Reproductive

Question 1

Leuprolide (MOA)

Answer 1

GnRH analog with agonist properties when used in pulsatile fashion; antagonist when used in continuous fashion (down regulates GnRH receptor in pituitary -> decreased FSH/LH)

Question 2

Leuprolide (CU)

Answer 2

Infertility (pulsatile), prostate cancer (continuous-use with flutamide), uterine fibroids (continuous), precocious puberty (continuous)

Question 3

Leuprolide (T)

Answer 3

Antiandrogen, nausea, vomiting

Question 4

Estrogens (ethinyl estradiol, DES, mestranol) (MOA)

Answer 4

Bind estrogen receptor

Question 5

Estrogens (ethinyl estradiol, DES, mestranol) (CU)

Answer 5

Hypogonadism or ovarian failure, menstrual abnormalities, HRT in post-menopausal women; use in men with androgen dependent prostate cancer

Question 6

Estrogens (ethinyl estradiol, DES, mestranol) (T)

Answer 6

Increased risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina with DES exposure in utero, increased risk of thrombi. Contraindication - ER + breast cancer, history of DVTs.

Question 7

Clomiphene (MOA)

Answer 7

Selective ER modulator. Antagonist of estrogen receptors in hypothalamus. Prevents normal feedback inhibition and increases release of LH and FSH from pituitary, which stimulates ovulation.

Question 8

Clomiphene (CU)

Answer 8

Infertility due to anovulation (PCOS)

Question 9

Clomiphene (T)

Answer 9

Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances

Question 10

Tamoxifen (MOA)

Answer 10

Selective ER modulator. Antagonist on breast tissue; agonist at uterus, bone; associated with endometrial cancer, thromboembolic events

Question 11

Tamoxifen (CU)

Answer 11

Treat and prevent ER + breast cancer

Question 12

Raloxifene

Answer 12

Selective ER modulator. Agonist on bone; antagonist at uterus; also increases risk of thromboembolic events; decreases resorption of bone -> used to treat osteoporosis

Question 13

Anastrozole/exemestane

Answer 13

Aromatase inhibitors used in postmenopausal women with breast cancer

Question 14

Progestins (MOA)

Answer 14

Bind progesteron receptos; decreased growth and increased vascularization of endometrium

Question 15

Progestins (CU)

Answer 15

Used in oral contraceptives and in treatment of endometrial cancer and abnormal uterine bleeding

Question 16

Mifepristone (MOA)

Answer 16

Competitive inhibitor of progestins at progesterone receptors

Question 17

Mifepristone (CU)

Answer 17

Termination of pregnancy. Administered as misoprostol (PGE1)

Question 18

Mifepristone (T)

Answer 18

Heavy bleeding, GI effects (n/v, anorexia), abdominal pain

Question 19

Oral contraception

Answer 19

Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge -> no LH surge -> no ovulation.
Progestins cause thickening of cervical mucus, thereby limiting access of sperm to uterus. Progestins also inhibit endometrial proliferation, thus making endometrium less suitable for implantation of an embryo

Question 20

Oral contraceptive (contraindications)

Answer 20

smokers > 35 y/o (increased risk of CV events), puts with hx of thromboembolism and stroke or hx of estrogen-dependent tumor

Question 21

Terbutaline

Answer 21

B2-agonist that relaxes the uterus; used to decrease contraction frequency in women during labor

Question 22

Danazol (MOA)

Answer 22

Synthetic androgen that acts as partial agonist at androgen receptors

Question 23

Danazol (CU)

Answer 23

Endometriosis and hereditary angioedema

Question 24

Danazol (T)

Answer 24

Weight gain, edema, ace, hirsutism, masculinization , decreases HDL levels, hepatotoxicity

Question 25

Testosterone, methyltestosterone (MOA)

Answer 25

Agonist at androgen receptors

Question 26

Testosterone, methyltestosterone (CU)

Answer 26

Treats hypogonadism and promotes development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury

Question 27

Testosterone, methyltestosterone (T)

Answer 27

Masculinization in females; decreased intratesticular testosterone in males by inhibiting LH release-> gonadal atrophy. Premature closure of epiphyseal plates. Increased LDL. Decreased HDL. HTN. Polycythemia. Prostatic growth.

Question 28

Finasteride

Answer 28

5alpha-reductase inhibitor (decreased conversion of testosterone to DHT). Useful in BPH. Also promotes hair growth-used to treat male-pattern baldness

Question 29

Flutamide

Answer 29

Nonsteroidal competitive inhibitor of androgens at the testosterone receptor. Used in prostate carcinoma.

Question 30

Ketoconazole

Answer 30

Inhibits steroid synthesis. Used in treatment of PCOS to prevent hirsutism. Can cause gynecomastia and amenorrhea.

Question 31

Spironolactone

Answer 31

Inhibits steroid binding, 17alpha-hydroxylase, and 17,20-desmolase. Used in treatment of PCOS to prevent hirsutism. Can cause gynecomastia and amenorrhea.

Question 32

Tamsulosin

Answer 32

Alpha1-antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective for prostatic receptors not found in vasculature.

Question 33

Sildenafil, Vardenafil (MOA)

Answer 33

Inhibit phosphodiesterase 2-> increase in cGMP, smooth muscle relaxation in the corpus cavernosum, increased blood flow, and penile erection. Fill the penis.

Question 34

Sildenafil, Vardenafil (CU)

Answer 34

Erectile dysfunction

Question 35

Sildenafil, Vardenafil (T)

Answer 35

HA, flushing, dyspepsia, impaired blue-green color vision. Risk of life-threatening hypotension in pts taking nitrates.