repro pharmacology Flashcards
leuprolide
“can be used in LIEU of GnRH”
GnRH analog
-agonist when used in pulsatile way
-antagonist when used in continuous fashion
used for: infertility(pulsatile), prostate cancer (continuous), uterine fibrinoids (continuous), precocious puberty (continuous)
toxicity: antiandrogen, nausea/vomiting
how to treat prostate cancer w a GnRH analog?
continuous leuprolide + flutamide
why is leuprolide antagonist when used continuously?
downregulates the GnRH receptors in pituitary –> decreased FSH/LH
three drug estrogens
ethinyl estradiol, DES, mestranol
estrogens
ethinyl estradiol, DES, mestranol
mechanism: bind estrogen receptors
women use: hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women
men use: androgen-dependent prostate cancer
toxicity of estrogens?
risk of endometrial cancer, postmenopausal bleeding, clear cell adenocarcinoma of vagina for women exposed to DES in utero, risk of thrombi
contraindications for estrogens?
breast cancer, history of DVTs
SERMs
3?
selective estrogen receptor modulators
clomiphene, tamoxifen, raloxifene
clomiphene
SERM; antagonist at estrogen receptors in hypothalamus –> prevents normal feedback inhibition and increases release of LH and FSH from pituitary, which stimulates ovulation
use: infertility due to anovulation
toxicity: hot flashes, ovarian enlargement, multiple simultaneous pregnancies and visual disturbances
tamoxifen
SERM, antagonist on breast tissue, agonist at uterus and bone
use: treat and prevent ER + breast cancer
toxicity: thromboembolism, endometrial cancer
raloxifene
SERM, agonist on bone, antagonist on uterus
use: decreases reabsorption of bone so treats osteoporosis
toxicity: thromboembolism
hormone replacement therapy
used for relief or prevention of menopausal symptoms (hot flashes and vaginal atrophy) and osteoporosis ( by increasing estrogen and decreasing osteoclast activity)
problem and solution with estrogen replacement therapy?
unopposed ERT increases the risk of endometrial cancer so progesterone is added
anastrozole
aromatase inhibitor used in postmenopausal women with breast cancer
exemestane
aromatase inhibitor used in postmenopausal women with breast cancer
progestins
mech: bind progesterone receptors, decreasing endometrial growth and increasing its vascularization
use: oral contraceptives, endometrial cancer and abnormal uterine bleeding
mifepristone (RU-486)
mech: competitive inhibitor of progestins at progesterone receptors
* *administer with misoprostol (PGE1)
use: termination of pregnancy
toxicity: heavy bleeding, GI effects (nausea/vomiting, anorexia), abdominal pain
sildenafil and vardenafil
“-fils FILL the penis”
mech: inhibit phosphodiesterase 5, causing increased cGMP, smooth muscle relaxation in the corpus cavernosum, increases blood flow, and penile erection
use: erectile dysfunction
toxicity: headache, flushing, dyspepsia, impaired blue-green color vision; risk of life threatening hypotension in patients taking nitrates
“Hot, Headache, Heartburn, Hypotension”
tamsulosin
alpha1 antagonist used to treat BPH by inhibiting SM contraction
selective for alpha1A,D receptors found on prostate
oral contraception
synthetic progestins and estrogen
they inhibit LH/FSH and prevent estrogen surge –> no LH surge –> no ovulation
progestins cause thickening of cervical mucus (limits access of sperm to uterus) and inhibit endometrial proliferation (less suitable for implantation)
contraindications for oral contraception
do not use synthetic progestins and estrogen (contraceptives) with smokers>35yo (risk of CV events), patients with history of thromboembolism and stroke or history of estrogen-dependent tumor
terbutaline
B2 agonist that relaxes the uterus
used to decrease contraction frequency in women during labor
danazol
synthetic androgen that acts as partial agonist at androgen receptors
use: endometriosis and hereditary angioedema
toxicity: weight gain, acne, edema, hirsutism, masculinization, decreased HDL, hepatotoxicity
testosterone and methyltestosterone
mech: agonist at androgen receptors
use: treats hypogonadism, promotes development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury
toxicity of testosterone or methyltestosterone
- -masculinization in females
- -decreased intratesticular testosterone in males by inhibiting release of LH via negative feedback –> gonadal atrophy
- -premature closure of epiphyseal plates
- -increases LDL, decreases HDL
4 antiandrogens
finasteride
flutamide
ketoconazole
spironolactone
what converts testosterone to dihydrotestosterone (DHT)?
which is stronger?
5alpha reductase
DHT is more potent
finasteride
an antiandrogen
5alpha reductase inhibitor (less T is converted to DHT)
use: BPH, hair loss/male pattern baldness
what is used to treat balding/male pattern balding?
finasteride promotes hair growth
- to prevent male pattern hair loss, give a drug that will encourage female breast growth
flutamide
an antiandrogen
nonsteroidal competitive inhibitor of androgens at the testosterone receptor
use: prostate carcinoma
ketoconazole
an antiandrogen
inhibits steroid synthesis (inhibits 17,20-desmolase)
spironolactone
an antiandrogen
inhibits steroid binding, 17alpha-hydroxylase, and 17,20-desmolase
what are ketoconazole and spironolactone used to treat?
polycystic ovarian syndrome to prevent hirsutism
side effects of ketoconazole and spironolactone
gynecomastia and amenorrhea
