Bisphosphonates

Question 1

When we talk about osteotherapy drugs we talk about antiresorptive and anabolic. What does antiresorptive and anabolic mean?

Answer 1

• antiresorptive = inhibit bone reabsorption

- anabolic = building, in this instance its bone rebuilding

Question 2

What affect does estrogen have on bone health?

1 - inhibits osteoclasts formation by reducing RANK-L
2 - inhibits osteoblasts activation
3 - inhibits monocyte proliferation
4 - inhibits osteoclasts directly

Answer 2

1 - inhibits osteoclasts formation by reducing RANK-L

- stimulates osteoblasts

Question 3

What are selective oestrogen receptor modulator medication that can be given to patients with osteoporosis?

1 - drugs that regulate non-estrogen receptors
2 - drugs that regulate all estrogen receptors
3 - drugs that regulate estrogen receptors on breast tissue only
4 - drugs that regulate estrogen receptors on bones only

Answer 3

2 - drugs that regulate all estrogen receptors

- inhibits/down regulates osteoclast activity

Question 4

If you have a patient that has previously had a fracture, hormone therapy (HRT or Selective Oestrogen Receptor Modulators) is not going to be potent enough for treatment. What is the 1st line treatment for patients who have previously had a fracture who you suspect may have osteoporosis?

1 - antibiotics
2 - steroids
3 - bisphosphonates
4 - RANK-L medication

Answer 4

3 - bisphosphonates

Question 5

If you have a patient that has previously had a fracture, hormone therapy (HRT or Selective Oestrogen Receptor Modulators) is not going to be potent enough for treatment. The 1st line treatment for patients who have previously had a fracture is bisphosphonates. What are the 3 drugs we need to know, remembering ADZ might help?

1 - Disodium pamidronate, Alendronic acid and Denosumab
2 - Denosumab, Alendronic and Zolendronic acid
3 - Disodium pamidronate, Alendronic and Zolendronic acid
4 - Disodium pamidronate, Zolendronic acid and Etoricoxib

Answer 5

3 - Disodium pamidronate, Alendronic and Zolendronic acid

Question 6

Selective oestrogen receptor modulator medication can be given to patients with osteoporosis, which are drugs that act on estrogen receptors. For example in bone they inhibits/down regulates osteoclast activity. Which of the following is the drug commonly used in the UK?

1 - Methotrexate
2 - Tamoxifen
3 - Raloxifene
4 - Prednisolone

Answer 6

3 - Raloxifene

Question 7

If you have a patient that has previously had a fracture, hormone therapy (HRT or Selective Oestrogen Receptor Modulators) is not going to be potent enough for treatment. The 1st line treatment for patients who have previously had a fracture is bisphosphonates. The 3 drugs we need to know are:

1 - Alendronic acid
2 - Disodium pamidronate
3 - Zolendronic acid

What is the basic mechanism of action of this group of drugs?

1 - induce osteoblast proliferation
2 - induce osteocyte proliferation
3 - induce osteoblast apoptosis
4 - induce osteoclasts apoptosis

Answer 7

4 - induce osteoclasts apoptosis

• bisphosphonates have a similar structure to inorganic pyrophosphate
• bisphosphonates are incorporated into bone matrix
• bisphosphonates accumulates in osteoclasts and inhibits inhibit Farnesyl Pyrophosphate Synthase (FPS)
• FPSinhibition induces apoptosis of osteoclasts

Question 8

If you have a patient that has previously had a fracture, hormone therapy (HRT or Selective Oestrogen Receptor Modulators) is not going to be potent enough for treatment. The 1st line treatment for patients who have previously had a fracture is bisphosphonates, with the 3 core drugs being Alendronic acid, Disodium pamidronate and Zolendronic acid. These drugs work by inhibiting osteoclasts, but they must be taken in a very specific manner. What is this manner?

1 - 1/wk, empty stomach with full glass of water while standing, no food for 30 minutes after
2 - 1/wk, empty stomach intravenously, no food for 30 minutes after
1 - 3/wk, empty stomach with full glass of water while standing, no food for 30 minutes after
1 - 1/wk, empty stomach with full glass of water while standing

Answer 8

1 - 1/wk, empty stomach with full glass of water while standing, no food for 30 minutes after

Question 9

If you have a patient that has previously had a fracture, hormone therapy (HRT or Selective Oestrogen Receptor Modulators) is not going to be potent enough for treatment. The 1st line treatment for patients who have previously had a fracture is bisphosphonates, with the 3 core drugs being Alendronic acid, Disodium pamidronate and Zolendronic acid. What is the most common side effect of these drugs?

1 - rickets disease
2 - oesophagitis/gastritis (oral agents)
3 - osteonecrosis of the jaw (rare)
4 - atypical femoral fractures (rare)

Answer 9

2 - oesophagitis/gastritis (oral agents)

Question 10

Osteoprotegerin is a inhibitory factor released by osteoblasts. Osteoprotegerin binds RANK-L and inhibits osteoclasts maturation. There are synthetic forms of osteoprotegerin that can have the same effect, which are classed as RANK-L inhibitors. What is the core drug that we need to know that comes under this category?

1 - bisphosphonate
2 - denosumab
3 - estrogen
4 - triparitide

Answer 10

2 - denosumab

- very expensive

Question 11

What core drug do we need to know that is an anabolic (means to build things) drug that increases bone formation?

1 - bisphosphonate
2 - denosumab
3 - estrogen
4 - triparitide

Answer 11

4 - triparitide

Question 12

Triparitide is a hormone regulator and is the core drug that we need to know that is an anabolic (means to build things) drug that increases bone formation. What is the mechanism of action of this drug?

1 - inhibits PTH
2 - induces constant secretion of PTH
3 - inhibits calcitonin and vitamin D
3 - induces a pulsatile secretion of PTH

PTH = parathyroid hormone

Answer 12

• triparitide is a recombinant analogue of parathyroid hormone (essentially a copy of PTH)
• forms pulses of PTH stimulating both osteoblasts and osteoclasts
• BUT stimulates osteoblast more and increases bone formation