HRT Self-Medication: Information Accuracy and Risks of HRT
It’s a fact that some transsexuals choose—usually because it’s the only option available to them—to self-prescribe hormones and/or androgen-blocking drugs. 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.
Because the populations are so different, this article is arranged in two sections, one reporting on MTFs and one on FTMs.
There are no generally agreed upon recommended dosages, or recommended drugs within categories. The following recommendations are based upon three sources, but the categorization of drugs into “recommended” and “less recommended” come 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 risk of serious bone density loss, and taking only estrogen does not significantly lower testosterone levels. You should only be using 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 some confusion, the abbreviation for micrograms 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.
Recommended anti-androgens and their dosage:
|cyproterone acetate (injectable Androcur Depot)||100-150 mg/day orally||Antigonadotropic.|
|spironolactone||100-200 mg/day orally||Works by interfering with testosterone or DHT production. Also has receptor-blocking properties. Originally developed as a diuretic, it has antihypertensive properties.|
Less recommended anti-androgens and their dosage:
|medroxyprogesterone||5-10 mg/day orally ,||Antigonadotropic. Less effective than cyproterone and spironolactone|
|150 mg/month intramuscular injection|
|nilutamide||300 mg/day orally||Androgen receptor blocker. Not as effective for MTF hormone therapy, because it can potentially stimulate androgen production.|
|flutamide||250 mg three times a day, orally||Works by interfering with testosterone or DHT production. Not as effective for MTF hormone therapy, because it can potentially stimulate androgen production.|
Recommended estrogens and their dosages:
|ethinyl estradiol||100 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. Can be obtained as the oral contraceptive pill, which is always combined with progestogen.|
|conjugated estrogens||5-10 mg/day orally 1.25-2.5 mg/day orally ||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 estradiol||2-4 mg/day orally 6-8 mg/day orally 10 mg/2 weeks to 200 mg/month intramuscular injection ||Most 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 simultaneously||Patches are replaced twice weekly. Low number of estrogen-induced side effects. Can cause skin irritation. Most expensive form. Very strongly recommended for patients over the age of 40, because of the risk of thromboembolism.|
|estriol||4-6 mg/day orally ||In cross-gender hormone treatment, high doses are necessary.|
 Asscheman and Gooren 1992
 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. (See Appendix A: Self-Reported Dosage Recommendations from Electronic Mailing List) 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, which has 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 dose of estrogen than recommended by Asscheman and Gooren, 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 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.
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 oestrogens.” (van Kesteren et al 1997) A 1998 study in which estrogen was administered by injection or orally reported incidence of thromboembolic events as “negligible” (Schlatterer et al).
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 hemorraging (Schenenberger & Knee 2001). In one case study, prolactin-producing pituitary adenoma was linked with long-term estrogen use (Kovacs et al 1994). In 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 “suggest that the risk of inducing prolactinomas through cross-gender hormone treatment is likely to be small.” (Gooren et al 1985)
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 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.
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 daily she was already taking. 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 increases in depressive mood changes (Asscheman, Gooren, & Eklund). Depression has been tied to both high and low testosterone levels in women (Rohr 2002) and to the isolation of transsexuals (Rauchfleisch 1998).
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.
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.
Only a testosterone ester is necessary, unless one is taking testosterone undecanoate, in which case a progestogen may be supplemented. Taking only a testosterone is preferred to avoid the requirement of progestogen, and because they are more widely available.
Recommended testosterones and their dosages:
|testosterone esters (transdermal, enanthate, Sustanon, cypionate)||200-250 mg/2 weeks intramuscular injection 250-400 mg/2-3 weeks intramuscular injection ||Androgen treatment has an unfavorable effect on the lipid profile. Oral androgens such as mesterolone and fluoxymesterone are too weak for the induction of virilization.|
|testosterone undecanoate||160-240 mg/day orally ||Not available in the U.S. Does not suppress menstruation in half the patients, and in these cases, can be supplemented with progestogens.|
 Asscheman & Gooren 1992
 Futterweit 1998
Progestogens and their dosages (Asscheman & Gooren 1992):
|medroxyprogesterone acetate||5 mg, 1-2 tablets/day or 150 mg intramuscularly/3 months|
|lynestrenol||5 mg, 1-2 tablets/day|
|norethisterone||5 mg, 1 or 2 tablets/day|
Non-Medical Sources of Information on Hormone Dosage
Hormone regimens for transmen are less complicated, and there are fewer drugs to choose from, apparently reducing the temptation to play the armchair pharmacist. Unlike MTFs, there do not appear to be any electronic mailing lists dedicated to do-it-yourself hormone use for FTMs. A review of twenty-seven responses to an online survey of FTM hormone use and surgery indicate most are taking low to normal amounts of testosterone, and none of the 27 reviewed were taking anti-estrogens or progestogens. (FTM Survey)
Websites from non-medical sources give information on recommended or typical dosage of testosterone. A survey of these sources is available in Appendix B: Website Hormone Recommendations for FTMs.
Testosterone Enhancers or Precursors
A variety of products marketed to body builders as nutritional supplements are popular among transmen as alternatives to testosterone. If you’re considering using supplements marketed as anabolic steroids or replacements for anabolic steroids, that the characteristics of anabolic steroids are that they help create muscle (anabolic), but have weak masculinizing (androgenic) properties. As a result, in the amounts sufficient to produce masculinizing effects, there is a risk of liver damage, particularly when taking these products orally.Of eleven survey respondents who used DHEA without testosterone, no one reported more than slightly noticeable results. Three respondents using large quantities of norandrostenediol and androstendiol had some noticeable results within two to fifteen months. (FTM Survey)
An elevated plasma level of total (free and protein-bound) homocysteine (tHcy) is a risk factor independent of other known risk factors for cardiovascular disease. Increased levels of tHcy were found in FTMs on hormone therapy (Giltay et al 1998). Androgen treatment in 122 female-to-male transsexuals was also associated with weight increase greater than 10% in 17.2% of the subjects (Asscheman et al 1989). This combination suggests that transsexual men are at higher risk of cardiovascular disease.
An article dealing specifically with the risks of self-treatment by transsexual men 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).
An article dealing specifically with the risks of self-treatment by transsexual men also noted elevation of liver enzymes (Becerra Fernandez et al 1999). The liver enzyme abnormalities in a 1989 study that included both MTFs and FTMs 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 (Asscheman el al).
An article dealing specifically with the risks of self-treatment by transsexual men noted increased rates of hyperprolactinemia (Becerra Fernandez et al 1999). The complications of hyperprolactinemia are limited, but can include blindness and hemorraging (Shenenberger & Knee 2001).
Polycythemia and Bleeding Disorders
Possible side effects of testosterone use include polycythemia, or having too many red blood cells, and suppression of some clotting factors. Polycythemia can kill by thrombosis or hemorrhage. Suppression of clotting factors, particularly when combined with the use of anticoagulants, can also result in hemorrhage.
Adenoma – A benign tumor in the epithelial tissue—the tissue covering the insides and outsides of parts of the body– in which the cells of the tumor form glandular structures or in which the cells come from glandular epithelium.
Anabolic steroids – Any of a group of synthetic derivatives of testosterone, having pronounced anabolic properties and relatively weak androgenic properties, which are used mainly to promote growth and repair body tissues.
Androgen – general term for any male sex hormone.
Anti-androgen – A substance which interferes with the function of an androgen, or male sex hormone, by taking over the androgen’s receptors.
Antigonadotropic- Reducing the growth and/or function of the gonads.
Cyproterone acetate – An agent with anti-androgen and progesterone-releasing properties. It competes at the receptor sites with androgens and reduces their effects.
DHEA – An androgenic steroid hormone secreted largely by the adrenal cortex and found in human urine, or synthetic preparation of this hormone used as a nutritional supplement.
DHT – Dihydrotestosterone. An androgen derived from testosterone and having tumor-suppressing capabilities useful in the treatment of certain breast cancers.
Diuretic – An agent that promotes the excretion of urine.
Estradiol – A potent estrogen.
Estrogen – A generic term for any of a number of female sex hormones. Estrogen is formed in ovaries and testes, has various functions in both sexes, and in females causes the development of secondary sex characteristics. It is used in oral contraceptives, to relieve discomfort of menopause, and to treat osteoporosis and breast and prostate cancer.
Estrogenic- – Having an action similar to that of an estrogen.
Hemorrhage – Bleeding.
Homocysteine – An amino acid used normally by the body in cellular metabolism and the manufacture of proteins. Elevated concentrations in the blood are thought to increase the risk for heart disease by damaging the lining of blood vessels and enhancing blood clotting.
Hyperprolactinemia – An increased level of prolactin.
Orchiectomy – The surgical removal of the testicles.
Phytoestrogen - A naturally occurring compound of plants, such as soybeans, or plant products, such as whole grain cereals, that acts like estrogen in the body.
Progestogen – A term applied to any substance capable of stimulating the uterine changes essential for implantation and growth of a fertilized ovum.
Prolactin – A hormone that prepares the pregnant female’s breasts for milk production.
Prolactinoma – A pituitary gland tumor that secretes prolactin.
Spironolactone – A steroid derivative that blocks the action of aldosterone, steroid hormone that regulates the salt and water balance in the body. Used as a diuretic primarily in the treatment of hypertension.
Testosterone – Male sex hormone secreted by the testes and responsible for triggering the development of sperm and of many secondary sexual characteristics.
Thromboembolism – Obstruction of a blood vessel with a clot of fibrin— an elastic, insoluble, whitish protein— carried by the blood stream.
Thrombosis – Formation of a thrombus— platelets, fibrin, and pieces of other cells— that obstruct a blood vessel at the place where the thrombus is formed.
Appendix A: Self-Reported Dosage Recommendations from Electronic Mailing List
|Regimen as described on mailing list||Does the regimen match the guidelines available?|
|1.||First two weeks:4mg estradiol valerate per day
10mg Provera per dayThird week:10mg estradiol cypionate per day
50mg Depo-Provera injection
|This regimen includes normal dose of a recommended estrogen source and a dose of a less effective anti-androgen. The source of anti-androgen is cycled between oral and intramuscular injection.|
|2.||Month 1 –
5 mg Premarin per day
200 mg of Aldactone per dayMonth 2 –
Increase Aldactone to 300 mgMonth 3 –
Continue Premarin and Aldactone
Add 10 mg Provera per day
|This regimen is using recommended sources of estrogen and anti-androgen, both within normal recommended dosage.This regimen increases the anti-androgen above the recommended dose.This regimen further increases the anti-androgen dose by adding a second, less effective source of anti-androgens.|
|3.||50mg Androcur per day
Eight 10mcg ethinyl estradiol per day
|This regimen uses lower than normally recommended doses of recommended anti-androgen and estrogen.|
|4.||Ethinyl estradiol .05mg twice a day
Spironalactone 100mg twice a day
Proscar 5mg once a day
|This regimen uses a lower than recommended dose of estrogen with a normal dose of anti-androgen. It also includes a hormone-blocker used to prevent hair loss.|
|5.||Ethinyl estradiol 25 micrograms a day||This regimen does not include anti-androgens, but uses a potent, recommended estrogen at a below normal dose.|
|6.||1.25 mg Premarin
25 -50 mg spironalactone per day for the 1st month or so and gradually increase
|This regimen uses lower than normal doses of recommended estrogen and anti-androgen sources.|
|7.||2mg estradiol twice a day
Spironalactone 100mg twice a day
Proscar 5mg once a dayAdded medoxyprogesterone 10mg daily
|This regimen started with normal doses of estrogen and anti-androgen, then increased the anti-androgen above normal dosage by adding another, less effective anti-androgen. It also includes a hormone-blocker used to prevent hair loss.|
|8.||Premarin 5mg per day
Spironalactone 200mg per day
|This regimen includes normal doses of recommended estrogen and anti-androgen sources.|
|9.||estradiol valerate 20 mg every two weeks
finasteride 20 mg every week
progestins 50 mg every month
|This regimen includes an intramuscular injection of a recommended estrogen and a hormone-blocker used to prevent hair loss. Progestins are the class of drug to which Depo-Provera belong; the exact progestin used here is unknown, but based on this dosage, this is possibly IM. The combined dosage of estrogen is probably within recommendations.|
|10.||Elleste Solo 5mg sublingually twice a day
Depo-Provera 150 mg monthly
|This regimen includes a higher than recommended dose of estrogen, and three times the normal dose of anti-androgen.|
|11.||estradiol 4 mg per day
Provera 5 mg orally per day
Spironalactone 200 mg per day
1 aspirin per day for clotting
|This regimen includes a normal dose of estrogen, and two sources of anti-androgens: one recommended source and one less effective source. The combined doses of anti-androgens are above normal.|
|12.||Estrofem 2mg tab, sublingual three times a day
Provera 10mg per day
|This regimen includes normal doses of a recommended estrogen and a less-effective anti-androgen.|
|This regimen includes recommended sources of estrogen and anti-androgen at normal doses.|
|14.||1 c.c. of estradiol cypionate intramuscular injection every three weeks (5mg/ml),
oral estradiol 2mg daily
200 mg spiro
1/4 tablet of Proscar daily(supervised regimen)
|This regimen includes two sources of estrogen: one oral at a low normal dose and one intramuscular injection. Depo-Estradiol, a source of estradiol cypionate, is 5mg/mL, so the dose is probably around 5 mg every three weeks, less than half the recommended dose. The regimen also includes a normal dose of a recommended anti-androgen and a hormone-blocker used to prevent hair loss.|
|15.||For ten days:estrofem 2 mg
Premarin 1.25 mgFor five days:Nothing
|This regimen includes normal doses of estrogen and anti-androgen from recommended sources, but the regimen is cycled with a resultant lower than normal dose of each substance.|
|16.||Premarin 2.5 mg
Estrofem 4 mg
Spirotone 200 mg
|This regimen includes a normal dose of a recommended anti-androgen, and a combination of estrogens resulting in a normal dose.|
|17.||Two 100 Climara patches per weekTwo Aldactone100 mg||This is probably the recommended .1 mg patch at the recommended dosage of two per day, used simultaneously, as well as a recommended anti-androgen.|
|18.||Prempro 2.5 mg twice a day||Prempro is a combination of Premarin (a conjugated estrogen) and Cyrin (an anti-androgen) containing a lower than recommended dose of estrogen and either a low or normal dose of anti-androgen (Prempro 2.5 or Prempro 5.0, where the number indicates the number of milligrams of medroxyprogesterone acetate.)|
|19.||Premarin 2.5 mg/dayEstrofem 4 mg/day||This regimen includes two sources of estrogen, resulting in a normal dose, but no anti-androgens.|
|20.||Premarin 2.5 mg per day
Provera 10 mg per day
spironalactone 200 mg per day
|This regimen includes a lower than recommended dose of estrogen, and two sources of anti-androgens with a resultant twice the normal recommended dose.|
|21.||40 mg estradiol valerate IM every 2 weeks
200 mg Prometrium per day
50 mg Androcur per day
|This regimen includes a normal dose of estrogen, a low dose of anti-androgen, and a dose of progesterone. No dosage recommendations were available. Several TS internet sources recommend its use to control mood swings, while some individuals reported that it created mood swings.|
Appendix B: Website Hormone Recommendations for FTMs
Recommendations from the “Hormone Therapy for F2M Transsexuals” website
Testosterone Cypionate Pre-op 200-400mg/2-4wks
Testosterone Enanthate Pre-op 200-400mg/2wks
Testosterone transdermal film No Pre-op recommendation
Post-op 4-6mg/day (1 film changed daily)
Methyl Testosterone No Pre-op recommendation
Fluoxymesterone No Pre-op recommendation
Danazol Pre-op 200-400mg/day
Tamoxifen Citrate Pre-op 20-40mg/day
Goserelin Acetate Pre-op 3.6mg/month
(3.6mg implant is for 1 month; 10.8 mg implant is for 3 months)
Nafarelin Acetate Pre-op 1600mcg/day (2 sprays into each nostril twice a day)
Leuprolide Acetate Pre-op 3.75-7.5mg/month
Recommendations from the Alamo Boyz “FTM Surgical Recommendation” website
Testosterone Cypionate Pre-op 200-400mg/2-4wks
Recommendations from the “Notes on Gender Transition: FTM 101 — The Invisible Transsexuals” website
Testosterone Cypionate and Testosterone Enanthate Pre-op 200 ml/cc, lcc every two weeks
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