are listed.

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

Parenteral Safety

Oral Safety

Source

Estradiol

Excellent

Good

Synthetic (plant-based)

Estradiol Valerate

Excellent

Good

Synthetic (plant-based?)

Estradiol Cypionate

Good

n/a

Synthetic (plant-based?)

Quinestrol

n/a

Fair

?

Estropipate

n/a

Fair

Synthetic (plant-based)

Esterified Estrogens

n/a

Fair

Synthetic (plant-based)

Conjugated Estrogens

n/a

Fair

Live animals

Ethinyl Estradiol

n/a

Poor

Synthetic

Popular estrogens

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:

Name

Safety

Source

Progesterone

Excellent

Yams or Soy Beans

Hydroxyprogesterone Caproate

Good

Synthetic

Dydrogesterone

Good

Synthetic

Medroxyprogesterone Acetate

Fair

Synthetic

Norethindrone Acetate

Fair

Synthetic

Popular progesteronic compounds

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:

Name

Safety

Efficacy

Spironolactone

Excellent

Good

Finasteride

Excellent

*

Cyproterone Acetate

Fair

Excellent

Popular anti-androgens

*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 pre-op 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

Anti-hormones

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