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Pharmacology > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

What compounds do NSAIDs work on?

A

COX-1

COX-2

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2
Q

What is the action of the COX enzymes?

A

Convert arachidonic acid to proteinoids

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3
Q

Where is COX-1 found?

A

Most tissues

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4
Q

Where is COX-2 found?

A

Active tissues

Inflamed tissues

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5
Q

What are the homeostatic functions of COX-1?

A

GI protection (acid + mucus)
Platelet aggregation
Vascular resistance
Renal blood flow

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6
Q

What are the homeostatic functions of COX-2?

A

Renal homeostasis
Tissue repair + healing
Reproduction (uterine contractions)
Inhibition of platelet aggregation

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7
Q

What are the pathological functions of COX-1?

A

Chronic inflammation
Chronic pain
Raised blood pressure

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8
Q

What are the pathological functions of COX-2?

A

Chronic inflammation
Chronic pain
Fever
Blood vessel permeability

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9
Q

What are the prostanoids?

A 
PGE2
PGE2α
PGD2
PGI2
TXA2
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10
Q

What is PGI2 also known as?

A

Prostacyclin

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11
Q

What is TXA2 also known as?

A

Thromboxane

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12
Q

What is the action of NSAIDs?

A

Competitive inhibition of COX enzymes -> reduction of prostanoid synthesis

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13
Q

What are the analgesic effects of NSAIDs?

A

Reduced PGE2 synthesis in dorsal horn
Reduced neurotransmitter release
Reduced excitability of neurones in pain relay

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14
Q

What are the anti-inflammatory effects of NSAIDs?

A

Reduction in prostaglandin synthesis
Decreased vasodilation
Decreased swelling

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15
Q

What are the antipyretic effects of NSAIDs?

A

Inhibition of hypothalamic COX-2

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16
Q

What is the order of selectivity? (COX-1 -> COX-2)

A 
Aspirin 
Ibuprofen 
Naproxen 
Diclofenac
Celecoxib
Parecoxib
Etoricoxib
17
Q

What are the GI side effects of NSAIDs?

A

Decrease mucuc + HCO3
Increase acid secretion
Decrease mucosal blood flow

Nausea
Peptic ulceration
Exacerbate IBD

18
Q

What are the renal side effects of NSAIDs?

A 
Reduce GFR
Increase creatinine 
Reduce renal medullary blood flow 
Increase salt + water retention 
Decrease renin secretion

Oedema
Hypertension
Hyperkalaemia

19
Q

What are the CVS side effects of NSAIDs?

A

Increase salt + water retention
Vasoconstriction

Exacerbate HF

20
Q

When are NSAIDs contraindicated?

A

Drugs

  • sulphonylurea
  • methotrexate
  • warfarin

RA

Children <12 = Reye’s syndrome

21
Q

What is paracetamol?

A

Non-NSAID, non opiate analgesic

22
Q

What is the indication for paracetamol?

A

Mild to moderate pain

Fever

23
Q

What is the mechanism of paracetamol?

A

COX-2 selective inhibition in spinal cord

24
Q

What is NAPQI?

A

N-acetyl-p-benzoquinone imine

Minor oxidation product of paracetamol

25
Q

What is used in paracetamol overdose?

A

Acetyl-cysteine - glutathione thiol replacement

Pharmacology (27 decks)

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