Pharmacotherapy of Osteoporosis Exam 1

Question 1

What are the two groups of pharmacological treatment approaches?

Answer 1

• those that stimulate bone formation

- those that inhibit bone resorption

Question 2

prescriptions that stimulate bone formation

Answer 2

Parathyroid analogs

Question 3

prescriptions that inhibit bone formation

Answer 3

• Calcitonin-Salmon
• SERMs & hormone therapy
• Bisphosphonates
• Denosumab

Question 4

Parathyroid analog drugs

Answer 4

• Teriparatide (Forteo®)
• Abaloparatide (Tymlos®)
• Key is low and intermittent dosing

Question 5

Parathyroid analogs MOA

Answer 5

• Increase in mature osteoblasts
• Inhibits apoptosis of osteoblasts and osteocytes
• Offsets glucocorticoid-induced osteoporosis by inhibition of apoptosis

Question 6

Parathyroid analogs adverse effects

Answer 6

• Hypercalcemia
• Orthostatic hypotension (dizziness)
• Osteosarcoma

Question 7

Bisphosphonate drugs

Answer 7

• Alendronate (Fosamax®, Binosto®, +)
• Risedronate (Actonel®, Atelvia®, +)
• Ibandronate (Boniva®, +)
• Zoledronate (Reclast®, +)

Question 8

Bisphosphonates MOA

Answer 8

• Bind to hydroxyapatite crystals and embed in the skeleton

- Inhibits osteoclasts

Question 9

Bisphosphonates Adverse Effects

Answer 9

• GI upset
• Esophagitis
• Osteonecrosis (of the jaw)
• Flu-like febrile illness
• Hypocalcemia in patients who are vitamin D deficient

Question 10

Bisphosphonate Kinetics

Answer 10

• Oral (Alendronate, Risedronate, Ibandronate) and poorly absorbed
• absorption reduced by Ca++, antacids, iron, etc
• renal excretion
• Transient hypocalcemia (muscle pain) esp in pts who are VitD deficient

Question 11

Hormone therapy MOA

Answer 11

• Osteoclast differentiation is suppressed
• Apoptosis of pre-osteoclasts is increased
• Osteoblast lifespan is increased

Question 12

Hormone therapy adverse effects

Answer 12

• Clots (venous thromboembolisms), MI, stroke

* Advantages may not outweigh the risks for long term use

Question 13

Selective Estrogen-Receptor Modulators (SERMs)

Answer 13

Raloxifene (Evista®)

Question 14

Selective Estrogen-Receptor Modulators (SERMs)

Answer 14

Raloxifene (Evista®)

Question 15

Selective Estrogen-Receptor Modulators (SERMs) MOA

Answer 15

• ER agonist in bone

- ER antagonist in breast and uterus

Question 16

Raloxifene

Answer 16

Positive profile for
• Breast cancer 
• Dec. LDL and total cholesterol 
• No increased endometrial
growth (no inc. cancer risk)

Question 17

Raloxifene adverse effects

Answer 17

• Hot flashes
• Embolisms
• Stroke

Question 18

SERM with hormone replacement

Answer 18

• Bazedoxifene with conjugated estrogens
• Combination of estrogens with SERM makes it a tissueselective estrogen complex (TSEC)
• Target group: Post-menopausal women with a uterus

Question 19

SERM with hormone replacement goal

Answer 19

Relief from vasomotor symptoms PLUS maintenance of bone density

Question 20

SERM with hormone replacement advantage

Answer 20

Decreased endometrial hyperplasia compared to hormone therapy alone

Question 21

Calcitonin-Salmon MOA

Answer 21

• Inhibits osteoclasts
• Lowers plasma calcium and phosphate levels
• Encourages bone formation

Question 22

Denosumab (Prolia®) MOA

Answer 22

• Antibody to RANKL
• Stops activation of osteoclasts
• If a patient has hypocalcemia, this largely takes away their ability to increase plasma calcium naturally