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Muscular, Derma & Senses > NSAIDs 💊 > Flashcards

NSAIDs 💊 Flashcards

1
Q

3 properties of NSAIDS

A
  1. Anti inflammatory
  2. Anti pyretic
  3. Analgesic
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2
Q

Inflammation in Wound Healing and Thrombosis

A
  1. Inflammation
  2. Proliferation
  3. Maturation
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3
Q

Inflammation in Diease > atherosclerosis

A
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4
Q

Inflammation in disease > rheumatoid arthritis

How do synovial cells destroy cartilage?

A
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5
Q

What is the role of Prostanoids?

A

Regulate and increase inflammatory response.

Relates to products if the cyclooxygenase pathway:

Prostaglandins
Thromboxanes
Prostacyclins

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6
Q

Structure of Prostanoids

A
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7
Q

Biosynthesis of Prostanoids

A

Cell membrane phospholipids ==
Arachidonic acid == (by COX1 & COX2)=
PGG2==
PGH2==
PGE2 or PGF2 or PGD2

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8
Q

Production of Prostanoids

A

Prostacyclin = IP = endothelial

Thromboxane A2 = platelets, kidney

Prostaglandin D2 = mast cells, brain, airway

Prostaglandin E2 = brain, vascular smooth muscle, kidney

Prostaglandin F2a = uterus, airways, eyes

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9
Q

Similarities between COX1 and COX2

A
  1. Isoenzymes:
    COX1 gene on Chromosome 9,
    COX2 gene on Chromosome 1
  2. 65% identical amino acid sequence
  3. Structure: long narrow channel open at one end
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10
Q

Differences between COX1 and COX2

A
  1. VALINE 523 in COX2 = creates additional side pocket vs.
    BULKY ISOLEUCINE 523 in COX1
  2. VALINE 434 widens additional side pocket in COX2 vs.
    ISOLEUCINE 434 in COX1
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11
Q

Mode of action NSAIDs

A

Block the uptake and binding of arachidonic acid to COX1/2 at Arg120

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12
Q

Common structural features of NSAIDs

A
  1. Acidic centre
  2. Aromatic/heteroaromatic ring
  3. Additional centre of lipophilicity
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13
Q

Aspirin (salicylate) = how does it interact with COX?

A
  1. Aspirin acetylates SER530 = so arachidonic acid cannot reach the catalytic centre.
  2. Arg-120 I’m COX1/2 stabilises carbohydrate group of aspirin.
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14
Q

Is Aspirin a reversible or irreversible COX1 and COX2 inhibitor?

A

Irreversible!! (THE ONLY)

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15
Q

Side effects of ASPIRIN?

A

Peptic ulcers

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16
Q

What are the 2 groups of Arylalkanoic acid?

A
  1. Aryl and hetero-arylacetic acids
    = Indomethacin, sulindac, diclofenac, nabumetone.
  2. Aryl and hetero-propionic acids
    = ibuprofen
17
Q

Aryl and hetero-arylacetic acids

Table

A
18
Q

Selective COX2 Inhibitors
= celecoxib and rodecoxib

What went wrong?

A
  1. COX1 produces Thromboxane A22 for platelet aggregation and vasoconstriction.
  2. COX2 Catalyses prostacyclin synthesis, which counteracts thromboxanr A22, triggering vasodilation and platelet inhibition.
  3. Selective COX2 Inhibitors decrease prostacyclin production, creating conditions that can cause thrombosis events

Muscular, Derma & Senses (20 decks)

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