Lecture 4 - Bone Drugs Flashcards

1
Q

Calcium Supplements

A

clinical application: Ca2+ deficiency

MOA: increase bone mineralization and decrease PTH release

SE: 
constipation
urolithiasis
prostate cancer
GI upset 

Contraindications:
Hypercalcemia
Ventricular fibrillation (Ca-gluconate only)

give Ca-carbonate with food because stomach H+ secretion is needed to free Ca2+

Ca-citrate for pts taking a PPI

subcutaneous infiltration of IV infusion is less toxic with Ca-gluconate than CaCl2

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2
Q

What are the SE of Ca2+ supplements?

A

constipation
urolithiasis
prostate cancer
GI upset

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3
Q

What is the MOA of Ca2+ supplements?

A

increase bone mineralization and decrease PTH release

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4
Q

What are the contraindications of Ca2+ supplements?

A
Hypercalcemia
Ventricular fibrillation (Ca-gluconate only)
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5
Q

What are the different types of Ca2+ supplements?

A

Ca2+ gluconate (IV)
Ca2+ chloride (IV)
Ca2+ carbonate (PO)
Ca2+ citrate malate (PO)

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6
Q

What should you tell pts who you prescribe ca-carbonate in regards to timing of taking the medication?

A

take with food because stomach H+ secretion is needed to free Ca2+

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7
Q

When prescribing Ca2+ supplements to pts, what must you do?

A

also prescribe Vitamin D when osteoporosis medicines are taken

Ca2+ + Vitamin D = vertebral fracture decreased up to 16% and hip fx by up to 30%

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8
Q

What are the different vitamin D supplements?

A
Cholecalciferol (VtD3) 
Ergocalciferol (VtD2) 
Calcifediol (25-OH D3) 
Calcitriol (1,25 OH D3) 
Doxercalciferol (A alpha OH D2) 
Paricalcitol
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9
Q

What is the MOA of Vitamin D supplements?

A

increase Gl Ca2+ and PO4 absorption

decrease PTH gene transcription

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10
Q

What are the indications for vitamin D supplements?

A
Vt D deficiency 
Hypoparathyroidism 
Rickets
Ostemalacia
Osteoporosis 
Secondary hyperparathyroidism
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11
Q

What are the adverse effects of Vitamin D supplements?

A
hypervitaminosis D
Hypercalcemia
Hypophosphatemia
Hypercalciuria
GI hemorrhage 
Angioedema 
Abnormal lipids, GI upset, edema, HA
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12
Q

What are the contraindications for Vitamin D supplements?

A

hypersensitivity to drug

hypercalcemia

hypervitaminosis D

malabsorption syndrome

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13
Q

Which vitamin D supplement is most commonly used?

A

calitriol is often the preferred agent due to fast onset and offset (12h) and faster approach to steady state (72-96h)

calcitriol may cause more hypercalcemia than either paricalcitol or doxercalciferol

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14
Q

hPTH 1-34

A

teriparatide

indications:
severe osteoporosis
(only in pts at high risk of fx)

SE: 
angina
hypotension
rash
swelling
hyperuricemia
GI upset
asthenia
dizziness
cough 
rhinitis
contraindications:
hypersensitivity to teripartide 
Paget's disease 
open epiphyses (kids and adolescents) 
prior radiation 
bone malignancy 
hypercalcemia 

long term use casues osteosclerosis and osteosarcomas in rodents

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15
Q

What are the indications for teriparatide?

A

severe osteoporosis

only in pts at high risk of fx

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16
Q

What are the SE of teriparatide?

A
angina
hypotension
rash
swelling
hyperuricemia
GI upset
asthenia
dizziness
cough 
rhinitis
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17
Q

What are the contraindications of teriparatide?

A
hypersensitivity to teripartide 
Paget's disease 
open epiphyses (kids and adolescents) 
prior radiation 
bone malignancy 
hypercalcemia
18
Q

Calcimemetics

A

cinacalcet

increases sensitivity of Ca2+ sensing receptors to Ca2+ in parathyroid cells
decreases PTH release

19
Q

Cinacalcet

A

a calcimemtic

indications:
hyperthyroidism
hypercalcemia associated with parathyroid carcinoma

SE: 
cardiac arrythmia 
heart failure
seizure 
electrolyte imbalance 
anemia 
bone fx
paresthesia
GI upset
arthralgia
myalgia
asthenia
HA
depression
dehydration
fatigue 

contraindications:
hypocalcemia

sometimes used off label to treat forms of secondary hyperparathyrodisim

20
Q

What are the indications for cinacalcet?

A

hyperthyroidism
hypercalcemia associated with parathyroid carcinoma

sometimes used off label to treat forms of secondary hyperparathyrodisim

21
Q

What are the SE of cinacalcet?

A
cardiac arrythmia 
heart failure
seizure 
electrolyte imbalance 
anemia 
bone fx
paresthesia
GI upset
arthralgia
myalgia
asthenia
HA
depression
dehydration
fatigue
22
Q

What are the contraindications of cinacalcet?

A

hypocalcemia

23
Q

SERMs

A

replace continuous estrogen-progestin that increases the risk of breast cancer, pulmonary embolism, stroke, and coronary heart disease
estrogen receptor agonist in bone, while estrogen receptor antagonist in endometrium and breast
reduce breast cancer, but not stroke or embolism

24
Q

Raloxifene

A

SERM

indication:
prevention and treatment of osteoporosis
prophylaxis of invasive breast cancer

SE:
retinal vascular occlusion, venous thromboembolism (d/t increase in hepatic clotting factor production)
hot flashes
leg cramps

contraindications:
pregnancy
hx of venous thromboembolism

decreases breast cancer incidence

25
What are the indications for raloxifene?
prevention and treatment of osteoporosis | prophylaxis of invasive breast cancer
26
What are the SE of raloxifene?
retinal vascular occlusion, venous thromboembolism (d/t increase in hepatic clotting factor production) hot flashes leg cramps
27
What are the contraindications of raloxifene?
pregnancy hx of venous thromboembolism decreases bre
28
Which bisphosphonates are used?
``` alendronate (PO) risedronate (PO) pamidronate (PO) ibandronate (PO or IV) zoledronate (IV) ```
29
Bisphonphonates
indications: prevention and treatment of osteoporosis (except Pamidronate) Padget's disease (except Ibandronate) Osteolytic lesions of multiple myeloma and breast cancer (excpet pamidronate and zoledronate) hypercalcemia associated with malignancy (Pamidronate and zoledronate ONLY) ``` SE: arthralia myalgia jaw osteonecrosisprimarily in cancer pts atypical femur fx esophageal ulcer nephrotoxicity GI upset ``` Contraindications: hypersensitivity to drug hypocalcemia esophageal disease unable to sit up for 30 minutes after taking drug orally adequate renal function is necessary for use of intravenous BPs 30% of pts initial transient flu-like illness "drug holidarys" after 5 years due to atypical femur fx
30
What is the indication for bisphosphonates?
prevention and treatment of osteoporosis (except Pamidronate) Padget's disease (except Ibandronate) Osteolytic lesions of multiple myeloma and breast cancer (excpet pamidronate and zoledronate) hypercalcemia associated with malignancy (Pamidronate and zoledronate ONLY)
31
What are the SE of bisphosphonates?
``` arthralia myalgia jaw osteonecrosisprimarily in cancer pts atypical femur fx esophageal ulcer nephrotoxicity GI upset ```
32
What are the contraindications of bisphosphonates?
hypersensitivity to drug hypocalcemia esophageal disease unable to sit up for 30 minutes after taking drug orally
33
Denosumab
a fully monoclonal human antibody produced against RANKL indication: prevention and treatment of osteoporosis bone metastases from solid tumors ``` SE: endocarditis cellulitis electrolyte imbalance pancreatitis hypersensitivity reaction Jaw osteonecrosis in cancer pts atypical femur fxs GI upset asthenia URI fatigue dyspnea ``` Contraindications: hypocalcemia pregnancy injected SubQ every 6 months for osteoporosis and monthly for malignancy
34
What are the indications for denosumab?
prevention and treatment of osteoporosis | bone metastases from solid tumors
35
What are the SE of denosumab?
``` endocarditis cellulitis electrolyte imbalance pancreatitis hypersensitivity reaction Jaw osteonecrosis in cancer pts atypical femur fxs GI upset asthenia URI fatigue dyspnea ```
36
What are the contraindications of denosumab?
hypocalcemia | pregnancy
37
Calcitonin
decreases serum calcium by: decreasing absorption in the gut decreasing reabsorption in the kidney increasing deposition in bone (directly inhibiting osteoclast; activating osteoblasts)
38
Salmon calcitonin
longer half life than human nasal spray or subQ injections indication: hypercalcemia padget's disease osteoporosis ``` SE: hypocalcemia hypersensitivity seizure cancer flushing nausea ```
39
What is the indication for salmon calcitonin?
hypercalcemia padget's disease osteoporosis
40
What are the SE of salmon calcitonin?
``` hypocalcemia hypersensitivity seizure cancer flushing nausea ```