NSAIDs Flashcards

1
Q

LO
Historical perspectives of NSAIDs
Safety considerations and withdrawal
Best practice guidelines

A
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2
Q

Where do all NSAIDs come from?

A

derived form natural products eg salicin (from willow tree bark)

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3
Q

simialar struc drug to salicin w SE GI bleeds?

A

aspirin

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4
Q

What did ibuprofen come from? drug

A

ibufenac
(had tox issues :()

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5
Q

functions of COX-1 enzymes- they are constitutive and catalyse what? and for what?

A

catalyse formation of prostaglandins for normal physiological function:

  • stomach mucus production
  • regulation of gastric acid
  • kidney water excretion
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6
Q

functions of COX-2 enzymes - they are induced and used for signalling what?

A

pain and inflammatory response:

  • stimulated by immune response
  • by inflammatory cytokines + growth factors
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7
Q

why does selectively suppressing COX2 dec chance of SEs?

A

mainly mediated through suppression of COX2

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8
Q

how can COX-1 activity be decreased/inhibited?

A

traditional NSAIDs

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9
Q

how can COX-2 activity be decreased/inhibited? 3

A

traditional NSAIDs
selective COX2 NSAIDs
Anti-inflammatory stimuli IL10

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10
Q

how can COX-2 activity be increased

A

inflammatory stimuli IL1/ IL6/ IL8/ Trauma

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11
Q

what are some examples of selective COX2 inhibitors?

A

celecoxib
(rofecoxib - withdrawn as inc CV risk, heartattack, stroke)

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12
Q

celecoxib still available but has lots of SE such as…

A

angina
cough
diarrhea
GI discomfort

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13
Q

what are some side effects of selective COX2 enzymes?/ how they cause SEs

A

inhibit vasodilation + vasodilator PGs (needed for normal GFR)

reduced GFR

increase risk of heart failure

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14
Q

what are NSAIDs with reduced GI and stomach adverse effects?
(aka COX2 preferential inhibitors)

A

meloxicam
Etodolac
nabumetone
(nimesulide)

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15
Q

COX2 preferential inhibitors indicated for what?

A

exacerbation of OA- pain and inflamm (BNF)

also inhibit osme COX1 but inc affinity for COX2

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16
Q

what main 2 types of px at risk of NSAIDs?

A

renal impairment px
HF px

17
Q

forest plot explained (p520)

A
18
Q

what is the legal legislation for oral diclofenac use?

A

associated with small increase risk of CV side effects therefore no longer under P, required POM

19
Q

diclofenac esp at high doses may be associated w what?

A

increased risk of arterial thrombotic events eg MI/ stroke

20
Q

ibuprofen has no risk at low doses up to….

A

1200mg

(so 400mg tds)

21
Q

ibuprofen >2400mg higher risk of…

A

heart attack and strokes

22
Q

limited data for SEs/ safety of ibuprofen for which doses?

A

1200mg-2400mg
below: safe
above: not safe

23
Q

what is the MHRA and NICE recommended over the counter NSAID use?

A

ibuprofen at higher doses
or ideally naproxen

24
Q

what must be prescribed if px at risk of getting GI SE form NSAIDs?

A

gastric protection!!!

25
Q

link between NSAID and COVID19?

A

no evidence of extra harm/ disease deterioration.
continue paracetamol and topical NSAIDs for localised kneww pain etc where needed

26
Q

best NSAIDs to use?

A

paracetamol or topical where possible

27
Q

avoid NSAID use in which px where possible?

A

older px.

28
Q

what to do before prescribing?

A

do full risk assessment inc gastro protection where needed

29
Q

NSAIDs SGT————————

which risk factors need to be considered before using an NSAID?

A

I.e. think about the lifestyle advice

  • Renal impairment
  • Older px
  • HF px
  • Any CV. Risk factors
  • High chance of GI AEs
30
Q

mechanism via which NSAIDs work to reduce pain?

A

NSAIDs inhibit enzyme COX: stops conversion of arachidonic acid  thromboxanes, PGs, (prostacyclins)

Selective NSAID: celecoxib: high CVD risk. Weigh up risks and benefits w px.

Lower PG, dec inflammation + pain

Majority: Non selective

31
Q

describe events leading -> MTX toxicity

A

NSAIDs excreted renally, so is MTX. Compete for same excreted pathways if NAID wins, MTX build up can accumulate very quick and toxicity can be fatal.

32
Q

MTX tox SE/ symptoms seen?

A
  • Sore throat
  • Fever
  • Cough
33
Q

What drug-drug interactions need to be considered in Rheumatoid Arthritis patients?

A

Methotrexate
NSAIDs may worsen condition