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MD1 Locomotor > Drugs to Treat Inflammation > Flashcards

Drugs to Treat Inflammation Flashcards

1
Q

What do glucocorticoids inhibit?

A

Arachidonic acid release and metabolism

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2
Q

What do NSAIDs inhibit?

A

Cyclo-oxygenases

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3
Q

What do cysteinyl leukotriene 1 receptor antagonists inhibit?

A

LTD4 and LTD5 actions

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4
Q

Why are prostaglandins not commonly used as a drug?

A

Too unstable and expensive

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5
Q

What prostaglandin is used in pulmonary hypertension?

A

Epoprostenol PGI2 analogue

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6
Q

What are the effects of NSAIDs?

A

Anti-inflammatory = palliative for manifestations of inflammation
Analgesic - limit hyperalgesic effects of prostaglandins
Anti-pyretic

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7
Q

What are the indications for NSAIDs as an anti-inflammatory?

A

Acute and chronic conditions

  • Rheumatoid arthritis
  • Gout > NOT aspirin
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8
Q

Why is aspirin not used in gout?

A

Competes with uric acid for transporter > makes condition worse

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9
Q

When are NSAIDs indicated as an analgesic?

A

Headache
Menstrual pain
Musculoskeletal pain

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10
Q

Are NSAIDs curative?

A

No, palliative

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11
Q

What are the gastro-protective roles of PGE2?

A

Increases mucus secretion
Reduces gastric acid secretion
Promotes blood flow
Promotes angiogenesis

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12
Q

How do NSAIDs cause cause gastrointestinal adverse effects?

A

Inhibit mucosal synthesis of PGI2 and PGE2

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13
Q

How do NSAIDs increase bleeding time?

A

Decrease TXA2 synthesis > impaired platelet aggregation

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14
Q

How do NSAIDs cause renal and vascular adverse effects?

A

Compromise renal blood flow
- Decrease prostacyclin dilation
Increase blood pressure
- Decrease PGE2 natriuresis

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15
Q

When may NSAIDs cause renal failure?

A

Hypovolaemic
Underlying renal disease
Heart failure

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16
Q

In which demographic is renal failure caused by NSAIDs more common?

A

Elderly

17
Q

What is aspirin-sensitive asthma?

A

Respond to NSAIDs with bronchospasm

18
Q

What proportion of people with asthma are affected with aspirin-sensitive asthma?

A

10%

19
Q

How does asprin resolve inflammation?

A

Suppression of pro-inflammatory compounds

Promotion of substances that resolve inflammation

20
Q

Why is aspirin use contra-indicated in children?

A

Reye’s syndrome

- Liver toxicity, particularly associated with viral infection in children under 12

21
Q

How are aspirin-triggered lipoxins formed?

A

Acetylated COX2

22
Q

What are aspirin-triggered lipoxins?

A

Inflammation-resolving lipids

Aren’t usually made

23
Q

How does the use of aspirin in cardiovascular disease work?

A 
Increases ratio of PGI2/TXA2 in blood vessels, via loss of COX activity in platelets, which
- Selectively reduces thromboxane
- Prostacyclin preserved
Dilates vessels
Diminishes platelet reactivity
24
Q

What are the effects of paracetamol?

A

Analgesic

Anti-pyretic

25
Q

Which demographic is paracetamol especially used in?

A

Children

26
Q

Does paracetamol have anti-inflammatory effects?

A

No

27
Q

What is the mechanism of action of paracetamol?

A

Still uncertain

28
Q

What does paracetamol cause in overdose?

A

Irreversible liver failure

29
Q

What are the differences between different structural classes of NSAIDs?

A

Potency
Half lives
Make them more or less helpful in different applications

30
Q

What are the indications for glucocorticoids?

A 
Physiological replacement; eg: Addison's disease
Anti-inflammatory
- Asthma
- Topical
- Hypersensitivity states
- Rheumatoid arthritis
31
Q

What is the mechanism of action of glucocorticoids?

A

Gene regulatory effects > anti-inflammatory effects

  • Transactivation
  • Transrepression
32
Q

What is transactivation in terms of glucocorticoid action?

A

Transcription factors interact with promoter regions of target genes

33
Q

What is transrepression in terms of glucocorticoid action?

A

Protein-protein interaction

Glucocorticoid receptor binds to pro-inflammatory transcription factors > blocks their effects

34
Q

What is neutralisation of TNF-alpha used as a treatment in?

A

Rheumatoid arthritis

35
Q

What are the adverse effects of neutralisation of TNF-alpha?

A

Reactivation of latent TB

Other developing infections need aggressive antibiotic treatment

MD1 Locomotor (17 decks)

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