Lecture 119

Question 1

Large family of signaling molecules derived from arachidonic acid (AA)

Answer 1

Eicosanoids

Question 2

Prostaglandins (PGE2, PGF-alpha, PGD2), prostacyclin (PGI2), thromboxanes (TXA2), and leukotrienes all belong to what family?

Answer 2

Eicosanoids

Question 3

Polyunsaturated fatty acid released from membrane phospholipids by phospholipase A2 (PLA2)

Answer 3

Arachidonic acid (AA)

Question 4

AA can be metabolized by COX, into:

Answer 4

Prostanoids

Question 5

What COX is constitutively expressed in most tissues?

Answer 5

COX-1

Question 6

“Housekeeping” roles: gastric mucosal protection, platelet function

Answer 6

COX-1

Question 7

What pharmacological target contributes significantly to inflammatory processes?

Answer 7

COX-2

Question 8

General mechanism of NSAIDs

Answer 8

Inhibit cyclooxygenases, thereby decreasing synthesis of prostanoids (PGE2, PGI2, TXA2, etc.)

Question 9

All NSAIDs reversibly inhibit COX1 and/or COX2, except ____

Answer 9

Aspirin

Question 10

Aspirin belongs to what classification of NSAIDs?

Answer 10

Salicylates

Question 11

Indomethacin, ketorolac, diclofenac belong to which NSAID class?

Answer 11

Acetic acid derivatives

Question 12

Ibuprofen and naproxen belong to which NSAID class?

Answer 12

Propionic acid derivatives

Question 13

Meloxicam and piroxicam belong to which NSAID class?

Answer 13

Enolic acid derivatives

Question 14

Celecoxib selectively inhibits ____

Answer 14

COX-2

Question 15

Most NSAIDs are weak ____

Answer 15

Acids

Question 16

Where do NSAIDs accumulate after repeated dosing?

Answer 16

Inflamed tissues and synovial fluid

Question 17

How do NSAIDs lower fevers?

Answer 17

Inhibits PGE2 synthesis in the hypothalamus

Question 18

All NSAIDs come with an increased CV risk escept ____

Answer 18

Low-dose aspirin

Question 19

NSAIDs have a limited effect on ____

Answer 19

Severe visceral pain

Question 20

Which NSAIDs are used to encourage the closure of ductus arteriosus in neonates?

Answer 20

Indomethacin and ibuprofen

Question 21

Niacin-induced flushing can be reduced by ____, by ____

Answer 21

Aspiring, by blocking PGD2 release

Question 22

Aspirin should be avoided in children with viral illness due to:

Answer 22

Reye syndrome

Question 23

COX-2 selective inhibitors have a ____ GI ulceration risk and a ____ CV risk

Answer 23

Lower, higher

Question 24

Platelets precominantly have ____, which generates ____, ____ platelet aggregation and local vasoconstriction

Answer 24

COX-1, TXA2, promoting

Question 25

Endothelial cells precominantly have ____, which generates ____, ____ platelet aggregation and causes vasodilation

Answer 25

COX2, PGI2, inhibits

Question 26

Non-aspirin NSAIDs block both TXA2 (platelet) and PGI2 (endothelial) transiently, but the net effect often favors ____

Answer 26

Thrombosis and higher CV risk

Question 27

Low-dose aspirin irreversibly inactivates platelet COX-1 in ____

Answer 27

Portal circulation

Question 28

NSAIDs can precipitate ____, especially in patients with heart failure, cirrhosis, hypovolemia, or pre-existing renal disease

Answer 28

Acute kidney injury

Question 29

____ maintain renal blood flow, NSAIDs block these vasodilatory effect

Answer 29

Prostanoids (PGE2 and PGI2)

Question 30

Why NSAID class is most likely to cause tinnitus?

Answer 30

Salicylates

Question 31

Rare hematologic adverse effects of NSAIDS:

Answer 31

Aplastic anemia, agranulocytosis

Question 32

Taking NSAIDs past 20 weeks of pregnancy increases the risk of

Answer 32

Oligohydraminos (low amniotic fluid)

Question 33

Taking NSAIDs past 30 weeks of pregnancy increases the risk for:

Answer 33

Premature closure of the ductus arteriosus

Question 34

NSAIDS are contraindicated before ____ surgery due to increased MI and stroke risk

Answer 34

Coronary artery bypass graft

Question 35

NSAIDs shouldn't be taken with ____ due to increased risk of bleeding

Answer 35

Anticoagulants/antiplatelets and SSRIs

Question 36

ACE inhibitors and NSAIDs shouldn't be combined due to risk of:

Answer 36

Acute kidney injury

Question 37

The combination of diuretics and NSAIDs can reduce diuretic efficacy by ____

Answer 37

Promoting Na+ and water retention

Question 38

Why shouldn't NSAIDs be combined with lithium?

Answer 38

SNAIDs may increase lithium reabsorption to potentially toxic levels

Question 39

MOA of aspirin

Answer 39

Irreversible acetylation of COX1 and COX2 at an allosteric site

Question 40

Aspirin is rapidly hydrolyzed by esterases to ____, which is ____

Answer 40

Salicylic acid, reversible COX inhibitor

Question 41

Apsirin half-life

Answer 41

20 minutes

Question 42

Rheumatic fever and Kawasaki disease are treated with which NSAID?

Answer 42

Aspirin

Question 43

Asthma, nasal polyps, and bronchospasm are a triad of adverse effects of ____

Answer 43

Aspirin, aspirin-exacerbated respiratory disease (AERD)

Question 44

Tinnitus, vertigo, hyperventilation, and respiratory alkalosis are a sign of ____ toxicity

Answer 44

Salicylate

Question 45

Severe salicylate poisoning presents with

Answer 45

Metabolic acidosis, hyperthermia, CNS effects, pulmonary edema

Question 46

A depletion of gluathione and accumulation of NAPQI is casued by ____ overdose

Answer 46

Acetaminophen

Question 47

Acetaminophen overdose can cause:

Answer 47

Hepatotoxicity and acute liver failure