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Flashcards in repro pharmacology Deck (34)
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1

leuprolide

"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

2

how to treat prostate cancer w a GnRH analog?

continuous leuprolide + flutamide

3

why is leuprolide antagonist when used continuously?

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

4

three drug estrogens

ethinyl estradiol, DES, mestranol

5

estrogens

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

6

toxicity of estrogens?

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

7

contraindications for estrogens?

breast cancer, history of DVTs

8

SERMs
3?

selective estrogen receptor modulators
clomiphene, tamoxifen, raloxifene

9

clomiphene

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

10

tamoxifen

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

use: treat and prevent ER + breast cancer

toxicity: thromboembolism, endometrial cancer

11

raloxifene

SERM, agonist on bone, antagonist on uterus

use: decreases reabsorption of bone so treats osteoporosis

toxicity: thromboembolism

12

hormone replacement therapy

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

13

problem and solution with estrogen replacement therapy?

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

14

anastrozole

aromatase inhibitor used in postmenopausal women with breast cancer

15

exemestane

aromatase inhibitor used in postmenopausal women with breast cancer

16

progestins

mech: bind progesterone receptors, decreasing endometrial growth and increasing its vascularization

use: oral contraceptives, endometrial cancer and abnormal uterine bleeding

17

mifepristone (RU-486)

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

18

sildenafil and vardenafil

"-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"

19

tamsulosin

alpha1 antagonist used to treat BPH by inhibiting SM contraction

selective for alpha1A,D receptors found on prostate

20

oral contraception

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)

21

contraindications for oral contraception

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

22

terbutaline

B2 agonist that relaxes the uterus

used to decrease contraction frequency in women during labor

23

danazol

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

24

testosterone and methyltestosterone

mech: agonist at androgen receptors

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

25

toxicity of testosterone or methyltestosterone

--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

26

4 antiandrogens

finasteride
flutamide
ketoconazole
spironolactone

27

what converts testosterone to dihydrotestosterone (DHT)?
which is stronger?

5alpha reductase

DHT is more potent

28

finasteride

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

use: BPH, hair loss/male pattern baldness

29

what is used to treat balding/male pattern balding?

finasteride promotes hair growth

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

30

flutamide

an antiandrogen
nonsteroidal competitive inhibitor of androgens at the testosterone receptor

use: prostate carcinoma