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This chapter will be most useful after having a basic understanding of the material in Chapter 40, Estrogens and Progestins, Chapter 41, Androgens, and Chapter 66, Contraception and Pharmacotherapy of Obstetrical and Gynecological Disorders in Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition. In addition to the material presented here, these chapters in the 12th Edition contain:

  • The biosynthesis and physiological and pharmacological actions of the estrogens, progestins, and androgens

  • A detailed discussion of gonadotropin and gonadal steroid concentrations during the menstrual cycle, the effects of cyclical gonadal steroids on the reproductive tract, and the metabolic effects of estrogens, progestins, and androgens

  • A detailed discussion of fertility induction and the general principles of drug therapy of pregnant women, and the prevention or arrest of preterm labor

  • A detailed discussion of the secretion and transport of testosterone, the physiological and pharmacologic effects of androgens, and the effects of androgens at different stages of life


  • Describe the mechanisms of action of estrogens, progestins, and androgens.

  • Understand the therapeutic use and side effects of postmenopausal hormone replacement therapy.

  • Understand the therapeutic uses and side effects of contraceptive therapy.

  • Describe the therapeutic use of selective estrogen receptor modulators, antiestrogens, and aromatase inhibitors.

  • Describe the use of testosterone in the treatment of male hypogonadism.

  • Describe the use of androgen receptor antagonists and 5α-reductase inhibitors to treat metastatic prostate cancer and benign prostatic hypertrophy, respectively.

  • Understand the side effects of the 17α-alkylated androgens used by athletes to enhance performance.


Anabolic steroids (various 17α-alkylated androgens)

Anastrozole (ARIMIDEX)

Bicalutamide (CASODEX, others)

Clomiphene (CLOMID, SERPPHENE, others)

Conjugated equine estrogens (PREMARIN)

Conjugated estrogens + medroxyprogesterone acetate (PREMPRO, PREMPHASE)

Dutasteride (AVODART)

Estradiol + drospirenone (ANGELO)

Estradiol + norethindrone (PREFEST)

Estradiol cypionate (DEPO-ESTRADIOL, others)

Estradiol micronized (ESTRACE, others)

Estradiol nonmicronized (FEMTRACE)

Estradiol topical gel (ESTROGEL)

Estradiol transdermal (ALORA, CLIMERA, ESTRADERM, VIVELLE, others)

Estradiol vaginal ring (ESTRING)

Estradiol vaginal tablets (VAGIFEM)

Estradiol valerate (DELESTROGEN, others)

Estrogen esterified esters (MENEST)

Estropipate (ORTHO-EST, OGEN, others)

Ethinyl estradiol + norethindrone (FEMHRT)

Exemestane (AROMASIN)

Finasteride (PROSCAR)

Flutamide (EULEXIN)


Fulvestrant (FASLODEX)

Letrozole (FEMARA)

Medroxyprogesterone acetate (MPA; PROVERA, DEPO-PROVERA)

Megestrol acetate (MEGACE, others)

Mifepristone (RU 38486; MIFEPREX)

Nilutamide (NILADRON)

Progesterone micronized (PROMETRIUM)

Progesterone slow-release intrauterine device (PROGESTASERT)

Progesterone vaginal gel (CRINONE, PROCHIEVE)

Progesterone vaginal insert (ENDOMETRIN)

Raloxifene (EVISTA)

See Table 28-1 for brand names and formulations of oral contraceptives

See Table 28-2 for brand names and formulations of agents used for hormone replacement therapy

Synthetic conjugated estrogens (CENESTIN; ENJUVIA)


Testosterone (HISTERONE, others)

Testosterone buccal tablet (STRIANT)

Testosterone cypionate (DEPO-TESTOSTERONE, others)

Testosterone enanthate (DELATESTRYL, others)

Testosterone gel (ANDROGEL, TESTIM)

Testosterone patch (ANDRODERM)

Testosterone undecanoate (ANDRIOL)

Toremifene (FARESTON)

Ulipristal (ELLA, ELLAONE)

Table 28-1Brand Names and Formulations of Oral Contraceptives

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