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Pharmacology > EXAM #4: NSAIDs AND GOUT > Flashcards

EXAM #4: NSAIDs AND GOUT Flashcards

1
Q

What types of chronic conditions does inflammation underlie?

A

Asthma

RA

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2
Q

What are the four cardinal signs of inflammation?

A

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

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3
Q

What are the non-AA and cytokine proinflammatory mediators?

A

Bradykinin
Substance P
Histamine
5-HT

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4
Q

What are the arachnadonic acid proinflammatory mediators?

A

Prostaglandins
Thromboxanes
Prostacyclin

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5
Q

What cytokine is highly proinflammatory?

A

TNF-a

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6
Q

What is the primary MOA / target of the NSAIDs?

A

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

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7
Q

Is acetaminophen an NSAID?

A

NO

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8
Q

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

A

Conversion of arachnadonic acid to prostaglandins (PGE2 and PGI2)

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9
Q

What is the specific function of COX-1?

A

“Housekeeping”

  • Maintains homeostasis
  • Constitutively expressed
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10
Q

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

A

Synthesis of PG that protect the stomach lining

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11
Q

What is the specific function of COX-2?

A
  • Production of inflammatory molecules
  • PGI2
  • “inducible”
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12
Q

Where in the AA pathway do corticosteroids block?

A

Phospholipase A2

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13
Q

What is the MOA of aspirin?

A

Hydrolyzed to salicylic acid, which is a reversible COX inhibitor

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14
Q

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

A

Binds to plasma proteins

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15
Q

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

A
  • Analgesia

- Antipyretic

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16
Q

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

A

Anti-inflammatory

17
Q

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

A
  • Blocks PG in the CNS to RESET temp. in thalamus
  • Dilation of BV
  • Sweating
  • Decrease in temperature
18
Q

How does ASA prolong bleeding time?

A

COX-1 inhibition prevents thromboxane formation

19
Q

What are the major side effects associated with ASA?

A

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

20
Q

List the non-selective COX inhibitors.

A 
ASA 
Ibuprofen
Indomethacin 
Ketorolac
Naproxen 
Oxaprozin
Piroxicam
Sulindac
21
Q

What is Indomethacin commonly used to treat?

A

1) Gout

2) Ankylosing spondylitis

22
Q

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

A

Less side effects

23
Q

What is the feared complication of COX-2 inhibitors?

A

Cardiovascular thrombotic events

24
Q

List the COX-2 selective inhibitors.

A

Celecoxib
Etoricoxib
Meloxicam

25
Q

What is the MOA of Acetaminophen?

A

Unknown

26
Q

What is the major toxicity associated with Acetaminophen?

A

Hepatotoxicity

27
Q

What is the therapeutic dose of Acetaminophen?

A

15mg/kg

28
Q

What dose of Acetaminophen produces liver necrosis?

A

150 mg/kg

29
Q

What dose of Acetaminophen produces liver failure?

A

350 mg/kg

30
Q

What is the MOA of Capsaicin?

A
  • 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
Q

What do you need to remember about prescribing NSAIDs?

A

No one best NSAID for everyone

32
Q

What is Gout associated with?

A

Hyperuricemia

33
Q

What is the goal of gout therapy?

A

Control pain and inflammation

34
Q

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

A

Indomethacin

35
Q

What is the MOA of Colchicine?

A

Anti-inflammatory effects mediated by inhibiting leukocyte migration and phagocytosis

36
Q

What are the xanthine oxidase inhibitors?

A

Allopurinol

Febuxostat

37
Q

How is allopurinol used clinically?

A

To prevent flares i.e. given between gout attacks

38
Q

What is the MOA of Probenecid and Sulfinpyrazone?

A

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

39
Q

When is Febuxostat prescribed typically?

A

When the patient stops tolerating Allopurinol

Pharmacology (64 decks)

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