Block 2 Flashcards
what is the mechanism of action of estrogen
diffuse across membrane
bind to intracellular receptors
hormone receptor complex binds to a hormone response element
what is the effect of estrogen on the bone
decreases osteoclast activity
what is the effect of estrogen on the RAAS system
increases angiotensinogen
what is the effect of estrogen having high enterohepatic circulation
increases the synthesis of clotting factors and plasma angiotensinogen
does estrogen or progesterone have a favorable effect on the lipid profile
estrogen: increases HDL, decreases LDL
what are 7 uses of estrogen
primary hypogonadism in females
androgen dependent prostatic tumors
menopause hormonal therapy
hirsutism
PCOS
acne
menopause hormonal therapy
what drug can be used in women with a history of breast cancer when estrogens are contraindicated
Paroxetine (SSRI)
name 5 adverse effects of estrogen use
increased risk of endometrial/breast cancer
thromboembolism
migraine
postmenopausal bleeding
edema
estrogen use is contraindicated in situations such as (6)
liver disease
untreated hypertension
porphyria cutanea tarda
thromboembolism disorders
high risk for breast cancer
estrogen dependent neoplasms/endometrial hyperplasia
name 5 uses of progesterone
contraception
menopause hormone therapy
endometrial hyperplasia/cancer
increase appetite (megestrol acetate in cancer or AIDS)
prevent recurrent miscarriages
what is the effect of progesterone on bone
can cause osteoporosis
what is the effect of progesterone on the lipid profile
increases LDL, decreases HDL
adverse effects of progesterone use include (5)
changes in libido
hirsutism
acne
osteoporosis
change in libido
what are 2 examples of drugs which act as antiestrogens
Clomiphene
Fulvestrant
what is the mechanism of action of fulvestrant
increases intracellular degradation of ERalpa receptor which protecting ERbeta–>decreases estrogen effect
Fulvestrant, an antiestrogen, is used in what 2 conditions
breast cancer in women resistant to Tamoxifen and aromatase inhibitors
breast cancer with endometrial risk
what is the mechanism of action of Clomiphene
partial agonist at estrogen receptors causes interference of negative feedback on the hypothalamus and pituitary, leading to increased FSH/LH, allowing for an increase in ovulation and pregnancy
what is Clomiphene used for
infertility (ovulation induction)
what are 3 adverse effects of Clomiphene, an antiestrogen
multiple births
visual disturbances
increased risk of ovarian cancer/ovarian enlargement
what are 2 examples of selective estrogen receptor modulators
Tamoxifen
Raloxifene
what is the mechanism of action of selective estrogen receptor modulators
estrogenic in some issues, antiestrogenic in others
what is the mechanism of action of tamoxifen, a selective estrogen receptor modulator
competitive antagonist for estrogen receptors in breast tissue
agonist in bone and endometrium
how is tamoxifen metabolism
it’s a prodrug converted to active form in the liver by CYP2D6/3A4
what is tamoxifen, a selective estrogen receptor modulator, used for
estrogen receptor positive breast cancer
what are 5 adverse effects of tamoxifen
thromboembolism/pulmonary embolism
increased risk for endometrial cancer
hypercalcemia
cataracts
bone pain
what is the mechanism of action of Raloxifene, a selective estrogen receptor modulator
agonist effect on bone
antagonist effect on endometrium and breast
what are 2 uses of Raloxifene, a selective estrogen receptor modulator
prevention of osteoporosis in postmenopausal women
reduce risk of invasive breast cancer in postmenopausal women
what is an adverse effect of Raloxifene, a selective estrogen receptor modulator
thromboembolism
what is Toremifene used for
metastatic breast cancer
-ozole is a suffix used for what drug class
what are 2 other drugs in this class
aromatase inhibitors
Exemestane, Testolactone
what is the mechanism of action of aromatase inhibitors
block the conversion of androgens–>estrogen leads to increase in GnRH with increases FSH and LH
name 3 uses of aromatase inhibitors
estrogen dependent postmenopausal breast cancer
metastatic breast cancer
ovulation induction
name 2 adverse effects of aromatase inhibitors
osteoporosis with prolonged use
acne
what drug class is used for prepubertal cryptorchism
gonadotropins (FSH/LH)
what drug class can be used to aid with infertility in hypogonadal men
gonadotropins (FSH/LH)
what are 3 adverse effects of gonadotropin use
multiple pregnancies
ovarian hyperstimulation syndrome
gynecomastia
what is the mechanism of action of gonadotropin agonists
pulsatile release increases FSH/LH release
continuous release increases FSH/LH release for 7-10 days, then decreases
what is an example of a gonadotropin analog
gonadorelin
what type of action does gonadorelin have
short acting gonadotropin–>increased FSH and LH release
what are the uses of gonadorelin, a short acting gonadotropin
diagnosis of hypogonadism
infertility
what type of drug action does goserelin have
long acting continuous release–>decreased FSH/LH
in what 5 situations is goserelin, a long acting gonadotropin analog, used
endometriosis
uterine leiomyoma
precocious puberty
breast/ovarian cancer
early pubertal transgender adolescents
what are 3 adverse effects of gonadotropin analogues
symptoms of menopause
gynecomastia in men
osteoporosis with long term use
GnRH receptor antagonists have the suffix ___
-relix
what is the mechanism of action of combined oral contraceptives
negative feedback to reduce levels of FSH/LH –> decreased ovulation, atrophy of glands, slowing of tubal motility and ova transport, thickens cervical mucus
in combined oral contraceptive pills, estrogen reduced __, progesterone reduced __
estrogen reduces FSH
progesterone reduces LH
what are 5 uses of combined oral contraceptives
endometriosis
hirsutism
PCOS
reduce endometrial/ovarian/colorectal cancer
primary dysmenorrhea
if severe adverse effects such as __ (4) occur with combined oral contraceptive use, use must be immediately withdrawn
thromboembolism
hepatic adenoma
depression
increased risk of breast cancer/cerebrovascular disorders
combined oral contraceptive use is contraindicated if a patient has __ (9)
thromboembolic disease
coronary disease
cerebrovascular disease
smoking
migraines
undiagnosed vaginal bleeding
mild hypertension
gallbladder disease
convulsive disorders
combined oral contraceptives should be avoided with use of what other drugs
enzyme inducers
antibiotics
mini pills are classified as __ only pills
progesterone
what is the mechanism of action of mini pills (progesterone only pills)
decrease frequency of GnRH release–>decreased midcycle LH surge
thickening of cervix mucus
__ drugs are used when estrogen is contraindicated
mini (progesterone only)
in what 5 cases are mini pills uses
chronic smokers
hepatic disease
hypertension
psychosis
history of thromboembolism
what are 2 adverse effects of mini pill (progesterone only) use
doesn’t completely suppress ovulation–>irregular fertile periods
amenorrhea
