chapter 29- reproduction Flashcards
what is the mechanism of action of finasteride
selective inhibitor of type 2 5alpha-redutcase (inhibits peripheral testosterone conversion to DHT)
where is type 2 5alpha-reductase highly expressed
prostate
what is the mechanism of action of dutasteride
inhibits both type 1 and type 2 5alpha-reductase
what is the clinical application of finasteride
androgenic alopecia and BPH
what is the clinical application of dutasteride
BPH
what are some side effects seen with finasteride and dutasteride
breast tenderness, decreased libido, ED, ejaculatory disorder
what are some contraindications for finasteride/dutasteride use
known/suspected pregnancy; women and children
what symptoms does finasteride and dutasteride improve
symptoms of decreased urine flow
what is the mechanism of action of anastrozole and letrozole
competitive inhibitors of aromatase
what is the mechanism of action of exemestane and formestane
irreversible (covalent) inhibitors of aromatase
what is the clinical application of anastrozole, letrozole, exemestane, formestane
treatment and prevention of estrogen receptor-positive early stage, locally advanced and metastatic breast cancer
what is the most serious common adverse effect seen with anastrozole, letrozole, exemestane, formestane use
osteoporotic fractures
what is the mechanism of action of tamoxifen
estrogen recetor antagonist in breast tissue and partial agonist in endometrium and bone
what is the mechanism of action of clomiphene
estrogen receptor antagonist in hypothalamus and anterior pituitary gland and a partial agonist in ovaries
what is the mechanism of action of raloxifene
estrogen receptor agonist activity in bone, but antagonist in breast and endometrium
what is the clinical application of tamoxifen
prevention of breast cancer; palliative treatment of metastatic breast cancer
what is the clinical application of clomiphene
female infertility due to ovulatory disorder (induces ovulation)
what is the clinical application of bazedoxifene
osteoporosis
what is the clinical application of ospemifene
vulvovagnial atrophy, vaginal dryness
what is the clinical application of fulvestrant
treatment of ER positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy
what are some adverse effects seen with tamoxifen
malignant neoplasm of endometrium, strokes, hot flashes, abnormal menstruation
what are some adverse effects seen with clomiphene
thromboembolism; ovarian cysts, ovarian hypertrophy, vasomotor symptoms
what are some adverse effects seen with fulvestrant
nausea, asthenia, pain, vasodilation (hot flashes)
what are some contraindications for tamoxifen
history of DVT or PE
what are some contraindications for clomiphene
pregnancy; uncontrolled thyroid or adrenal dysfunction; liver disease; endometrial carcinoma; ovarial cysts; organic intracranial lesion
what are some contraindications for fulvestrant
pregnancy
what are some contraindications for flutamide
severe hepatic impairment
what are some contraindications for spironolactone
anuria, hyperkalemia, acute renal insufficiency
what are some contraindications for mifepristone
chronic adrenal failure, ectopic pregnancy, inherited porphyria, undiagnosed adnexal mass
what is the clinical application of flutamide
metastatic prostate cancer; BPH
what are some adverse effects seen with flutamide
hepatotoxicity, disorders of hematopoietic system
what are some adverse effects seen with spironolactone
hyperkalemic metabolic acidosis, GI hemorrhage, agranulocytosis, SLE
what is the mechanism of action of spironolactone
aldosterone receptor antagonist that also has significant antagonist activity at the androgen receptor
what derivation of spironolactone is sometimes used as progestin in some estrogen-progestin contraceptives
drospirenone
what are some adverse effects seen with mifepristone
prolonged bleeding time, bacterial infections, sepsis
what is the clinical application of mifepristone
abortion (through day 63 of pregnancy)
what is the clinical application of asoprisnil
investigational agent for treatment of endometriosis and uterine leiomyomata (fibroids)
what is the mechanism of action of mifepristone
progesterone receptro antagonist
what is the mechanism of acute of asoprisnil
progesterone receptor antagonist that inhibits growth of tissues derived from endometrium and myometrium
what combination estrogen-progestin contraception participants have the highest androgenic activity
Norgestrel and levonorgestrel
what combination estrogen-progestin contraception participants have moderate androgenic activity
norethindrone and norethindone acetate
what combination estrogen-progestin contraception participants have low androgen receptor cross reactivity
ethynodiol, norgestimate, gestodene, desogestrel
what combination estrogen-progestin contraceptive component can also be used as emergency contraception (morning after)
Levonorgestrel
what are some adverse effects for progestin-only contraceptives
irregular periods, breast tenderness, nausea, dizziness, headache
what are some contraindications for progestin-only contraceptives
acute liver disease, benign or malignant liver tumors, known/suspected breast cancer, pregnancy
what progestin-only contraceptive can be given parenterally every 3 months
medroxyprogestoerone acetate
what are some contraindications for androgens used for hormone replacement
breast cancer in men; prostate cancer; pregnancy when used in women
