NSAIDs

Question 1

Name 3 chemical mediators of inflammation.

Answer 1

1) kinins
2) histamine
3) neuropeptides

Question 2

Give an example of a kinin.

Answer 2

bradykinin

Question 3

Give an example of a neuropeptide.

Answer 3

substance P

Question 4

Tissue destruction leads to release of _____ and synthesis of _____.

Answer 4

chemical mediators; eicosanoid mediators

Question 5

Where do eicosanoid mediators derive from?

Answer 5

arachadonic acid

Question 6

What is the target of an NSAID?

Answer 6

COX-1 and COX-2

Question 7

By inhibiting COX1 and 2, production of ____ and ____ will decrease.

Answer 7

inflammatory prostaglandins; thromboxanes

Question 8

COX is the major synthetic enzyme for ___ and ____.

Answer 8

prostaglandins (PGs); thromboxane A2 (TXA2)

Question 9

What are the 4 therapeutic uses of an NSAID?

Answer 9

1) analgesia
2) antipyretic
3) anti-inflammatory
4) antithrombogenesis

Question 10

How is analgesia achieved by an NSAID?

Answer 10

inhibition of inducible COX-2 at sites of tissue injury

Question 11

How is an antipyretic affect achieved by an NSAID?

Answer 11

inhibition of inducible COX-2 in the hypothalamus

Question 12

How is an anti-inflammatory affect achieved by an NSAID?

Answer 12

inhibition of inducible COX-2 at sites of inflammation

Question 13

How is an antithrobogenesis affect achieved by an NSAID?

Answer 13

inhibition of constituitive COX-1 in platelets

Question 14

Name 5 common side affects of NSAIDs.

Answer 14

1) GI ulcers, bleeding, nausea
2) increased bleeding problems
3) renal failure and nephritis
4) interference with uterine contractions
5) increased thrombotic events

Question 15

Aspirin group

Answer 15

irreversible inhibition of COX-1 AND COX-2

Question 16

traditional NSAIDs group

Answer 16

reversible inhibition of COX-1 and COX-2

Question 17

acetaminophen group

Answer 17

inhibits COX-2 in CNS ONLY

Question 18

cox-2 selective inhibitors group

Answer 18

selective reversible inhibition of COX-2 ONLY

Question 19

Name the 5 chemical classes of traditional NSAIDs.

Answer 19

1) salicylates
2) pyrazolone derivatives
3) acetic/carboxylic acids
4) oxicam derivatives
5) propionic acid derivatives

Question 20

What are salicylates used for?

Answer 20

analgesic, antipyretic, anti-inflammatory

Question 21

What are pyrazolone derivatives used for?

Answer 21

analgesic, antipyretic, anti-inflammatory

Question 22

What are acetic/carboxylic acids used for?

Answer 22

analgesic, antipyretic, anti-inflammatory

Question 23

What are oxicam derivatives used for?

Answer 23

analgesic, antipyretic, anti-inflammatory

Question 24

What are propionic acid used for?

Answer 24

analgesic, antipyretic, anti-inflammatory

Question 25

What is aspirin used for?

Answer 25

analgesic, antipyretic, anti-inflammatory, antithrombotic

Question 26

Name 2 Pyrazolone derivatives.

Answer 26

1) phenylbutazone

2) oxyphenbutazone

Question 27

Name 4 acetic/carboxylic acids.

Answer 27

1) Indomethacin
2) Sulindac
3) Ketorolac
4) Nabumetone

Question 28

Name 2 oxicam derivatives.

Answer 28

1) piroxicam

2) meloxicam

Question 29

Name 5 proprionic acid derivatives.

Answer 29

1) ibuprofen
2) naproxen
3) ketoprofen
4) flurbiprofen
5) oxaprozin

Question 30

Name one positive and one negative to pyrazolone derivative use.

Answer 30

positive: more potent and longer lasting
negative: serious toxicities with chronic use or misuse

Question 31

Name one positive and one negative to pyrazolone acetic/carboxylic acid use.

Answer 31

positive: fewer toxic rxns than pyrazolones
negative: more total adverse rxns; limited to arthritis

Question 32

Name one positive and one negative to oxicam derivative use.

Answer 32

positive: Potent, extremely long half-lives (15-50 hrs)
negative: Potent, extremely long half-lives (15-50 hrs)

Question 33

Name one positive and one negative to proprionic acid derivative use.

Answer 33

positive: better tolerated than other NSAIDs
negative: general NSAID risks

Question 34

What is acetaminophen used for?

Answer 34

Analgesic; antipyretic

Question 35

What is a positive to acetaminiophen use?

Answer 35

less GI side effects

Question 36

What is celecoxib (Celebrex) used for?

Answer 36

Analgesic, antipyretic, anti-inflammatory

Question 37

What is a positive to celecoxib (Celebrex) use?

Answer 37

less GI side effects

Question 38

Treatment of ____ pain usually requires opiod analgesics.

Answer 38

visceral

Question 39

Treatment of visceral pain usually requires _____.

Answer 39

opiod analgesics

Question 40

What is visceral pain caused by?

Answer 40

direct stimulation of sensory nerves (Aδ)

Question 41

What is the dose for anti-inflammatory NSAID affects?

Answer 41

> 4g/day

Question 42

What is the mechanism of action for the anti-platelet affect seen with NSAIDs?

Answer 42

inhibition of platelet aggregation

Question 43

Why is platelet clumping prevented for the life of the platelet?

Answer 43

platelets cannot synthesize new COX-1

Question 44

Where is the largest concentration of acetylsalicylic acid?

Answer 44

in the portal vein

Question 45

_____ is rapidly hydrolyzed to salicylate by esterases in blood.

Answer 45

Acetylsalicylic acid

Question 46

Acetylsalicylic acid is rapidly hydrolyzed to _____ by _____ in blood.

Answer 46

salicylate; esterases