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Endocrine 2 > Osteoporosis Pharmacology > Flashcards

Osteoporosis Pharmacology Flashcards

1
Q

What controls the formation of 1,25-OH vitamin D?

A

PTH

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2
Q

how does M-CSF affect bone metabolism?

A

increase osteoclast activity

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3
Q

how does OPG affect bone metabolism?

A

decrease osteoclast activity

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4
Q

how does RANKL affect bone metabolism?

A

increase osteoclast activity

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5
Q

Which cytokines are osteoclastic?

A

IL-1, IL-6

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6
Q

how do IGF-1, IGF-2 affect bone metabolism?

A

osteoblastic

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7
Q

What is the recommended daily allowance for Calcium?

A

1200mg/day < RDA < 2500 mg/day

supplement may be needed in pts taking PPI’s

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8
Q

What is the recommended daily allowance for Vit D3?

A

adult: 400U

low sunlight areas: 2000U/day

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9
Q

When is active Vit D (calcitriol, paricalcitol) needed?

A

needed when renal pathology is present

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10
Q

What are downsides of calcium preparations?

A

not effective in absence of Vit D

Constipation sometimes seen

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11
Q

What is management of osteoporosis in PREmenopausal women?

A
  1. Exercise (weightbearing)
  2. 1200-2500 mg/day calcium
  3. Vit D
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12
Q

What is the management of osteoporosis in POSTmenopausal women?

A

Calcium + Vit D3 (risk of kidney stone if calcium > 2500mg/day)
-raloxifene or bisphosphonate often needed

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13
Q

Whats the osteoporosis treatment efficacy from most effective to least?

A
  1. Vit D, Ca2+, PTH
  2. Calcitonin, Bisphosphonate
  3. Estrogen, denosumab
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14
Q

Although Estrogen + Progestin therapy decreases fx risk, why are they bad?

A

increases Heart attacks, strokes, breast cancer, VTE’s

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15
Q

What is the recommended pharm for osteoporosis? What is the mechanism of action?

A

Raloxifene - selective estrogen receptor modulator

  1. Partial agnostic at Estrogen Receptor A
  2. Antagonist at Estrogen Receptor B
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16
Q

Where are ERa and ERb located? what drug acts on these receptors?

A

ERa - cortical bone
ERb - trabecular bone
Raloxifene - ERa partial agnoist, ERb antagonist

17
Q

What is the physiological results of SERMs? Raloxifene

A
  1. ERa agonist, ERb antagonist
  2. reduce IL-6, TNF-a, M-CSF
  3. decreased responsiveness of RANK receptor to RANKL
  4. stimulation of OPG formation

net fx: reduce osteoclast activation, osteoblasts left unopposed

18
Q

What are potential risks of SERMs?

A
  1. Teratogenesis
  2. DVT, thrombotic stroke
  3. hot flashes
19
Q

What is conjugated estrogen/bazedoxifene (SERM) reserved for?

A

women with a uterus

20
Q

What are the benefits of Raloxifene? (4)

A
  1. increase bone density in spine/long bones
  2. decrease hip/spine fx
  3. reduced breast cancer
  4. decrease in uterine cancer
21
Q

What is the mechanism of action of Bisphosphonates?

A
  • directly incorporate into bone

- reduce osteoclastic dissolution of hydroxyapatite in bone (paget’s dissease, hyperPTH)

22
Q

What are alendronate, etidronate, zoledronic acid?

A

Bisphosphonates - osteoporosis, fracture healing

23
Q

What are side fx of bisphosphonates?

A
  1. may erode esophagus
  2. OSTEONECROSIS of jaw - seen w glucocorticoids, dental procedures
  3. Atypical femur fracture
24
Q

What diuretic can be used in osteoporosis therapy?

A

Thiazide Diuretics - decrease Ca secretion

-rarely used primary for osteoporosis

25
Q

What is Teriparatide? What are its uses?

A

Parathormone

-reserved for high risk of fracture or sever osteoporosis or unresponsive osteoporosis

26
Q

What is Denosumab?

A

monoclonal Ab to RANK-L - prevents osteoclastic activation

27
Q

What are contraindications for Denosumab?

A
  1. Multiple myeloma
  2. Corticosteroids
  3. Dental surgery
  4. Radiation, chemo
  5. inability to take Vit D, Ca
28
Q

What are Risks of Denosumab?

A
  1. Mandibular necrosis

2. Hip fractures

29
Q

Who is Denosumab used in? (3)

A
  1. patients intolerant, unresponsive to bisphosphonates
  2. Women on aromatase inhibitors
  3. men with prostate cancer on GnRH inhibitors
30
Q

What is the Tx for osteoporosis in Pregnancy?

A

Calcium

Vit D

31
Q

What is the Tx for osteoporosis in Men?

A

Androgen if low test

same as women (exercise, Ca, Vit D, sometimes bisphosphonate) - NEVER estrogen or SERMS

32
Q

What is the Tx for osteoporosis induced by Aromatase Inhibitors?

A

SOC: Bisphosphonates
Ca, Vit D
consider substituting raloxifene for aromatase inhibitor

33
Q

What is the Tx for osteoporosis in short term spinal fractures?

A

Calcitonin

34
Q

What is the use of Calcitonin? (acute and chronic use)

A

Short Term - Spinal Fractures
Chronic - Paget’s Disease, HyperPTH
-Ca and phosphate excretion in kidney increased

35
Q

What is the Tx for post-low trauma bone fx or glucocorticoid induced osteoporosis?

A

Ca + Vit D3 + (bisphosphonate or parathormone or short term calcitonin)

36
Q

What is the osteoporosis Tx with HyperPTH?

A

cinacalcet

37
Q

What are Cinacalcet, Etelcalcetide?

A

Calcimimetics - activates CASR in parathyroid gland (reduce Ca, PO3)

38
Q

What are the uses of calcimimetics?

A

HyperPTH from:

  1. Chronic Kidney disease
  2. Parathyroid carcinoma
39
Q

What are side fx of Calcimimetics?

A

Cardiac arrhythmia

New or worsening heart failure

Endocrine 2 (17 decks)

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