Cook: Drugs are bad, m'kay.... Flashcards
oxytocin
Uses: induction of labor, contractions after C-section or during uterine surgery, control postpartum hemorrhage, abortion
prostaglandins
use: onset of labor
dinoprostone
PGE2
use: induce labor
misoprostol
PGE1
use: induce labor
carboprost tromethamine
15-methyl-PGF2
use: induce labor
tocolytics
Use: delay premature parturition to slow delivery long enough for therapeutic measures including glucocorticoid therapy to increase pulmonary surfactant
CI: intra-amniotic infection, fetal demise, severe fetal growth restriction, pre-eclampsia
magnesium sulfate
tocolytic
MOA: decrease Ca availability
oral (laxative), parenteral
Tx: anticonvulsant (depress CNS, block peripheral NM transmission), hypomagnesemia, preeclampsia, eclampsia
also neuroprotective to fetus
excretion: renal: Mg reabsorbed
CI: myasthenia gravis, caution in renal insufficiency
AE: flushing, blurry vision/ headache, nausea, hypotension,, lethargy, pulmonary edema
toxicity: loss of pateller reflexes, decreased urine output, respiratory depression
indomethacin
tocolytic
MOA: COX inhibitor
AE: GI, platelet dysfunction
fetus: premature closure of ductus arteriosus, oligohydramnios
caster oil
herbal
tocolytic (Cook)
induce labor (article)
blue cohosh
herbal
tocolytic (Cook)
induce labor (article)
black cohosh
herbal
tocolytic (Cook)
induce labor (article)
oil of evening primrose
herbal
tocolytic (Cook)
induce labor (article)
gonadotropins
Use: female infertility in anovulatory women or women with hypogonadism, in vitro fertilization; male infertility reserved for time fertility is desired
Risk: multiple pregnancy (preferred in men due to this)
PULSATILE
pregnancy diagnostic kit
Ab to B subunit of CG
qualitative CG detection in urine
How can you determine the exact time of ovulation?
measure urinary LH: ovulation occurs 36 hours after onset of LH surge
menotropin
IM: FSH and LH
SC: rFSH
chorinoic gonadotropin
IM
CG: binds LH receptor
estrogen MOA
nuclear receptor: receptor/ligand complexes bind DNA near HRE (hormone response element)
native: rapidly degrades so can’t use
ethinyl estradiol
synthetic estrogen
decreased hepatic metabolism
use: combination pill
SERM (selective estrogen receptor modulator)
estrogen activity is tissue selective
activity: bone, brain, liver
no activity or antagonistic: breast, endometrium
Tx: breast CA
tamoxifen
SERM
raloxifene
SERM
combination pill (contraception)
estrogen: ethanol estradiol or mestranol
progestin: norethindrone, norgestrel, or levonorgestrel
MOA: prevents LH and FSH release by feedback inhibition
CI: thromboembolic disease, cerebral vascular disease, MI, CAD, congenital hyperlipidemia, breast CA, endometrial CA
off label use: polycystic ovary syndrome
mini-pill (contraception)
progestin only
blocks ovulation in ONLY 60-80% of cycles, impair sperm transport by thickening cervical mucus, decreases motility of ovules in oviduct, alters endometrium to impair implantation
slightly HIGHER failure rate than combination pill
for: breastfeeding women, over 35 yrs and smoke
postcoital contraception
morning after pill: two doses levonorgestrel separated by 12 hours
first does within 72 hours
most effective emergency contraception
contragestation
antiprogestin
mifepristone- RU48
antiprogestin: block progesterone binding to receptor
use: termination of pregnancy within 49 days
clomiphene
anti-estrogen: pure antagonist
act on ER in hypothalamus to block feedback inhibition of natural estrogens and stimulate GnRH which stimulates LH/FSH leading to ovulation
use: ovulation induction
fulvestrant
anti-estrogen: pure antagonist
act on ER in hypothalamus to block feedback inhibition of natural estrogens and stimulate GnRH which stimulates LH/FSH leading to ovulation
use: ovulation induction
mestranol
synthetic estrogen
decreased hepatic metabolism
use: combination pill
norethindrone
progestin
use: combination pill
norgestrel
progestin
use: combination pill
levonorgestrel
progestin
use: combination pill, morning after pill
gonadorelin acetate
synthetic GnRH
IV pulsatile pump
AE: phlebitis
cetrorelix
GnRH antagonist
Tx: in vitro fertilization (delay premature LH surge to delay ovulation to allow collection of ova) following FSH therapy
ganirelix
GnRH antagonist
degarelix
GnRH antagonist
Tx: prostate CA
goserelin acetate
GnRH agonist: initially increases LH then decreases LH and testosterone due to receptor down-regulation
Tx: prostate CA
triptorelin
GnRH agonist: initially increases LH then decreases LH and testosterone due to receptor down-regulation
Tx: prostate CA
leuprolide
GnRH agonist: initially increases LH then decreases LH and testosterone due to receptor down-regulation
Tx: prostate CA
histrelin
GnRH agonist: down-regulates receptors
Tx: precocious puberty
nafarelin
GnRH agonist
Tx: precocious puberty and endometriosis
estrogen esters
estrogen: conjugated esters of estrogen, esters of estradiol
onapristone
antiprogestin: pure antagonist
anastrozole
aromatase inhibitor
letrozole
aromatase inhibitor
androgens
injection, oral, transdermal
ester: more lipid soluble, longer duration
binding of testosterone to androgen receptor that binds to DNA response element
conversion to DHT in some tissues (prostate, not muscle or kidney): more potent
use: androgen deficient man, endometriosis, PMS, elderly men to maintain muscle mass (prefer injection because transdermal can tear off skin)
testosterone
androgen
testosterone transdermal patches
androgen
methyl-testosterone
testosterone derivative
testosterone propionate
testosterone derivative
testosterone cypionate
testosterone derivative
danazol
weak testosterone
Tx: PMS
flutamide
androgen receptor antagonist
Tx: prostate CA
AE: hepatic, 3x administration
bicalutamide
androgen receptor antagonist
Tx: prostate CA
finasteride
inhibitor of 5alpha-reductase
Tx: BPH, male pattern baldness
should not be touched by pregnant women: absorbed in skin and causes birth defects in male fetus
men should not donate blood
anabolic steroids
abused by athletes
AE: low T, decreased libido, decreased spermatogenesis, HEPATOTOXICITY, CHD
ER alpha
estrogen receptor
female reproductive tract: uterus, vagina, ovary and many other tissues
ER Beta
estrogen receptor
prostate gland and ovary
estrogen actions
- increase HDL, lower LDL (lower CHD in pre-menopausal women)
- breast development
- bone maturation, close epiphyseal plates, antagonizes bone resorption, shapes pelvis
- increase muscle of myometrium
- increase libido
- increase hepatic proteins (TBG, transcortin, SHBG, clotting factors)
estrogen adverse effects
- TUMORS (breast, uterus, testis, bone, kidney, etc.)
2. VENOUS THROMBOEMBOLISM: increase risk of stroke (elevated in women that smoke)
progesterone actions
- aids in maintaining pregnancy
- inhibits uterine contraction
- alveolobular development of breast secretary apparatus
- decrease HDL, increase LDL
- body temperature rise at ovulation
- depressant and hypnotic effects on brain
estrogen and progesterone therapeutic uses
native: rapidly degraded by liver so can’t use orally
ex of uses: prostate and breast CA, fertility control, hormone replacement therapy (menopause, osteoporosis, ovarian failure), dysfunctional uterine bleeding (irregular menstrual cycle), ovulation induction in infertile women
DES (diethylstilbesterol)
synthetic non-steroidal estrogen
Tx: prostate CA
clorotrianisene
synthetic non-steroidal estrogen
Tx: prostate CA
benefits of shorter or fewer hormone free intervals with oral contraceptives
decrease menstrual symptoms: headache, bloating, menstrual pain
non-contraceptive benefits of oral contraceptives
- reduced dysfunctional uterine bleeding and dysmenorrhea
- menstrual regularity, increased hemoglobin
- combination pill: raise SHBG: decrease androgens: less hirsutism and acne
adverse effects of oral contraceptives
- general
- old formulations (high dose ethinyl estradiol)
- combination pill
- low dose ethinyl estradiol
- extended/continous cycle
- with antibiotics (which ones)
- drugs that decrease contraceptive effectiveness
- N/V, breast tenderness and enlargement
- old formulations (greater than 50mcg ethinyl estradiol): more MI, stroke
- combination pill: venous thromboembolism esp. smokers
- low dose ethinyl estradiol: breakthrough bleeding
- unexpected bleeding
- contraceptive failure: penicillins, tetracyclines
- rifampin, anti-HIV, anticonvulsants, St. John’s wort
progesterone adverse effects
acne, weight gain
transdermal patch (contraception)
ethinyl estradiol and progestin
new patch each week, patch free for one week
AE: skin irritation, break through bleeding first 2 cycles
CI: women over 90kg (198 lbs)
vaginal contraceptive ring
ethinyl estradiol and progestin
inserted intravaginally by patient: in place 3 weeks, one week ring free
considerations: do NOT remove for more than 3 hr, NOT effective until in place 7 days, rapid return to fertility after removal
injectable contraceptive
progesterone only: medroxyprogesterone
every 3 months
AE: amenorrhea, irregular bleeding, weight gain, headache, decreased bone density
considerations: DISCONTINUE after 2 years, delayed return to fertility (6-12 months)
contraceptive implant
progesterone only: etonogestrel
effective 3 years
AE: same as all progestins
Cu IUD
spermacidal effective 15-20 years (recommend removal at 10 yr) fertility quickly restored after removal use: contraception, dysmenorrhea AE: cramping
progestin releasing IUD
levonorgestrel
effective 5 yrs
use: contraception, dysmenorrhea
AE: irregular bleeding for 6-12 mo
condoms (male and female)
barrier contraceptive
protect against STDs
diaphragm/cervical cap
barrier protection with spermicide (in place 6 hr before and after sex)
unclear if it protects from STDs
spermacide
nonoxynol-9 (a surfactant)
foam, gel, cream, suppository, lube for condom/diaphragm
only effective for 1 hr: reapplication necessary
MUST be in contact with cervix
AE: less effective, irritation of vaginal mucosa, TSS
sponge
barrier with spermicide
moisten and place over cervix: effective immediately and up to 24 hr: MUST remain in place 6 hr after intercourse
NOT as good as diaphragm
calendar method of contraception
calculate ovulation taking temperature
avoid intercourse on presumed fertile days
HIGH FAILURE rate
types of emergency contraception
- oral contraceptives: NOT recommended
- copper IUD
- two dose progestin
AE: N/V with ethanol estradiol, headache, breast tenderness, abdominal pain
oxandrolone
anabolic steroid with less conversion to estrogens and less inhibition of testosterone synthesis
nicalutamide
androgen receptor antagonist
Tx: prostate CA
less hepatotoxic and once a day administration compared to flutamide
cyproterone acetate
androgen receptor antagonist: competes with DHT for androgen receptor, prevents translation to nucleus
Tx: acne, baldness, hirsutism, virilizing syndrome, inhibit libido in sex deviant males
spironolactone
aldosterone antagonist, competes for testosterone receptor
Tx: hyperaldosteronism, HTN, hirsuitism
nifedipine
tocolytic
MOA: Ca channel blocker
AE: flush, headache, dizzy palpitations, nausea
increased CO to compensate for vasodilation
other: MI, pulmonary edema, hypoxia, hypotension, atrial fibrillation
terbutaline
tocolytic
MOA: Beta mimetic
ritodrine
tocolytic
MOA: Beta mimetic
beta mimetic
tocolytic
AE: maternal cardiotoxicity and death
other: hyperglycemia, pulmonary edema
fetus: hypoglycemia, cardiotoxicity
