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Pharm 3: Reproductive Medications > pharmacology of gonadal hormones and inhibitors > Flashcards

pharmacology of gonadal hormones and inhibitors Flashcards

(59 cards)

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1
Q

What are the estrogen medications

A

estradiol
estrone
ethinyl estradiol

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2
Q

what are the SERMS

A

clomiphene
raloxifene
tamoxifen

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3
Q

What are the progesterone agonist/antagonists

A

ulipristal acetate

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4
Q

what are the anti-progestin meds

A

mifepristone

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5
Q

what is the major hormone active during the follicular phase of the menstraul cycle

A

estradiol

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6
Q

what is the dominant estrogen in postmenopausal women

A

estrone

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7
Q

what is the common synthetic estrogen

A

ethinyl

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8
Q

what are steroid hormones

A

progestogens

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9
Q

why use estrogen + progesterone

A

estrogen: potentiates progesterone so lower doses can be used, allows for endometrial growth, so less break-through bleeding
progesterone: protects against estrogen-induced endometrial hyperplasia

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10
Q

What is the MOA of estrogens

A

agonist to the estrogen receptor

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11
Q

what is the clinical use of estrogens

A

oral contraceptive
menopausal hormone therapy
gynecologic disorders

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12
Q

what is the MOA of combination oral contraceptives

A

-suppresses LH and FSH by interfering with hypothalamic gonadotropin-releasing hormone (GnRH) and pituitary gonadotropin secretion
-ovulation is suppressed through inhibition of mid-cycle LH surge
-suppress ovarian folliculogenesis via suppression of pituitary FSH secretion

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13
Q

what are the progestin-related mechanisms of COC

A

endometrium becomes less suitable for implantation
cervical mucus thickens and becomes less permeable to penetration by sperm
impairment of normal tubal motility and peristalsis

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14
Q

what are noncontraveptive benefits of COCs

A

abnormal or dysfunctional uterine bleeding
dysmenorrhea
PMS and PMDD
Endometriosis
adenomyosis
functional ovarian cysts
PCOS
hormone replacement in women with primary hypogonadism
hyperandrogenism

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15
Q

what are the possible AE of COC

A

HTN
Thromboembolism
changes in lipids
bleeding irregularities
nausea
mood changes
breast changes
weight gain
headache

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16
Q

what are the AE of estrogen deficiency

A

vasomotor symptoms

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17
Q

what are the AE of estrogen excess

A

chloasma (melasma)
monorrhagia and clotting
increased breast size

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18
Q

what are the AE of progestin deficiency

A

breakthrough bleeding
delayed withdrawal bleeding
dysmenorrhea
heavy flow/clots

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19
Q

what are the AE of progestin excess

A

candidiasis
appetite increase
depression
fatigue
libido decrease

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20
Q

what are the AE of androgen excess

A

Acne
hirsutism
libido increase
oily skin/scalp
edema

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21
Q

what are the contraindications for estrogen-containing contraceptions

A

thromboembolic disorders
smokers > 35yo
breast cancer
impaired liver function
abnormal vaginal bleeding
pregnancy
cardiac disease
migraine

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22
Q

what are drug interactions iwth COC

A

anticonvulsants: phenytoin, carbamazepine, barbiturates, topiramate
antibiotics: Rifampin
drugs to treat HIV

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23
Q

what is the MOA of emergency contraception

A

works by delaying/blocking ovulation
must be used within 72 hours of unprotected intercourse

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24
Q

what are options for emergency contraception

Study These Flashcards
A

levonorgestrel (Plan B)
Ulipristal (high dose progestin)
COC ( higher dose hormones)
Copper IUD

25
what is the MOA of levonorgestrel for EC
prevents ovulation or fertilization, alters endometrium
26
when is levonorgestrel contraindicated
known of suspected pregnancy
27
what are the AE of levonorgestrel
generally well tolerated, may cause GI upset, re-administer if vomiting within 2 hours
28
what is the MOA of ulipristal (ella)
binds to progesterone receptor. inhibitors/delays ovulations, alters endometrium. selective progesterone receptor modulator
29
when is ulipristal contraindicated
known of suspected pregnancy
30
what are the AE of ulipristal
generally well tolerated, may cause headache, nausea, dysmenorrhea, dizziness, fatigue
31
What is mifepristone
medical abortion - synthetic steroid compound anti-progesterone used for medical abortion
32
what is the MOA of Mifepristone
competitively binds to progesterone receptor (blocks progesterone receptor). antagonizing endometrial and myometrial effects, leads to contraction-inducing activity. disrupts implanted embryo
33
when can Mifepristone be used
less than 49 days (7 weeks) pregnant
34
what medication do you take after mifepristone
misoprostol (prostaglandin) for expulsion of products of conception
35
what are the goals of HRT
decrease symptoms which may include vasomotor symptoms (hot flashes), mood lability, vaginal atrophy, sleep disturbances
36
What are the risks of HRT
prematurely stopped because of increased incidence of cardiovascular events and breast cancer
37
what is HRT protective against
osteoporosis colon cancer
38
what are the contraindications of HRT
history of breast cancer history of coronary heart disease previous hx of DVT/PE history of CVA or TIA acute liver disease unexplained vaginal bleeding risk of endometrial cancer
39
what does SERMs stand for
Selective estrogen receptor modulators
40
What are the SERM medications
Tamoxifen Raloxifene Clomiphene
41
What is Tamoxifen
breast cancer tx: antagonists in breast, agonists at bone and endometrium
42
what is Raloxifene
osteoporosis treatment: antagonists in breast and endometrium, agonist at bone (less risk of endo ca vs tamo)
43
what is Clomiphene
ovulation induction: antagonists at hypothalamus, weak agonists in other tissues (prevent E neg feedback loop).
44
what are the AE of SERMs
flushing, hot flashes mood changes, depression GI upset vaginal bleeding bone marrow suppression (rare)
45
what are the contraindications of SERMs
warfarin therapy hx DVT/PE hx CVA/TIA endometrial cancer
46
what is ospemifene
antagonist s in breasts, agonists in vaginal tissue and endometrium
47
what is toremifene
antagonists in breast, agonists in bone and endometrium (very similar to tamoxifen)
48
What does prostate cancer rely on
testosterone
49
what reduces the levels of androgen hormones with drugs to prevent the prostate cancer cells from growing
ADT
50
what is ADT
androgen deprivation therapy - reduces levels of androgen hormones
51
what are the ADT types
surgical castration continuous GnRH agonists (leuprolide) and antagonists anti-androgens (flutamide)
52
What is LHRH
Luteinizing hormone - releasing hormone
53
What is the MOA of Leuprolide
inhibitor of gonadotropin secretion. results in transient increase in LH/FSH which leads to transient increase in testosterone and estrogen BUT continuous GnRH agonist use results in decrease in LH/FSH and suppression of testosterone production in males and estrogen production in females
54
what is the ASE of leuprolide
HA depression GI decreased libido
55
what are the indications of leuprolide
prostate CA endometriosis uterine fibroids used for some IVF protocols
56
What is flutamide
synthetic, nonsteroidal anti-androgen
57
what are the AE of Flutamide
GI distress gynecomastia impotence hot flashes liver failure
58
what is the MOA of flutamide
competes with natural hormone for binding to the androgen receptor. blocks effects of androgens on target organs
59
what are the contraindications of flutamide
severe hepatic impairment

Pharm 3: Reproductive Medications (2 decks)

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