EXAM #4: NSAIDs AND GOUT Flashcards Preview

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Flashcards in EXAM #4: NSAIDs AND GOUT Deck (39):
1

What types of chronic conditions does inflammation underlie?

Asthma
RA

2

What are the four cardinal signs of inflammation?

1) Redness
2) Swelling
3) Heat
4) Pain

3

What are the non-AA and cytokine proinflammatory mediators?

Bradykinin
Substance P
Histamine
5-HT

4

What are the arachnadonic acid proinflammatory mediators?

Prostaglandins
Thromboxanes
Prostacyclin

5

What cytokine is highly proinflammatory?

TNF-a

6

What is the primary MOA / target of the NSAIDs?

Inhibition of prostglandin production by inhibiting COX-1 and COX-2

7

Is acetaminophen an NSAID?

NO

8

What is the general function of COX-1 and 2?

Conversion of arachnadonic acid to prostaglandins (PGE2 and PGI2)

9

What is the specific function of COX-1?

"Housekeeping"
- Maintains homeostasis
- Constitutively expressed

10

What is the important function associated with COX-1 and side effects of NSAIDs?

Synthesis of PG that protect the stomach lining

11

What is the specific function of COX-2?

- Production of inflammatory molecules
- PGI2
- "inducible"

12

Where in the AA pathway do corticosteroids block?

Phospholipase A2

13

What is the MOA of aspirin?

Hydrolyzed to salicylic acid, which is a reversible COX inhibitor

14

Why is there a high potential for drug-drugs interactions with aspirin?

Binds to plasma proteins

15

What are the dose-dependent effects of ASA at a LOW dose?

- Analgesia
- Antipyretic

16

What are the dose-dependent effects of ASA at a HIGH dose?

Anti-inflammatory

17

Describe the mechanism of the anti-pyretic effects seen with ASA?

- Blocks PG in the CNS to RESET temp. in thalamus
- Dilation of BV
- Sweating
- Decrease in temperature

18

How does ASA prolong bleeding time?

COX-1 inhibition prevents thromboxane formation

19

What are the major side effects associated with ASA?

1) GI Tract upset
2) GI irritation due to a loss of GI protective PGs
3) Platelet inhibition

20

List the non-selective COX inhibitors.

ASA
Ibuprofen
Indomethacin
Ketorolac
Naproxen
Oxaprozin
Piroxicam
Sulindac

21

What is Indomethacin commonly used to treat?

1) Gout
2) Ankylosing spondylitis

22

What is the major advantage of COX-2 selective inhibitors?

Less side effects

23

What is the feared complication of COX-2 inhibitors?

Cardiovascular thrombotic events

24

List the COX-2 selective inhibitors.

Celecoxib
Etoricoxib
Meloxicam

25

What is the MOA of Acetaminophen?

Unknown

26

What is the major toxicity associated with Acetaminophen?

Hepatotoxicity

27

What is the therapeutic dose of Acetaminophen?

15mg/kg

28

What dose of Acetaminophen produces liver necrosis?

150 mg/kg

29

What dose of Acetaminophen produces liver failure?

350 mg/kg

30

What is the MOA of Capsaicin?

- Binds vanilloid receptor
- Releases substance P
- Prolonged use depletes stores of Substance P in the PNS and spinal cord

*This depletion of Substance P is analgesic*

31

What do you need to remember about prescribing NSAIDs?

No one best NSAID for everyone

32

What is Gout associated with?

Hyperuricemia

33

What is the goal of gout therapy?

Control pain and inflammation

34

What is the primary drug to treat an acute gout attack?

Indomethacin

35

What is the MOA of Colchicine?

Anti-inflammatory effects mediated by inhibiting leukocyte migration and phagocytosis

36

What are the xanthine oxidase inhibitors?

Allopurinol
Febuxostat

37

How is allopurinol used clinically?

To prevent flares i.e. given between gout attacks

38

What is the MOA of Probenecid and Sulfinpyrazone?

Inhibit tubular absorption of uric acid and increase renal clearance of uric acid

39

When is Febuxostat prescribed typically?

When the patient stops tolerating Allopurinol

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