pharmacology of gonadal hormones and inhibitors Flashcards
What are the estrogen medications
estradiol
estrone
ethinyl estradiol
what are the SERMS
clomiphene
raloxifene
tamoxifen
What are the progesterone agonist/antagonists
ulipristal acetate
what are the anti-progestin meds
mifepristone
what is the major hormone active during the follicular phase of the menstraul cycle
estradiol
what is the dominant estrogen in postmenopausal women
estrone
what is the common synthetic estrogen
ethinyl
what are steroid hormones
progestogens
why use estrogen + progesterone
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
What is the MOA of estrogens
agonist to the estrogen receptor
what is the clinical use of estrogens
oral contraceptive
menopausal hormone therapy
gynecologic disorders
what is the MOA of combination oral contraceptives
-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
what are the progestin-related mechanisms of COC
endometrium becomes less suitable for implantation
cervical mucus thickens and becomes less permeable to penetration by sperm
impairment of normal tubal motility and peristalsis
what are noncontraveptive benefits of COCs
abnormal or dysfunctional uterine bleeding
dysmenorrhea
PMS and PMDD
Endometriosis
adenomyosis
functional ovarian cysts
PCOS
hormone replacement in women with primary hypogonadism
hyperandrogenism
what are the possible AE of COC
HTN
Thromboembolism
changes in lipids
bleeding irregularities
nausea
mood changes
breast changes
weight gain
headache
what are the AE of estrogen deficiency
vasomotor symptoms
what are the AE of estrogen excess
chloasma (melasma)
monorrhagia and clotting
increased breast size
what are the AE of progestin deficiency
breakthrough bleeding
delayed withdrawal bleeding
dysmenorrhea
heavy flow/clots
what are the AE of progestin excess
candidiasis
appetite increase
depression
fatigue
libido decrease
what are the AE of androgen excess
Acne
hirsutism
libido increase
oily skin/scalp
edema
what are the contraindications for estrogen-containing contraceptions
thromboembolic disorders
smokers > 35yo
breast cancer
impaired liver function
abnormal vaginal bleeding
pregnancy
cardiac disease
migraine
what are drug interactions iwth COC
anticonvulsants: phenytoin, carbamazepine, barbiturates, topiramate
antibiotics: Rifampin
drugs to treat HIV
what is the MOA of emergency contraception
works by delaying/blocking ovulation
must be used within 72 hours of unprotected intercourse
what are options for emergency contraception
levonorgestrel (Plan B)
Ulipristal (high dose progestin)
COC ( higher dose hormones)
Copper IUD
what is the MOA of levonorgestrel for EC
prevents ovulation or fertilization, alters endometrium
when is levonorgestrel contraindicated
known of suspected pregnancy
what are the AE of levonorgestrel
generally well tolerated, may cause GI upset, re-administer if vomiting within 2 hours
what is the MOA of ulipristal (ella)
binds to progesterone receptor. inhibitors/delays ovulations, alters endometrium.
selective progesterone receptor modulator
when is ulipristal contraindicated
known of suspected pregnancy
what are the AE of ulipristal
generally well tolerated, may cause headache, nausea, dysmenorrhea, dizziness, fatigue
What is mifepristone
medical abortion - synthetic steroid compound
anti-progesterone used for medical abortion
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
when can Mifepristone be used
less than 49 days (7 weeks) pregnant
what medication do you take after mifepristone
misoprostol (prostaglandin) for expulsion of products of conception
what are the goals of HRT
decrease symptoms which may include vasomotor symptoms (hot flashes), mood lability, vaginal atrophy, sleep disturbances
What are the risks of HRT
prematurely stopped because of increased incidence of cardiovascular events and breast cancer
what is HRT protective against
osteoporosis
colon cancer
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
what does SERMs stand for
Selective estrogen receptor modulators
What are the SERM medications
Tamoxifen
Raloxifene
Clomiphene
What is Tamoxifen
breast cancer tx: antagonists in breast, agonists at bone and endometrium
what is Raloxifene
osteoporosis treatment: antagonists in breast and endometrium, agonist at bone (less risk of endo ca vs tamo)
what is Clomiphene
ovulation induction: antagonists at hypothalamus, weak agonists in other tissues (prevent E neg feedback loop).
what are the AE of SERMs
flushing, hot flashes
mood changes, depression
GI upset
vaginal bleeding
bone marrow suppression (rare)
what are the contraindications of SERMs
warfarin therapy
hx DVT/PE
hx CVA/TIA
endometrial cancer
what is ospemifene
antagonist s in breasts, agonists in vaginal tissue and endometrium
what is toremifene
antagonists in breast, agonists in bone and endometrium (very similar to tamoxifen)
What does prostate cancer rely on
testosterone
what reduces the levels of androgen hormones with drugs to prevent the prostate cancer cells from growing
ADT
what is ADT
androgen deprivation therapy - reduces levels of androgen hormones
what are the ADT types
surgical castration
continuous GnRH agonists (leuprolide) and antagonists
anti-androgens (flutamide)
What is LHRH
Luteinizing hormone - releasing hormone
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
what is the ASE of leuprolide
HA
depression
GI
decreased libido
what are the indications of leuprolide
prostate CA
endometriosis
uterine fibroids
used for some IVF protocols
What is flutamide
synthetic, nonsteroidal anti-androgen
what are the AE of Flutamide
GI distress
gynecomastia
impotence
hot flashes
liver failure
what is the MOA of flutamide
competes with natural hormone for binding to the androgen receptor. blocks effects of androgens on target organs
what are the contraindications of flutamide
severe hepatic impairment
