Dose range | Comment | |
Transfeminine regimens* | ||
Estrogens¶ | ||
Oral: estradiol (17-beta-estradiol valerate) | 2 to 6 mg/day | Although some providers give higher doses of oral estradiol (greater than 6 mg/day), we suggest that only doses less than or equal to 6 mg/day be used. |
Transdermal: estradiol patch | 0.025 to 0.2 mg per 24 hours, changed once or twice weekly, depending on specific preparation type | Lower risk of thromboembolism compared with oral estrogen preparations. |
Transdermal: estradiol gel | 0.25 to 1.25 mg applied once a day | Lower risk of thromboembolism compared with oral estrogen preparations. |
Parenteral | ||
Estradiol valerate | 5 to 20 mg IM every two weeks | Prolonged time to onset of effect and steady state, greater risk of accumulation and overdose. |
Estradiol cypionate | 2 to 10 mg IM every week | |
Antiandrogens* | ||
Spironolactone | 100 to 300 mg/day oral | Monitor blood pressure and electrolytes. |
Cyproterone acetate | 10 mg/day oral | 10 mg daily for a maximal duration of 2 years is recommended. |
GnRH agonists | ||
Leuprolide | 3.75 to 7.5 mg IM depot monthly or 11.25 mg IM depot every 3 months | Inhibits gonadotropin secretion. |
Goserelin | 3.6 mg SQ implant monthly | Expensive. |
Transmasculine regimens | ||
TestosteroneΔ | ||
Parenteral | ||
Testosterone enanthate or cypionate | 50 to 100 mg IM or SQ every week or 100 to 200 mg IM every two weeks | Weekly injections produce less peak-trough variation in effect (eg, mood); injection site reaction may occur. |
Testosterone undecanoate◊ | 1000 mg IM every 10 to 12 weeks | Produces stable physiologic testosterone levels over 10 to 13 weeks. |
Transdermal | ||
Testosterone gel 1% and 1.6% | 5 to 10 grams of gel per day (equivalent to 50 to 100 mg/day testosterone) | Less variation in serum testosterone levels than injectable preparations; gel formulations can result in interpersonal transfer if contact occurs before fully dried (rare). |
Testosterone patch | 2.5 to 7.5 mg/day transdermal | Transdermal patch may produce lower serum testosterone levels and more skin irritation compared with gels. |
GnRH: gonadotropin-releasing hormone; IM: intramuscular; SQ: subcutaneous.
* Dose of estrogen should be adjusted according to serum 17-beta-estradiol levels (ie, 100 to 200 pg/mL) and effect. Lower doses of estradiol are generally sufficient for feminization goals when combined with an antiandrogen, GnRH agonist, or after gonadectomy. Antiandrogen therapy is discontinued after gonadectomy.
¶ Synthetic estrogens (eg, ethinyl estradiol) are not recommended, due to elevated risk of thromboembolic disease, cardiovascular mortality, and inability to regulate dose by measurement of serum levels.
Δ Doses of testosterone should be adjusted according to serum testosterone levels (ie, normal male range 320 to 1000 ng/dL) and effect. Time to onset of effect of parenteral preparations may be less than with transdermal preparations. Supplemental agents such as depot medroxyprogesterone 150 mg every 3 months or oral medroxyprogesterone 5 to 10 mg/day or oral lynestrenol 5 to 10 mg/day (not available in the United States) have been used as an add-on option when starting testosterone therapy to induce cessation of menses.
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