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Yr 3 Inflammatory and GI > Inflammation DRUGS > Flashcards

Inflammation DRUGS Flashcards

1
Q

Azathioprine- What does it do?
What does it treat?

A

Prodrug of mercaptopurine which affects purine salvage pathway and leads to incorrect DNA activity through false nucleotides being added.
Immunosuppressant

RA, crohns, UC

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2
Q

Azathioprine MOA

A

Prodrug of mercaptopurine
HPRT converts mercaptopurine to nucleoside monophosphate (TIMP)
TPMT (Thiopurine methyltransferase) converts TIMP to MeTIMP
MeTIMP inhibits new purine biosynthesis
6-thioguanine nucleotides are incorporated into DNA (false purines) causing apoptosis.

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3
Q

Methotrexate- What does it do?
What does it treat?

A

Competitive inhibitor of dihydrofolate reductase
Folic acid metabolised by dihydrofolate reductase to N5,N10-methylenetetrahydrofolic acid to make DNA bases (pyrimidines)
Decreases N5,N10-methylenetetrahydrofolic acid (which are used to make pyrimidines)
Stronger binding than folic acid (due to NH2)
Metabolised to polyglutamates= increased size and trapped in cell = prolonged action

Treats RA
Psoriasis
Crohn’s

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4
Q

What drug is the rescue therapy for methotrexate toxicity?

A

Leucovorin

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5
Q

Allopurinol - What does it do?
What does it treat?

A

Immunosuppresant- antimetabolite
Inhibitor of xanthine Oxidase (stops conversion of thiouric acid)
Higher affinity
Decreases production of uric acid
Allopurinol metabolised to oxypurinol= both active.
For gout.

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6
Q

Name 2 xanthine oxidase inhibitors

A

Febuxostat and allopurinol

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7
Q

Leflunomide - What does it do?
What does it treat?

A

For RA
Effects pyrimidine synthesis pathway, usually in lymphocytes.
Reversible inhibitor of dihydroorotate dehydrogenase.
Decreases synthesis of uridine.
therefore less nucleotide production for DNA.

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8
Q

How are prostaglandins made

A

Cell membrane phospholipids broken down by phospholipase A2 -> aracadonic acid broken down by Cyclooxygenase (COX) -> prostaglandin G2 (PGG2) -> prostaglandin H2 (PGH2) ->PGE2, PGF2a, PGD2

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9
Q

Explain the COX enzyme

A

Membrane embedded protein
Makes prostaglandins
Hydrophobic channel into active site
HEME Active site
Arachidonic acid is the substrate
Aspirin binds at serine 529

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10
Q

What is the difference between COX1 and COX2

A

COX1- metabolism, used all time
has isoleucine
COX2 - Inflammation response
has valine
Hydrophilic side pocket in structure

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11
Q

Where is COX3 and what drug works on it?

A

In the brain, paracetamol

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12
Q

What do all the COX enzymes have in common?

A

Hydrophobic binding channel
Catalytic site
Acylation site
Arginine for binding carboxylic acids

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13
Q

What do NSAIDS do in short

A

Inhibit cyclooxygenase from making prostaglandin G2 from arachidonic acid

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14
Q

What type of NSAID is aspirin

A

A salicylate

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15
Q

What makes aspirin special when it comes to binding to COX compared to other salicylates?

A

All other salicylates are competitive inhibitors, aspirin binds to serine 529 and acylates it!
Irreversible inhibition-> blocks access of arachidonic acid to active site.

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16
Q

How do competitive Non-selective NSAIDS work?

A

Affect COX1 and COX2
act competitively against arachidonic acid.
Inhibition is reversible so increasing conc. of arachidonic acid overcomes activity

17
Q

Name the 3 subclasses of Competitive Non selective NSAIDs

A

Arylalkanoic acids
N-arylanthranilic acids
Enolic acids

18
Q

What is the general structure for Competitive Non selective NSAIDs?

A

Flat surface—1 c spacer—- acidic group
|
|
lipophilic area

19
Q

What other pathway does diclofenac also inhibit

A

Lipooxygenase (therefore decreases production of leukotrienes)

20
Q

What are N-arylanthranilic acids?

A

Nitrogen bioisosteres of salicylic acid

21
Q

Give an example of a arylalkanoic acid

A

profens
Ibuprofen
Naproxen

22
Q

Give an example of an N-Arylanthranilic Acid

A

Fenamic acids
Mefanamic acid

23
Q

What are enolic acids?

A

oxicams
Non-carboxylic acid NSAIDS
Inhibit COX thru changing conformation to peroxy radical precursor of prostaglandin G2

24
Q

Give an example of an enolic acid

A

Piroxicam

25
Q

Give a summary of competitive non-selective NSAIDS

A

Act by mimicking the binding interactions of arachidonic acid

26
Q

What are COX-2 selective inhibitors- how do they have function

A

COXIBS
COX-2 expressed during inflammation
Competitive mechanism
COX-1 effect is reversible inhibition
COX-2 has irreversible inhibition

27
Q

Give an example of a COX-2 selective NSAID

A

Celecoxib, paracoxib

28
Q

Why do COX-2 selective NSAIDS have some effect on COX-1?

A

Blocks entry of arachidonic acid as molecule is bulky - no ionic interactions to hold in place however

29
Q

Why were refecoxib and valdecoxib withdrawn

A

toxicity as too selective to COX-2- causes heart attacks and strokes and CV effects.

30
Q

How are COX-2 selective NSAIDS fit for function?

A

The fit into the hydrophilic pocket in COX-2 which isn’t present in COX-1

Yr 3 Inflammatory and GI (15 decks)

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