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Sys Pharm Bones and Joints > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

NSAIDs types?

A
  1. Non-selective
  2. COX-2 Inhibitors
  3. Paracetamol
    (ACETAMINOPHEN)
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2
Q

Non-selective NSAIDs drugs?

A
  1. Aspirin
  2. Naproxen
  3. Indomethacin
  4. Diclofenac
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3
Q

Aspirin effects?

A

Anti-inflammatory
Analgesic
Antipyretic
Antiplatelet

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4
Q

Aspirin anti-inflammatory effect mechanism?

A
  • ↓ vasodilation

* ↓ increase in vascular permeability

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5
Q

Aspirin Analgesic effect mechanism?

A

• ↓ sensitization of nociceptive fibres to stim by inflammatory mediators
o Analgesic ceiling – does not block direct nociceptive activation

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6
Q

Aspirin Antipyretic effect mechanism?

A

• Act on hypothalamus & reset thermostat

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7
Q

Aspirin Antiplatelet effect mechanism?

A

• Block TXA2 (platelet agg) > Block PGI2 (platelet inhibition)

o Blocks both but PGI2 restored faster by new COX
synthesis

o TXA2 restored only by new platelet formation

o Low dose aspirin à useful as a blood thinner

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8
Q

Aspirin Side effects?

A

• Not to be prescribed to

children with viral infections –> Reye’s syndrome (rare but life-threatening)

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9
Q

What happens in Reye’s syndrome?

A 
o Encephalitis
o Liver swelling
o Vomiting
o Delirium
o Convulsions
o Loss of consciousness
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10
Q

Naproxen plasma half life?

A

Long T ½ (12-24h)

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11
Q

Naproxen uses?

A

Dysmenorrhea – more effective in women

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12
Q

Indomethacin uses?

A
  • Strong anti-inflammatory

* Steroid-like ↓ PLA2

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13
Q

Indomethacin Side effects?

A

• CNS: confusion, depression, psychosis

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14
Q

Diclofenac plasma half life?

A

Short T ½ (<2hrs)

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15
Q

Diclofenac uses?

A
  • Less GI risk due to short T ½

* But longer T ½ in synovial fluid

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16
Q

GIT Side Effects of NSAIDs?

A
  • Dyspepsia
  • Nausea, vomiting
  • Ulcer
17
Q

GIT Side Effects of NSAIDs mechanism?

A

Prostaglandins have a protective function to ↓ acid, ↑ bicarbonate & mucus

18
Q

Renal Side Effects of NSAIDs?

A
  • Edema
  • Hypertension
  • Hyperkalemia
  • Acute renal failure
19
Q

Renal Side Effects of NSAIDs:
• Edema
• Hypertension

Mechanism?

A
  • ↓ PGE2 (inhibits reabs)

* ↑ Na+ and water reabs at TAL

20
Q

Renal Side Effects of NSAIDs:
• Hyperkalemia
• Acute renal failure

Mechanism?

A
  • ↓ PGI2 (which stim RAAS)

* Suppression of renin and aldosterone secretion

21
Q

Pseudo-allergic Side Effects of NSAIDs?

A
  • Rash
  • Itch
  • Nasal congestion
  • Anaphylaxis
22
Q

Asthma Side Effects of NSAIDs?

A

• Bronchospasm in susceptible (excess

leukotrienes)

23
Q

Pseudo-allergic and Asthma Side Effects of NSAIDs Mechanism?

A
  • Inhibition of arachidonic acid à prostaglandins

* Shunt arachidonic acid to produce leukotrienes

24
Q

Bleeding Side Effects of NSAIDs?

A
  • Bruising

* Bleeding

25
Q

Bleeding Side Effects of NSAIDs mechanism?

A

Due to antiplatelet activity

26
Q

NSAIDs contraindications?

A

Avoid NSAIDs in 3rd trimester of pregnancy:

May cause premature closure of ductus arteriosus

27
Q

COX-2 Inhibitors drugs?

A

Coxibs eg. Celecoxib

28
Q

COX-2 Inhibitors Mechanism of Action?

A

• Selective inhibition of COX-
2 (inducible) reduces GIT side effects

• Mainly anti-inflammatory, analgesic

29
Q

COX-2 Inhibitors Side Effects?

A
  1. Avoid in late pregnancy (3rd trimester)
  2. Renal toxicity
  3. Effects on ovulation
  4. GIT sparing incomplete
  5. Increase risk of thrombosis
30
Q

Why avoid cox-2 inhibitors in late pregnancy (3rd trimester)?

A

o Premature closure of ductus arteriosus

31
Q

Why do cox2 inhibitors cause Renal toxicity?

A

o Due to COX-2 in kidney

32
Q

How do cox2 inhibitors cause effects on ovulation?

A

o Delayed follicular rupture

33
Q

Why is GIT sparing incomplete due to cox2 inhibitors?

A

o Due to impairment of wound healing

34
Q

Significance of cox2 inhibitors causing increased risk of thrombosis?

A

o ↑ CVS death

  • COX2 produces prostacyclin (inhibits clotting) but not TXA2 (promotes clotting)
  • COX2 block > shunt more arachidonic acid to COX1 > produce more TXA2 > prostacyclin
35
Q

Paracetamol mechanism of action?

A

• CNS-selective COX inhibitor. May
also involve serotonin relays or
receptors

36
Q

Paracetamol uses?

A
  • Good analgesic
  • Potent antipyretic
  • Spares the GIT
  • Safe for children with few side effects
  • (not potent as anti-inflammatory)
37
Q

Paracetamol Side Effects?

A

• Liver damage
o Exacerbated by chronic alcohol use
o Should not occur at therapeutic doses
in healthy individuals

  • Allergy
  • Nausea/vomiting

Sys Pharm Bones and Joints (2 decks)

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