NSAIDs Flashcards

1
Q

Hilton’s law

A

The nerve supplying a joint also supplies the muscles that move the joint, the skin over the joint, and the insertion of the muscles

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2
Q

Characteristics of somatic pain

A

Aching
Often constant
Dull or sharp
Worse with movement
Well localised unless deep

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3
Q

4 steps on the WHO analgesic ladder

A

Nonopioids
Weak opioids
Strong opioids
Nerve block/epidural/PCA pump/spinal stimulators

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4
Q

Which type of pain goes up the WHO analgesics ladder and which type goes down

A

Acute goes down
Chronic and cancer goes up

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5
Q

NSAID MOA

A

Inhibition of COX enzymes preventing prostaglandin formation

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6
Q

Which NSAIDS inhibit COX1 and COX2

A

Aspirin
Ibuprofen
Diclofenac
Ketoprofen

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7
Q

Which NSAIDS are selective COX2 inhibitors

A

Rofecoxib
Celecoxib
Etoricoxib
Meloxicam
MERC

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8
Q

How does the MOA of aspirin differ from those of ibuprofen diclofenac and ketoprofen

A

All inhibit COX 1+2
Ibuprofen, diclofenac, and ketoprofen also have additional mechanisms

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9
Q

Effects of aspirin

A

Analgesic
Antipyretic
Anti inflammatory

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10
Q

Effects of ibuprofen diclofenac and ketoprofen

A

Analgesic
Anti inflammatory

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11
Q

Most prescribed NSAID in UK

A

Naproxen

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12
Q

Function of COX enzymes

A

Catalyse formation of prostaglandins from Arachidonic acid

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13
Q

3 classes of prostaglandins

A

Prostaglandins D E and F
Prostacyclin
Thromboxane A

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14
Q

What type of molecule are prostaglandins

A

Tissue hormones

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15
Q

How far do prostaglandins travel from site of production to site of action

A

Work on cells within tissue that produced them
Don’t diffuse far

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16
Q

PGE2 actions

A

Vasodilation of renal art
Suppress lymphocytes
Sensitises peripheral nerve endings
Inhibits gastric acid secretion
Fever
Uterine relaxation

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17
Q

PGD2 actions

A

Vasodilation
Bronchoconstriction

18
Q

PGI2 action

A

Vasodilation of renal artery
Inhibits platelet aggregation
Bronchodilation
Inhibit gastric secretion
Sensitise afferent nerve endings to pain

19
Q

PGF alpha actions

A

Vasoconstriction + dilation
Bronchoconstriction
Uterine contraction

20
Q

TXA2 actions

A

Vasoconstriction
Induce platelet aggregation
Bronchoconstriction
Uterine contraction

21
Q

How many types of prostaglandin receptor are there and what receptor type are they

A

9
G protein coupled receptor

22
Q

Which COX enzyme is physiologic and which is inducible

A

COX1 physiologic
COX2 inducible

23
Q

What enzyme catalyses the conversion of cell membrane phospholipids to arachadonic acid

A

Phospholipase A2

24
Q

What conditions increase COX2 in joints

A

OA
RA

25
Q

What molecules cause COX2 increase in joints effected by OA and RA

A

IL1, TNF, IL17 -> stim iNOS -> induces COX2

26
Q

Production of Which prostaglandin in joints can be directly activated by mechanical stress

A

PGE2

27
Q

Which COX isoforms is predominant in the stomach

A

COX1

28
Q

Where is COX1 and COX2 found in the stomach

A

1 - in crypts
2 - superficial mucosa

29
Q

How is COX1 beneficial in the stomach

A

Produces PGE2 which protects gastric mucosa

30
Q

Why are long term NSAIDs harmful to the stomach

A

Long term COX1 inhibition blocks PGE2 production leading to gastritis and gastric ulcers

31
Q

Why are NSAIDs given as GI preparations

A

Decrease risk of gastric ulcers

32
Q

Effects of PGE2 on gastric mucosa

A

Incr mucus secretion
Incr cell regeneration
Incr HCO3 release
Incr blood flow
Decr H+ secretion

33
Q

Effects of PGI2/prostacyclin and thromboxane A2 on the cardiovascular system

A

PGI2 vasodilation, prevents platelet aggregation
Thromboxane A2 vasoconstriction, promotes platelet aggregation

34
Q

Where is COX1 and COX2 found in the cardiovascular system

A

COX1 - platelets
COX2 - endothelium

35
Q

What type of spinal cord transmission is COX2 important in

A

Nocioceptive

36
Q

What increases COX2 in the kidney

A

Salt deprivation

37
Q

Protective effects of PGE2 and PGI2 in the kidney

A

PGE2 regulates Na reabsorption
PGI2 incr K secretion by stimulating renin
Vasodilation

38
Q

Which COX enzyme is more harmful

A

COX2

39
Q

What drug type has the suffix -coxib

A

Selective COX2 inhibitor

40
Q

What adverse effect is associated with rofecoxib diclofenac celecoxib and high dose ibuprofen

A

Increased cardiovascular risk

41
Q

Is GI risk higher in selective COX2 inhibitors or non selective NSAIDs

A

Non Selective NSAIDs

42
Q

How many COX enzymes do humans have

A

COX1
COX2
COX3 - non functional