MOA Flashcards
USED IN T1DM AND T2DM to regulate postprandial glucose
pramlintide
rapidly contracts the uterine smooth muscle through activation of serotonin and alpha adrenergic receptors to
deliver the placenta AFTER LABOR IS OVER!!!!
(will abort the baby if given during labor)
ergonovine maleate
methylergonovine maleate
when giving glucocorticoids what type of dose do you start with
high dose then taper down to lowest effective dose
repaglinide, nateglinide (meglitinides)
NOT a sulfa drug, these that close the K channel, depolarize the membrane, and cause insulin to be exocytosed
rhPTH (1-84)
recombinant PTH that binds to receptor to stimulate the RANK ligand to cause
OSTEOCLASTIC and BLASTIC activity
used in tx of hypOparathyroidism
tolbutamide, chlorpropamide, tolazamide
1st gen sulfonylureas that close the K channel, depolarize the membrane, and cause insulin to be exocytosed
calcitonin
inhibits bone resporption of Ca and phos by osteoclasts
antagonizes the actions of PTH
acarbose and miglitol
alpha glucosidase inhibitors that delay CHO digestion and decrease intestinal glucose absorption
androgen receptor antagonists
reduce male sex accessory organ function
flutamide
bicalutamide
nilutamide
inhibits bone resporption of Ca and phos by osteoclasts
antagonizes the actions of PTH
calcitonin
DPP-4 inhibitors that inhibit the the enzyme that degrades GLP-1 (increasing insulin secretion)
“gliptins”
hMG
used for FSH properties
** develops the ovarian follicles and stimulates estrogen **
** stimulates spermatogenesis **
(also has LH but FYI)
in ART
what are females given to ensure the transfer of the embryo
progesterone
iodide
rapidly decreases the synthesis and release of T3 and T4 for a short term effect
short term (1-2 week) tx with glucocorticoids does what to the HPA axis
not likely to cause the life threatening adrenal insufficiency problems
exemestane
irreversible inhibitor of aromatase (enzyme in the final step in estrogen synthesis)
DOC for breast CA tx of POST menopausal women
nifedipine
stops uterus smooth muscle contractions (CCB)
prevents early labor
works on OT receptors in the uterus to
induce labor (DOC)
prevent hemorrhage
stimulate milk let down reflex
oxytocin
spironolactone
mineralocorticoid receptor antagonist
“gliflozin”
SGLT-2 inhibitors that inhibit the Na-glucose co-transporter in the kideny
bromocriptine
dopamine agonist-
leads to suppression of hepatic glucose production
decreases postmeal plasma glucose levels
suppress testosterone synthesis and spermatogeneis
long acting GnRH analogues and antagonists antiandrogen MOA
SGLT-2 inhibitors that inhibit the Na-glucose co-transporter in the kideny
“gliflozin”
cholecalciferol (skin)
ergocalciferol (diet)
calcitriol (active)
(vitamin D)
increases GI Ca and phos absorption
must be adequate for optimal absorption of Ca
decreses renal excretion of Ca and Phos
equal anti inflammatory and salt retaining effects
hydrocortisone
cortisone
lots of SALT RETAINING effects
NO
anti-inflammatory effects
aldosterone
fludrocortisone
what do you do to decrease the suppression on the adrenal gland caused by glucocorticoids
give on alternate days
estradiol, estrone, estriol endocervical gland effects
cervical mucus
LH agonist
binds to the LH receptor
** stimulates progesterone to make the corpus luteum **
** stimulates testosterone production in the testes **
hCG
chronic tx with glucocorticoids does what to the HPA axis
suppresses it to the point where it can cause life threatening adrenal insufficiency
this can last for months
inhibit LH secretion
inhibiting the creation of steroids by the testes
estrogen antiandrogen MOA
gradually inhibits the synthesis of T4
propylthiouracil and methimazole
mifepristone
receptor antagonist of
both
glucocorticoids
and
progesterone
metformin
(1) decreases gluconeogenesis, glycogenolysis, and CHO intestinal absorption (2) increases insulin sensitivity
1st- hCG (for up to a year)
2nd- add hMG (for a few months)
male fertility tx
beta blocker that inhibits the peripheral conversion of T4 to T3
propanalol
emergency only use to stop early labor by short term cervicouterine relaxation
nitroglycerin
anti-fibrinolytic that inhibits the activation of plasminogen
reduces death due to postpartum hemorrhage
“along with standard uterotonic therapy”
tranexamic acid
indomethacin
inhibits COX to reduce prostaglandin synthesis
and delay early labor
radioactive iodine 131
in small amounts it is diagnostic but in large amounts it is curative
progesterone effects on uterus
converts endometrium to secretory state
needed to maintain pregnancy
progesterone thermogenic effects
increases body temp
antiestrogen that is
antagonist in the breast AND the uterus
agonist in the bone and liver
raloxifene
diazoxide
raises blood sugar by inhibiting insulin secretion or decreasing glucose utilization
“glitazone”
thiazolidinediones that increase insulin sensitivity by binding to PPARy receptor
thiazolidinediones that increase insulin sensitivity by binding to PPARy receptor
“glitazone”
bile acid sequestrant that lowers A1C somehow
colesevelam
tamoxifen
antiestrogen that is
agonist in uterus and bone
antagonist in breast
(used for estrogen dependent breast CA in pre and post menopausal women)
“glutides” and exenatide
GLP-1 agonists (act like GLP-1 to increase release of insulin and decrease release of glucagon
cetrorelix
ganirelix
GnRH antagonist
LD: suppresses LH
HD: suppresses FSH
goal is to suppress endogenous LH and FSH
propylthiouracil
gradually blocks the conversion of T4 to T3
anastrozole
letrozole
nonsteroidal
inhibitor of aromatase
(final step in estrogen synthesis)
long acting GnRH analogues and antagonists ART MOA
suppress LH and FSH for
inhibits PTH secretion
alters the physical chemical properties of the bone mineral
calcium
19- nortestosterones
norethindrone
norgestrel
levonorgestrel
norgestimate
derived from testosterone and have both progestin and androgenic activity
progesterone
medroxyprogesterone
megestrol acetate
progesterone derivatives
liothyronine sodium
synthetic T3- shorter half life and duration of action than T4
cortisone MOA
must be converted to hydrocortisone in the liver to be active
less potent than hydrocortisone
propanalol
beta blocker that inhibits the peripheral conversion of T4 to T3
propylthiouracil and methimazole
gradually inhibits the synthesis of T4
alpha glucosidase inhibitors that delay CHO digestion and decrease intestinal glucose absorption
acarbose and miglitol
hCG
LH agonist
binds to the LH receptor
** stimulates progesterone to make the corpus luteum **
** stimulates testosterone production in the testes **
in small amounts it is diagnostic but in large amounts it is curative
radioactive iodine 131
nitroglycerin
emergency only use to stop early labor by short term cervicouterine relaxation
a steroid
irreversible inhibitor of aromatase
(final step in estrogen synthesis)
exemestane
NOT a sulfa drug, these that close the K channel, depolarize the membrane, and cause insulin to be exocytosed
repaglinide, nateglinide (meglitinides)
1st gen sulfonylureas that close the K channel, depolarize the membrane, and cause insulin to be exocytosed
tolbutamide, chlorpropamide, tolazamide
antiestrogen that is
antagonist in the hypothalamus
agonist everywhere else
clomiphene
estradiol, estrone, estriol ovary effects
prepare follicle cells for ovulation (with FSH)
what are females given to ensure the embryo transfer
progesterone
progesterone derivatives
derivatives of progestin:
progesterone
medroxyprogesterone
megestrol acetate
antibody that binds to and inhibits the RANK ligand causing
OSTEOCLAST INHIBITION
used in osteoporosis
denosumab
oxytocin
works on OT receptors in the uterus to
induce labor (DOC)
prevent hemorrhage
stimulate milk let down reflex
synthetic T3- shorter half life and duration of action than T4
liothyronine sodium
ergonovine maleate
methylergonovine maleate
rapidly contracts the uterine smooth muscle through activation of serotonin and alpha adrenergic receptors to
deliver the placenta AFTER LABOR IS OVER!!!!
(will abort the baby if given during labor)
alpha glucosidase inhibitors that delay CHO digestion and decrease intestinal glucose absorption
acarbose and miglitol
estradiol, estrone, estriol pubertal effects
female secondary sex characteristics
close the epiphysis
danazol
weak progestin, androgen, and glucocorticoid
decreases function of the ovaries
female fertility tx
(fertilization)
1st- hMG (for 9-12 days)
2nd- hCG (1 dose)
**in sequence**
male fertility tx
1st- hCG (for up to a year)
2nd- add hMG (for a few months)
used for FSH properties
** develops the ovarian follicles and stimulates estrogen **
** stimulates spermatogenesis **
hMG
testosterone, methyltestosterone virilizing effects
spermatogenesis
sexual development
rapidly decreases the synthesis and release of T3 and T4 for a short term effect
iodide
lowers dopamine levels which leads to suppression of hepatic glucose production
bromocriptine
long acting GnRH agonist
initially causes an LH surge
BUT THE ULTIMATE EFFECT IS
INHIBITION OF GONADOTROPIN RELEASE
(goal is to reduce androgens)
leuprolide
goserelin
mifepristone
antiprogestin that blocks progestin binding to the progesterone receptor
relaxes the uterus
stops premature labor
mag sulfate
estrogen antiandrogen MOA
inhibit LH secretion
inhibiting the creation of steroids by the testes
antiestrogen that is
agonist in uterus and bone
antagonist in breast
(used for estrogen dependent breast CA in premenopausal women)
tamoxifen
“dronates”
PCP bond analogs of pyrophosphate that
INCORPORATE INTO BONE
inhibit osteoclasts
DOC for osteoporosis
synthetic T4- takes 4-6 weeks to reach steady state
levothyroxine sodium
estradiol, estrone, estriol vaginal epithelium effects
stimulate proliferation
mitotane
inhibitor of corticosteroid synthesis
adrenocorticolytic
causes adrenocorticol atrophy
(destroys the gland)
estrogens
long acting GnRH analoges and antagonists
androgen receptor antagonists
5-alpha reductase inhibitors
antiandrogens
(list of groups)
GLP-1 agonists (act like GLP-1 to increase release of insulin and decrease release of glucagon
“glutides” and exenatide
repeated applications with glucocorticoids causes a ___ effect
depot effect
(increases absorption)
denosumab
antibody that binds to and inhibits the RANK ligand causing
OSTEOCLAST INHIBITION
used in osteoporosis
estradiol, estrone, estriol metabolic effects
makes liver proteins (that bind to hormones)
increases HDL and reduces LDL
Na and H20 retention
progesterone’s effect on early labor
it PROPHYLACTICALLY prevents
not an acute tx
“paratides”
teraparatide, abaloparatide
PTH analogs that intermittently stimulate the PTH receptor to cause
OSTEOBLASTIC activity
used in osteoporosis
only anabolic osteoporosis drug
calcium
inhibits PTH secretion
alters the physical chemical properties of the bone mineral
glyburide, glipizide, glimepride
2nd gen sulfonylureas that close the K channel, depolarize the membrane, and cause insulin to be exocytosed
finasteride
dutasteride
5 alpha reducatse inhibitors
stop the conversion of testosterone to DHT
decreases DHT and PSA
increases total testosterone (so might make more estrogen)
GnRH antagonist
LD: suppresses LH
HD: suppresses FSH
goal is to suppress endogenous LH and FSH
cetrorelix
ganirelix
antiestrogen that is
pure estrogen receptor antagonist
effective in pts w/ tamoxifen resistant tumors
fulvestrant
testosterone, methyltestosterone effects on puberty and embryo
development of secondary sex characteristics
flutamide
bicalutamide
nilutamide
androgen receptor antagonists
reduce male sex accessory organ function
in times of stress, what do you do with glucocorticoids
INCREASE THE DOSE
fludicortisone
mimics the effects of aldosterone
mineralcorticosteroid and glucocorticosteroid effects
weak progestin, androgen, and glucocorticoid
decreases function of the ovaries
danazol
“gliptins”
DPP-4 inhibitors that inhibit the the enzyme that degrades GLP-1 (increasing insulin secretion)
hydrocortisone
cortisone
prednisone
methylprednisone
dexamethasone
fluticasone
anti-inflammatory glucocorticoids
increase glucose, FFA, and amino acids in blood
antagonize insulin
redistribute fat
increase SNS heart effects
Na and H20 retention (some)
bone loss
immunosuppression
only anti inflammatory effects
NO
salt retaining effects
methylpredinsolone
fluticasone
dexamethasone
traimcinolone
betamethasone
2nd gen sulfonylureas that close the K channel, depolarize the membrane, and cause insulin to be exocytosed
glyburide, glipizide, glimepride
clomiphene
antiestrogen that is
antagonist in the hypothalamus
agonist everywhere else
progesterone effects on breasts
loguloalveolar development
stops uterus smooth muscle contractions (CCB)
prevents early labor
nifedipine
fulvestrant
antiestrogen that is
pure estrogen receptor antagonist
effective in pts w/ tamoxifen resistant tumors
PCP bond analogs of pyrophosphate that
INCORPORATE INTO BONE
inhibit osteoclasts
DOC for osteoporosis
“dronates”
5 alpha reducatse inhibitors
stop the conversion of testosterone to DHT
decreases DHT and PSA
increases total testosterone (so might make more estrogen)
finasteride
dutasteride
lots of anti inflammatory effects
some salt retaining effects
prednisone
prednisolone
acarbose and miglitol
alpha glucosidase inhibitors that delay CHO digestion and decrease intestinal glucose absorption
spironolactone
androgen receptor antagonist
competes for androgen and estrogen receptors when
AT VERY HIGH DOSES
prednisone MOA
must be converted to prednisolone in the liver to be active
pramlintide
USED IN T1DM AND T2DM to regulate postprandial glucose
testosterone, methytestosterone anabolic effects
increases bones
amino acids getting into muscles
RBC mass
antagonizes steroids
tranexamic acid
anti-fibrinolytic that inhibits the activation of plasminogen
reduces death due to postpartum hemorrhage
“along with standard uterotonic therapy”
nonsteroidal
inhibitor of aromatase
(final step in estrogen synthesis)
anastrozole
letrozole
estradiol, estrone, estriol uterus effects
endometrial cell division and growth
(in the follicular phase)
androgen receptor antagonist
competes for androgen and estrogen receptors when
AT VERY HIGH DOSES
spironolactone
estradiol, estrone, estriol effects on blood clotting
makes clotting protein
increases platelet adhesiveness
progesterone effects on endocervical glands
cervical mucus
ketoconazole
inhibitor of corticosteroid synthesis
at high dose this antifungal inhibits steroid synthesis
NON-SELECTIVE
used in pre-op suppression
raloxifene
antiestrogen that is
antagonist in the breast AND the uterus
agonist in the bone and liver
PTH analogs that intermittently stimulate the PTH receptor to cause
OSTEOBLASTIC activity
used in osteoporosis
only anabolic osteoporosis drug
“paratides”
teraparatide, abaloparatide
levothyroxine sodium
synthetic T4- takes 4-6 weeks to reach steady state
raises blood sugar by inhibiting insulin secretion or decreasing glucose utilization
diazoxide
derived from testosterone and have both progestin and androgenic activity:
norethindrone
norgestrel
levonorgestrel
norgestimate
19- nortestosterones
recombinant PTH that binds to receptor to stimulate the RANK ligand to cause
OSTEOCLASTIC activity
used in tx of hypOthyroidism
rhPTH (1-84)
estradiol, estrone, estriol bone
maintain bone mass
stop resorption
increases GI Ca and phos absorption
must be adequate for optimal absorption of Ca
decreses renal excretion of Ca and Phos
cholecalciferol (skin)
ergocalciferol (diet)
calcitriol (active)
estradiol, estrone, estriol breast effeccts
ductal epithelial cells
mag sulfate
relaxes the uterus
stops premature labor
antiprogestin that blocks progestin binding to the progesterone receptor
mifepristone
gradually blocks the conversion of T4 to T3
propylthiouracil
1st- hMG (for 9-12 days)
2nd- hCG (1 dose)
**in sequence**
female fertility tx
(fertilization)
inhibits COX to reduce prostaglandin synthesis
and delay early labor
indomethacin
colesevelam
bile acid sequestrant that lowers A1C somehow
(1) decreases gluconeogenesis, glycogenolysis, and CHO intestinal absorption (2) increases insulin sensitivity
metformin
leuprolide
goserelin
long acting GnRH agonist
initially causes an LH surge
BUT THE ULTIMATE EFFECT IS
INHIBITION OF GONADOTROPIN RELEASE
(goal is to reduce androgens)
metyrapone
inhibitor of corticosteroid synthesis
SELECTIVE inhibitor of the last enzyme in cortisol synthesis
used short term
ok for preggos
IM DM drugs
GLP-1 agonists
pramlintide
insulin