Reproductive Flashcards
Leuprolide
MOA: GnRH analog with agonist properties when used in pulsatile fashion; antagonist when used in continuous fashion (downregulates GnRH receptor in pituitary–> decreased FSH/LH)
USES: infertility (pulsatile), prostate cancer (continuous–use with flutamide), uterine fibroids (continuous), precocious puberty (continuous)
TOXICITY: antiandrogen, nausea, vomiting
Ethinyl estradiol
MOA: synthetic estrogen–binds estrogen receptors
USES: hypogonadism or ovarian failure, menstrual abnormalities, HRT in post menopausal women, use in men with androgen-dependent prostate cancer (increases SHBG and decreases free andogrens)
TOXICITY: increased risk of endometrial cancer, bleeding in post menopausal women, increased risk of thrombi, contraindicated in ER + breast cancer, history of DVTs
DES
MOA: synthetic estrogen–binds estrogen receptors
USES: hypogonadism or ovarian failure, menstrual abnormalities, HRT in post menopausal women, use in men with androgen-dependent prostate cancer (increases SHBG and decreases free andogrens)
TOXICITY: increased risk of endometrial cancer, bleeding in post menopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi, contraindicated in ER + breast cancer, history of DVTs
Mestranol
MOA: synthetic estrogen–binds estrogen receptors
USES: hypogonadism or ovarian failure, menstrual abnormalities, HRT in post menopausal women, use in men with androgen-dependent prostate cancer (increases SHBG and decreases free andogrens)
TOXICITY: increased risk of endometrial cancer, bleeding in post menopausal women, increased risk of thrombi, contraindicated in ER + breast cancer, history of DVTs
Clomiphene
MOA: SERM–antagonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and increases release of LH and FSH from pituitary, which stimulates ovulation.
USES: treatment of infertility due to anovulation (e.g. PCOS)
SIDE EFFECTS: May cause hot flashes, ovarian enlargement (partial estrogen agonist in ovaries), multiple simultaneous pregnancies, and visual disturbances
Tamoxifen
MOA: SERM–antagonist on breast tissue, agonist at uterus and bone
USES: treat and prevent ER+ breast cancer
SIDE EFFECTS: endometrial cancer, thromboembolic events
Raloxifene
SERM–agonist on bone, antagonist at uterus and breast
USES: decreases resorption of bone and used to treat osteoporosis
SIDE EFFECTS: increased risk for thromboembolic events, but no increased risk of endometrial cancer (vs tamoxifen)
Anastrozole
Aromatase inhibitor used in post menopausal women with ER+ breast cancer
Progestins
MOA: bind progesterone receptors–decreases growth and increases vascularization of endometrium
USES: oral contraceptives and treatment of endometrial cancer (blocks estrogen induced endometrial hyperplasia) and abnormal uterine bleeding
Mifepristone
MOA: competitive inhibition of protestins at progesterone receptors
USES: termination of pregnancy. Administered with misoprostol (PGE1)
SIDE EFFECTS: heavy bleeding, GI effects, abdominal pain
Combination oral contraceptives
Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge–>no LHZ SURGE–>no ovulation
Progestins cause thickening of cervical mucus, limiting access of sperm to uterus. They also inhibit endometrial proliferation, this making endometrium less suitable for the implantation of embryo
CONTRAINDICATIONS: smokers >35y (increased CV events), patients with history of thromboembolism and stroke or history of estrogen-dependent tumor
Danazol
MOA: synthetic androgen that acts as partial agonist at AR–>inhibits gonadotropin release and decreases estrogen
USES: endometriosis and hereditary angioedema
SIDE EFFECTS: weir gain, edema, acne, hirsutism, masculinization
Testosterone
MOA: agonist at androgen receptors
USES: treats hypogonadism and promotes development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury
SIDE EFFECTS: causes masculinization in females, decreases intratesticular testosterone in males by inhibiting release of LH via negative feedback–> gonadal atrophy, premature closure of epiphyseal plates
Methyltestosterone
MOA: agonist at androgen receptors
USES: treats hypogonadism and promotes development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury
SIDE EFFECTS: causes masculinization in females, decreases intratesticular testosterone in males by inhibiting release of LH via negative feedback–> gonadal atrophy, premature closure of epiphyseal plates
Finasteride
MOA: 5alpha reductase inhibitor–decreases the conversion of testosterone to DHT
USES: BPH, make pattern baldness
