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HORMONE THERAPY: HRT MEDICATIONS SUMMARY

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NOTE: The information on this page and the pages for each medication were originally published online at www.savina.com in the "FAQ: Hormone Therapy for M2F Transsexuals" by Confluence Publications. The aforementioned web site seems to have folded, however. The new definitive location for the FAQ is www.gender-id.com, but the following detailed drug information is not included at the new site. As this information is highly sought after in the Transgender Community a copy of a portion of that FAQ is being reprinted here. Information not included in the original has also been added.

Estrogens

    The following estrogens are popular for treatment of male-to-female transsexuals:

    Name Safety and Efficacy Source
    Estradiol Valerate Excellent Synthetic (plant-based?)
    Estradiol Cypionate Good Synthetic (plant-based?)
    Estradiol Good Synthetic (plant-based)
    Ethinyl Estradiol Fair Synthetic
    Quinestrol Fair ?
    Estropipate Fair Synthetic (plant-based)
    Esterified Estrogens Fair Synthetic (plant-based)
    Conjugated Estrogens Fair Live animals or synthetic
    Table 1: 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 Efficacy Source
    Micronized Progesterone Excellent Highly variable Yams or Soy Beans
    Hydroxyprogesterone Caproate Good Variable Synthetic
    Dydrogesterone* Good Variable Synthetic
    Medroxyprogesterone Acetate Fair Variable Synthetic
    Norethindrone Acetate Fair Variable Synthetic
    Table 2: 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.

    * 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.

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 Action
    Spironolactone Excellent Good DHT Blocker
    Finasteride Excellent Good (1) Type II 5-AR Inhibitor
    Dutasteride Excellent Excellent (2) Type I & II 5-AR Inhibitor
    Micronized Progesterone Excellent Variable 5-AR Inhibitor (3)
    Cyproterone Acetate Fair Excellent Testosterone Blocker
    Flutamide Fair (4) Excellent Testosterone Blocker
    Bicalutamide Fair Good Testosterone Blocker
    Table 3: Popular anti-androgens

    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.

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).

    Name Safety and Efficacy
    Goserelin Acetate Excellent
    Nafarelin Acetate Excellent
    Leuprolide Acetate Fair
    Table 4: Anti-hormones


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