Reproductive Flashcards
what is leuprolide
GnRH analog
leuprolide mechanism
pulsatile –> GnRH agonist
continuous –> GnRH antagonist (downregulates receptor) –> decrease FSH and LH
clinical use of pulsatile leuprolide
infertility
clinical use of continuous leuprolide (3)
- prostate cancer (with flutamide)
- uterine fibroids
- precocious puberty
three types of estrogen drugs
- ethinyl estradiol
- DES
- mestranol
clinical use of estrogens (3)
- hypogonadism or ovarian failure
- HRT
- androgen-dependent prostate cancer
side effects of estrogens
- increase risk endometrial cancer
2. increase risk thrombi
complications in female baby from DES exposure in utero
clear cell adenocarcinoma of vagina
contraindications for estrogen administration
ER+ breast cancer
history of DVTs
clomiphene drug class
selective estrogen receptor modulators (SERMs)
tamoxifen drug class
selective estrogen receptor modulators (SERMs)
raloxifene drug class
selective estrogen receptor modulators (SERMs)
clomiphene mechanism
antagonist at estrogen receptors in hypothalamus
prevents feedback inhibition –> increase LH and FSH release –> stimulates ovulation
clinical use clomiphene
infertility due to anovulation (i.e. PCOS)
side effects clomiphene (4)
- hot flashes
- ovarian enlargement
- multiple pregnancies
- visual disturbances
tamoxifen mechanism
estrogen receptor antagonist in breast, agonist in bone and uterus
clinical use tamoxifen
ER+ breast cancer
side effects tamoxifen (2)
- endometrial cancer
2. thromboembolic events
raloxifene mechanism
estrogen receptor agonist in bone, antagonist in uterus
clinical use raloxifene
osteoporosis (decreases resorption of bone)
side effects raloxifene (1)
- thromboembolic events
clinical use hormone replacement therapy (HRT) (2)
- relief of menopausal symptoms
2. osteoporosis (increase estrogen –> decrease osteoclast activity)
side effects HRT (2)
- endometrial cancer (unopposed estrogen, so add progesterone)
- cardiovascular risk
what is anastrozole
aromatase inhibitor
what is exemestane
aromatase inhibitor
clinical use anastrozole
used in postmenopausal women with breast cancer
clinical use exemestane
used in postmenopausal women with breast cancer
progestin mechanism
bind progesterone receptors –> decrease growth and increase vascularization of endometrium
clinical use progestin (2)
- oral contraceptives
2. endometrial cancer
mifepristone (RU-486) mechanism
competitive inhibitor of progestin (at progesterone receptors)
clinical use mifepristone
termination of pregnancy (give with misoprostol – PGE1)
side effects mifepristone (2)
- heavy bleeding
2. GI effects
mechanism oral contraceptives
estrogen and progestins inhibit LH/FSH –> prevent estrogen surge –> prevent ovulation
progestins: thickening of cervical mucus (sperm can’t get in) and inhibit endometrial proliferation (can’t implant)
contraindications for oral contraceptives (3)
- smokers > 35
- hx of thromboembolism or stroke
- hx estrogen-dependent tumor
what is terbutaline
beta-2 agonist
mechanism terbutaline
beta-2 agonist –> relaxes uterus –> decrease contraction frequency
what drug decreases contraction frequency during labor?
terbutaline (beta-2 agonist)
what is danazol?
synthetic androgen
mechanism danazol
synthetic androgen, partial agonist at androgen receptors
clinical use danazol (2)
- endometriosis
2. hereditary angioedema
side effects danazol (5)
- weight gain
- edema
- acne, hirsuitism, masculinization
- decrease HDL
- hepatotoxicity
mechanism testosterone
agonist at androgen receptors
mechanism methyltestosterone
agonist at androgen receptors
clinical use testosterone / methyltestosterone (3)
- hypogonadism
- promotes secondary sex characteristics
- anabolism for burn/injury recovery
side effects testosterone / methyltestosterone (4)
- masculinization
- inhibits release LH (negative feedback) –> gonadal atrophy
- premature closure epiphyseal plates
- increase LDL, decrease HDL
what are four antiandrogens?
- finasteride
- flutamide
- ketoconazole
- spironolactone
what is finasteride?
5-alpha reductase inhibitor
mechanism finasteride
inhibits 5-alpha reductase –> prevents conversion of testosterone to DHT
clinical use finasteride (2)
- BPH
2. male-pattern baldness (hair growth)
what is flutamide?
nonsteroidal competitive inhibitor of androgens at the testosterone receptor
clinical use flutamide
prostate carcinoma
what is ketoconazole?
antiandrogen, inhibits 17,20-desmolase
ketoconazole mechanism
inhibits 17,20-desmolase –> inhibits steroid synthesis
what is spironolactone?
antiandrogen
mechanism spironolactone
inhibits steroid binding
clinical use ketoconazole
PCOS (prevent hirsuitism)
what does tamoxifen do to LDL levels?
normalizes LDL and cholesterol in ovarian failure from breast cancer
clinical use spironolactone
PCOS (prevent hirsuitism)
what two drugs are used in PCOS to prevent hirsuitism?
spironolactone and ketoconazole
side effects spironolactone (2)
- gynecomastia
2. amenorrhea
side effects ketoconazole (2)
- gynecomastia
2. amenorrhea
what is tamsulosin?
alpha-1 antagonist used to treat BPH
mechanism tamsulosin
alpha-1 antagonist –> inhibits smooth muscle contraction
selective for alpha-1 receptors on prostate and not on vasculature
clinical use tamsulosin
BPH
mechanism sildenafil
inhibits phosphodiesterase 5 –> increase cGMP –> smooth muscle relaxation in corpus cavernosum –> erection
mechanism vardenafil
inhibits phosphodiesterase 5 –> increase cGMP –> smooth muscle relaxation in corpus cavernosum –> erection
clinical use sildenafil
erectile dysfunction
clinical use vardenafil
erectile dysfunction
side effects sildenafil
- headache
- flushing
- impaired blue-green vision
- heartburn (dyspepsia)
- risk life-threatening hypotension in pts taking nitrates
side effects vardenafil
- headache
- flushing
- impaired blue-green vision
- heartburn (dyspepsia)
- risk life-threatening hypotension in pts taking nitrates
can you use sildenafil/vardenafil in patients taking nitrates?
NO!! (risk life-threatening hypotension)
