Gender Dysphoria Medication

Updated: Apr 24, 2019
  • Author: Mohammed A Memon, MD; Chief Editor: Glen L Xiong, MD  more...
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Medication

Medication Summary

The goal of pharmacotherapy is to inhibit or promote the expression of secondary sex characteristics in males and females.

According to the largest study to date of transgender people in the United States, transgender women are at increased risk for venous thromboembolism (VTE) and ischemic stroke, particularly if they initiate some form of estrogen therapy. Researchers identified 2842 transfemales (assigned male at birth but transitioning to female) and 2118 transmales (assigned female at birth) from electronic health records and followed them for an average of 3.5 to 4 years from the first evidence of their transgender status. They then matched these two groups to a large cohort of cisgender men and women. Results show transwomen had a 1.9-fold higher risk of VTE over the full follow-up interval compared with cisgender men and about a 2-fold higher risk relative to cisgender women. The risk of ischemic stroke for transwomen was about 1.2-fold higher than for cisgender men and 1.9-fold higher than for cisgender women. [24, 25]

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Progestins

Class Summary

These agents may be used to inhibit the secretion of pituitary gonadotropins.

Medroxyprogesterone (Depo-Provera, Provera)

Medroxyprogesterone may reduce the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary by decreasing the amount of gonadotropin-releasing hormone (GnRH) secreted by the hypothalamus. This suppression, in turn, suppresses sex characteristics in males.

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Gonadotropin-Releasing Hormone Agonists

Class Summary

Gonadotropin-releasing hormone (GnRH) analogs produce a hypogonadotrophic-hypogonadal state by down-regulation of the pituitary gland.

Leuprolide (Eligard, Lupron Depot, Lupron Depot-Ped)

Leuprolide suppresses ovarian and testicular steroidogenesis by decreasing luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels. With long-term administration, this agent suppresses gonadotropic responsiveness to endogenous gonadotropin-releasing hormone (GnRH), thereby reducing secretion of LH and FSH, which, in turn, reduces ovarian and testicular steroid production.

Goserelin (Zoladex)

Goserelin suppresses ovarian and testicular steroidogenesis by decreasing luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels. With long-term administration, this agent suppresses gonadotropic responsiveness to endogenous gonadotropin-releasing hormone (GnRH), thereby reducing secretion of LH and FSH, which, in turn, reduces ovarian and testicular steroid production.

Nafarelin (Synarel)

Nafarelin is an analog of gonadotropin-releasing hormone (GnRH) that is approximately 200 times more potent than natural endogenous GnRH. With long-term administration, this agent suppresses gonadotropic responsiveness to endogenous GnRH, thereby reducing secretion of LH and FSH, which, in turn, reduces ovarian and testicular steroid production.

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Aldosterone Antagonists, Selective

Class Summary

Aldosterone antagonists may block androgen receptors.

Spironolactone (Aldactone)

Spironolactone is an aldosterone antagonist that competes with testosterone and dihydrotestosterone receptor sites. It also reduces free testosterone levels as more is bound by the increased quantity of sex hormone–binding globulin (SHBG). It is used most effectively in combination with an oral contraceptive.

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Antineoplastics, Antiandrogens

Class Summary

Antiandrogens are another group of agents used as a first-line therapy for hirsutism. However, the teratogenic potential of these drugs means that they should be used in conjunction with adequate contraception in women of reproductive age.

Flutamide

Flutamide is a nonsteroidal antiandrogen that inhibits androgen uptake or binding of androgen to target tissues.

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Oral Contraceptives

Class Summary

Oral contraceptives inhibit ovarian androgen production and are probably the first choice for young women with hirsutism who do not want to become pregnant. Oral contraceptives are inexpensive, and they promote regular uterine bleeding. Oral contraceptives can be used in combination with antiandrogens or other agents.

Ethinyl Estradiol, drospirenone, and levomefolate (Beyaz)

This combination of estrogen and progestin suppresses ovarian production of androgens.

Ethinyl estradiol and norethindrone (Estrostep Fe)

This combination of estrogen and progestin suppresses ovarian production of androgens.

Ethinyl estradiol and norgestimate (Ortho Tri-Cyclen)

This combination of estrogen and progestin suppresses ovarian production of androgens.

Ethinyl Estradiol and Drospirenone (Yaz)

This combination of estrogen and progestin suppresses ovarian production of androgens.

Norethindrone acetate and ethinyl estradiol (Ortho-Novum, Nortrel, Cyclofem)

This combination of estrogen and progestin suppresses ovarian production of androgens.

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Estrogen Derivatives

Class Summary

These hormones are used for replacement therapy in hypogonadism associated with a deficiency or absence of endogenous testosterone or estrogen.

Estrogens, conjugated (Premarin)

Estrogen is important in the development and maintenance of the female reproductive system and secondary sex characteristics, promoting the growth and development of the vagina, uterus, fallopian tubes, and breasts. It affects the release of pituitary gonadotropins; causes capillary dilatation, fluid retention, and protein anabolism; increases the water content of cervical mucus; and inhibits ovulation.

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Androgens

Class Summary

Androgens are used for replacement therapy in hypogonadism associated with a deficiency or absence of endogenous testosterone.

Testosterone (Testim, Androderm, Depo-Testosterone, Androderm, AndroGel)

Testosterone is an anabolic steroid that promotes and maintains secondary sex characteristics in androgen-deficient males.

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