Repro Pharm

Question 1

Leuprolide mech

Answer 1

GnRH analog
Agonist if pulsatile
antagonist if continuous (downregulates GnRH receptor in pituitary -> decreased FSH/LH -> low T/E in M/F

Question 2

Leuprolide clinical use

Answer 2

Pulsatile - Infertility

Continuous - prostate cancer (+ flutamide), uterine fibroids, precocious puberty

Question 3

Leuprolide tox

Answer 3

Antiandrogen, n/v

Question 4

Methyltestosterone/testosterone mech.

Answer 4

Agonist at androgen receptors

Question 5

Methyltestosterone use

Answer 5

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

Question 6

Methyltestosterone tox

Answer 6

masculinization in females, reduces intratesticular T in males by inhibiting release of LH (via negative feedback), gonadal atrophy, premature closure of epiphyseal plates, Increased LH, decreased HDL

Question 7

Antiandrogens

Answer 7

Finasteride, Flutamide, Ketoconazole, Spironolactone

Question 8

Finasteride

Answer 8

5a reductase inhibitor (decreased conversion of T to DHT). Useful in BPH. Also promotes hair growth (treats male pattern baldness (to treat use something that encourages female breast growth)). Side Effects: impotence, decreased sexual function, gynecomastia.

Question 9

Flutamide

Answer 9

A nonsteroidal competitive inhibitor of androgens at the T receptor. Use - prostate cancer

Question 10

Ketoconazole

Answer 10

Inhibits steroid synthesis (inhibits 17,20-desmolase)

Question 11

Spironolactone

Answer 11

Inhibits steroid binding

Question 12

Ketoconazole, Spironolactone

Answer 12

treat PCOS to prevent hirsutism. Side effects = gynecomastia & amenorrhea

Question 13

Estrogens

Answer 13

ethinyl estradiol, DES, mestranol

Question 14

Estrogen mech

Answer 14

Bind E receptors

Question 15

Estrogens Use

Answer 15

Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; use in men with androgen dependent prostrate cancer.

Question 16

Estrogen Tox

Answer 16

increased risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi

Question 17

Estrogen contraindications

Answer 17

ER (+) breast cancer, hx of DVTs

Question 18

SERMs

Answer 18

Clomiphene, Tamoxifen, Raloxifene

Question 19

Clomiphene mech

Answer 19

SERM; partial E receptor agonist in hypothalamus. Prevents normal feedback inhibition & increased release of LH & FSH from pituitary, which stimulates ovulation.

Question 20

Clomiphene use

Answer 20

Used to treat infertility & PCOS.

Question 21

Clomiphene tox

Answer 21

May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances

Question 22

Tamoxifen mech & use

Answer 22

antag on breast tissue, agonist for endometrium (cancer risk) & bone (prevents loss). TX - prevent recurrence of ER(+) breast cancer.

Question 23

Raloxifene mech & tx

Answer 23

Agonist on bone, Antag endometrium. reduces bone resorption of bone. TX - osteoporosis

Question 24

Hormone Replacement Therapy

Answer 24

used for relief of menopause sx & osteoporosis (increased estrogen, decreased osteoclast activity). Unopposed estrogen replacement therapy increases the risk of endometrial cancer, so progesterone is added. Poss increased CV risk.

Question 25

Anastrozole/exemestane

Answer 25

Aromatase inhibitors used in postmenopausal women with breast cancer.

Question 26

Progestins mech

Answer 26

bind progesterone receptors, reduce growth, increase vascularization of endometrium

Question 27

Progestin use

Answer 27

oral contraceptives, endometrial cancer, abnorm uterine bleeding.

Question 28

Mifepristone (RU-486) mech

Answer 28

competitive inhibitor of progestins at progesterone receptors

Question 29

Mifepristone (RU-486) use

Answer 29

termination of pregnancy, admin w/misoprostol (PGE1)

Question 30

Mifepristone (RU-486) tox

Answer 30

heavy bleeding, GI, abdominal pain

Question 31

Oral contraception

Answer 31

Estrogen & progestin inhibit LH/FSH -> prevent E surge -> no LH surge -> no ovulation. Progestins thicken surgical mucous, limiting sperm access. Progestins also inhibit endometrial proliferation, thus making it less suitable for the implantation of embryo.

Question 32

OCP contraindications

Answer 32

smoker>35 due to increased risk of cardiovascular events, hx of thromboembolism, stroke, E-dependent tumor

Question 33

Tertbutaline

Answer 33

Beta2 agonist | relaxes uterus, reduces premature uterine contractions, (also bronchodilates)

Question 34

Tamsulosin

Answer 34

alpha1 antagonist Tx- BPH by inhibiting smooth mm contraction. Selective fro alpha 1A,D receptors in prostate (alpha 1b = vascular)

Question 35

Sildenafil, vardenafil mech

Answer 35

Inhibit phosphodiesterase 5, prevents breakdown of cGMP, causes smooth mm relaxation in the corpus cavernosum, increases blood flow & penile erection. (NO & ANP also activate cGMP 2nd msgr to increase cGMP)

Question 36

Sildenafil, vardenafil use

Answer 36

erectile dysfunction

Question 37

Sildenafil, vardenafil tox

Answer 37

headache, flushing, dyspepsia, impaired blue/green color vision. risk of life-threatening hypoTN in pts taking nitrates.

Question 38

Danazol mech

Answer 38

synthetic androgen; partial agonist at receptors

Question 39

Danazol use

Answer 39

endometriosis & hereditary angioedema

Question 40

Danazol tox

Answer 40

weight gain, edema, acne, hirsutism, masculinization, decreased HDL, hepatotox