Pharm of Osteoporosis (Fitz)

Question 1

T score of -1 to -2.5 indicates__

T score of -2.5 to -4 or higher indicates__

Answer 1

osteopenia

osteoporosis

Question 2

this Ca supplement NEEDS ACID to dissolve and for absorption, taken “at” or “after” meals, less stomach acid with aging

Answer 2

Ca carbonate

Question 3

this Ca supplement does not require stomach acid for absorption, may be taken between meals, but costs more

Answer 3

Ca citrate

Question 4

when does the Vit D requirement exceed >800 IU/day?

Answer 4

• GI malabsorption disorders
• If on corticosteroids, certain anticonvulsants, loops, heparin
• elderly who have less exposure/response to sunlight, less hydroxylation in liver and kidney

Question 5

adverse effect of Glucocorticoids?

Answer 5

Impairs vit D absorption and imapirs metabolic activation in liver and kidney

Lowers serum Ca

Question 6

adverse effect of carbamazepine and phenytoin?

Answer 6

induction of CYP450, hepatic inactivation of Vit D

Lowers serum Ca

Question 7

adverse effect of Furosemide?

Answer 7

Ca wasting

lowers serum Ca

Question 8

list drug classes mentioned in lecture that are responsible for secondary cause of osteoporosis:

Answer 8

glucorticoids-prednisone, methyprednisolone, budesonide

anticonvulsants-carbamazepine, phenytoin

loop diuretics-furosemide

Question 9

what effect do the following hormones have on Ca resorption:
Calcitonin: ___
PTH: ___

Answer 9

calcitonin: decrease Ca resorption

PTH: increase Ca resorption

Question 10

effect of 1,25(OH)-D3 (calcitriol) in Ca absorption?

Answer 10

increase absorption of Ca in intestine

Question 11

list SERMs for osteoporosis

Answer 11

Raloxifene and Tamoxifen

Question 12

List bisphosphonates for osteoporosis

Answer 12

the “-dronates”

alendronate, ibandronate, pamidronate, risedronate, zolendronate

Question 13

list biologicals for osteoporosis

Answer 13

teraparatide and calcitonin

Question 14

list Abs for osteoporosis

Answer 14

denosumab

Question 15

which drug classes inhibit OSTEOCLASTS and are anti-resorptive tx?

Answer 15

SERMs
Bisphosphonates
Biologicals-Calcitonin
Abs

Anabolic tx that activates OSTEOBLASTS=Teraparatide (biological)

Question 16

Benefits of Estrogen HRT in ALL tissues? Risks?

Answer 16

benefits: Increased bone health, decreased menopause symptoms
risks: increase breast cancer, increased uterine cancer, increase heart attack, increase stroke, increased osteoporosis

Question 17

SERMs (raloxifene) and Bisphosphonates are FDA approved for __

Answer 17

prevention AND tx

tx only=calcitonin, terparatide, denosumab

Question 18

MOA of estrogens and SERMs in osteoclasts? MOA in breast epithelium

Answer 18

agonists at estrogen receptors in osteoclasts

antagonists at estrogen receptors in breast epithelium

Question 19

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

Answer 19

Raloxifene

Question 20

__ has a worse endometrial adverse effect profile than Raloxifene and will have increased uterine bleeding and cancer with this drug

Answer 20

Tamoxifen

-Raloxifene is NOT associated with bag bleeding or an increased risk of endometrial hyperplasia or cancer

Question 21

what is a major risk associated with HRT & estrogens, Raloxifene, and Tamoxifen?

Answer 21

all increase the risk of venous thromboembolic events

MI, stroke

Question 22

MOA of Bisphosphonates?

Answer 22

inhibit FPP synthase

inhibit bone resorption through effects on osteoclasts

Question 23

contraindication for using bisphosphonates?

adverse events associated with oral bisphosphonates?

Answer 23

pre-existing hypocalcemia is a contraindication

esophagitis and esophageal ulcer are well-recognized adverse events associated with oral bisphosphonates

Question 24

how to administer bisphosphonate?

Answer 24

• 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)

Question 25

how to improve bisphosphonate compliance?

Answer 25

IV Zoledronate 5 mg, 1x per yr --> 100% bioavailability d/t IV, high potency improved convenience, compliance, and efficacy

Question 26

rare complication seen in pts taking bisphosphonates?

Answer 26

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%

Question 27

issues with chronic bisphosphonate use?

Answer 27

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

Question 28

Denosumab is a monoclonal Ab against __, inhibits __ formation, administered __ at 6 month intervals. It increased BMD and reduces risk of fx

Answer 28

RANKL Osteoclast SubQ

Question 29

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

Answer 29

Calcitonin

Question 30

this drug is is administered intermittently, and stimulates osteoblastic activity (anabolic). Has very short t1/2, no deposition in bone

Answer 30

Teriparatide

Question 31

Teriparatide is reserved for these pts:

Answer 31

Reserved for high risk pts: his cost, risk of osteosarcoma

Question 32

approved indications for Teriparatide?

Answer 32

- 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

Question 33

these osteoporosis drugs are effective in men:

Answer 33

bisphosphonates

Question 34

__ is a CaSR activator that lowers PTH levels by increasing sensitivity of CaSR to extracellular Ca

Answer 34

Cinacalcet

Question 35

what drug to tx overactive PT gland in dialysis pts with CKD?

Answer 35

Cinacalcet also used to tx high blood Ca levels in pts with PT cancer