Liu Med Chem

Question 1

4 bisphosphonates:

Answer 1

alendronate
ibandronate
risedronate
zoledronic acid

Question 2

What drug class is denosumab?

Answer 2

RANKL inhibitor

Question 3

Two selective estrogen receptor modulators (SERMs)?

Answer 3

raloxifene

bazedoxifene

Question 4

What is an anabolic osteoporosis drug?

Answer 4

teriparatide

Question 5

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

Answer 5

calcium phosphate

Question 6

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

Answer 6

bind to calcium

Question 7

What does the R2 group in bisphosphonates determine?

Answer 7

antiresorptive potency

Question 8

Do bisphosphonates have good or poor bioavailability?

Answer 8

poor

Question 9

Do bisphosphonates have high or low solubility?

Answer 9

low

Question 10

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

Answer 10

heartburn
esophageal irritation
esophagitis

Question 11

Bisphosphonates given IV can cause injection reactions.

a. true
b. false

Answer 11

a. true

Question 12

What is a serious AE of bisphosphonates?

Answer 12

osteonecrosis of the jaw

Question 13

What condition should be resolved before starting bisphosphonates?

Answer 13

hypocalcemia

Question 14

___ abnormalities are a contraindication for oral bisphosphonates.

Answer 14

esophageal

Question 15

Which bisphosphonate is contraindicated with renal impairment?

Answer 15

zoledronic acid

Question 16

What does denosumab bind to?

Answer 16

RANKL

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

Question 17

3 AEs of the RANKL inhibitor denosumab?

Answer 17

osteonecrosis of the jaw
skin infection
hypocalcemia (serious)

Question 18

What effect does the flexible side chain of SERMS have?

Answer 18

anti estrogen effect

Question 19

Raloxifene is an __ in osteoblasts and osteoclasts estrogen receptors.

a. agonist
b. antagonist

Answer 19

a. agonist

Question 20

Raloxifene is an __ on breast and uterine estrogen receptors.

a. agonist
b. antagonist

Answer 20

b. antagonist

Question 21

The CYP system is not involved in metabolism of SERMS.

a. true
b. false

Answer 21

a. true

Question 22

What is a serious AE of SERMs?

Answer 22

thrombosis of retinal vein

Question 23

3 contraindications for the SERM raloxifene?

Answer 23

• venous thromboembolic events
• nursing mothers
• pregnancy

Question 24

Where is calcitonin-salmon metabolized?

Answer 24

kidney

Question 25

Should a person with salmon allergy receive calcitonin-salmon?

Answer 25

no

Question 26

__ is an anabolic osteoporosis drug

Answer 26

teriparatide

Question 27

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

Answer 27

osteoblastic, osteoclastic

Question 28

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

Answer 28

prostaglandins

Question 29

Which nsaid irreversibly inhibits cox1 and cox2?

Answer 29

aspirin forms covalent bond

Question 30

Aspirin works via acetylation of __

Answer 30

serine 529

Question 31

Ibuprofen forms __ bonds a. covalent b. noncovalent

Answer 31

b. noncovalent works via steric interference

Question 32

The anion group of nsaids is usually what functional group?

Answer 32

carboxyl group aka carboxylic acid

Question 33

Indomethacin is an __ derivative

Answer 33

acetic acid

Question 34

Ibuprofen is a __ derivative

Answer 34

propionic acid

Question 35

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

Answer 35

alpha methyl

Question 36

Selective nsaids inhibit which cox?

Answer 36

cox2 too large to fit in cox1

Question 37

Does acetaminophen have antiinflammatory activity?

Answer 37

no target: cox or other (not fully understood)

Question 38

What is the metabolite of acetaminophen that causes hepatotoxicity?

Answer 38

NAPQI

Question 39

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

Answer 39

cox1

Question 40

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

Answer 40

cox2

Question 41

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

Answer 41

a. competitive competitive and reversible

Question 42

Which is non-competitive? a. non-aspirin nsaids b. aspirin

Answer 42

b. aspirin

Question 43

Which has a BBW for cardiovascular events and GI bleeding? a. cox 1 inhibitors b. cox 2 inhibitors

Answer 43

b. cox 2 inhibitors

Question 44

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

Answer 44

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

Question 45

TXA2 is produced primarily by __ activity a. cox1 b. cox2

Answer 45

a. cox1

Question 46

PGI2 is produced by __ activity a. cox1 b. cox2

Answer 46

b. cox2