Therapeutic Considerations

Question 1

What is the oldest NSAID?

Answer 1

aspirin

Question 2

How does aspirin differ from other NSAIDs?

Answer 2

It acts in an irreversible manner, by acetylating the active site serene residue in both COX-1 and COX-2

Question 3

Aspirin increases the plasma concentration of which substance? Consequence?

Answer 3

acetazolamids; CNS toxicity

Question 4

Which drug may inhibit the anitplatelet effect of aspirin?

Answer 4

ibuprofen

Question 5

Limited reports about aspirin state what in regarding to methotrexate?

Answer 5

salicylates may enhance methotrexate toxicity

Question 6

What does aspirin increase the risk of?

Answer 6

bleeding in anticoagulated patient

Question 7

Which NSAID has the longest half-life and few adverse effects?

Answer 7

naproxen

Question 8

Which NSAID is used for analgesia in surgical patients? How long can it be used for?

Answer 8

ketorolac; it can be used for no more than 3-5 days

Question 9

Which NSAID has the greatest selectivity for COX-2?

Answer 9

nabumetone

Question 10

How to fenamates compare to aspirin?

Answer 10

Fenamates have less anti-inflammatory activity and higher toxicity

Question 11

How does acetaminophen compare to aspirin?

Answer 11

it has analgesic and antipyretic effects similar to aspirin, but the anti-inflammatory effect of acetaminophen is insignificant because of its weak inhibition of peripheral cyclooxygenase

Question 12

Which COX isoform may acetaminophen block in the CNS?

Answer 12

COX-3

Question 13

What is the consequence of acetaminophen overdose?

Answer 13

hepatic failure

Question 14

What is the antidote for acetaminophen overdose?

Answer 14

N-acetylcysteine

Question 15

Celecoxib decreases the efficacy of which other class of drugs?

Answer 15

ACE inhibitors

Question 16

What is the the benefit of COX-2 selective inhibitors?

Answer 16

they may decrease gastropathy and nephropathy associated with NSAID use

Question 17

What are the therapeutic considerations of alprostadil?

Answer 17

PGE1 analogue with vasodilator properties
used primarily for maintaining patent ductus arterioles in tetralogy of Fallot, Eisenmenger pulmonary hypertension, and aortic valve atresia

Question 18

What are the therapeutic considerations of misoprostol?

Answer 18

PGE1 analogue with vasodilator properties
also used in peptic ulcer disease
cytoprotective effets likely mediated by increasing gastric mucus and bicarb production
antisecretory effects mediated via inhibition of basal and nocturnal gastric secretion by parietal cells

Question 19

What are the therapeutic considerations of carboprost?

Answer 19

PGE2-alpha analogue that stimulates uterine contraction for abortifacient activity
luteolytic activity controls fertility

Question 20

What are the therapeutic considerations of latanoprost, bimatoprost, and travoprost?

Answer 20

PGF2-alpha analogues with vasodilator properties, ocular hypotensive agents

Question 21

What are the therapeutic considerations of epoprostenol?

Answer 21

prostacyclin analogue that stimulates vasodilation of pulmonary and systemic arterial vasculature; also inhibits platelet aggregation

Question 22

What are the therapeutic considerations of zileutin?

Answer 22

avoid concurrent use of dihydroergotamine, ergoloid mesylates, eronovine, and methylergonovine due to increased risk of ergotism (nausea, vomiting, vasospastic ischemia)

Question 23

What are the therapeutic considerations of montelukast and zafirlukast?

Answer 23

they are not indicated for acute asthma attacks and are generally not appropriate as monotherapy for asthma
they are secreted in breast milk