Lecture 12/ 13 Flashcards

Anti-inflammatories

1
Q

Acetylsalicylic acid

A

ASA, Derivative of salicylic acid by adding ester, better tolerated

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2
Q

NSAIDs action

A

Inhibit production of certain inflammatory mediators

Decrease prostaglandins and thromboxane production

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3
Q

PGI2

A

Vasodilator, hyperalgesia, stops platelet aggregation

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4
Q

TXA2

A

thrombotic, vasoconstrictor

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5
Q

PGF2X

A

Bronchoconstrictor, myometrial contraction

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6
Q

PGD2

A

Inhibits platelet aggregation, vasodilation

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7
Q

PGE2

A

Vasodilator, hyperalgesic

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8
Q

LTC4, LTD4 and LTE4

A

Bronchoconstrictors, increase vascular permeability

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9
Q

PAF

A

Vasodilator, increases vascular permeability, bronchoconstrictor, chemotoxin

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10
Q

Cyclo-oxygenases

A

The second enzymes in a cascade that leads to production of many mediators called prostanoids

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11
Q

Phospholipase A2

A

enzymes that create reactive intermediates from phospholipids in the plasma membrane of all cells

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12
Q

Arachadonate

A

Substrate for all cyclo-oxygenases

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13
Q

Thromboxine

A

Prevalent in platelets, normal function is to cause/facilitate clot formation

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14
Q

Analgesic properties

A

reduces certain pains

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15
Q

Anti-pyretic

A

Lowers raised temperatures

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16
Q

COX enzymes

A

Has a peroxidase site and a cyclo-oxygenase site
Made up of two identical subunits with 2 catalytic sites
Anchored into ER membrane
Channel by which arachadonate has to enter

17
Q

COX-1

A
Splice variant (often referred t as COX3)
Constitutively expressed -> on all the time in vast majority of body cells
18
Q

COX enzymes in stomach endothelial cells

A

Trigger secretion of mucus to produce critical lining to protect cells from acidic pH
Therefore too much aspirin inhibits mucus production and can lead to ulceration

19
Q

COX3

A

Largely expressed in the CNS and the brain
Not much known about its action
thought to be where paracetamol exerts most of its action

20
Q

COX2

A

Inducible enzyme triggered by inflammation, growth factors and tumour promoters, leads to prostaglandin production

21
Q

Aspirin selectivity

A

Some selectivity towards COX1

22
Q

Ibuprofen selectivity

A

Doesn’t distinguish well but slight preference to COX1

23
Q

Paracetamol selectivity

A

COX3 preference

24
Q

Coxibs selectivity

A

New NSAIDs with imrpoved selectivity for COX2