Bone Mineral homeostasis drugs

Question 1

Intracellular calcium is where?

Answer 1

mitochondria/ER

Question 2

Extracellular calcium is 40% albumin boundand 10% complexed to phosphate, citrate and 50% free ionized calcium

Answer 2

Parathyroid responds to the free ionized calcium

Question 3

Denusomab

Answer 3

mAB to RANKL. It blocks osteoclasta ctivation by RANKL and thus inhibits osteoporosis. Also used to increase bone mass in patients with breast/prostate cancer

Question 4

Calcitriol—in active Vit D.

Answer 4

Stimulates calcium and phosphate absorption in the GI. Induces Calbindin. Not a vitamin!!!

Question 5

Calcipotriol

Answer 5

used in psoriasis

Question 6

Cinacalcet

Answer 6

Binds allosterically to Calcium sensing receptors and makes the body think there is more calcium in the blood than there really is. Turns off PTH at lower calcium levels.

Question 7

When would you use cinacalcet?

Answer 7

hyperparathyroidism and parathyroid carcinoma

Question 8

What are bisphosphonates

Answer 8

non-hydrolyzable pyrophosphate analogs. They inhibit bone resorption. Effective in osteoporosis

Question 9

How are bisphosphonates absorbed

Answer 9

Poorly in the gut. Must take them after overnight fast with water and no food for 30min. Now given in weekly dose form.

Question 10

Big AE of bisphosphonates

Answer 10

Osteonecrosis of the Jaw…jaw bone exposure, swelling, loosening of teeth. Dentists make it worse as 80% of the instances of osteonecrosis follow dental work

Question 11

Which type of bisphosphonates are most likely to cause osteonecrosis of the jaw?

Answer 11

The 3rd generation drugs that are used to treat ppl with cancer.

Question 12

Why would you give a cancer pt bisphosphonates

Answer 12

Prevent bone loss caused by chemo

Question 13

Which type of cancers are bisphosphonates receommended in?

Answer 13

Bone Mets, Breast, prostate

Question 14

Ibandronate

Answer 14

2nd generation (10-100x potency)

Question 15

Risedronate

Answer 15

3rd gen bisphosphonate (1k to 10k potency) . Cancer pts with bone mets. IV, may onlyneed one dose

Question 16

WHat else can you give Risedronate for?

Answer 16

Paget’s disease

Question 17

Raloxifene

Answer 17

Estrogen Receptor modulator

Question 18

What is Raloxifene for?

Answer 18

Osteoporosis

Question 19

Raloxifene mech

Answer 19

Inhibits osteoclasts without causing breast cancer.

Question 20

What is a PTH analog

Answer 20

Activates adenylyl cyclase which raises cAMP levels. High cAMP can be measured in the urine for parathyroid function

Question 21

PTH analogs used for

Answer 21

hypoparathyroidism

Question 22

Teriparatide

Answer 22

PTH analog…only first 34 amino acids.

Question 23

HOw does Teriparatide work?

Answer 23

Stimulates bone formation directly. We know that low doses of PTH activate osteoblasts without ativating osteoclasts…maybe thats whats going on.

Question 24

When would you give Teriparatide?

Answer 24

after bisphosphonate therapy in women

Question 25

Zoledronate?

Answer 25

the other 3rd gen bisphosphonate

Question 26

When would you use Teriparatide?

Answer 26

In women post bisphosphonate…bisphosphonates like Ibandronate would prevent reabsorption and then you use the Teriparatide to kick start bone growth

Question 27

Zoledronic acid

Answer 27

bisphosphonate…cancer pts with bone mets