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PLAB Pharmacology > Reproductive Pharmacology > Flashcards

Reproductive Pharmacology Flashcards

1
Q

Leuprolide–mechanism pulsatile vs. continuous

A
  • pulsatile: GnRH analog with agonist properties
    • “Leuprolide can be used in lieu of GnRH”
  • continuous: antagonist properties
    • downregulates GnRH receptor in pituitary –> decrease FSH/LH
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2
Q

Leuprolide–use

A
  • uterine fibrinoids
  • endometriosis
  • precocious puberty
  • prostate cancer
  • infertility
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3
Q

name the estrogens

A
  • ethinyl estradiol
  • DES
  • mestranol
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4
Q

estrogens–mechanism

A
  • bind estrogen receptors
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5
Q

estrogens–use

A
  • hypogonadism or ovarian failure
  • menstrual abnormalities
  • hormone replacement therapy in postmenopausal women
  • use in men with androgen dependent prostate cancer
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6
Q

estrogens–toxicity

A
  • inc risk of endometrial cancer
  • bleeding in postmenopausal women
  • clear cell adenocarcinoma of vagina in demales exposed to DES in utero
  • inc risk of thrombi
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7
Q

what are the contraindications for estrogens?

A
  • ER + breast cancer
  • history of DVTs
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8
Q

name 3 selective estrogen receptor modulators

A
  • clomiphene
  • tamoxifen
  • raloxifene
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9
Q

clomiphene–mechanism

A
  • antagonist at estrogen receptors in hypothalamus
  • prevents normal feedback inhibition and increase release of LH and FSH from pituitary which stimulate ovulation
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10
Q

clomiphene–use

A
  • infertility due to anovulation
    • ie. PCOS
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11
Q

clomiphene–toxicity

A
  • hot flashes
  • ovarian enlargement
  • multiple simultaneous pregnancies
  • visual disturbances
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12
Q

tamoxifen–mechanism

A
  • antagonist at breast
  • agonist at bone, uterus
  • increase risk of thromboembolic events and endometrial cancer
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13
Q

tamoxifen–use

A
  • treat and prevent recurrence of ER/PR + breast cancer
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14
Q

raloxifene–mechanism

A
  • antagonist at breast, uterus
  • agonist at bone
    *
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15
Q

raloxifene–use

A
  • osteoporosis
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16
Q

raloxifene–toxicity

A
  • inc risk of thromboembolic events but no increased risk of endometrial cancer (vs tamoxifen)
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17
Q

name 3 aromatase inhibitors

A
  • anastrozole
  • letrozole
  • exemestane
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18
Q

aromatase inhibitors–mechanism

A
  • inhibit peripheral conversion of androgens to estrogens
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19
Q

aromatase inhibitors–use

A
  • ER + breast cancer in post menopausal women
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20
Q

hormone replacement therapy–use

A
  • used for relief or prevention of menopausal symptoms (ie. hot flashes, vaginal atrophy)
  • tx of osteoporosis
    • inc estrogen, dec osteoclast activity
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21
Q

why is progesterone added to hormone replacement therapy?

A
  • unopposed estrogen replacement therapy inc risk of endometrial cancer, so have to add progesterone
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22
Q

hormone replacement therapy–toxicity

A
  • possible cardiovascular risk
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23
Q

name the progestins

A
  • levonorgestrel
  • medroxyprogesterone
  • etonogestrel
  • norethindrone
  • megestrol
  • others when combined with estrogen
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24
Q

progestins–mechanism

A
  • bind progesterone receptors
  • decrease growth and increase vascularization of endometrium
  • thicken cervical mucus
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25
Q

progestins–use

A
  • contraception–pill, IUD, implant, depot injection
  • endometrial cancer
  • abnormal uterine bleeding
  • progestin challenge
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26
Q

explain the progestin challenge

A
  • presence of withdrawal bleeding excludes anatomic defects (ie. Asherman syndrome) and chronic anovulation without estrogen
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27
Q

name the antiprogestins

A
  • mifepristone
  • ulipristal
28
Q

antiprogestins–mechanism

A
  • competitive inhibitors of progestins at progesterone receptors
29
Q

antiprogestins–use

A
  • termination of pregnancy
    • mifepristone with misoprostol
  • emergency contraception
    • ulipristal
30
Q

what do you have to administer with Mifepristone?

A

misoprostol

31
Q

Mifepristone–toxicity

A
  • (antiprogestin)
  • heavy bleeding
  • GI effects
    • nausea
    • vomiting
    • anorexia
  • abdominal pain
32
Q

explain combined contraception

A
  • progestins + ethinyl estradiol
    • estrogens and progestins inhibit LH/FSH and thus prevent estrogen surge
      • no estrogen surge –> no LH surge –> no ovulation
    • progestins cause thickening of cervical mucus, so limit access of sperm to uterus
      • progestins also inhibit endometrial proliferation –> endometrium is less suitable to the implantation of the embryo
  • forms include pill, patch, and vaginal ring
33
Q

what are contraindications for combined contraception?

A
  • smokers > 35 yo
    • inc risk of cardiovascular events
  • pts with increased risk of cardiovascular dz
    • including history of venous thromboembolism, coronary artery dz, stroke
  • migraine (especially with aura)
  • breast cancer
34
Q

copper intrauterine device–mechanism

A
  • produces local inflammatory rxn toxic to sperm and ova
  • prevent fertilization and implantation
  • hormone free
35
Q

copper intrauterine device–use

A
  • long acting reversible contraception
  • most effective emergency contraception
36
Q

copper intrauterine device–toxicity

A
  • heavier or longer menses
  • dysmenorrhea
  • risk of PID with insertion
37
Q

what is a contraindication for copper intrauterine devices?

A
  • active pelvic infection
38
Q

terbutaline, ritodine–use

A
  • decrease contraction frequency in women during labor
39
Q

terbutaline, ritodine–mechanism

A
  • beta 2 agonists that relax the uterus
40
Q

danazol–mechanism

A
  • synthetic androgen that acts as a partial agonist at androgen receptors
41
Q

danazol–use

A
  • endometriosis
  • hereditary angiodema
42
Q

danazol–toxicity

A
  • weight gain
  • edema
  • acne
  • hirsutism
  • masculinization
  • decrease HDL levels
  • hepatotoxicity
43
Q

testosterone, methyltestosterone–mechanism

A
  • agonists at androgen receptors
44
Q

testosterone, methyltestosterone–use

A
  • treat hypogonadism
  • promote develop of secondary sex characterisitcs
  • stimulate anabolism to promote recovery after burn or injury
45
Q

testosterone, methyltestosterone–toxicity

A
  • causes masculinization in females
  • decrease intratesticular testosterone in males by inhibiting release of LH (negative feedback) –> gonadal atrophy
  • premature closure of epiphyseal plates
  • increase LDL
  • decrease HDL
46
Q

name 4 antiandrogens

A
  • finasteride
  • flutamide
  • ketoconazole
  • spironolactone
47
Q

what enzyme is used to convert testosterone to DHT?

A

5alpha reductase

48
Q

finasteride–mechanism

A
  • 5 alpha reductase inhibitor
    • decrease conversion of testosterone to DHT
49
Q

finasteride–use

A
  • BPH
  • male pattern baldness
50
Q

flutamide–mechanism

A
  • nonsteroidal competitive inhibitor at androgen receptors
51
Q

flutamide–use

A
  • prostate carcinoma
52
Q

ketoconazole–mechanism

A
  • inhibits steroid synthesis
    • inhibits 17, 20 desmolase
53
Q

ketoconazole–use

A
  • polycystic ovarian syndrome
    • to reduce androgenic symptoms
54
Q

ketoconazole–toxicity

A
  • gynecomastia
  • amenorrhea
55
Q

spironolactone–mechanism

A
  • inhibits steroid binding, 17 alpha hydroxylase, and 17, 20 desmolase
56
Q

spironolactone–use

A
  • polycystic ovarian syndrome
    • to reduce androgenic symptoms
57
Q

spironolactone–toxicity

A
  • gynecomastia
  • amenorrhea
58
Q

tamsulosin–mechanism

A
  • alpha 1 antagonist
  • inhibits smooth muscle contraction
  • selective for alpha1A, D receptors found on prostate vs. vascular alpha1B receptors
59
Q

tamsulosin–use

A
  • treat BPH
60
Q

name 3 phosphodiesterase type 5 inhibitors

A
  • sildenafil
  • vardenafil
  • tadalafil
61
Q

phosphodiesterase type 5 inhibitors–mechanism

A
  • inhibit PDE-5 –> inc cGMP –> prolonged smooth muscle relaxation in response to NO –> increase blood flow in corpus cavernosum of penis
    • “sildenafil, vardenafil, and tadalafil fill the penis”
  • decrease pulmonary vascular resistance
62
Q

phosphodiesterase type 5 inhibitors–use

A
  • erectile dysfunction
  • pulmonary hypertension
  • BPH
    • tadalafil only
63
Q

phosphodiesterase type 5 inhibitors–toxicity

A
  • headache
  • flushing
  • dyspepsia
  • cyanopia (blue tinted vision)
  • risk of life threatening hypotension in pts taking nitrates
    • “Hot and sweaty,” but then Headache, Heartburn, Hypotension
64
Q

minoxidil–mechanism

A
  • direct arteriolar vasodilator
65
Q

minoxidil–use

A
  • androgenetic alopecia
  • severe refractory hypertension

PLAB Pharmacology (17 decks)

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