Gonadal Hormone drugs

Question 1

Contraceptives dosage forms: Combination

Answer 1

Transdermal Patch: Ethinyl estradiol; norelgestromin

Invaginal ring: Ethinyl Estradiol; etonogestrel

Question 2

Contraceptives dosage forms: Progesterone only

Answer 2

Intra Uterine Device Levonorgestrel: Skyla (q3 years), Liletta (q4 years), Mirena/Kyleena (q5 years)

Subdermal implant: Etonogestrel (Nexplenon) q3 years

Injection (IM/SC): Medroxyprogesterone (q3 months)

Question 3

Mifepristone

Answer 3

• Postcoital contraception (morning after contraception)
• Glucocorticoid Receptor Antagonist
• Progesterone receptor antagonist (abortion of pregnancy)

Question 4

Therapeutic uses for estrogen/progestins

Answer 4

• Hormone replacement therapy (menopause –> reduces ovarian function and low estrogen; vasomotor symptoms)
• Progesterone nullifies increased estrogen related uterine cancer risk (for intact uterus pt)

Question 5

SERD: Raloxifene

Answer 5

• agonist on bone, antagonist on uterus/breast
• indicated for treatment and prophylaxis of osteoporosis in post menopausal women
• indicated for breast cancer prophylaxis

Question 6

SERD: Tamoxifen

Answer 6

indicated for the treatment and prophylaxis of breast cancer

Question 7

SERD: Bazedoxifene

Answer 7

• Reduces endometrial overgrowth (for those with intact uterus)
• may have estrogen like effects on breast and nlood
• Estrogen component provides benefit in hot flashes
• Combine with estrogen to make Duavee: indicated to treat menopausal hot flashes and to prevent post menopausal osteoporosis

Question 8

Aromatase inhibitors

Answer 8

• Anastrozole and Letrozole are reversible, nonsteroidal inhibitors
• Exemestane is an irreversible, steroidal inhibitors

Question 9

Selective Estrogen Receptor downregulator (SERD)

Answer 9

Fulvestrant

-pure estrogen receptor antagonist (no agonist activity)

Question 10

Androgens

Answer 10

• Principle: Testosterone
• 5 alpha reductase: DHT (potent)
• Levels rise sharply between ages 12-18
• levels gradually decline starting at age 30
• Excessive androgen stimulation: BPH, prostate cancer
• Excess DHT + miniaturized hair follicles with age: balding scalp

Question 11

Therapeutic uses for androgens

Answer 11

• Hormone replacement therapy (hypogonadism, post menopausal females also receiving estrogen)
• Anabolic (restores libido, fertility, muscle mass, strength)
• AIDSs related muscle wasting (increases muscle mass and strength)

Question 12

Androgens used in HRT

Answer 12

• Testosterone used in high first pass metabolism
• IM: Depo- Testosterone
• Transdermal: Androderm patch
• Topical: Androgel, Testim, Axiron, Vogelxo
• apply appropriately