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Disease & Defense > LEC 26 Inflammation and NSAIDs > Flashcards

LEC 26 Inflammation and NSAIDs Flashcards

1
Q

What characterizes an inflammatory response?

A
  • Transient local vasodilation
  • Increased capillary permeability
  • Infiltration of leukocytes and phagocytes
  • Resolution with or without tissue degeneration and fibrosis
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2
Q

What are the prostanoids involved in an inflammatory response?

A
  • Prostaglandin E2 (PGE2)
  • Prostacyclin I2 (PGI2)
  • Thromboxane A2 (TxA2)
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3
Q

Which two prostanoids are important for leukocyte attraction and adhesion to endothelial cells at a site of injury?

A
  • PGE2
  • TxA2
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4
Q

What effect to prostaglandins have on nocireceptors?

A

Prostaglandins increase the sensitivity of nocireceptors causing peripheral sensitization

Reveral of this is thought to be MOA of NSAIDs

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5
Q

Which prostanoid contributes to central sensitization?

A

PGE2

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6
Q

What part of the brain regulates body temperature?

A

Hypothalamus

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7
Q

How are fevers mediated?

A
  • COX-2 generation of PGE2
  • PGE2 crosses blood-brain barrier resulting in elevated body temp

NSAIDs inhibit COX-2 dependent PGE2 synthesis

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8
Q

How do NSAIDs work?

A

Inhibition of cyclooxygenase

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9
Q

Inhibition of COX-1 results in what?

A
  • decreased platelet fxn
  • removes gastric protection
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10
Q

Inhibition of COX-2 results in what?

A
  • antipyretic
  • analgesic and anti-inflammatory actions
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11
Q

Most NSAIDs are what kind of inhibitors of COX?

A

competitive, noncompetitive, or mixed REVERSIBLE

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12
Q

Aspirin is what kind of inhibitor of COX?

A

non-competitive, irreversible

Acetylates the isozyme in the AA-binding channel

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13
Q

What are the negative effects of COX-1 selective blockers?

A

GI toxicity

Ulcers, GI bleeds, stomach upset

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14
Q

What are the negative effects of COX-2 selective blockers?

A

Cardiovascular side effects

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15
Q

What is the common suffix for COX-2 selective inhibitors?

A

-coxib

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16
Q

What is the function of COX-1 normally?

A
  • cytoprotective for gastric epithelial cells
  • forms TXA2 in platelets and cause platelet activation and constriction of injured vessels

Largely accounts for gastric side effects via PGE2

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17
Q

What is the function of COX-2 normally?

A
  • BP regulation and inhibitors of hemostasis
  • Inhibition of COX-2 alone can cause HTN and an increase in thrombotic events
18
Q

What is aspirin’s MOA?

A
  • Acetylates serine 529 subunits of both COX 1 & 2 blocking AA
  • inhibition occurs in the endothelial cells and platelets
  • Endothelial cells can make new COX enzymes but platelets cannot (permenant inactivity for lifetime of platelet, 8-12 days)
19
Q

How long after taking aspirin is enough for a partial platelet pool recovery for a simple surgery?

A

3 Days

20
Q

Why is it important that synovial concentrations of NSAIDs are about half of the plasma concentration?

A

Makes NSAIDs effective for arthritis pain

21
Q

Where are NSAIDs metabolized?

A

Liver then renal exretion

22
Q

In the plasma, 95-99% of NSAIDs are found bound to what?

A

Plasma proteins like albumin

23
Q

Why are NSAIDs not removed by hemodialysis?

A

d/t high protein binding in the plasma

24
Q

What is the dose of a baby aspirin?

A

81 mg

25
Q

What are PGE2’s GI functions?

A
  1. Inhibit acid secretion
  2. Enhance mucosal blood flow
  3. Promote secretion of cytoprotective mucus in the intestine
26
Q

What are the adverse effects of selective COX-2 inhibitors?

A
  • Inhibit fxn of PGI2
  • PGI2 inibits platelet aggregation & the prothrombotic effects of TXA2
  • They do not inhibit TXA2 prodxn (COX-1)
  • TXA2 is unopposed (by PGI2) and results in prodxn of new platelets and increased platelet aggregation
  • INCREASED MIs AND STROKES
27
Q

What effect do PGE2 and PGI2 have on the kidney?

A
  • They are vasodilators of the afferent arteriole on each glomeruli
  • This dilation is needed to maintain normal kidney perfusion especially in: Dehydration, Hypovolemia, CHF, Liver cirrhosis, and CKD

Unopposed constriction results in decreased perfussion and GFR

28
Q

Why do you not give aspirin to pts under 20 y/o?

A

They can get Reye syndrome

acute encephalopathy, hepatomegaly, liver dysfunction, fatty liver

29
Q

What is the half-life of aspirin?

A

2-3 hours

30
Q

What is the half-life of diflunisal?

A

8-12 hours

31
Q

How are the effects of diflunisal different from aspirin?

A
  • 4-5x more potent analgesic/anti-inflammatory
  • weaker antipyretic
  • fewer platelet and GI side effects
32
Q

Which salicylate is not effective orally?

A

Mesalamine

given as an enema or suppository for ulcerative colitis

33
Q

What is the use of Indomethacin?

A

used to treat patent ductus arteriosis - successful closure in >70% of neonates

Has many adverse effects and is not a 1st line NSAID

33
Q

What adverse effects are associated with ketorolac?

A
  • high risk of renal dysfunction - max use of 5 days
  • Steven Johnson syndrome
  • gastric ulceration

PO & IM use; Potent analgesic but mod anti-inflam

33
Q

What do you combine with Diclofenac to prevent ulcers?

A

Misoprostol

34
Q

What is the advantage of naproxen over ibuprofen?

A

Naproxen has a longer half life allowing for BID dosing

35
Q

What is the only selective COX-2 inhibitor still on the market in the US?

A

Celecoxib

36
Q

What is the dosage limit for acetaminophen?

A

4 grams in 24 hours

37
Q

What is the dosage limit for elderly people for acetaminophen?

A

2 grams in 24 hours

38
Q

How many grams of acetaminophen to cause hepatotoxicity? to cause death?

A

Hepatotoxicity: 10-15 g
Death: >25 g

39
Q

How do you treat acetaminophen overdose?

A
  • Activated charcoal if it is still in the stomach
  • N-acetylcystine IV for glutathione repletion

Disease & Defense (37 decks)

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