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7262 MS Block 2 > Liu Med Chem > Flashcards

Liu Med Chem Flashcards

1
Q

4 bisphosphonates:

A

alendronate
ibandronate
risedronate
zoledronic acid

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2
Q

What drug class is denosumab?

A

RANKL inhibitor

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3
Q

Two selective estrogen receptor modulators (SERMs)?

A

raloxifene

bazedoxifene

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4
Q

What is an anabolic osteoporosis drug?

A

teriparatide

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5
Q

Bisphosphonates bind to hydroxyapatite portion of the bone and can bind to and stabilize what?

A

calcium phosphate

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6
Q

What does the R1 group (OH) in bisphosphonates help do?

A

bind to calcium

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7
Q

What does the R2 group in bisphosphonates determine?

A

antiresorptive potency

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8
Q

Do bisphosphonates have good or poor bioavailability?

A

poor

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9
Q

Do bisphosphonates have high or low solubility?

A

low

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10
Q

3 GI side effects of oral bisphosphonates (alendronate, ibandronate, risedronate)?

A

heartburn
esophageal irritation
esophagitis

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11
Q

Bisphosphonates given IV can cause injection reactions.

a. true
b. false

A

a. true

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12
Q

What is a serious AE of bisphosphonates?

A

osteonecrosis of the jaw

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13
Q

What condition should be resolved before starting bisphosphonates?

A

hypocalcemia

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14
Q

___ abnormalities are a contraindication for oral bisphosphonates.

A

esophageal

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15
Q

Which bisphosphonate is contraindicated with renal impairment?

A

zoledronic acid

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16
Q

What does denosumab bind to?

A

RANKL

prevents it rom binding to the RANK receptor on osteoclasts, inhibiting production of osteoclasts and increasing osteoclast apoptosis

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17
Q

3 AEs of the RANKL inhibitor denosumab?

A

osteonecrosis of the jaw
skin infection
hypocalcemia (serious)

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18
Q

What effect does the flexible side chain of SERMS have?

A

anti estrogen effect

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19
Q

Raloxifene is an __ in osteoblasts and osteoclasts estrogen receptors.

a. agonist
b. antagonist

A

a. agonist

20
Q

Raloxifene is an __ on breast and uterine estrogen receptors.

a. agonist
b. antagonist

A

b. antagonist

21
Q

The CYP system is not involved in metabolism of SERMS.

a. true
b. false

A

a. true

22
Q

What is a serious AE of SERMs?

A

thrombosis of retinal vein

23
Q

3 contraindications for the SERM raloxifene?

A
  • venous thromboembolic events
  • nursing mothers
  • pregnancy
24
Q

Where is calcitonin-salmon metabolized?

A

kidney

25
Q

Should a person with salmon allergy receive calcitonin-salmon?

A

no

26
Q

__ is an anabolic osteoporosis drug

A

teriparatide

27
Q

Teriparatide increases bone mass/strength by preferential stimulation of __ activity over _ activity

A

osteoblastic, osteoclastic

28
Q

NSAIDs reduce pain, inflammation, fever by preventing synthesis of __

A

prostaglandins

29
Q

Which nsaid irreversibly inhibits cox1 and cox2?

A

aspirin

forms covalent bond

30
Q

Aspirin works via acetylation of __

A

serine 529

31
Q

Ibuprofen forms __ bonds

a. covalent
b. noncovalent

A

b. noncovalent

works via steric interference

32
Q

The anion group of nsaids is usually what functional group?

A

carboxyl group

aka carboxylic acid

33
Q

Indomethacin is an __ derivative

A

acetic acid

34
Q

Ibuprofen is a __ derivative

A

propionic acid

35
Q

What group in ibuprofen increases anti-inflammatory activity and reduces AEs?

A

alpha methyl

36
Q

Selective nsaids inhibit which cox?

A

cox2

too large to fit in cox1

37
Q

Does acetaminophen have antiinflammatory activity?

A

no

target: cox or other (not fully understood)

38
Q

What is the metabolite of acetaminophen that causes hepatotoxicity?

A

NAPQI

39
Q

Which cox is involved in maintenance of gastric mucosa, renal function, and normal cellular function?

A

cox1

40
Q

Which cox is induced by cytokines, growth factors, and inflammatory sites?

A

cox2

41
Q

Non-aspirin nsaids exert anti-inflammatory effect by ___ and reversible activity site inhibition of cox.

a. competitive
b. non-competitive

A

a. competitive

competitive and reversible

42
Q

Which is non-competitive?

a. non-aspirin nsaids
b. aspirin

A

b. aspirin

43
Q

Which has a BBW for cardiovascular events and GI bleeding?

a. cox 1 inhibitors
b. cox 2 inhibitors

A

b. cox 2 inhibitors

44
Q

Selective nsaid CV AEs:

When the balance is tipped in favor of __ vasoconstriction and platelet clumping are more likely to occur.

a. PGI2
b. TXA2

A

b. TXA2

selective block cox2, causing a shift to cox1 and more TXA2 production

45
Q

TXA2 is produced primarily by __ activity

a. cox1
b. cox2

A

a. cox1

46
Q

PGI2 is produced by __ activity

a. cox1
b. cox2

A

b. cox2

7262 MS Block 2 (10 decks)

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