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IDT Spring > Medchem for Osteoporosis > Flashcards

Medchem for Osteoporosis Flashcards

1
Q

what are the names of the selective estrogen receptor modulators (SERMs)?

A

Lasoxifene and Raloxifene

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2
Q

what are the names of the Bisphosphonates?

A

Alendronate
Etidronate
Ibandronate
Pamidronate
Risedronate
Zoledronic Acid

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3
Q

Other agents for osteoporosis are calcitonin, cinacalcet, teriparatide, inorganic salts, denosumab, vitamin D, and romosozumab

A
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4
Q

which SERM has estrogen agonist activity in bone and CV system, and antagonistic activity in breast and uterus?

A

Raloxifene

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5
Q

Bisphosphonates are pyrophosphate analogues with a _____________ backbone. They bind to the __________ portion of the bone to inhibit ________ proliferation and activity, and decrease __________.
They are not ______ and are excreted unchanged

A

nonhydrolyzable
hydroxyapatite, osteoclast, bone resorption
metabolized

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6
Q

which bisphosphonate was the first approved and is 1,000 fold more potent than etidronate? what SE can it cause that is prevented by taking it with a glass of water and remaining upright for 30 min?

A

alendronate
esophagitis

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7
Q

Alendronate is used to treat?

A

osteoporosis and Paget’s disease

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8
Q

Etidronate is used to treat?

A

Paget’s disease, but not osteoporosis

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9
Q

Ibandronate is used to treat?
what is its bioavailability?

A

osteoporosis in postmenopausal women
0.6%

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10
Q

Pamidronate is used to treat?

A

hypercalcemia of malignancy

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11
Q

Risedronate is used to treat?

A

osteoporosis, Paget’s disease, and glucocorticoid-induced osteoporosis

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12
Q

Zoledronic Acid is used to treat?

A

hypercalcemia of malignancy

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13
Q

which drug is a peptide hormone consisting of 32 amino acids?

A

Calcitonin

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14
Q

Calcitonin is used to treat?
what formulation is best?

A

postmenopausal osteoporosis, hypercalcemia of malignancy, and Paget’s disease
calcitonin from salmon

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15
Q

which drug requires concomitant oral administration of calcium?

A

calcitonin

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16
Q

what is the MOA of Cinacalcet?
it is used to treat?

A

calcimimetic agent that increases binding of calcium to the calcium sensing receptor, this activates phospholipase C to inhibit PTH release
secondary hyperparathyroidism in pts with CKD on dialysis and hypercalcemia in pts with parathyroid cancer

17
Q

what is the MOA of Teriparatide? it is recommended to be taken with?
it is used to treat?

A

enhances osteoblasts and osteoclasts to increase bone formation
calcium and vit D
postmenopausal osteoporosis with high fracture risk and increase bone mass of men with osteoporosis who have a high risk of fracture

18
Q

what are the inorganic salts?

A

Calcium salts
gallium nitrate
sodium fluoride
strontium ranelate

19
Q

why are calcium salts used?

A

improve absorption of calcium

20
Q

why is gallium nitrate used?

A

treats hypercalcemia of malignancy. inhibits bone resorption

21
Q

which organic salt is contraindicated in pts with severe renal impairment?

A

gallium nitrate

22
Q

why is sodium fluoride used? why is it only combined with calcium?

A

promotes proliferation and activity of osteoblasts to treat osteoporosis
by itself, causes inferior bone tissue and can increase fracture risk
as a combo improves bone mass and decreases risk of vertebral fractures

23
Q

when is strontium ranelate used?

A

when pts can’t tolerate bisphosphonates

24
Q

Denosumab is used to treat?
MOA?
more or less potent than bisphosphonates?
how is it administered?

A

menopausal osteoporosis and bone metastases
inactivates RANKL which normally binds to RANK receptors and cause bone resorption, thus reducing bone resorption.
more potent
twice per year as a SC injection

25
Q

which population benefits from vit D supplementation?

A

elderly because they often have reduced renal function

26
Q

Romosozumab:
MoA?

A

binds and inactivates sclerostin to prevent inhibition of bone formation by allowing Wnt-B-catenin to bind to LPR 5/6

27
Q

when Wnt binds to LPR 5/6 and the Frizzled family receptor, inhibition of the _______ destruction complex occurs and then accumulates to enter the nucleus, leading to transcription of ____________ and bone formation.
When sclerostin binds to LPR 5/6, the ________ destruction complex is assembled, and _______ is degraded, so ___________ are not activated, leading to increased bone resorption and decreased bone formation.

A

B-catenin, Wnt-responsive genes
B-catenin, B-catenin, Wnt-responsive genes

IDT Spring (22 decks)

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