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
2
Q
Leuprolide–use
A
- uterine fibrinoids
- endometriosis
- precocious puberty
- prostate cancer
- infertility
3
Q
name the estrogens
A
- ethinyl estradiol
- DES
- mestranol
4
Q
estrogens–mechanism
A
- bind estrogen receptors
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
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
7
Q
what are the contraindications for estrogens?
A
- ER + breast cancer
- history of DVTs
8
Q
name 3 selective estrogen receptor modulators
A
- clomiphene
- tamoxifen
- raloxifene
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
10
Q
clomiphene–use
A
- infertility due to anovulation
- ie. PCOS
11
Q
clomiphene–toxicity
A
- hot flashes
- ovarian enlargement
- multiple simultaneous pregnancies
- visual disturbances
12
Q
tamoxifen–mechanism
A
- antagonist at breast
- agonist at bone, uterus
- increase risk of thromboembolic events and endometrial cancer
13
Q
tamoxifen–use
A
- treat and prevent recurrence of ER/PR + breast cancer
14
Q
raloxifene–mechanism
A
- antagonist at breast, uterus
- agonist at bone
*
15
Q
raloxifene–use
A
- osteoporosis
16
Q
raloxifene–toxicity
A
- inc risk of thromboembolic events but no increased risk of endometrial cancer (vs tamoxifen)
17
Q
name 3 aromatase inhibitors
A
- anastrozole
- letrozole
- exemestane
18
Q
aromatase inhibitors–mechanism
A
- inhibit peripheral conversion of androgens to estrogens
19
Q
aromatase inhibitors–use
A
- ER + breast cancer in post menopausal women
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
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
22
Q
hormone replacement therapy–toxicity
A
- possible cardiovascular risk
23
Q
name the progestins
A
- levonorgestrel
- medroxyprogesterone
- etonogestrel
- norethindrone
- megestrol
- others when combined with estrogen
24
Q
progestins–mechanism
A
- bind progesterone receptors
- decrease growth and increase vascularization of endometrium
- thicken cervical mucus
25
progestins--use
* contraception--pill, IUD, implant, depot injection
* endometrial cancer
* abnormal uterine bleeding
* progestin challenge
26
explain the progestin challenge
* presence of withdrawal bleeding excludes anatomic defects (ie. Asherman syndrome) and chronic anovulation without estrogen
27
name the antiprogestins
* mifepristone
* ulipristal
28
antiprogestins--mechanism
* competitive inhibitors of progestins at progesterone receptors
29
antiprogestins--use
* termination of pregnancy
* mifepristone with misoprostol
* emergency contraception
* ulipristal
30
what do you have to administer with Mifepristone?
misoprostol
31
Mifepristone--toxicity
* (antiprogestin)
* heavy bleeding
* GI effects
* nausea
* vomiting
* anorexia
* abdominal pain
32
explain combined contraception
* 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
what are contraindications for combined contraception?
* 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
copper intrauterine device--mechanism
* produces local inflammatory rxn toxic to sperm and ova
* prevent fertilization and implantation
* hormone free
35
copper intrauterine device--use
* long acting reversible contraception
* most effective emergency contraception
36
copper intrauterine device--toxicity
* heavier or longer menses
* dysmenorrhea
* risk of PID with insertion
37
what is a contraindication for copper intrauterine devices?
* active pelvic infection
38
terbutaline, ritodine--use
* decrease contraction frequency in women during labor
39
terbutaline, ritodine--mechanism
* beta 2 agonists that relax the uterus
40
danazol--mechanism
* synthetic androgen that acts as a partial agonist at androgen receptors
41
danazol--use
* endometriosis
* hereditary angiodema
42
danazol--toxicity
* weight gain
* edema
* acne
* hirsutism
* masculinization
* decrease HDL levels
* hepatotoxicity
43
testosterone, methyltestosterone--mechanism
* agonists at androgen receptors
44
testosterone, methyltestosterone--use
* treat hypogonadism
* promote develop of secondary sex characterisitcs
* stimulate anabolism to promote recovery after burn or injury
45
testosterone, methyltestosterone--toxicity
* 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
name 4 antiandrogens
* finasteride
* flutamide
* ketoconazole
* spironolactone
47
what enzyme is used to convert testosterone to DHT?
5alpha reductase
48
finasteride--mechanism
* 5 alpha reductase inhibitor
* decrease conversion of testosterone to DHT
49
finasteride--use
* BPH
* male pattern baldness
50
flutamide--mechanism
* nonsteroidal competitive inhibitor at androgen receptors
51
flutamide--use
* prostate carcinoma
52
ketoconazole--mechanism
* inhibits steroid synthesis
* inhibits 17, 20 desmolase
53
ketoconazole--use
* polycystic ovarian syndrome
* to reduce androgenic symptoms
54
ketoconazole--toxicity
* gynecomastia
* amenorrhea
55
spironolactone--mechanism
* inhibits steroid binding, 17 alpha hydroxylase, and 17, 20 desmolase
56
spironolactone--use
* polycystic ovarian syndrome
* to reduce androgenic symptoms
57
spironolactone--toxicity
* gynecomastia
* amenorrhea
58
tamsulosin--mechanism
* alpha 1 antagonist
* inhibits smooth muscle contraction
* selective for alpha1A, D receptors found on prostate vs. vascular alpha1B receptors
59
tamsulosin--use
* treat BPH
60
name 3 phosphodiesterase type 5 inhibitors
* sildenafil
* vardenafil
* tadalafil
61
phosphodiesterase type 5 inhibitors--mechanism
* inhibit PDE-5 --\> inc cGMP --\> prolonged smooth muscle relaxation in response to NO --\> increase blood flow in corpus cavernosum of penis
* "sildena**fil**, vardena**fil**, and tadala**fil** **fill** the penis"
* decrease pulmonary vascular resistance
62
phosphodiesterase type 5 inhibitors--use
* erectile dysfunction
* pulmonary hypertension
* BPH
* tadalafil only
63
phosphodiesterase type 5 inhibitors--toxicity
* headache
* flushing
* dyspepsia
* cyanopia (blue tinted vision)
* risk of life threatening hypotension in pts taking nitrates
* "**H**ot and sweaty," but then **H**eadache, **H**eartburn**,** **H**ypotension
64
minoxidil--mechanism
* direct arteriolar vasodilator
65
minoxidil--use
* androgenetic alopecia
* severe refractory hypertension
