Lecture 12: NSAIDs/Aspirin Flashcards

1
Q

ASA: mechanism

A

IRREVERSIBLY inhibits COX-1 and COX-2 = NON-SELECTIVE COX INHIBITOR

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2
Q

Antiplatelet effect of aspirin lasts…(DAYS)

A

8 to 10 days (once they’ve lost their COX they’ve lost them forever)

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3
Q

ASA: clinical indication –> antiplatelet (mechanism)

A

PGE2 and TXA2 enhances pla aggregation –> MI (acute and prophylactically), unstable angina, CVA, TIA

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4
Q

ASA: clinical indication –> anti-inflammatory (mechanism)

A

PGE2 and PGI2 increase vascular permeability & leukocyte infiltration

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5
Q

ASA: clinical indication –> analgesic (mechanism)

A

PGE2, PGI2 in PNS and PGE2 in CNS increase neuron membrane excitability/pain sensitization

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6
Q

ASA: clinical indication –> anti-pyretic (mechanism)

A

PGE2, PGF2alpha, PGI2 increase body temperature

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7
Q

ASA: 4 clinical indications (summary)

A

Antiplatelet, anti-inflammatory, analgesic, anti-pyretic

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8
Q

ASA: adverse Effects

A

GI: pain, N/V, ulcer; Heme: bleeding; Respiratory: brochospasm; Renal: increased creatinine and acid/base disorders; CV: HTN, fluid retention

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9
Q

ASA: adverse Effects –> explain GI

A

PGE2 decreases stomach acid and increases mucus

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10
Q

ASA: adverse Effects –> explain creatinine

A

PGE2 and PGI2 cause afferent arteriole vasodilation and increased renin –> both increase GFR, so inhibition DECREASES GFR and INCREASES creatinine

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11
Q

COX inhibitors and blood pressure (increase/decrease)

A

INCREASE

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12
Q

Other adverse effects of aspirin

A

Tinnitus (effect on cochlear hair cells), rash, Reye’s syndrome

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13
Q

Describe Reye’s syndrome

A

Acute onset encephalopathy, liver dysfunction, fatty infiltration of liver and other organs

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14
Q

Because of Reye’s, aspirin is contraindicated in…

A

Individuals under 20 years of age who have a fever

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15
Q

Describe aspirin hypersensitivity

A

Anapylactic response with rhinitis, angioedema, urticaria, bronchospasm, nasal polyposis

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16
Q

Samter’s triad

A
  1. Aspirin sensitivity, 2. Asthma, 3. Nasal polyps
17
Q

How to treat aspirin overdose

A

Urine alkalinization to increase excretion of ionised salicylate

18
Q

Aspirin and dialysis

A

Aspirin is highly protein bound AND widely distributed, so dialysis will not remove medicine from the body

19
Q

Aspirin is metabolized __________ but excreted __________

A

Hepatically and renally

20
Q

Why does aspirin’s half life increase in overdose?

A

Conjugation enzyme becomes saturated

21
Q

ASA: overdose sx

A

Hearing issues: cochlear hair cells; decreased vision/headache; N/V; bleeding; fever (uncoupling of oxidative phosphorylation –> heat release)

22
Q

ASA: overdose –> acid base derangements (3)

A

ASA stimulates resp medullary drive center –> respiratory alkalosis; uncoupling of oxidative phosphorylation results in lactic acid –> metabolic acidosis , late stage intoxication results in decreased mental status –> respiratory acidosis

23
Q

T/F: ASA overdose can cause death

A

True

24
Q

Ibuprofen: mechanism

A

REVERSIBLE non-selective COX inhibitor

25
Q

Ibuprofen: clinical indications (4)

A

Anti-inflammatory, analgesic, anti-pyretic, antiplatelet (but not used for this purpose)

26
Q

Ibuprofen: adverse effects

A

GI (pain, N/V, ulcer), heme (bleeding), renal (increased creatinine), CV (HTN, edema), allergy (angioedema, rash)

27
Q

Ibuprofen: BP

A

Increases

28
Q

Celecoxib: mechanism

A

SELECTIVE COX-2 inhibitor

29
Q

Celecoxib: clinical indications (3). What’s missing?

A

Anti-inflammatory, analgesic, anti-pyretic; NO ANTIPLATELET BECAUSE THIS IS MEDIATED BY COX-1

30
Q

Celecoxib: adverse effects

A

GI (fewer, 1/2 as many ulcers), respiratory (fewer bronchospasm), renal (increased creatinine), CV (HTN, edema, MYOCARDIAL INFARCTION, allergy (angioedema, rash)

31
Q

Celecoxib: BP

A

Increases

32
Q

Acetaminophen: mechanism

A

WEAK COX-1 and COX-2 inhibitor with poorly understood mechanisms

33
Q

Acetaminophen: clinical indications (2). What’s missing?

A

Analgesic, anti-pyretic; NO ANTIPLATELET OR ANTI-INFLAMMATORY ACTIVITY

34
Q

Acetaminophen: adverse effects, contraindications

A

Severe, fatal hepatotoxicity, renal failure (acute tubular necrosis)

35
Q

What AE is NOT seen with acetaminophen?

A

GI bleeds