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LOCO > 27 - NSAID > Flashcards

27 - NSAID Flashcards

(46 cards)

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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

20
Q

Mode of action of NSAIDs

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A

Inhibit the production of prostaglandins

21
Q

How does COX help in the production of prostaglandins

Study These Flashcards
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

Study These Flashcards
A

Prostacyclins
Prostaglandins
Thromboxanes

23
Q

Function of prostacyclines (PGI)

Study These Flashcards
A

Vasodilation, Hyperalgesia, Stops Platelet Aggregation

24
Q

Function of thromboxanes

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A

Thrombotic, vasoconstrictor

25
PG F2
Bronchoconstrictor, myometrial constriction
26
PG D2
Inhibits platelet aggregation, vasodilator
27
PG E2
Vasodilator, Hyperalgesic
28
Difference between COX2 and COX1
the hydrophobic channel of cox1 is narrower and cox2 is wider and less rigid (has higher intrinsic activity)
29
Where is COX-1 found and why
Brain, Lungs, Kidney, Stomach, Uterus, Skin | As prostaglandins are needed for normal function
30
Prostaglandin receptor
G-protein coupled receptor
31
COX2
Inducible by pro-inflammatory cytokines
32
COX-2 in joints
Causes vasodilation + symptoms | nitric oxide synthase can induce
33
What type of COX is in the stomach
COX1 isoform
34
Where are the COX1s in the stomach
In crypts
35
What is the function of COX1 in the stomach
To decrease the gastric acid secretion and increase the mucus secretion to protect the gut
36
Where is COX2 in the stomach
Superficial mucosa (small amouts)
37
What condition can NSAIDs lead to in the stomach
Ulceration as blocks the mucus and increases acid
38
Aspirin in the CVS system
Gives long lasting protection of platelet aggregation by stopping thromboxane (which aggregates platelets)
39
Which COX enzymes are present in the nervous system
Both however not in the same location
40
Function of PG in the kidney
Vasodilate the afferent arteriole
41
Where is COX2 present in the kidney
Macula densa
42
What do NSAIDs do in the kidney
Vasoconstrict the afferent areriole and decrease GFR
43
NSAIDs with Rapid competitive reversible binding of COX1/2
Ibuprofen | Piroxicam
44
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 )
Diclofenac | Idomethacin
45
NSAIDs which rapid, reversible binding followed by covalent modification of COX1 and or COX2 non-competitive irreversible
Aspirin
46
Adverse effect of Rofecoxib
CVS events such as strokes

LOCO (25 decks)

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