From the Guidelines
Hormone therapy for transgender women typically includes estrogen and anti-androgens, with estradiol and spironolactone being the most common medications used to help a man look like a woman. The typical regimen includes estrogen and an adjunct antiandrogen to enable lower doses of the estrogen to be used 1. Estrogens can be taken through oral, transdermal, or parenteral routes, and the most common medications are estradiol (available as pills, patches, or injections) and spironolactone, which blocks testosterone.
Some key points to consider when using hormone therapy for transgender women include:
- Typical starting doses are 2-4mg daily of oral estradiol or 0.1mg patches changed twice weekly, along with 100-200mg daily of spironolactone 1
- Cyproterone acetate is another anti-androgen used outside the US 1
- Some regimens also include progesterone (100-200mg daily) after 1-2 years of therapy 1
- These medications promote breast development, soften skin, reduce body hair, redistribute fat to create a more feminine appearance, and decrease muscle mass
- Effects develop gradually over 2-5 years
- Regular blood tests are necessary to monitor hormone levels and potential side effects, as this therapy requires medical supervision due to risks including blood clots, liver problems, and potential cardiovascular issues 1
It's also important to note that hormone therapy is very effective in the development of secondary sex characteristics and is medically necessary for many transgender individuals, given strong evidence showing that gender-affirming hormone therapy improves quality of life and relieves the psychological distress seen in gender dysphoria 1.
From the FDA Drug Label
Estradiol valerate injection, USP
Estrogen administration should be initiated at the lowest dose approved for the indication and then guided by clinical response rather than by serum hormone levels (e.g., estradiol, FSH).
The medication used in transgender medicine to help a man look like a woman is Estradiol.
- Estradiol is an estrogen therapy that can help with feminization.
- It is essential to use the lowest dose approved for the indication and monitor clinical response. 2
From the Research
Medications Used in Transgender Medicine
The medications used to help a man look like a woman in transgender medicine include:
- Estrogen, typically in the form of estradiol, to induce feminizing changes 3, 4
- Anti-androgens, such as cyproterone acetate or spironolactone, to suppress testosterone levels and prevent masculinization 3, 4, 5
- Gonadotropin-releasing hormone agonists (GnRH-a) as an alternative to anti-androgens 3
Comparison of Anti-Androgens
A randomized controlled trial compared the anti-androgenic effects of cyproterone acetate and spironolactone in transgender women, finding that:
- Cyproterone acetate had a higher testosterone suppression efficacy than spironolactone 5
- A higher proportion of participants achieved female range testosterone levels with cyproterone acetate (90%) compared to spironolactone (19%) 5
Risks and Benefits of Hormone Therapy
The risks and benefits of hormone therapy in transgender women include:
- Increased risk of thromboembolism, depending on the dose and route of estrogen administration 4, 6
- Potential risks of depression and osteoporosis 6
- Low risk of hormone-sensitive cancer, with no increased risk of breast cancer compared to women and no increase in prostate cancer compared to men 6, 7
- Improved mental health and life satisfaction with gender-affirming hormone treatment (GAHT) 7