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Flashcards in Repro Drugs Deck (53)
1

Mechanism of leuprolide

GnRH analog with agonist properties when used in pulsatile fashion

antagonist when used in continuous fashion (downregulates GnRH receptor in pituitary --> decreased FSH/LH)

2

Pulsatile use of leuprolide

infertility

3

Continuous use of leuprolide

prostate cancer (following androgen receptor blockade with flutamide)
uterine fibroids
precocious puberty

4

Toxicity of leuprolide

antiandrogen, nausea, vomiting

5

Name the estrogens

ethinyl estradiol, DES, mestranol

6

Mechanism of estrogens

bind estrogen receptors

7

Use of estrogens in females

hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy in postmenopausal women

8

Use of estrogens in males

androgen-dependent prostate cancer

9

Toxicity of estrogens

increase risk of endometrial cancer
bleeding in postmenopausal women
clear cell adenomcarcinoma of the vagina (in women exposed to DES in utero)
increased risk of thrombi

10

Contraindications to estrogen use

ER+ breast cancer
history of DVTs

11

Name the selective estrogen receptor modulators

clomiphene, tamoxifen, raloxifene

12

Mechanism of clomiphene

antagonist at estrogen receptors in the hypothalamus
prevents normal feedback inhibition and increases release of LH and FSH from pituitary to stimulate ovulation

13

Use of clomiphene

infertility due to anovulation (PCOS)

14

Toxicity of clomiphene

hot flashes
ovarian enlargement
multiple simultaneous pregnancies
visual disturbances

15

Mechanism of tamoxifen

antagonist at breast
agonist at bone, uterus

16

Use of tamoxifen

to treat and prevent recurrence of ER/PR+ breast cancers

17

Toxicity of tamoxifen

increased risk of thromboembolic events
increased risk of endometrial cancer

18

Mechanism of raloxifene

antagonist at breast, uterus
agonist at bone

19

Use of raloxifene

to treat osteoporosis

20

Toxicity of raloxifene

increased risk of thromboembolic events only

21

Use of hormone replacement therapy

to relieve or prevent menopause symptoms (hot flashes, vaginal atrophy)
to treat osteoporosis (increase estrogen, decrease osteoclast activity)

22

Toxicity of hormone replacement therapy

unopposed estrogen replacement therapy --> increased risk of:
- endometrial cancer (so add progesterone)
- cardiovascular risk (possibly)

23

Mechanism and use of anastrozole/exemestane

aromatase inhibitors used in postmenopausal women with ER+ breast cancer

24

Mechanism of progestins

bind progesterone receptors and decrease growth and vascularization of the endometrium

25

Use of progestins

oral contraceptives
treatment of endometrial cancer
abnormal uterine bleeding

26

Mechanism of mifepristone

competitive inhibitor of progestins at progesterone receptors

27

Use of mifepristone

termination of pregnancy (administered with misopristol (PGE1)

28

Toxicity of mifepristone

heavy bleeding
GI effects (nausea, vomiting, anorexia)
abdominal pain

29

Mechanism of oral contraception (progestins and estrogen)

estrogen and progestins inhibit LH/FSH and thus prevent the estrogen surge
no estrogen surge prevents an LH surge and thus no ovulation occurs

30

Mechanism of progestins in OCP

thicken cervical mucus
inhibit endometrial proliferation (less suitable for implantation)

31

Contraindications for OCP use

smokers >35 years old (increase CVD risk)
patients with history of thromboembolism and stroke
history of estrogen-dependent tumor

32

Mechanism and use of terbutaline and ritodrine

beta2-agonist that relax uterus
used to decrease contraction frequency in women during labor (prolong labor)

33

Mechanism of danazol

synthetic androgen that acts as partial agonist at androgen receptors

34

Use of danazol

endometriosis
hereditary angioedema

35

Toxicity of danazol

weight gain
edema
acne
hirsutism
masculinization
decrease HDL levels
hepatotoxicity

36

Mechanism of testosterone, methyltestosterone

agonists at androgen receptors

37

Use of testosterones

treat hypogonadism
promote development of secondary sex characteristics
stimulate anabolism to recovery after burn or injury

38

Toxicity of testosterones

masculinization in females
decreased intratesticular testosterone in males by inhibiting release of LH (via negative feedback) --> gonadal atrophy
premature closure of epiphyseal plates
increased LDL and decreased HDL

39

Antiandrogens

finasteride, flutamide, ketoconazole, sprionolactone

testosterone --> DHT via 5-alpha reductase

40

Mechanism of finasteride

5alpha-reductase inhibitor (decreases conversion of testosterone to DHT)

41

Use of finasteride

BPH to decrease size and male pattern baldness

42

Mechanism of flutamide

nonsteroidal competitive inhibitor at androgen receptors

43

Use of flutamide

prostate carcinoma

44

Mechanism of ketoconazole

inhibits steroid synthesis (inhibits 17,20 desmolase)

45

Mechanims of spironolactone

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

46

Use of ketoconazole and spironolactone

to treat PCOS to reduce androgenic symptoms

47

Side effects of ketoconazole and sprinonolactone

gynecomastia and amenorrhea

48

Mechanism and use of tamulosin

alpha1-antagonist used to treat BPH by inhibiting smooth muscle contraction
selective for alpha1A,D receptors (found on prostate) vs. vascular alpha1B receptors

49

Mechanism of sildenafil, vardenafil, tadalafil

inhibit PDE5 --> increased cGMP and smooth muscle relaxation in corpus cavernosum --> increased blood flow and penile erection

50

Use of sildenafil, vardenafil, tadalafil

erectile dysfunction

51

Toxicity of sildenafil, vardenafil, tadalafil

headache, flushing, dyspepsia, cyanopsia (blue-tinted vision)

risk of life-treatening hypotension in patients taking nitrates

52

Mechanism of minoxidil

direct arteriolar vasodilator

53

Use of minoxidil

androgenetic alopecia
severe refractory hypertension