Reproductive Pharm EC

Question 1

Leuprolide (MOA, Use, Tox)

Answer 1

GnRH analog (agonist if pulsatile, antagonist if continuous)

Infertility (pulsatile)
Prostate cancer (continuous-used w/ flutamide)
Uterine fibroids (continuous) 
Precocious puberty (continuous)

Antiandrogen effects, N/V

Question 2

Testosterone, Methyltestosterone (MOA, Use, Tox)

Answer 2

Androgen agonist

Hypogonadism (promote secondary sex characteristics)
Burn or injury (stimulates anabolism)

Masculinization in females,
Reduces intratesticular testosterone in males by inhibiting release of LH - gonadal atrophy
Premature closure of epiphyseal plates
Increase LDL, decrease HDL

Question 3

Finasteride (MOA, Use)

Answer 3

Antiandrogen
5-a-reductase inhibitor (inhibit conversion to DHT)

BPH
Promotes hair growth

Question 4

Flutamide (MOA, Use)

Answer 4

Antiandrogen
Nonsteroidal testosterone receptor antagonist

Prostate carcinoma

Question 5

Ketoconazole (MOA, Use, Tox)

Answer 5

Inhibits steroid synthesis (17,20 desmolase)

PCOS to prevent hirsutism

Gynecomastia
Amenorrhea

Question 6

Spironolactone (MOA, Use, Tox)

Answer 6

Inhibits steroid binding (antiandrogen)

Treats hirsutism in PCOS

Gynecomastia
Amenorrhea

Question 7

Ethinyl, Estradiol, DES, Mestranol (MOA, Use, Tox)

Answer 7

Bind estrogen receptors (estrogens)

Hypogonadism or ovarian failure
Menstrual abnormalities
HRT in postmenopausal women
Use in men w/ andro dependent prostate cancer

Increase endometrial cancer risk, bleeding in postmenopausal women, increased risk of thrombi,

CONTRAINDICATED IN ER+ BREAST CANCER AND HISTORY OF DVTs

Question 8

Clomiphene (MOA, Use, Tox)

Answer 8

SERM
Partial estrogen receptor agonist in hypothalamus

Stimulates ovulation (treats infertility and PCOS)

Hot flashes, ovarian enlargement, multiple pregnancies, visual disturbances

Question 9

Tamoxifen (MOA, Use)

Answer 9

SERM
Antagonist at breast,

ER+ breast cancer

Question 10

Raloxifene (MOA, Use)

Answer 10

SERM
Antagonist at breast, agonist at bone

Osteoporosis
ER+ breast cancer

Question 11

Anastrozole/Exemestane

Answer 11

Aromatase inhibitors used in postmenopausal women with breast cancer

Question 12

Progestins (MOA, Use)

Answer 12

Bind progesterone receptors and reduce growth and increased vascularization of endometrium

Used in oral contraceptives
Endometrial cancer
Abnormal uterine bleeding

Question 13

Mifepristone/RU-486 (MOA, Use, Tox)

Answer 13

Progestin antagonist

Abortion (w/ misoprostol (PGE1)

Heavy bleeding, GI effects, Abdominal pain

Question 14

Oral contraception (Synthetic progestins, estrogen)

Answer 14

Inhibit LD/FSH and prevent estrogen surge (no ovulation)

Progestins cause thickening of cervical mucus and inhibit endometrial proliferation

CONTRAINDICATIONS: Smokers >35, Hx of thromboembolism/stoke, or history of estrogen-dependent tumor

Question 15

Terbutaline (MOA, Use)

Answer 15

Beta-2 agonist that relaxes the uterus

Reduces premature uterine contractions

Question 16

Tamsulosin (MOA, Use)

Answer 16

alpha-1a,d antagonist (inhibit SM contraction)

BPH

Question 17

Sildenafil, Vardenafil (MOA, Use, Tox)

Answer 17

Inhibit PDE5, increase cGMP, SM relaxation in corpus cavernosum, increased blood flow

Erectile dysfunction

Headache, flushing, dyspepsia, vision changes
LIFE THREATENING HYPOTENSION W/ NITRATES

Question 18

Danazol (MOA, Use, Tox)

Answer 18

Synthetic androgen that acts as partial agonist

Endometriosis and hereditary angioedema

Weight cain, edema, acne, hirsutism, masculinization
Decrease HDL levels, hepatotoxicity