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LOCO > 27 - NSAID > Flashcards

27 - NSAID Flashcards

1
Q

What is the definition of pain

A

An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage

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2
Q

Allodynia

A

Pain due to a stimulus which does not normally provoke pain

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3
Q

Hyperalgesia

A

An increased response to a stimulus which is normally painful

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4
Q

Acute pain

A

Injury due to tissue damage which will heal soon ( can be post-operative)

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5
Q

Types of chronic pain

A

Nociceptive
Neuropathic
Visceral
Mixed

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6
Q

Examples of nociceptive pain

A

Osteoarthritis and rheumatoid

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7
Q

Symptoms of nociceptive pain

A

Aching, constant
may be dull or sharp
worse with movement
well localised

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8
Q

What is Hilton’s law

A

Nerves that supply a joint capsule also supply the muscles that move that joint and the skin over the joint

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9
Q

Total value of NSAIDs and COX2s

A

35% of the market

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10
Q

WHO analgesic ladder

A

1) Non opiods, NSAIDs
2) Weak opioids
3) Strong opioids, methadone
4) Nerve block, epidural, PCA pump

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11
Q

What is the MoA for NSAIDs

A

Inhibit COX1 + COX2

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12
Q

What percentage of COX-2 has to be inhibited to be effective as an anti-inflammatory

A

80%

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13
Q

Aspirin

A

Cox-1 and COX-2 inhibitor

Anlagesic, antipyretic, anti-inflammatory

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14
Q

Ibuprofen, diclofenac, ketoprofen

A

COX 1 and COX2 inhibition + additional mechanisms

Analgesic and anti-inflammatory

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15
Q

Selective COX-2 inhibitors

A

Rofecoxib
Celecoxib
Meloxicam

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16
Q

structure of COX1 and 2

A

Hydrophobic channel with an active site

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17
Q

NSAIDs mainly for inflammation

A

Aceclofenac, etoricoxib, fenbufen, tiaprofenic acid

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18
Q

NSAIDs for inflammation and pain

A

Acematcin, celecoxib, diclofenac, ibuprofen, indomethacin, naproxen and piroxicam

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19
Q

NSAIDs mainly for pain

A

Paracoxib

20
Q

Mode of action of NSAIDs

A

Inhibit the production of prostaglandins

21
Q

How does COX help in the production of prostaglandins

A

Arachidonic acid is inserted into the hydrophobic channels in COX1 and COX2
interacts with molecular oxygen to produce pg

22
Q

What is produced from Arachidonic acid

A

Prostacyclins
Prostaglandins
Thromboxanes

23
Q

Function of prostacyclines (PGI)

A

Vasodilation, Hyperalgesia, Stops Platelet Aggregation

24
Q

Function of thromboxanes

A

Thrombotic, vasoconstrictor

25
Q

PG F2

A

Bronchoconstrictor, myometrial constriction

26
Q

PG D2

A

Inhibits platelet aggregation, vasodilator

27
Q

PG E2

A

Vasodilator, Hyperalgesic

28
Q

Difference between COX2 and COX1

A

the hydrophobic channel of cox1 is narrower and cox2 is wider and less rigid (has higher intrinsic activity)

29
Q

Where is COX-1 found and why

A

Brain, Lungs, Kidney, Stomach, Uterus, Skin

As prostaglandins are needed for normal function

30
Q

Prostaglandin receptor

A

G-protein coupled receptor

31
Q

COX2

A

Inducible by pro-inflammatory cytokines

32
Q

COX-2 in joints

A

Causes vasodilation + symptoms

nitric oxide synthase can induce

33
Q

What type of COX is in the stomach

A

COX1 isoform

34
Q

Where are the COX1s in the stomach

A

In crypts

35
Q

What is the function of COX1 in the stomach

A

To decrease the gastric acid secretion and increase the mucus secretion to protect the gut

36
Q

Where is COX2 in the stomach

A

Superficial mucosa (small amouts)

37
Q

What condition can NSAIDs lead to in the stomach

A

Ulceration as blocks the mucus and increases acid

38
Q

Aspirin in the CVS system

A

Gives long lasting protection of platelet aggregation by stopping thromboxane (which aggregates platelets)

39
Q

Which COX enzymes are present in the nervous system

A

Both however not in the same location

40
Q

Function of PG in the kidney

A

Vasodilate the afferent arteriole

41
Q

Where is COX2 present in the kidney

A

Macula densa

42
Q

What do NSAIDs do in the kidney

A

Vasoconstrict the afferent areriole and decrease GFR

43
Q

NSAIDs with Rapid competitive reversible binding of COX1/2

A

Ibuprofen

Piroxicam

44
Q

NSAIDs which Rapid lower affinity reversible binding, followed by time-dependent, high affinity slowly reversible binding of COX1/2 (gives immediate effect, comes out then goes back, slow to break down )

A

Diclofenac

Idomethacin

45
Q

NSAIDs which rapid, reversible binding followed by covalent modification of COX1 and or COX2 non-competitive irreversible

A

Aspirin

46
Q

Adverse effect of Rofecoxib

A

CVS events such as strokes

LOCO (25 decks)

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