module 16 antiresorptive agents, bone anabolic agents

Question 1

antiresorptive agents

Answer 1

HRT
SERMs
Bisphosphonates
Calcitonin

Question 2

Antiresorptive agents MOA

Answer 2

suppression of osteoclasts
- prevents or slows bone loss
No inc. in bone mass
- little initially because mineralization of resorption cavities

Question 3

HRT drug

Answer 3

estrogen

Question 4

estrogen MOA

Answer 4

suppresses transcription of genes encoding cytokines that induce osteoclasts

Question 5

estrogen use

Answer 5

maintain bone mass

stop bone loss

Question 6

estrogen AE

Answer 6

CV disease
breast cancer
endometrial cancer

Question 7

estrogen EDU

Answer 7

take with progestin to dec. risk of endometrial cancer

Risks outweigh benefit

Question 8

selective estrogen Rc modulator (SERMs) med

Answer 8

raloxifene

Question 9

raloxifene MOA

Answer 9

binds to estrogen Rc

• agonist in bone
• antagonist in endometrium/breast

Question 10

raloxifene use

Answer 10

prevent/tx osteoporosis

inc. BMD
dec. vertebral rx risk

Question 11

raloxifene AE

Answer 11

inc. risk venous thromboembolism

Question 12

raloxifene EDU

Answer 12

dec. LDL

Question 13

bisphosphate meds

Answer 13

alendronate
risedronate
ibandronate
pamidronate
zoledronate

Question 14

bisphosphate MOA

Answer 14

localize to bone reabsorption sites and inhibit osteoclast activity
concentrated in bone matrix, when bone reabsorption occurs -> bisphosphonate release

Question 15

bisphosphate use

Answer 15

prevent/tx osteoporosis
- inc. spine and hip BMD
- dec. spine fx risk 
hypercalcemia 
metastatic bone disease
paget's

Question 16

bisphosphate AE

Answer 16

osteoblast/osteoclast activity coupled
- dec. osteoclast = dec. osteoblast 
reflux
esophagitis
esophageal ulcers
LT: hypermineralization and structure changes 
osteonecrosis of jaw

Question 17

bisphosphates Admin

Answer 17

low oral bioavailability: 1-5%
- take on empty stomach before 1st meal
- 30 minutes before other meds
70% renally excreted
30% absorbed to bone

Question 18

bisphosphates EDU

Answer 18

remain upright 30 min. after taking

have meal before lying down

Question 19

Bisphosphates med admin

Answer 19

Alendronate: PO: daily or weekly

risedronate: PO: daily, weekly, monthly
ibandronate: PO: monthly, IV: q3 months
pamidronate: IV
zoledronate: IV: once a year

Question 20

Calcitonin MOA

Answer 20

binds and activates calcitonin Rc on osteoclasts

-> dec. activity

Question 21

calcitonin use

Answer 21

osteoporosis
hypercalcemia
Paget’s
dec. vertebral bone loss/fx

Question 22

calcitonin admin

Answer 22

slow clearance

peptide: SubQ, IM, nasal
- no PO

Question 23

calcitonin EDU

Answer 23

derived from salmon

- 40x higher affinity for calcitonin Rc

Question 24

fluoride

Answer 24

at high concentrations inc. trabecular bone mass

- unclear whether effective in prevention fx

Question 25

PTH, bone anabolic agent, med

Answer 25

teriparatide

Question 26

teriparatide MOA

Answer 26

intermittent stimulation by exogenous PTH | -> anabolism/formation of bone

Question 27

teriparatide use

Answer 27

inc. BMD for pts w/ large bone loss: BMD > 3 below nml osteoporosis

Question 28

teriparatide admin

Answer 28

daily dosing | peptide: no PO absorption, given SubQ

Question 29

denosumab MOA

Answer 29

human monoclonal antibody: inhibits RANKL | -> inhibits osteoclast formation, function, and survival

Question 30

denosumab AE

Answer 30

preg. category X postmenopausal: - back pain - extremitiy pain - inc. cholesterol - musculoskeletal pain - cystitis Hormone albation r/t CA: - arthralgia - musculoskeletal pain

Question 31

denosumab admin

Answer 31

SubQ: q6 month

Question 32

RANKL

Answer 32

produced by osteoblast, binds to osteoclast - > reabsorption inc. after menopause

Question 33

denosumab monitoring

Answer 33

creatinine | Ca