Pharm of Osteoporosis (Fitz) Flashcards
T score of -1 to -2.5 indicates__
T score of -2.5 to -4 or higher indicates__
osteopenia
osteoporosis
this Ca supplement NEEDS ACID to dissolve and for absorption, taken “at” or “after” meals, less stomach acid with aging
Ca carbonate
this Ca supplement does not require stomach acid for absorption, may be taken between meals, but costs more
Ca citrate
when does the Vit D requirement exceed >800 IU/day?
- GI malabsorption disorders
- If on corticosteroids, certain anticonvulsants, loops, heparin
- elderly who have less exposure/response to sunlight, less hydroxylation in liver and kidney
adverse effect of Glucocorticoids?
Impairs vit D absorption and imapirs metabolic activation in liver and kidney
Lowers serum Ca
adverse effect of carbamazepine and phenytoin?
induction of CYP450, hepatic inactivation of Vit D
Lowers serum Ca
adverse effect of Furosemide?
Ca wasting
lowers serum Ca
list drug classes mentioned in lecture that are responsible for secondary cause of osteoporosis:
glucorticoids-prednisone, methyprednisolone, budesonide
anticonvulsants-carbamazepine, phenytoin
loop diuretics-furosemide
what effect do the following hormones have on Ca resorption:
Calcitonin: ___
PTH: ___
calcitonin: decrease Ca resorption
PTH: increase Ca resorption
effect of 1,25(OH)-D3 (calcitriol) in Ca absorption?
increase absorption of Ca in intestine
list SERMs for osteoporosis
Raloxifene and Tamoxifen
List bisphosphonates for osteoporosis
the “-dronates”
alendronate, ibandronate, pamidronate, risedronate, zolendronate
list biologicals for osteoporosis
teraparatide and calcitonin
list Abs for osteoporosis
denosumab
which drug classes inhibit OSTEOCLASTS and are anti-resorptive tx?
SERMs
Bisphosphonates
Biologicals-Calcitonin
Abs
Anabolic tx that activates OSTEOBLASTS=Teraparatide (biological)
Benefits of Estrogen HRT in ALL tissues? Risks?
benefits: Increased bone health, decreased menopause symptoms
risks: increase breast cancer, increased uterine cancer, increase heart attack, increase stroke, increased osteoporosis
SERMs (raloxifene) and Bisphosphonates are FDA approved for __
prevention AND tx
tx only=calcitonin, terparatide, denosumab
MOA of estrogens and SERMs in osteoclasts? MOA in breast epithelium
agonists at estrogen receptors in osteoclasts
antagonists at estrogen receptors in breast epithelium
what is the SERM of choice d/t its safety and efficacy..it is usually chosen for osteoporosis prevention when there is an independent need for breast CA prophylaxis
Raloxifene
__ has a worse endometrial adverse effect profile than Raloxifene and will have increased uterine bleeding and cancer with this drug
Tamoxifen
-Raloxifene is NOT associated with bag bleeding or an increased risk of endometrial hyperplasia or cancer
what is a major risk associated with HRT & estrogens, Raloxifene, and Tamoxifen?
all increase the risk of venous thromboembolic events
MI, stroke
MOA of Bisphosphonates?
inhibit FPP synthase
inhibit bone resorption through effects on osteoclasts
contraindication for using bisphosphonates?
adverse events associated with oral bisphosphonates?
pre-existing hypocalcemia is a contraindication
esophagitis and esophageal ulcer are well-recognized adverse events associated with oral bisphosphonates
how to administer bisphosphonate?
- take with a full glass of water in morning
- do NOT eat or drink anything for at least 30 mins after taking (Ibandronate: 60 mins)
- do NOT lie down for at least 30 mins (Ibandronate: 60 min)
how to improve bisphosphonate compliance?
IV Zoledronate 5 mg, 1x per yr –> 100% bioavailability d/t IV, high potency
improved convenience, compliance, and efficacy
rare complication seen in pts taking bisphosphonates?
Osteonecrosis of the jaw
most commonly in pts w:
-receiving IV bisphosphonates, ~90%
-Dx with MM, breast CA, and prostate CA, ~85%
-having tooth extractions, dental trauma, ~60%
issues with chronic bisphosphonate use?
Bps remain in bone for decades-there is no known way to remove Bps from bones
-consider periodic reevaluation of continued BP tx, particularly pts who have been tx for > 5 yrs
Denosumab is a monoclonal Ab against __, inhibits __ formation, administered __ at 6 month intervals. It increased BMD and reduces risk of fx
RANKL
Osteoclast
SubQ
this hormone tx inhibits osteoclast action (anti resorptive), has a modest effect < bisphosphonates, given 200 IU nasally/day, DECREASE PAIN WITH ACUTE VERTEBRAL COMPRESSION FX
Calcitonin
this drug is is administered intermittently, and stimulates osteoblastic activity (anabolic). Has very short t1/2, no deposition in bone
Teriparatide
Teriparatide is reserved for these pts:
Reserved for high risk pts: his cost, risk of osteosarcoma
approved indications for Teriparatide?
- postmenopausal women with osteoporosis at HIGH RISK for fx
- increase bone mass in men with primary or hypogonadal osteoporosis at HIGH RISK for fx
- tx of men and women with osteoporosis with sustained, systemic glucocorticoid tx at HIGH RISK for fx
these osteoporosis drugs are effective in men:
bisphosphonates
__ is a CaSR activator that lowers PTH levels by increasing sensitivity of CaSR to extracellular Ca
Cinacalcet
what drug to tx overactive PT gland in dialysis pts with CKD?
Cinacalcet
also used to tx high blood Ca levels in pts with PT cancer
