NSAIDs Flashcards

1
Q

This enzyme is responsible for the production of arachidonic acid (precursor to prostaglandins)

A

phospholipase A2

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2
Q

COX2 is generally inducible, but constitutively active in the following tissues:

A

kidney, female reproductive tract, and CNS

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3
Q

What enzymes convert PGH2 into biologically active prostanoids?

A

tissue-specific isomerases

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4
Q

effects of PGI2 (aka prostacyclin)

A

Inhibition of platelet aggregation, vasodilation, renin release (autoregulatory), natriuresis

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5
Q

effects of TXA2 (thromboxane)

A

vasoconstriction and promotion of platelet aggregation

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6
Q

Effects of PGE2 (‘classical’ prostaglandin’)

A

causes pain (via sensitisation of nociception neurons) and fever (through the hypothalamus), increases vascular permeability, + gastric effects (inhibits stomach acid secretion and promotes gastric cytoprotection, which is why NSAIDs that inhibit PGE2 can cause upset stomach)

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7
Q

Effects of PGF2alpha

A

uterine contraction, vaso- and bronchoconstriction

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8
Q

Effects of PGD2

A

same as PGI2 (vasodilation, bronchoconstriction, inhibition of platelet aggregation), except without the increased renin production

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9
Q

This NSAID irreversibly acetylates COX at Ser529, inhibiting prostanoid production

A

aspirin. All other NSAIDs function reversibly.

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10
Q

Why does aspirin function as an anti-platelet blood-thinning drug?

A

Its effect on platelets persists throughout their life, while endothelial cells which produce PGI2 can regenerate COX

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11
Q

Which drug causes Reye’s syndrome following viral infection in pediatrics?

A

aspirin

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12
Q

What is the treatment for hepatotoxicity caused by paracetamol + alcohol abuse?

A

N-acetyl cysteine (NAC) to replenish glutathione

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13
Q

Adverse effects of NSAIDs

A

-gastric upset due to lowered PGE2 levels
-Idiosyncratic pseudoallergic response (MRGPRX2-mediated)
-bleeding on aspirin
-aspirin-induced asthma (arachidonic acid is redirected to LOX –> leukotriene production)
-chronic (type C ADR) kidney defects

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14
Q

This is a COX2-selective inhibitor

A

celecoxib

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15
Q

These are NSAIDs apart from aspirin

A

paracetamol, ibuprofen, naproxen

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