Endocrine III Flashcards
female hormone that inhibits the release of FSH and LH, helps with female maturation, and prepares the endometrial lining for implantation
estrogen
female hormone that inhibits the release of FSH and LH, and prepares and maintains the endometrial lining after implantation
progestin
what are 4 things that can occur with estrogen use?
decrease bone resorption
retain Na and water
increase HDL + TG
decrease LDL
what are 3 pathological things that can occur with progesterone use?
increase body temp
decrease HDL
increase LDL
what are 3 uses for estrogen?
contraceptive
HRT
female hypogonadism
what are 4 uses for progesterone?
contraceptive
HRT
endometriosis
adjunct for endometrial/breast cancer
what are anti-estrogens used for?
hormone-sensitive (ER+) breast cancer
how are most contraceptives metabolized?
by the liver
what should we monitor in patients who are taking contraceptives? (7)
chest pain
SOB
severe calf/thigh pain
severe headaches
dizziness
weakness/numbness
breast lumps
constant ratio of E and P in each tablet
monophasic
E to P ratio changes once during cycle
biphasic
E to P ratio changes twice
triphasic
tablets of one strength (color) x 21 days + 7 days of inactive tablets (different color), to make up the 28 day dosing cycle
monophasic OC
which types of OCs attempt to mimic the rising and falling pattern of estrogen and progesterone during the normal menstrual cycle?
biphasic and triphasic
what makes biphasic and triphasic different from monophasic?
bi and tri = same estrogen amount each day, but progesterone amount increases half-way through the cycle
tablets of one strength (color) for 7-10 days
tablets of another strength for the next 11-14 days
additional 7 days of inactive tablet, to make the full 28 day dosing cycle
biphasic
3 different doses (colors), one for each week, and a 4th dose of hormone-free (inactive tablets) during the last week
triphasic
4 doses of estrogen and two (middle) sequences of progesterone
quadri-phasic
what regimen of OC should we start with?
monophasic with 20mcg of estrogen and progesterone
how does the progesterone-only OC work?
inhibit LH surge (final signal for ovulation) = inhibits ovulation
thickened mucus in cervix prevents sperm passage from entering uterus
what does the mini-pill have?
low dose progesterone
how does the IUD work?
progesterone is released in small amounts, providing 5 years of continuous contraception
what is the IM version of the mini pill?
depo-provera (IM)
what do postcoital contraceptives contain?
only progesterone
what is plan B one-step? how should it be taken?
one dose levonorgestrel
within 72 hours of unprotected coitus
how many doses is next choice?
2 doses
what is ella? how should it be taken?
ulipristal acetate
within 120 hours of unprotected coitus
how does smoking affect the complications of OC?
increases embolic risk
what is important to remember about CYP3A4-inducing medications and OC?
CYP3A4 inducers increase the risk of unintended pregnancy for oral and implant contraceptives
progesterone antagonist that prevents implantation
mifepristone
progesterone antagonist that is used for abortion (unwanted pregnancy) via a single dose and is only intended for emergency postcoital contraception
mifepristone + misoprostol
aldosterone antagonist that includes only progesterone + an antihypertensive property
drospirenone
the conception drug that is considered an anti-estrogen drug
clomiphene
clomiphene MOA
inhibits estrogen’s negative feedback, allowing increased secretion of FSH and LH
what are 2 important things to tell a patient about clomiphene?
ovulation occurs 5-10 days after final dose
increases chance of multiple pregnancies to 10%
what are the ADR of clomiphene? (2)
increase clotting factor synthesis
increased afterimages
which patients should not take clomiphene?
patients with thromboembolic disease
what could HRT be used to prevent, but comes with the risk of blood clots, heart attack, stroke, and cancer?
osteoporosis
low bone mass and deterioration of bone tissue
osteoporosis
osteoporosis bone fragility increases the susceptibility to fractures in which areas? (3)
hip
spine
wrist
what is used as a diagnostic criteria to help predict future fracture risk?
bone mineral density (BMD)
what is essential in helping treat a patient with osteoporosis?
calcium + vitamin D supplements
what helps to decrease fall and fracture risk in patients with osteoporosis?
weight-bearing exercises
-dronate
biphosphonates
how do bisphosphonates treat osteoporosis? (4)
bind strongly to and accumulate in bone
inhibit bone reabsorption
increase BMD at spine and hip
decrease incidence of fractures
why should bisphosphonates be taken on an empty stomach?
is very hydrophilic and has bioavailability less than 10% that decreases with food
what happens to bisphosphonates in the body?
50% goes to bone
50% excreted by kidneys
what are the ADR of alendronate, ibandronate, and risedronate?
esophageal reflux/heart burn
how should bisphosphonates be taken? (2)
upright position
take with glass of water 30 mins before food
when is the best time to take bisphosphonates?
first thing in the morning
which bisphosphonate has a higher F, and is only a once yearly infusion?
zoledronate (IV)
what are the ADR of zoledronate?
osteonecrosis of the jaw (usually after major dental sx)
what are 2 ADR of bisphosphonates?
flu-like symptoms
kidney damage
tissue specific estrogen agonist / antagonist
SERM (selective estrogen receptor modulator)
-xifen
SERM
estrogen agonist/antagonist
MOA of tamoxifen
estrogen agonist in bone, uterus, liver
estrogen antagonist in breast
MOA of raloxifene?
estrogen agonist in bone
estrogen antagonist in breast and endometrial tissue
SERM drugs approved for postmenopausal osteoporosis (2)
raloxifene
bazedoxifene/estrogen
ADR of raloxifene as a estrogen agonist (2)
thromboembolic disease
afterimages
why are SERMs an agonist in some tissues and antagonist in other tissues?
has a unique drug receptor conformation that interacts with co-activators and co-repressors in different tissues
peptide that is composed of 32 amino acids, that binds to osteoclasts and inhibits bone resorption
calcitonin
what is calcitonin used to treat? (3)
osteoporosis in women over 5 years postmenopausal
paget’s disease of bone
hypercalcemia
how does calcitonin treat osteoporosis?
“calcitonin carries osteoporosis on it’s back”
increases spinal bone mass
how does calcitonin treat hypercalcemia? (2)
decreases tubular reabsorption of calcium
promotes renal excretion of calcium, phosphate, sodium, magnesium, and potassium
what are some ADR of calcitonin as a nasal spray? (6)
rhinitis
irritation of nasal mucosa
epistaxis
sinusitis
back pain/arthralgia
headache
what are some ADR of calcitonin as an injection?
nausea
flushing
what hormone regulates calcium and phosphate metabolism in the bone and kidney?
PTH (parathyroid hormone)
synthetic PTH use to treat osteoporosis in women at high risk for fracture and for primary or hypogonadal osteoporosis in men at high risk of fracture
teriparatide
teriparatide MOA (2)
stimulates osteoblast function
increase calcium absorption from GI tract and kidney
why is there a black box warning for teriparatide?
osteosarcoma risk in rats
post-partum depression medication that mimics the action of allopregnanolone - increasing the activity of GABAa receptors
zuranolone
-nolone
PPD drug
what are the ADR of zuranolone? (2)
drowsiness
dizziness
medication approved for moderate to severe PPD, used IV
brexanolone
medications used for labor and delivery (4)
oxytocin
PG E1
PG E2
misoprostol
what are the risks with drugs for labor and delivery, especially oxytocin?
uterine rupture
uterine bleeding
ADR of PGs E1 and E2?
N/V/D
cramping
why is hyperprolactinemia an ADR of antipsychotics?
blocks inhibitory effect of dopamine on prolactin secretion since they are dopamine receptor antagonists
3 dopamine receptor agonists used to treat hyperprolactinemia
bromocriptine
cabergoline
pergolide
which of the 3 dopamine receptor agonists have the least ADRs?
cabergoline
what are potential ADR with dopamine receptor agonists? (5)
psychosis/hallucinations
headache
n/v
postural hypotension
nasal congestion
