Menopause and Osteoporosis Pharmacology Flashcards
Treatment method for mild vulvovaginal symptoms
vaginal moisturizers or lubricants → alleviate dryness, burning, itching, dyspareuria
Treatment method for moderate to severe vulvovaginal symptoms
non-systemic vaginal estrogen product → cream, ring, tablet, insert
Oral drugs that is FDA approved for dyspareunia
ospemifene
Ospermifenese is a SERM (selective estrogen receptor modulator) and what is the MOA in helping vulvovaginal symptoms ?
activates estrogen pathwaays in some tissues and blocks in others
agonist in endometrium
Adverse effects of ospermifenese
may cause vasomotor symptoms
what are the estrogen warnings for ospemifene?
endometrial cancer, DVT, stroke
vaginal insert that is FDA approved for dyspareunia → “treat painful intercourse due to menopause without FDA boxed safety warning”
prasterone
nonpharmacologic methods to treat vasomotor symptoms
wear layers, lower room temperatures, decrease intake of spicy food/caffeine/ hot drinks, exercisse, maintain healthy body weight, don’t smoke, relaxation techniques
Treatment of vasomotor symptoms as well as preventing endometrial hyperplasia in a patient with intact uterus?
If they had hysterectomy?
progestin + estrogen
just estrogen
In treating vasomotor symptoms, which systemic progesterone product has shown better outcomes - medroxyprogesterone acetate (MPA) or micronized progesterone?
micronized progesterone
Tissue selective estrogen complex approved for moderate to severe vasomotor symptoms and prevent osteoporosis
conjugated estrogen + bazedoxifene
Nonhormonal products that can be used to treat vasomotor symptoms
SSRI (paroxetine), SNRI (venlafaxine), clonidine, gabapentin
How effective are phytoestrogens (plant compounds, soy, flaxseed, alfalfa) and black cohosh?
should not be recommended
What is the reality of custom prepared or compounded hormone therapies?
lack evidence regarding safety/efficacy/quality
no support saliva testing for adjustments
same risks as traditional therapies
not FDA supported
Lifestyle modifications for healthier bones
< 3 drinks/day, exercise, stop smoking, increase dietary calcium intake, lower caffeine intake
Receommended calcium intake in women 51 and older and the upper limit of calcium
1200 mg
2000 mg
If your patient is on a PPI what calcium supplement is recommended?
calcium citracte
why is taking calcium carbonate (tums) contraindicated in patients taking PPI?
PPI will decrease absorption
what is the recommended Vitamin D intake in patients > 70 years?
800 units
4,000 units
What are the 3 main sources of vitamin D?
sunlight, diet, supplements
what organs are involved in creating the metabolically active form of vitamin D (1,25-dihydroxy)?
liver and kidney
What meds increase bone resorption?
glucocorticoids
levothyroxine
SGLT2 inhibitors
What meds increase osteoclast and/or decrease osteoblast activity?
antiretrovirals
heparin
thiazolidinediones
vitamin A
What meds decrease estrogen and sex hormone concentrations?
GnRH
DMPA
Med that increase renal calcium elimination
loop diuretics
Med that can cause calcium malabsorption
PPI
Med that increases Vitamin D metabolism
anticonvulsants
This is used to identify patients at risk for osteoporosis or osteoporotic fractices and to determine if need further evaluation (DXA scan) or pharmacologic intervention
Fracture Risk Assessment Tool (FRAX)
What are the two values you receive with FRAX?
- 10 year probability of ANY major osteoporotic fracture
2. 10 year probability of hip fracture
What is the gold standard for BMD measurements?
DXA Scan (central dual energy Xray absorptiometry)
Who is recommended to receive DXA scan?
all women +65 years
Why is DXA the gold standard fro BMD?
precise and stable calibration, short scan times, low radiation doses
T score between -1 and -2.5 indicates
osteopenia
T score <2.5 indicates
osteoporosis
If your patients has low trauma vertebral or hip fracture and meets the criteria to get central DXA scan (regardless of the score) what should you recommend?
bone healthy lifestyle
Calcium (1,000-1,2000/day)
Vitamin D (800-1,000/day)
If your patient has: low trauma hip or vertebral fx osteoporosis FRAX risk >20% FRAX risk for hip >3% + osteopenia what should you give and when should get next DXA?
prescription therapy
DXA in 2 years
First line prescritpion therapy for osteoporosis
alendronate, risedronate, zoledronic acid, denosumab
Second line prescription therapy for osteoporosis
ibandronate, raloxifene, teriparatide, abaloparatide
Third line prescription therapy for osteoporosis
calcitonin
What are the two types of agents approved for treating osteoporosis?
anti-resorptive and anabolic therapies/formation agents
Which three bisphosphonates are first line in preventing the breakdown of bone and decreasing the risk of hip fractures?
risedronate, alendronate, zoledronic acid
Which bisphosphonate is not considered first line since the decrease in risk of hip fractures has not been proven?
ibandronate
What is important about when to take bisphosphonate?
take prior to food/other meds
Which bisphosphonate should be taken immediately after breakfast (unlike the others)?
risedronate (atelvia)
two recommendations to decrease the side effects seen when taking bisphosphonates
take with water and remain upright after taking → decreases reflux
contraindications for taking bisphosphonates
CrCl < 30-35
pregnancy
uncorrected hypocalcemia
Rare ADE seen in bisphosphonates
MSK pain, osteonecrosis of jaw, typical (subtrochanteric) femur fractures
contraindications and ADE of oral bisphosphonates
serious GI conditions or can’t sit/stand after dose
GI complaints
When should you consider a “drug holiday” for oral bisphosphonates?
after 5 years (3 years if on IV)
Your patient can go on “drug holiday” if they meet what criteria?
no significant fracture history, hip BMD T score < 2.5, fracture risk isn’t high
This drug is antiresorptive → prevents osteoclast formation by binding to nuclear factor kappa ligant (RANKL)
denosumab → rank ligand inhibitor
This is secreted by osteoblasts and normally activates osteoclast precursors → promoting osteolysis and increasing serum calcium levels
RANKL
What is the difference between Prolia and Xgeva?
Prolia is first line and Xgeva is not indicated for osteoporosis
Contraindications for denosumab (prolia)
uncorrected hypocalcemia or pregnancy
This is the prefered antiresorptive treatemtn in patients with renal failure
denosumab (prolia)
Antiresorptive that decreases bone resorption by acting as estogen agonist in bone → second line
raloxifene
contraindications of ratoxifene
history or current VTE, pregnancy, use of other SERMs
Adverse effects of ratoxifene → why its 2nd line
thromboemolic events, hot flashes, increase risk of fatal stroke
These anabolic agents mimic the effects of endogenous hormones to stimulate osteoblast function and increases rate of bone formation
PTH analogs → teriparatide or abaloparatide
This is recombinant form of endogenous PTH that mimics endocrine effects of endogenous PTH
teriparatide
analog of PTH related protein that mimics paracrine effects of endogenous PTH rP
abaloparatide
How are PTH analogs efficatious?
low intermittent concentrations of PTH for short period actually INCREASES bone formation
contraindications for PTH analogs
increased risk of osteosarcoma
ADE of PTH analogs
orthostatic hypotension and hypercalcemia, urolithiasis, increased uric acid, osteosarcoma
Last line in treating osteoporosis
calcitonin
Antiresorptive that inhibits osteoclastic bone resorption by antagonizing the effects of PTH (similar to human calcitonin)
calcitonin
contraindication for calcitonin
hypersensitive to salmon derived products
ADE of calcitonin
hypocalcemia, hypersensitivity reactions, nausea, flushing, local inflammation, rhinitis, epistaxis