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262B Pharmacology > L10 - NSAIDs > Flashcards

L10 - NSAIDs Flashcards

1
Q

What is the COX enzyme substrate and products?

A

substrate: arichidonic acid
products: thromboxane, prostaglandins, prostacyclins

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2
Q

How do NSAIDs work?

A

they inhibit COX to cause a reduction in the mediators produced by it (thromboxane, prostaglandins, prostacyclins)

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3
Q

Where is COX1 found and what function is it involved in?

A
  • expressed in almost all cells
  • involved in PGE1, PGE2 and PGI2 production in the stomach which is involved in the mucous layer which protects the stomach lining from the acidic contents of the stomach
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4
Q

What roles do PGE2 and PGI2 have? How are they produced and where?

A
  • produced by COX1 enzyme which is found in most cells

- have a gastroprotective role by stimulating mucosal secretion and inhibiting gastric acid production

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5
Q

Why do NSAIDs produce GI side effects?

A

Because the NSAID drugs that inhibit COX1 enzyme reduce the mucous layer of the stomach which results in ulcerations or perforations for example

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6
Q

What NSAIDs non-selectively inhibit COX enzyme? i.e. inhibit COX1 and COX2

A
  • aspirin
  • paracetamol
  • ibuprofen
  • diclofenac
  • indomethacin
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7
Q

What is the NSAID that selectively inhibits COX2 enzyme? What are the associated risks and who is prescribed to use them?

A
  • celecoxib (Celebrex)
  • it increases the risk of heart attack so currently only prescribed to patients with GI side effects with NSAIDs and whose cardiovascular risk has been assessed
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8
Q

What is a feature of aspirin that makes it different from other NSAIDs?

A
  • it irreversibly binds via covalent bonding which means it has cumulative effects
  • it irreversibly binds to TXA2 which causes reduced rate of blood clot formation
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9
Q

What are the common adverse side effects of aspirin?

A
  • GIT effects incl. nausea and vomiting
  • microscopic bleeding
  • increased bleeding time
  • allergies
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10
Q

Aspirin has opposite effects in two different parts of the clotting process. Explain why and how dosing affects the effect.

A
  • in the portal circulation, aspirin affects TXA2 which normally causes platelet aggregation so has the effect of inhibiting platelet aggregation.
  • in the vascular endothelium aspirin affects PGI2 which normally inhibits platelet aggregation so has the effect of increased platelet aggregation
  • low dose affects the portal circulation more resulting in overall effect of reduced platelet aggregation
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11
Q

What effect does indomethacin have?

A

it is a potent anti-inflammatory agent

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12
Q

What effect does ibuprofen have?

A

anti-inflammatory and analgesic

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13
Q

What effect does diclofenac have?

A

analgesic treatment for inflammatory pain

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14
Q

What effects does paracetamol have?

A

analgesic and anti-pyretic, no anti-inflammatory

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15
Q

What is a feature about indomethacin?

A

more selective for COX1 so associated with more adverse side effects

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16
Q

What are the adverse effects of indomethacin?

A

GI upset, impaired renal function

17
Q

What is a feature of ibuprofen?

A

safest NSAID with fewer side effects but weaker anti-inflammatory properties compared to other NSAIDs

18
Q

What are the common side effects of ibuprofen?

A

GI disturbances

19
Q

What are 2 features of diclofenac?

A
  • more potent than indomethacin

- powerful analgesic systemically but achieve targeted effects when used locally as gel

20
Q

What are the side effects of diclofenac?

A

GI upset and headaches

21
Q

What are 4 features of paracetamol?

A
  • well absorbed when given orally
  • peak plasma after 30-60 min
  • health life 2-4 hours at therapeutic doses
  • narrow therapeutic range as toxic dose 2-3X max therapeutic dose causing hepatotoxicity
22
Q

What are the adverse effects of paracetamol?

A

adverse effects are uncommon at therapeutic doses, no GI effects, liver toxicity if regular high intake for a long time

23
Q

What are the adverse effects associated with NSAIDs?

A
  • GI
  • renal
  • headaches
  • dizziness
  • skin reactions
24
Q

What are is the effect of celecoxib (Celebrex)?

A

it has a high therapeutic potential for inflammatory conditions

262B Pharmacology (18 decks)

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