Pharmacology of Osteoporosis and Gout (Wolff)

Question 1

Calcitonin-salmon is similar in structure and function to human calcitonin synthesized by thyroid, but?

Answer 1

It has a longer half-life and greater potency

Question 2

Calcitonin-salmon inhibits the activity of?

Answer 2

Osteoclasts in order to decrease bone resorption

Question 3

What is the clinical application for Calcitonin-salmon?

Answer 3

Treatment of established osteoporosis but not prevention

Question 4

Bisphosphonates such as alendronate (and other -nate) are structural analogs of what normal constituent of bone?

Answer 4

Pyrophosphate

Question 5

What affect do Bisphosphonates have?

Answer 5

Inhibits bone resorption

Question 6

What is the clinical application for Bisphosphonates?

Answer 6

Drugs of first choice for postmenopausal osteoporosis, osteoporosis in men, and glucocorticoid induced osteoporosis

Question 7

What toxicities are noted with bisphosphonates?

Answer 7

1) Esophagitis
2) Osteonecrosis of jaw
3) Atypical femur fractures

Question 8

Which bisphosphonates is given by IV and it avoids the GI problems associated with other bisphosphonates?

Answer 8

Zoledronic acid

Question 9

What class of drug is raloxifene?

Answer 9

Selective Estrogen Receptor Modulator (SERM)

Question 10

Raloxifene exerts its agonist estrogen effects at?

It blocks theses effects at?

Answer 10

1) Bone

2) Breast and uterus

Question 11

What is the clinical application of raloxifene?

Answer 11

Prevents and treat postmenopausal osteoporosis

Question 12

Like estrogen, raloxifene increases the risk of?

Answer 12

1) Deep venous thrombosis
2) Pulmonary embolism
3) Stroke

Question 13

What is a truncated version of endogenous 1-84

PTH made by recombinant DNA technology that retains activity of full length PTH?

Answer 13

teriparatide (PTH 1-34)

Question 14

What is the clinical application of teriparatide?

Answer 14

Treat all forms of osteoporosis

Question 15

Teriparatide is the only drug for osteoporosis that has what effect?

Answer 15

Increases bone formation

Question 16

When teriparatide is given as a daily pulsed therapy, what predominates?

How is it administered?

Answer 16

1) Osteoblast responses

2) Once daily by using pre-filled injectors

Question 17

Denosumab is a monoclonal antibody that has what MOA?

Answer 17

RANKL inhibitor

Question 18

RANKL is a receptor activator of?

Answer 18

Nuclear factor kappa-B ligand

Question 19

By binding to RANKL, denosumab decreases the formation and function of?

Answer 19

Osteoclasts

Question 20

What is the clinical application of denosumab?

Answer 20

Treatment of osteoporosis in postmenopausal women at high risk for fracture

Question 21

How is denosumab administered?

Answer 21

Injected every 6 months SubQ

Question 22

What toxicities are noted with denosumab?

Answer 22

1) Delays fracture healing
2) Increases risk of new fractures
3) Osteonecrosis of jaw

Question 23

What is a natural antagonist of RANKL?

Answer 23

Osteoprotegerin (OPG)

Question 24

What is a major risk factor for osteoporosis in men?

So what is an important part of therapy?

Answer 24

1) Hypogonadism

2) Testosterone replacement

Question 25

What are contributors of osteoporosis in men with prostate cancer?

Answer 25

Glucocorticoids and androgen-deprivation therapy

Question 26

What are the agents of choice for osteoporosis in men? What is the alternative?

Answer 26

1) Bisphosphonates | 2) Denosumab

Question 27

What is a “calcimimetic” drug that binds to the calcium sensing receptors on the PTH gland?

Answer 27

cinacalcet

Question 28

What are the clinical applications of cinacalcet?

Answer 28

1) Primary hyperparathyroidism | 2) Secondary hyperparathyroidism due to CKD

Question 29

What therapy can be utilized for the initial treatment of acute gout?

Answer 29

NSAID therapy such as naproxen, indomethacin, and celecoxib

Question 30

If NSAID therapy is contraindicated then what is the next course of therapy to be considered in the treatment of acute gout?

Answer 30

Colchicine

Question 31

If colchicine is contraindicated then what is the next course of therapy to be considered in the treatment of acute gout?

Answer 31

Glucocorticoids

Question 32

Colchicine diffuses into cells to bind to? This blocks the formation of?

Answer 32

1) Tubulin | 2) Microtubules

Question 33

What is the therapy used to prevent recurrent gout that causes frequent attacks (more than twice a year)?

Answer 33

Urate-lowering therapy with allopurinol

Question 34

If allopurinol is not tolerated what should be used instead as an alternative urate-lowering therapy?

Answer 34

Febuxostat

Question 35

In patients with chronic/severe tophaceous gout, what is the last resort biological monotherapy used?

Answer 35

Pegloticase

Question 36

Allopurinol and Febuxostat are inhibitors of? They cause what to be excreted?

Answer 36

1) Xanthine oxidase | 2) Hypoxanthine and xanthine

Question 37

Pegloticase is a recombinant mammalian? It covalently attaches to? It converts uric acid to the far more solubule?

Answer 37

1) Uricase 2) Methoxy polyethylene glycol 3) Allantoin

Question 38

Rasburicase is a nonpegylated recombinant uricase for prevention of?

Answer 38

Acute uric acid nephropathy due to tumor lysis syndrome

Question 39

Probenecid is an organic acid that blocks? This has what effect?

Answer 39

1) Urate reabsorption more than urate secretion | 2) Increases excretion of urate

Question 40

Probenecid can be used to reduce urate levels in underexcreters with?

Answer 40

1) GFR > 60 ml/min | 2) No stones