repro pharmacology

Question 1

leuprolide

Answer 1

“can be used in LIEU of GnRH”
GnRH analog
-agonist when used in pulsatile way
-antagonist when used in continuous fashion

used for: infertility(pulsatile), prostate cancer (continuous), uterine fibrinoids (continuous), precocious puberty (continuous)

toxicity: antiandrogen, nausea/vomiting

Question 2

how to treat prostate cancer w a GnRH analog?

Answer 2

continuous leuprolide + flutamide

Question 3

why is leuprolide antagonist when used continuously?

Answer 3

downregulates the GnRH receptors in pituitary –> decreased FSH/LH

Question 4

three drug estrogens

Answer 4

ethinyl estradiol, DES, mestranol

Question 5

estrogens

Answer 5

ethinyl estradiol, DES, mestranol
mechanism: bind estrogen receptors

women use: hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women
men use: androgen-dependent prostate cancer

Question 6

toxicity of estrogens?

Answer 6

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

Question 7

contraindications for estrogens?

Answer 7

breast cancer, history of DVTs

Question 8

SERMs

3?

Answer 8

selective estrogen receptor modulators

clomiphene, tamoxifen, raloxifene

Question 9

clomiphene

Answer 9

SERM; antagonist at estrogen receptors in hypothalamus –> prevents normal feedback inhibition and increases release of LH and FSH from pituitary, which stimulates ovulation

use: infertility due to anovulation
toxicity: hot flashes, ovarian enlargement, multiple simultaneous pregnancies and visual disturbances

Question 10

tamoxifen

Answer 10

SERM, antagonist on breast tissue, agonist at uterus and bone

use: treat and prevent ER + breast cancer
toxicity: thromboembolism, endometrial cancer

Question 11

raloxifene

Answer 11

SERM, agonist on bone, antagonist on uterus

use: decreases reabsorption of bone so treats osteoporosis
toxicity: thromboembolism

Question 12

hormone replacement therapy

Answer 12

used for relief or prevention of menopausal symptoms (hot flashes and vaginal atrophy) and osteoporosis ( by increasing estrogen and decreasing osteoclast activity)

Question 13

problem and solution with estrogen replacement therapy?

Answer 13

unopposed ERT increases the risk of endometrial cancer so progesterone is added

Question 14

anastrozole

Answer 14

aromatase inhibitor used in postmenopausal women with breast cancer

Question 15

exemestane

Answer 15

aromatase inhibitor used in postmenopausal women with breast cancer

Question 16

progestins

Answer 16

mech: bind progesterone receptors, decreasing endometrial growth and increasing its vascularization
use: oral contraceptives, endometrial cancer and abnormal uterine bleeding

Question 17

mifepristone (RU-486)

Answer 17

mech: competitive inhibitor of progestins at progesterone receptors
* *administer with misoprostol (PGE1)

use: termination of pregnancy
toxicity: heavy bleeding, GI effects (nausea/vomiting, anorexia), abdominal pain

Question 18

sildenafil and vardenafil

Answer 18

“-fils FILL the penis”
mech: inhibit phosphodiesterase 5, causing increased cGMP, smooth muscle relaxation in the corpus cavernosum, increases blood flow, and penile erection

use: erectile dysfunction

toxicity: headache, flushing, dyspepsia, impaired blue-green color vision; risk of life threatening hypotension in patients taking nitrates
“Hot, Headache, Heartburn, Hypotension”

Question 19

tamsulosin

Answer 19

alpha1 antagonist used to treat BPH by inhibiting SM contraction

selective for alpha1A,D receptors found on prostate

Question 20

oral contraception

Answer 20

synthetic progestins and estrogen
they inhibit LH/FSH and prevent estrogen surge –> no LH surge –> no ovulation
progestins cause thickening of cervical mucus (limits access of sperm to uterus) and inhibit endometrial proliferation (less suitable for implantation)

Question 21

contraindications for oral contraception

Answer 21

do not use synthetic progestins and estrogen (contraceptives) with smokers>35yo (risk of CV events), patients with history of thromboembolism and stroke or history of estrogen-dependent tumor

Question 22

terbutaline

Answer 22

B2 agonist that relaxes the uterus

used to decrease contraction frequency in women during labor

Question 23

danazol

Answer 23

synthetic androgen that acts as partial agonist at androgen receptors

use: endometriosis and hereditary angioedema
toxicity: weight gain, acne, edema, hirsutism, masculinization, decreased HDL, hepatotoxicity

Question 24

testosterone and methyltestosterone

Answer 24

mech: agonist at androgen receptors
use: treats hypogonadism, promotes development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury

Question 25

toxicity of testosterone or methyltestosterone

Answer 25

• -masculinization in females
• -decreased intratesticular testosterone in males by inhibiting release of LH via negative feedback –> gonadal atrophy
• -premature closure of epiphyseal plates
• -increases LDL, decreases HDL

Question 26

4 antiandrogens

Answer 26

finasteride
flutamide
ketoconazole
spironolactone

Question 27

what converts testosterone to dihydrotestosterone (DHT)?

which is stronger?

Answer 27

5alpha reductase

DHT is more potent

Question 28

finasteride

Answer 28

an antiandrogen
5alpha reductase inhibitor (less T is converted to DHT)

use: BPH, hair loss/male pattern baldness

Question 29

what is used to treat balding/male pattern balding?

Answer 29

finasteride promotes hair growth

• to prevent male pattern hair loss, give a drug that will encourage female breast growth

Question 30

flutamide

Answer 30

an antiandrogen
nonsteroidal competitive inhibitor of androgens at the testosterone receptor

use: prostate carcinoma

Question 31

ketoconazole

Answer 31

an antiandrogen

inhibits steroid synthesis (inhibits 17,20-desmolase)

Question 32

spironolactone

Answer 32

an antiandrogen

inhibits steroid binding, 17alpha-hydroxylase, and 17,20-desmolase

Question 33

what are ketoconazole and spironolactone used to treat?

Answer 33

polycystic ovarian syndrome to prevent hirsutism

Question 34

side effects of ketoconazole and spironolactone

Answer 34

gynecomastia and amenorrhea