Information Accuracy and Risks of HRT


This article compares recommendations from medical and non-medical sources and explains conditions that could result from HRT, whether therapy is medically monitored or not.

This information is not provided or intended as a substitute for professional medical advice or care.

I am not a medical professional. Please also note that the glossary at the end of this article is just that: a glossary and not a dictionary.

The descriptions of the terms in the glossary are meant to help you interpret their use in this article only and are not comprehensive definitions.

*Related article: 5 MTF HRT Body Changes You Shouldn’t Expect When Transitioning

MTF Hormone Dosage

There are no generally agreed-upon recommended dosages or recommended drugs within categories. The following recommendations are based on three sources, but the categorization of drugs into “recommended” and “less recommended” comes from “Hormone Treatment in Transsexual People” (Asscheman and Gooren 1992).

Dosage recommendations and notes, unless otherwise noted, are also from Asscheman and Gooren.

It is recommended that MTFs take both an anti-androgen and a source of estrogen before having an orchiectomy and discontinue using anti-androgens after an orchiectomy (Asscheman & Gooren).

Taking only an anti-androgen incurs the risk of serious bone density loss, and taking only estrogen does not significantly lower testosterone levels.

You should only use one drug at the recommended dosage from each category.

Note that mg is an abbreviation for milligrams, not to be confused with µg, the abbreviation for micrograms.

A microgram is 1/1,000 of a milligram. To avoid confusion, the micrograms abbreviation is not used in these tables.

Other abbreviations that have been replaced for clarity are t.i.d., which is the Latin abbreviation for “three times a day,” p.o., which indicates an oral dose, and i.m., for intramuscular injections.

For common names and descriptions of commercially available preparations of the drugs, click the generic name.

5 MTF HRT Body Changes You Shouldn’t Expect When Transitioning

Recommended anti-androgens and their dosage:

Generic nameDosageNotes
cyproterone acetate (injectable Androcur Depot)100-150 mg/day orallyAntigonadotropins.
spironolactone100-200 mg/day orallyWorks by interfering with testosterone or DHT production. It also has receptor-blocking properties. Originally developed as a diuretic, it has antihypertensive properties.
Click here to view all MTF HRT Hormones [No prescription needed]

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Less recommended anti-androgens and their dosage:

Generic nameDosageNotes
medroxyprogesterone5-10 mg/day orally Antigonadotropic. Less effective than cyproterone and spironolactone
150 mg/month intramuscular injection
nilutamide300 mg/day orallyAndrogen receptor blocker. Not as effective for MTF hormone therapy because it can potentially stimulate androgen production.
flutamide250 mg three times a day, orallyWorks by interfering with testosterone or DHT production. Not as effective as MTF hormone therapy because it can potentially stimulate androgen production.

Recommended estrogens and their dosages:

Generic nameDosageNotes
ethinyl estradiol100 micrograms/day orally Most potent estrogenic drug. Slowly metabolized by the liver but has a large effect on other metabolic pathways in the liver. Very cheap and easily available. It can be obtained as the oral contraceptive pill, which is always combined with progestogen.
conjugated estrogens5-10 mg/day orally 1.25-2.5 mg/day orally The active dose in postmenopausal women is 0.625-1.25 mg, but for cross-gender hormone therapy, the active dose is 5-10 mg (Meyer et al., 1986). Largely metabolized at first liver passage. Conjugated estrogens in a dose of 2.5 and 5 mg orally per day are clearly associated with an increased risk of thrombosis.
17ß estradiol2-4 mg/day orally 6-8 mg/day orally 10 mg/2 weeks to 200 mg/month intramuscular injectionMost potent of the three forms of native estrogens in the human body. Produced synthetically. Largely metabolized at first liver passage.
50-100 micrograms/day transdermally two 0.1 mg patches, applied simultaneouslyPatches are replaced twice weekly. A low number of estrogen-induced side effects. It can cause skin irritation. Most expensive form. Very strongly recommended for patients over the age of 40 because of the risk of thromboembolism.
estriol4-6 mg/day orally In cross-gender hormone treatment, high doses are necessary.

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[1] Asscheman and Gooren 1992
[2] Lawrence
[3] Futterweit 1998

Non-Medical Sources of Information on Hormone Dosage

How reliable are websites and mailing lists created by other trans women for providing safe, accurate information about hormone therapy?

One way to gauge their reliability is to compare the concrete dosage recommendations against those provided by medical sources.

I subscribed to an electronic mailing list on which transsexuals who are self-medicating (primarily MTFs) exchange advice on hormone therapy and selected twenty-one individual posters who identified their own regimens, including drug names and dosage, and did not report dissatisfaction or ask for help in modifying their hormone regimens.

Of those, four (19%) reported hormone regimens that were within the guidelines given by Asscheman and Gooren or Lawrence.

Of those who were not within the guidelines, the differences ranged from the possibly ineffective to the potentially dangerous.

Five (25%) used an anti-androgen considered less effective by Asscheman and Gooren. Two (10%) reported cycling doses with no known therapeutic value.

Five (25%) used a higher dose of anti-androgen than recommended, and four (19%) used a lower dose of anti-androgen than recommended.

A high number (7, one-third) reported using a lower estrogen dose than Asscheman and Gooren recommended, while one used a higher-than-recommended dose.

Included in the numbers already reported, four (19%) used lower than recommended doses of both the anti-androgen and estrogen.

Three (14%) who did not report having had orchiectomies said they used no anti-androgen. Of those reported above, one trans woman was taking three times the normal dose of anti-androgen and another twice the normal dose of estrogen.

Phytoestrogens

Phytoestrogens work by weakly binding with estrogen receptors, giving, in some cases, very mild feminizing effects.

However, the doses required to achieve any effects at all are prohibitively large and toxic. (FAQ: Hormone Therapy for M2F Transsexuals) Most sources do not recommend that trans women use black cohosh, dong Quai, milk thistle, or any other phytoestrogenic herb as a replacement for hormone therapy, even as a low-dose measure, because of their inefficacy.

Because of the way that phytoestrogens compete with estrogen for receptors, using them in addition to hormone therapy may also be counterproductive.

Side Effects

Thromboembolism

Combined treatment with estrogen and cyproterone acetate is associated with increases in thromboembolic events (Asscheman, Gooren, & Eklund).

The more serious risk of thromboembolism, according to a later study by two of the same researchers, is greatly reduced by the use of transdermal estrogen therapy in patients over the age of 40, in whom “a high incidence of venous thromboembolism was observed with oral estrogens.

” (van Kesteren et al. 1997). A 1998 study in which estrogen was administered by injection or orally reported the incidence of thromboembolic events as “negligible” (Schlatterer et al.).

Hyperprolactinemia

In a 1989 retrospective study, combined treatment with estrogen and cyproterone acetate was associated with increases in hyperprolactinemia (Asscheman, Gooren, & Eklund).

An article dealing specifically with the risks of self-treatment by transsexual women also noted increased rates of hyperprolactinemia (Becerra Fernandez et al. 1999).

The complications of hyperprolactinemia are limited but can include blindness and hemorrhaging (Schenenberger & Knee 2001).

One case study linked prolactin-producing pituitary adenoma with long-term estrogen use (Kovacs et al. 1994).

In the study of elevated prolactin levels in transsexual women, of fifteen patients with persistently high prolactin levels, the patients were also reported to have developed enlarged pituitary glands.

The study linked elevated prolactin levels with higher estrogen dosage as well as with increased age and suggested using the lowest effective dosages of estrogen (Asscheman et al. 1988).

Another study of transsexual women with elevated prolactin levels “suggests that the risk of inducing prolactinomas through cross-gender hormone treatment is likely to be small.” (Gooren et al. 1985)

Liver Function

Combined treatment with estrogen and cyproterone acetate [an androgen blocker] is associated with transient elevation of liver enzymes (Asscheman, Gooren, & Eklund).

An article dealing specifically with the risks of self-treatment by transsexual women also noted the elevation of liver enzymes (Becerra Fernandez et al. 1999).

The liver function issues in the 1989 study were attributed to other causes, such as alcohol abuse and hepatitis B, and were mainly successfully treated, either with other medications or temporarily halting hormone treatment.

Osteoporosis

In a German case study, bone loss was reversed in an MTF woman by adding 2 mg of oral estradiol valerate daily to the 100 mg of cyproterone she was already taking daily.

She was losing bone mass at the rate of 5% per year while taking androgen-blockers without also taking estrogen (Hierl et al. 1999).

A case study comparing trans women who had been on estrogen for less than two years with those who’d been on it for longer found increased bone density in the women who’d been on estrogen longer (Reutrakul et al. 1998).

Depressive Mood Changes

In a 1989 retrospective study, combined treatment with estrogen and cyproterone acetate [an androgen-blocker] was associated with increased depressive mood changes (Asscheman, Gooren, & Eklund). Depression has been tied to both high and low testosterone levels in women (Rohr 2002) and transsexuals’ isolation (Rauchfleisch 1998).

Cholesterol Levels

An article dealing specifically with the risks of self-treatment by transsexual women noted higher levels of total cholesterol, LDL cholesterol, and triglycerides. (Becerra Fernandez et al 1999) However, the higher levels of cholesterol and triglycerides were still within normal levels (Citkowitz 2001, Isley 2002), and the lower incidence of other factors associated with heart disease, such as elevated plasma tHcy levels (Giltay et al. 1998), suggest this is an acceptable risk.

Hyperkalemia

Spironolactone use can cause hyperkalemia, an excessive amount of potassium in the blood. Hyperkalemia, an often symptomless condition, can cause serious kidney problems, including renal failure, and heart problems, including difficult-to-cure cardiac rhythm disturbances. (RxList).

People using spironolactone are advised to avoid excessive potassium in their diets, including salt substitutes containing potassium chloride.

Disclaimer*

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We are not medical professionals and are not endorsing self-medicating. We are just providing you with the resources to do so if you choose the route of self-medicating at your own risk.

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