Reproductive

Question 1

Leuprolide

Answer 1

1) Use: Infertility (Pulsatile), Prostate Cancer (continuous + flutamide), uterine fibroids (continuous), precocious puberty (continuous)2) Class/MOA: GnRH analog, pulsatile use=agonist properties, continous use=antagonist properites because downregulates GnRH receptor in pituitary causing decrease FSH/LH3) Side effects/ADEs: Antiandrogen, N/V4) Fun Facts Leuprolide can be used in lieu of GnRH

Question 2

Testosterone, methyltestosterone

Answer 2

1) Use: Hypogonadism, development secondary sex characteristics, stimulates anabolism to promote recovery after burn or injury2) Class/MOA: Agonist at androgen receptor3) Side effects/ADEs: Masculinization in females, reduces intratesticular testoerone b/c inhibit relase of LH causing gonadal atropy, premature closing epiphyseal plate, increase LDL, decrease HDL

Question 3

Finasteride

Answer 3

1) Use: BPH, hair growth male pattern baldness2) Class/MOA: Antiandrogen/5alpha reductase inhibitor (decrease conversion of testosterone to DHT)3) Side effects/ADEs: Female breast growth

Question 4

Flutamide

Answer 4

1) Use: Prostate carcinoma2) Class/MOA: Antiandrogen/ nonsteroidal competitive inhibitor of androgesn at testosterone receptor

Question 5

Ketoconazole

Answer 5

1) Use: Polycystic ovarian syndrome to prevent hirsutism2) Class/MOA: Antiandrogen/ inhibits 17,20 desmolase and inhibits steroid synthesis 3) Side effects/ADEs: Gynecomastia and amenorrhea

Question 6

Sprionolactone

Answer 6

1) Use: Polycytic ovarian syndrome prevent hirsuitsm
2) Class/MOA: Antiandrogen/inhibits steroid binding, 17alpha hydroxylase, and 17,20 desmolase.
3) Side effects/ADEs: Gynecomastia and amenorrhea

Question 7

Estrogens (ethinyl estradiol, DES, mestranol)

Answer 7

1) Use: Hypogonadism, ovarian failure, menstural abnormalities, HRT postmenopausal, men with androgen dependent prostate cancer2) Class/MOA: Binds estrogen receptors3) Side effects/ADEs: Increase risk endometrial cancer, bleed postmenopausal, vaginal clear cell adenocarcinoma if exposed to DES in utero, increase risk thormbi4) Fun Facts: contraindicated if ER positive breast cancer or history of DVTs

Question 8

Clomiphene

Answer 8

1) Use: Infertility and PCOS2) Class/MOA: SERM. Antagonist at estrogen receptors in hypothalamus, prevents normal feedback inhibition and increases relase of LH and FSH from pituitary and stimulates ovulaiton
3) Side effects/ADEs: Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances4) Fun Facts: Remember, infertile, take clomiphene have twins, seeing double

Question 9

Tamoxifen

Answer 9

1) Use: Treat and prevent recurrence ER positive breast cancer
2) Class/MOA: SERM/Antagonist on breast tissue, Agonist on endometrial tissue and bone. associated with thromboembolic events and endo cancer

Question 10

Raloxifene

Answer 10

1) Use: Osteoporosis

2) Class/MOA: SERM/Agonist on bone, reduces resorption of bone, also antagonist at uterus.

Question 11

Hormone Replacement Therapy

Answer 11

1) Use: Relief/prevent menopausal symptoms (hot flashes, vaginal atrophy) and osteoporosis2) Class/MOA: 3) Side effects/ADEs: Unopossed estrogen replacement therapy (ERT) causes increase endometrial cancer so add progesterone, possible increase in CV risk

Question 12

Anastrozole/ exemestane

Answer 12

1) Use: Postmenopausal women with breast cancer

2) Class/MOA: Aromatase inhibitor
When taking ANAbolic STeroids, add ANAStrozole.
EX-MEN forgot to take: EXEmestane

Question 13

Progestins

Answer 13

1) Use: OCP, Mirena IUD, treatment of endometrial cancer and abnormal uterine bleeding2) Class/MOA: Binds progesterone receptors, reduce growth and increase vascularizaiton of endometrium4) For OCP have to take at same time everyday so not as effective contraceptive

Question 14

Mifepristone (RU 486)

Answer 14

1) Use: Terminiation of pregnancy +misoprostol (PGE1)
2) Class/MOA: Competitive inhibitor of progestins at progesterone receptors
3) Side effects/ADEs: Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain

Question 15

Oral contraception (synthetic progestins, estrogen)

Answer 15

1) Use: Prevent pregnancy2) Class/MOA: Estrogen and progestins inhibit LH/FSH and prevent estrogen surges so no LH surge and no ovulaiton. Progestins cause thickenign of cervical mucus, limiting access of sperm to uterus. Also inhibits endometrial proliferation, making endometirum less suitable for implanation of embryo3) Side effects/ADEs: Contraindicated in smokers >35 yo becuase increase risk of DVT and CV events, patients with history of thormoembolism and storke or estrogen dependent tumor

Question 16

Terbutaline

Answer 16

1) Use: Reduces premature uterine contraction2) Class/MOA: B2 agonist that relaxes the uterus

Question 17

Tamsulosin

Answer 17

1) Use: BPH2) Class/MOA: Alpha 1 antagonist, inhibits smooth muscle contraction. Selective for alpha 1 A,D receptors on prostate (not vascular alpha 1B receptor)

Question 18

Sildenafil, vardenafil

Answer 18

1) Use: Erectile dysfunction2) Class/MOA: Inhibits phosphodiesterase 5, increase cGMP, smooth muscle relaxaiton in corpus cavernosum, increase blood flow and penile erection3) Side effects/ADEs: Headache, flushing, dyspepsia, impaired blue green color vision, risk of life threatening hypotension in patients taking nitrates “Hot and sweath” but then Headace, Heartburn, Hypotension4) Fun Facts: DON’T USE WITH NITRATES

Question 19

Danazol

Answer 19

1) Use: Endometriosis and hereditary angioedema (C1 esterase inhibitor deficiency)
2) Class/MOA: Synthetic androgen acts as partial agonist at andorgen receptors (on pituitary –> decr FSH and LH –> anovulatory = less pain)
3) Side effects/ADEs: Weight gain, edema, acne, hirsutism, masculinizaiton, decrease HDL levels, hepatotoxicity

Question 20

Fulvestrant

Answer 20

estrogen receptor antagonist for cancer pts, no agonist effects